PSYCHOPHARMACOLOGY

INTRODUCTION

Psychopharmacology is the study of drugs used to treat psychiatric disorders. It discusses many
psychoactive medications that alter synaptic transmission in the brain in certain and specific ways.
Medications that affect psychic function, behavior or experience are called psychotropic medications.
They have significant effect on higher mental functions; Psychopharmacological agents are first-line
treatment for almost all psychiatric ailments nowadays. With the growing availability of a wide range
of drugs to treat mental illness, the nurse practicing in modern psychiatric settings needs to have a
sound knowledge of the pharmacokinetics involved, the benefits and potential risks of
pharmacotherapy, as well as her own role and responsibility.

TERMS

Psychopharmacology- is the study of the effect of the drugs on affect, cognition, and behavior.
Efficacy refers to the maximal therapeutic effect that a drug can achieve.

Potency- describes the amount of the drug needed to achieve that maximum effect; low-potency
drugs require higher dosages to achieve efficacy, whereas high-potency drugs achieve efficacy at
lower dosages.

Half-life is the time it takes for half of the drug to be removed from the bloodstream. Drugs with a
shorter half-life may net to be given once a day.

Agonist- Drugs that activate receptors are termed agonist.

Antagonist- Drugs that binds to binds to but does not activate (block) a receptor.

Neurotransmitter – neurotransmitter are the chemical messengers that travel from one brain cell
to another cell and synthesized by enzymes from certain dietary amino acids or precursors. These are
stored in the axon terminals of the presynaptic neuron.

Receptors - Receptors are molecules situated on the cell membrane that are binding sites for
neurotransmitters.

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 Synapse
The synapse separates the two neurons (pre- and postsynaptic cells).

Drugs affect neurotransmission in several ways

Release: More neurotransmitters are released into the synapse from the storage vesicles in
presynaptic cell

Blockade : The neurotransmitters are pre-vented from binding to the postsynaptic receptors

Receptor sensitivity changes: The receptor becomes more or less responsive to the
neurotransmitter

Blocked reuptake: As the presynaptic cell does not reabsorb the neurotransmitter, it is retained
in the synapse, and therefore, enhances or prolongs the action

Interference with storage vesicles: Either released more or less

Precursor chain interference: The process that 'makes' the neurotransmitter is either synthesized
more or less

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Neurotransmission and drug effects at the synapse

SUBSTANCE LOCATTION FUNCTION

Brains have
neurotransmitters that are
synthesized from amino
molecules such as tyrosine,
tryptophan, and histidine.
Found in various regions
of the brain, amines affect
learning, emotions, motor
control, and other
activities.

Neuroamines Derived from tyrosine a Levels fluctuate with sleep and

Norepinephrine (NE) dietary Amino acid. wakefulness. Plays a role in charges in
Located in the Brainstem levels of attention and vigilance. Involved
(particularly the locus in attributing value to a stimulus and in the
Ceruleus). regulation of mood. Plays a role in
Effect: Can be excitatory affective and anxiety disorders.
or Inhibitory. Antidepressants block the reuptake of NE
into the presynaptic cell or inhibit
monoamine oxidise from metabolizing it.

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Dopamine (DA) Derived from tyrosine, a Involved in the control of complex,
dietary amino acid. movements motivation, and cognition and
Located mostly in the in regulating emotional responses. Many
brainstem (particularly drugs of abuse 9such as cocaine and
the substantianigra). amphetamines) cause DA release,
Effect: Generally suggesting a role in whatever makes things
excitatory.. pleasurable. Involved in the movement
disorders seen in Parkinson’s disease and in
many of the deficits seen in schizophrenia
and other forms of psychosis.
Antipsychotic drugs block DA receptors in
the postsynaptic cell.
Serotonin (5-HT) Derived from Level, fluctuate with sleep and
tryptophan, a dietary wakefulness, suggesting a role in arousal
amino acid. Located in and modulation of the general activity
the brain (particularly in levels of the CNS. Particularly the onset of
the raphe nuclei of the sleep. Plays a role in mood and probably in
brainstem). the delusions, hallucinations, and
Effect: Mostly inhibitor withdrawal of schizophrenia. Involved in
temperature regulation and the pain control
system of the body. LSD (the
hallucinogenic drug) acts at 5-HT receptor
sites. Plays a role in affective and anxiety
disorders. Antidepressants block its
reuptake into the presynaptic cel
Melatonin A further synthesis of Induces pigment lightening effects n skin
serotonin produced in the cells and regulates reproductive function in
pineal gland. animals. Role in humans is unclear.
Effect: Implicated in
seasonal affective
disorder and the sleep
wake cycle.
Acetylcholine Synthesized from Plays a role in the sleep wakefulness cycle.
choline. Located in the Signals muscles to become active.
brain and spinal cord but Alzheimer’s disease is associated with a
is more widespread in decrease in acetylcholine secreting
the peripheral nervous neurons. Myasthenia gravis (weakness of
system, particularly the skeletal muscles) results from a reduction
neuromuscular junction in acetylcholine receptors.
of skeletal muscle.
Effect: Can have an
excitatory or inhibitory
effect.

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Amino acids Found in all cells of the Implicatwd in schizophrenia; glutamate
Glutamate body, where it is used to receptors control the opening of ion
synthesize structural and channels that allow Calcium (essential to
functional proteins. neurotransmission ) to pass into nerve cells,
Also found in the CNS, propagating neuronal electrical impulses.
where it is stored in Its major receptor, NMDA, help regulate
synaptic vesicles and brain development. This receptor is
used as a blocked by drugs (such as PCP) that cause
neurotransmitter. schizophrenic like symptoms.
Effect: Excitatory. Overexposure to glutamate is toxic to
neurons and may cause cell death in stroke
and Huntington’s disease.
Gamma aminobutyric acid A glutamate derivative, Drugs that increase GABA function, such
(GABA) most neurons of the CNS as the benzodiazepines, are used to treat
have receptors. anxiety and to induce sleep.
Effect: Major transmitter
for post synaptic
inhibition on the CNS
Peptides
Peptides are chains of
amino acids found
throughout the body.
About 50 have been
identified to date, but their
role as neurotransmitters is
not well understood.
Although they appear in
very low concentrations in
the CNS, they are very
potent. They also appear to
play a “second messenger
role in neurotransmission;
that is, they modulate the
messages of the non
peptide neurotransmitters.
Endorphins and Widely distributed in the The opiates morphine and heroin bind to
enkephalins CNS. endorphin and enkephalin receptors on
Effect: Generally presynaptic neurons, blocking the release
inhibitory. of neurotransmitters and thus reducing
pain.

Substance P Spinal cord, brain and Found in pain transmission pathway.

sensory neurons Blocking the release of substance P by
associated with pain. morphine reduces pain.
Effect: Generally
excitatory.

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 Principles That Guide Pharmacologic Treatment

The following are several principles that guide the use of medications to treat psychiatric
disorders:
 A medication is selected based on its effect on the client’s target symptoms such as delusional
thinking, panic attacks, or hallucinations. The medication’s effectiveness is evaluated largely
by its ability to diminish or eliminate the target symptoms.
 Many psychotropic drugs must be given in adequate dosages for some time before their full
effect is realized. For example, tricyclic antidepressants can require 4 to 6 weeks before the
client experiences optimal therapeutic benefit.
 The dosage of medication often is adjusted to the lowest effective dosage for the client.
Sometimes a client may need higher dosages to stabilize his or her target symptoms, whereas
lower dosages can be used to sustain those effects over time.
 As a rule, older adults require lower dosages of medications than do younger clients to
experience therapeutic effects. It also may take longer for a drug to achieve its full therapeutic
effect in older adults.
 Psychotropic medications often are decreased gradually (tapering) rather than abruptly. This
is because of potential problems with rebound (temporary return of symptoms), recurrence of
the original symptoms, or withdrawal (new symptoms resulting from discontinuation of the
drug).
 Follow-up care is essential to ensure compliance with the medication regimen, to make
needed adjustments in dosage, and to manage side effects.
 Compliance with the medication regimen often is enhanced when the regimen is as simple as
possible in terms of both the number of medications prescribed and the number of daily
doses.

Classification of psychotropic drugs

4. Anxiolytics
3. Mood
1. Antipschotics 2. Antideressants and
stablizing drugs
Hyponsedatives

5. 6. Antiabuse 8. Drugs used in

7. Antiepileptics
Antiparkinsonian Drugs Child Psychiatry

9. Drugs used in
Dementia of 10. Others
Alzimer's type

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ANTIPSYCHOTIC DRUGS

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 ANTIPSYCHOTICS DRUGS
Antipsychotic are those psychotropic drugs, which are used for the treatment of psychotic symptoms.
Antipsychotic agent control some of the symptoms of schizophrenia, mania, and organic psychosis.
THE term Antipsychotics applied to drugs that reduce psychomotor excitement and control some
symptoms of schizophrenia without causing disinhibition, confusion or sleep.

These are also known as-

 Neuroleptic
 Major tranquilizers
 D2 Receptor blockers
 Antischizophrenic drugs

Pharmacology
Antipsychotics share the property of blocking dopamine receptors. This may account for therapeutic
action .Alpha isomer blocks dopamine receptors and is therapeutics, while beta isomer does not
block dopamine receptors and is not therapeutic. Both Alpha and Beta isomers block noradrenergic
and cholinergic receptors. The antiadrenergic action account for many side effects of the drug,
whileantidopaminergic actions on basal ganglia are responsible for the EPS(extra pyramidal
symptoms).Atypical antipsychotics have antiserotonergic (5-hydroxytryptamin or 5HT)
antiadrenergic and antihistaminergic actions. These are therefore called serotonin-dopamine
antagonists.

Pharmacokinetics
Antipsychotics when administered orally are absorbed variably from the gastrointestinal tract,with
uneven blood levels .they are highly bound to plasma as well as tissue proteins .Brain concentration
is higher than plasma concentration .They are metabolize in liver and mainly well absorbed from
jejunum and excreted from kidneys. The elimination half life varies from 10-24 hrs.
Most of the antipsychotics tend to have a therapeutic window, drug is ineffective. If the blood level is
higher than the upper limit of the window, it results in toxicity or the drug is again ineffective .

Indication
Organic psychiatric disorder
 Delirium
 Dementia
 Delirium tremens
 Drug induced psychosis and other organic mental disorders
Functional disorder
 Schizophrenia
 Schizoaffective disorder
 Paranoid disorder
Mood disorder
 Mania
 Major depression with psychotic symptoms

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  Childhood disorder
 Attention-deficit hyperactive disorder
 Autism
 Enuresis
Conduct disorder
 Neurotic and other psychiatric disorder
 Anorexia nervosa
 Intractable obsessive –compulsive disorder
 Sever, intractable and disabling anxiety
Medical disorder
 Huntington’s chorea
 Intractable hiccough
 Nausea and vomiting
 Tic disorder
 Eclampsia
 Heat stroke
 Severe pain in malignancy
 Tetanus

Side effect/adverse effect of antipsychotic drug –

Side effect the many different antipsychotic drugs share a broad pattern of unwanted effects that are
mainly related to their antidopaminergic, antiadrenergic and anticholinergic properties.
Extra pyramidal effect:
These are related to the antidopaminergic action of the drug of the basal ganglia. The effect on the
extra pyramidal system fall into four groups.

Acute
Akathesia
Dystonia

Parinsonian Tardive
Syndrome Dyskinsia

Acute Dystonia
It occurs soon after treatment begins, especially in young man .It is observed most often with
butyrophenones and with the piperazine group of phenothiazines.The main feature are torticollis

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,tongue protrusion,grimacing,andopisthotonus,an odd clinical picture which can easily be mistaken
for historionic behavior .It can be controlled by biperiden lactate 2 to 5 mg, given carefully by
intramuscular injection or in the most severe cases , by slow intravenous injection.

Akathesia
it is unpleasant feeling of physical restlessness and need to move which lead to an inability to keep
still. It occurs usually in the 1st two weeks of treatment with neuroleptic drugs, but may begins only
after several months. Akathesiais not controlled by antiparkinson drugs ,but when occurring early in
treatment it disappears if the dose is reduced.

Parinsonian Syndrome
This is the common side effect charateristised by Akinesian expressionless face and lack of
associated movements when walking, together with rigidity, termor, stooped posture and in, severe
cases, a festinant gait. This syndrome often takes a few weeks to appear after the drug has been taken
and then sometimes diminishes, even through the doses have not been reduced. The symptoms can
be controlled with antiparkinsonian drugs. However, it is not a good practice to prescribe
antiperkinsonian drugs prophylactically as a routine, because not all the patients will need them.
Moreover, these drugs themselves have undesirable effects in some patients, e.g., they occasionally
cause an acute organic syndrome, and possibly increase the incidence of tardive dyskinesia.

Tardive Dyskinsia
The last syndrome, tardive dyskinsia, is particularly serious because, unlike the other extrapyramidal
effects, it does not always recover when the drugs are stopped. It is characterized by chewing and
sucking movements, grimacing, choreoathetoid movements and possible akathisia. The last
mentioned usually affects the face but the limbs and the muscles of respiration may also be involved.
Tardive dyskinesia is more common among women, the elderly and the patients who have diffused
brain pathology. In about half the cases, tardive dyskinesia disappears when the drugs are stopped.
Estimates of the frequency of the syndrome are in different series, but it seems to develop in 20-40
percent of schizophrenic patients treated with long term antipsychotic drugs.

Classification:
TYPICAL ANTIPSYCHOTICS
a. Phenothiazine derivatives
• Aliphatic Derivative: CHLORPROMAZINE
• Piperidine Derivative:THIORIDAZINE
• Piperazine Derivative: FLUPENAZINE, PERPHENAZINE,
TRIFLUOPERAZINE
b.Thioxanthene Derivative: THIOTHIXENE
c. Butyrophenone: HALOPERIDOL

d. ATYPICAL ANTIPSYCHOTICS
• CLOZAPINE LOXAPINE
• OLANZAPINE QUETIAPINE
• RISPERIDONE MOLINDONE
• ZIPRASIDONE
• SERTINDOLE ARIPIPRAZOLE

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 CHLORPROMAZINE

Trade Name
jargactil, Thorozine

Classification
Dopamine receptor antagonists—phenothiazine

Dose
Oral: 300 to 1500 mg per day in divided doses, Parental: 25 to 100 mg per day IM only.

Mechanism of Indication Contraindica Side effect Nursing responsibility and

action tion management of side effect
Chlorpromazine Acute psychotic Comatose Dry mouth -Assess patient behaviour and
block dopamine episode in state,mylosup emotional status
neurotransmissio schizophrenia ression -Advise to patient take sips
n at postsynaptic and ,severe orally water frequently, advise
dopamine schizoaffective cardiovascular glycerine on the lip .suggest to
receptor site. disorder mania , disease take sugarless chewing gum and
Possesses strong depression ,severe CNS hard candy
anticholergenic psychotic depression, GI- -Advise high fiber diet and more
sedative and symptoms subcortical paralytic water intake. Tell the patient not
antiemetic effect, ,delusional brain damage. ileus, to take drug within 2 hr. of
moderate extra disorder and nausea antacid.
pyramidal effect substance Constipatio - Drug take with food or full
and slight induced n glass of milk. Dilute
antihistamine psychotic concentration in at least 60 ml
action. delirium, diluents just before
mental disorder administrating it, use tomato, or
due to a medical fruit juice , milk , simple syrup
condition ,carbonate beverages, coffee ,tea
,pervasive water , semisolid food such as
development soup & pudding .
disorder ,
Tourette’s

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syndrome GU - -Advise the patient that urine
,huntigsons Urinary may be darker.
disease . retention
,impotence.
CV – -Monitor patient’s blood
tachycardia, pressure for hypotension
Orthostatic -Advice the patient to get up
hypotension from bed and chair slowly.
,ECG -Monitor blood pressure lying
change and standing frequently.
-Document and report the
significant changes.
EPS: MONITOR PATIENTS EPS
Akathesia, -Assess patients behaviour and
acute emotional status.
dystonia -Inform the patient drowsiness
rabit generally subsides with
syndrome, continued therapy
drug -Warm the patient to avoid tasks
induced that require mental alertness or
Parkinson. motor skill until his responses to
Central the drug has been established.
nervous side -Evaluate the patient’s fine
effect - tongue movement for signs of
seizure tardive dyskinesia. These
,sedation , symptoms are potentially
irreversible.
-The drug should be withdrawn
at the first sign which is usually
vermiform movements of the
tongue.
- Urge the patient to avoid
alcohol.
Metabolic -Regularly check the patient’s
and CBC, as ordered for evidence of
endocrine blood dyscrasias
side effect : -Monitor the patients serum drug
cholestatic level the therapeutic serum level
jaundice , the therapeutic serum level for
agranulocyt chlorpromazine is 50 to
osis , mild 300mcg/ml and the toxic serum
leukopenia level greater than 750mg/ml.

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 Dermatologi -Urge the patient avoid excessive
cal side exposure to sunlight while taking
effect : chlorpromazine.
contact -Ensure that patient wear
dermatitis protective sun screen clothing
photosensiti and sunglasses while spending
vity reaction outdoors.
-Avoid skin contact with the oral
concentrate and syrup to prevent
dermatitis.
-Do not give CPZ by the s/c
route because severe tissue
necrosis may occur to prevent
irritation at the injection site ,
dilute the injection with sodium
chloride.
-Administration deep injection in
large muscles mass. Injection
should be diluted in sodium
chloride solution.
-Use CPZ cautiously in patient
with alcoholism, glaucoma ,
history of seizure ,impaired
cardiac hepatic , renal
,respiratory ,BPH ,urine
retention.

TRIFLUOPERAZINE HYDROCHLORIDE

Trade Name
Solazine, Terfluzine, Solazine, Flurazine

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Classification
Dopamine receptor antagonists—phenothiazine

Dose
Oral: 2-5 mg/day up to 40 mg/day, Parental: IM 1-2 mg up to 10 mg/day

Mechanism of Indication contraindicat Side effect Nursing responsibility

action ion management of side effect
A phenothiazine Acute Angle-closure frequent: Assess patient behaviour and
derivative that psychotic glaucoma, Hypotension, emotional status
blocks dopamine episodes in mylosuppressi Dizziness
at postsynaptic schizophrenia on, severe and syncope
receptor sites. and cardiac or (occur Monitor the patient's BP for
Possess strong schizoaffective hepatic frequently hypotension
extra pyramidal disorders, disease, after first Instruct the patient to rise
and antiemetic mania, severe injection, slowly from a lying or sitting
effects and weak depression with hypertension occasionally position to prevent hypotension.
anticholinergic psychotic or after Monitor blood
and sedative symptoms, hypotension Subsequent pressure lying and standing
effects delusional injections frequently. Document and
disorders, and rarely report significant changes
borderline with oral
personality doses).
disorder, and Occasionally
substance : Drowsiness give oral drugs along with food
induced during early to decrease GI effects, instruct
psychotic therapy, the patient not to take antacids
disorders due after long- within 1 hour of trifluoperazine
to a medical term therapy
condition, may
pervasive precipitate
developmental nausea,
disorder, vomiting
Tourette's dry mouth, -Advise to patient take sips
syndrome, Blurred orally water frequently, advise
Huntington s vision, glycerin on the lip .advice to
disease. lethargy, take fiber or semisolid diet
constipation
or nausea, -Administer deep injection in
nasal large muscle mass
congestion,
peripheral
edema, urine
retention.

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*Serious -Use trifuoperazine cautiously
reactions: in patients with Parkinson's
EPS- disease or seizure disorders
Akathesia,
acute -Observe the patient tor
dystonia, extrapyramidal symptoms, such
parkinsonian as gait changes, tremors, and
symptoms, abnormal movement in the
tardive trunk, neck Of extremities.
dyskinesia,
dizziness - The drug should be withdrawn
abrupt at the first sign
discontinuati
on after long- -Monitor the patient for fine
term therapy tongue movements, an early
may sign of tardive dyskinesia which
precipitate is usually vermiform
nausea, movements of the tongue
vomiting
and tremors. -Assess the patient or signs of a
Trifluoperazi therapeutic response
ne may lower inform the patient that
the seizure drowsiness generally subsides
threshold. with continued therapy

-Warn the patient to avoid tasks

that require mental alertness or
motor skills until his response
to the drug has been established
Blood Monitor the patients WBC
dyscrasias count for blood dyscrasias,
Such as anaemia, neutropenia,
pancytopenia and
thrombocytopenia.
these symptom are potentially
irreversible. Assess Symptoms
of infection .

photosenstivi -urges the patient to avoid

ty, alcohol and excessive exposure
skin rash to artificial light and sunlight
during trifluoperazine therapy

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 THIORIDAZINE

Trade name
Mellaril or Melleril

Classification
Trifluoro methyl phenothiazine

DOSE
10mg, 15mg, 25mg, 50mg, 100mg, 150mg, 200mg, tablets; 30mg/ml, 100mg/ml solution;
25mg/5mL suspension

Mechanism of Indication Contraindic Side effect Nursing responsibility

action ation management 0f side effect
Typical Thioridozine There is a Extrapyramid -Observe closely the sign of
antipsychotic, is a black –box al side effect : CNS depression , slowly,
includingthioridazin medication warning for symptoms of particularly from lying down to
e work to treat used to treat dementia- dystonia , us upright posture, dangle legs
psychosis by schizophreni related parkinsonism, few minutes before standing.
blocking dopamine a, psychosis akathesia ,and
(D2) receptor .These psychoticdis because it tardive -Medicine is make drowsy
medication are orderd, may increase dyskinesia avoid alcohol consumption and
effective in treating depressive the risk of .dystonic avoid to drive and machinery
the positive disorder, death reaction are work.
symptom of pediatric secondry to muscles
schizophrenia, such behavioural either spasm that - Be aware that patient may be
as hallucination disorders , cardiovascula may occur unable to adjust to extremes of
,delusion ,and and geriatric r or early on and temperature because drug effect
disorganization psychoneurot infectious involve the heat regularly centre in the
.Atypical ic effect . eyes , tongue hypothalamus patient may
antipsychotic ,also manifestation Thioridozine ,or neck , complain of being cold even at
called second . associated during room temperature, older
generation with a or adult are susceptible.
antipsychotics, are prolonged Supervision patient closely

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known to treat both QT interval. during early course of therapy
the positive and Patient with suicide is an inherent risk with
negative symptoms known heart any depressed patient.
of schizophrenia. arrhythmias
some negative or -Avoid alcohol during drug
symptoms include hypotensive therapy concomitant use
apathy , low energy , or enhances CNS depression
and flat affect . hypertensive effects.
heart disease
should also -Be aware that marked
also avoid drowsiness generally subside
this with continued therapy or
medication . reduction dosage.

- Do not drive, do not apply

heat pad or hot water bottles to
the body for external heat,
because of depression
conditioned available
behaviours, a secure burn may
result

Special Ask to patient report the onset

senses- nasal of any changes in visual acuity,
congetion, brownish coloring of vision, or
blurred vision, impairment of night vision to
pigmenory physician.
retinopathy.

GI – Monitor I& O ratio and bowel

xerostomia, elimination pattern, check for
constipation, abdominal distension and pain,
paralytic encourage adequate fluid intake
ileus. as prophylaxis for constipation
and xerostomia. phenthiazine at
least 1 h before or 1 h after an
antacid or antidiarrheal

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 medication.
Dilute liquid concentrate just
prior to administration with ½
glass od fruit juice, milk, water,
carbonated beverage, or soup

Vrogential – Thioridazinee may colour pink

amenorrhea, red to reddish brown
breast
engorrmrnt,
gynecomastia
galactorrhea,
urinary
retention.

Orthostatic hypotension may

CV- occur in early therapy, female
ventricular patients appear to more
dysrhythmias, susceptible than males, make
hypotension position changes slowly,
prolonged particularly from lying down to
QTC interval. us upright posture, dangle legs
few minutes before standing.

Skin Schedule Urge the patient avoid

dermatitis, excessive exposure to sunlight
rash while taking thioridozine
Ensure that patient wear
protective sun screen clothing
and sunglasses while
spendingoutdoors.Avoid skin.

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 TRIFLUPERAZINE HYDROCHLORIDE

Trade Name
Stelazine ,eskazinyl

Classification
Phenothiazine

Dose
1MG, 2MG, 5MG, 10MG, Schizophrenia outpatient -1-25mg PO q12hr, Inpatient- Initail 2-5mg PO
q12hr, Maintance Dose: 15-20mg/day, Not to exceed 40mg/day. Non Psychotic Anxiety -1-2mg PO
q12hr, Maximum Dose: 6mg/day; not to exceed 12 weeks

Mechanism Indication Contraindic Side effect Nursing responsibility

of action ation management of side effect
Block Schizophren Contraindicat Drowsiness, Medication is make drowsy
dopamine ia psychotic ed in CNS dizziness , during the day ,do not drive ,
D2post feature depression , lightheaddeness operate machinery or there
synaptic associated coma ,blood ,tiredness. trouble hazardous task ,avoid alcohol
receptor with mental dyscrasias , sleeping consumption ,rest in quiet
illness. Renal and extrapyramidal ,dimly light room ,heat
Nonsychotic gepatic reaction – ,massage therapy , may help if
anxiety imairement . Parkinson , the headache recur ,
disorder. dystonia , akathisia
,insomnia ,
neuroleptic
malingment
.cerebral edema ,
headache ,

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Gastrointestinal - -Eat small ,frequent meals
Dry mouth , rather than larger meals three
,constipation, times ,Eat low sugar ,low acid
nausea , vomiting , food ,chew xylitol chewing
diarrhea gum .

-Increase water intake and fiber

content in diet .eat moist food
such fruit vegetable and soup
.electrolyte intake to avoid
dehydration

CV - severe -Monitor blood pressure lying

hypotension and standing frequently
,tachycardia , document and report significant
cardiac arrest , changes.
DVT .
Dermatologic – -urges the patient to avoid
skin reaction alcohol and excessive exposure
,photosensitivity to artificial light and sunlight
reaction ,itching , during drug therapy liquid
butterfly shaped forms may cause a rash in a
rash on nose and skin contact occurs
cheeks
Hematology – -Monitor the patients WBC
blood dyscrasias , count for blood dyscrasias,
agranulocytopenia Such as anaemia, neutropenia,
,thrombocytopenia , pancytopenia and
aplastic anemia, thrombocytopenia.
bleeding these symptom are potentially
irreversible

Hepatic – jaundice , -Monitor liver function n test ,

liver damage , assess symptoms of jaundice ,
strict monitoring serum level ,
assess eye discolouration

Musculoskeletal - -Explain risk of dystonic

muscle twitching reaction and tardive dyskinesia,
,uncontrollable and tell patient to report
movement ,joint abnormal body movements.
pain ,swelling of
feet ankles

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 FLUPHENAZINE DECANOATE

Trade Name
Permitil, Prolixin, Prolixin Decanoate

Classification
Dopamine receptor antagonists—phenothiazine

Dose
Oral: 1-30 mg/day, Parental: 25 mg/ml once in 2 to 4 weeks

MECHAN Indication Contraindica Side effect Nursing responsibility or

ISM of tion management of side effect
action
A Schizophren Angle-closure Frequent -Monitor the patient’s blood
phenothiazi ia, mania glaucoma, Hypotension, pressure for hypotension
ne that with myelosuppres dizziness
antagonizes psychotic sion, severe and syncope -Avoid skin contact with the oral
dopamine symptoms, cardiac or (occur frequently concentrate and syrup to prevent
neurotrans organic hepatic after first contact dermatitis.
mission at brain disease, injection, and
synapses syndrome, severe occasionally after
by blocking chronic hypertension subsequent -Administration deep injection in
postsynapti schizophren hypotension. injections and large muscle mass.
c ia rarely with oral
doparmineg doses).

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ic receptors Occasionally: vermiform movements of the
in the brain somnolence, dry tongue.
mouth, blurred
vision, lethargy, -Inform the patient that drowsiness
peripheral edema generally subsides with continued
urine retention, therapy
constipation or
diarrhoea, nasal -Warn the patient Assess patient
congestion. behaviour and emotional status.
Serious reaction:
EPS-Akathesia, -Evaluate the patients fine tongue
acute dystonia, movement for signs of tardive
parkinsonian dyskinesia. This symptom
symptoms, potentially irreversible.
tradive
dyskinesia, abrupt - The drug should be withdrawn at
discontinuation the first sign which it usually to
after long-term avoid tasks that require mental
therapy may alertness or motor skills until his
precipitate response to the drug has been
nausea, vomiting established.
gastritis,
dizziness, and
tremors
,fluphenazine
may lower the
seizure threshold,
blood dyscrasias, -Complete blood count for blood
particularly dyscrasis. Monitor level of WBC ,
agranulocytosis low ANC level indicate D infection
and mild .
leukopenia

FLUPHENTHEXIOL

22
Tradename
Depixol , FLUANXOL

Classification
Thioxanthene

Dose
PO (adult) 1mg 3times daily initially; increase by 1mg every 2-3 days until desired response, usual
effective dose is 3-6 mg/day in divided doses (upto 12mg/day has been used); if insomnia occurs,
evening dose may be decrease. IM (adult): initiate with a 5-20mg test dose (use 5mg dose in
elderly/cachectic patients)as the 2% injection.

Mechanism of Indicatio Contraindicatio Side effect Nursing responsibility

action n n management of side effect
Fluepenthixol is Schizoph Hyperdenstivity , CNS – -Inform the patient drowsiness
a powerful renia extremely drowsiness generally subsides with
antagonist of excitable and ,hypokinesia continued therapy .
both D1 and over active ,hyperkinesia -Warm the patient to avoid
D2 dopamine patients : mania ,Parkinson , tasks that require mental
receptor ,porphyria , tremor ,akathisia alertness or motor skill until his
antagonist .Its coma ,pre- , dystonia responses to the drug has been
antipsychotic existing CNS ,dizziness , establishd.
activity is depression ,bone insomnia -Evaluate the patient’s fine
thought to be marrow ,overactivity , tongue movement for signs of
related to blocks suppression headache , tardive dyskinesia.
postsynaptic ,phaeochromocyt nervousness -These symptoms are
dopamine oma ,lactation. ,depression , potentially irreversible.
receptor in the seizure -The drug should be withdrawn
CNS . confusional at the first sign which is usually
state. vermiform movements of the
tongue.
-Urge the patient to avoid
alcohol.
GI – dry mouth , -Eat small , frequent meals
constipation , rather than larger meals three
nausea ,vomiting times ,Eat low sugar ,low acid
, abdominal pain food ,chew xylitol chewing gum
, dyspepsia , .
appetite changes. -Increase water intake and fiber
content in diet .eat moist food
such fruit vegetable and soup.
-Electrolyte intake to avoid
dehydration.
CVS – -Monitor blood pressure lying
hypotension ,QT and standing frequently
interval document and report significant
prolongation , changes.
tachycardia

23
 HALOPERIDOL

Trade Names
Serenace, Triperidol, Senorm-LA, Haldol

Classification
Dopamine receptor antagonists—butyrophenone

Dose
Oral: Oral: 0.5 to 5mg twice daily or three times daily /maximum: usually 100mg daily
Parentral – initial 2 to 5mg I/M, maximum – 100mg dail , First oral dose may be given
12 to 24 hr after last parentral dose .

Mechanism of Indication Contraindica Side effect Nursing responsibility

action tion management of side effect
an antipsychotic, Acute Angle-closure CV –cardiac -Assess patient behaviour
antiemetic and psychotic glaucoma, arrest and emotional status
antidyskinetic agent episodes in central ,hypertensio
that competitively schizophrenia nervous n, -Use haloperidol cautiously
blocks postsynaptic and system orthostatic in patients with
dopamine receptor schi1zoaffectiv depression, hypotension cardiovascular disease,
interrupts nerve e disorders, myelosuppres , hepatic or renal dysfunction
impulse movement mania, sion, Frequent: Keep the patient recumbent
and increases depression Parkinson's Blurred (head low and legs raised)
turnover of dopamine psychotic disease, vision, , for 30-60 minutes after
in the brain. symptoms, Severe orthostatic administration to minimize
Peripheral effects delusion cardiac or hypotension hypertensive.
include disorder hepatic ,
anticholinergic borderline disease. moperiphera - Monitor blood pressure
properties and alpha personality ledema lying and standing frequently
adrenergic blockage. disorder, and occasional: document and report

24
substance Difficulty significant changes.
induced urinating -Instruct the patent to rise
psychotic decreased slowly from a lying or sitting
disorder, thirst, position during haloperidol
delirium and dizziness, therapy.
dementia, decreased
mental sexual -Advise patient to take tablet
disorders due function, with food or full glass of
to a medical drowsiness, milk or water to reduce GI
condition, DISTRESS
pervasive
developmental -Dilute oral solution with a
disorder, Abdominal beverages such as cola or
1ourette s disturbance orange ,apple , or tomato
syndrome, nausea. juice
Huntington s vomiting
disease. lethargy -Urge the patient to avoid
Drymouth exposure to sunlight and any
,dehydration condition that may cause
,decrease dehydration or overheating
thrist, because they may increase
Difficulty in the risk of heat stroke.
urinating
-Suggest taking sips of water
or chewing sugarless gum to
help relieve dry mouth.

Serious -Caution the patient against

reactions: abruptly discontinuing
Extra haloperidol after long-term
pyramidal use.
symptoms -Inform patient that
(EPS) drowsiness generally
Akathisia, subsides with continued
acute therapy.
dystonia, -Warn the patient to avoid
tardive tasks that require mental
dyskanesia, alertness or motor skills until
and drug- his response to the drug has
induced been established.
Parkinsonis -Urge the patient to avoid
m alcohol
-Children are more
susceptible to dystonias
-Haloperidol use is not
recommended for children
younger than three year

25
 A decreased dosage is
recommended for the elderly
who are more susceptible to
extra pyramidal and
antichollnergic effects,
orthostatic hypotension and
sedation or a history of
seizures. Haloperidol may be
given undiluted by IV push.
Give IV push at a rate of 5
mg/minute
-Prepare haloperidol
deaconate IM injection using
a 21-guage needle. Slowly
inject the drug deep into the
upper outer quadrant of the
gluteus Maximus effects.
-Monitor the patient for fine
tongue movements, mask
like facial expression,
rigidity and tremor
-The therapeutic serum level
for haloperidol is 0.2 to 1
µg/ml and the toxic serum
level is greater than
1 µg/ml.

Agranulocyt -Monitor CBC,

osis ,anemia ESPECIALLY if patient has
, low WBC, HISORY of drug
Leukocytosi induced leukopenia or
s, neutropenia .
leukopenia . -Assess symptoms of
infection and provide
appropriate treatment

26
 PIMOZIDE

Trade name
Orap, Pimozoid

Classification
Antipsychotic

Dose
1-2mg po/day

Mechanism of Indication Contraindicat Side effect Nursing responsibility

action ion management of side
effect
The ability of Tourette Patient with Tremor, rigidity, -Tell patient to report
pimozide to suppress syndrom severe toxic hypersalivation, any sign symptoms of
motor and phonic CNS bradykinesia, ner neuroleptic
tics in tourettes depression or akathesia ,acute malignant and tardive
disorder is thought comatose dystonia ,tardive dyskinesia
to be primarly a states from any dyskinesia, - Patient should be
function of its cause . neuroleptic advice to report all
dopaminergic Liver disorder , malignant concurrent prescription
blocking activity blood syndrome and non prescription
.pimozide binds and dyscrasias ,and ,insomnia medication or herbal
inhibit the dopamine it should not be ,anxiety , product they are taking.
D2 receptorbin the used in confusion , - Inform patient that
CNS .act as depressive nightmares these drugs may cause
anantagonist of the disorder or ,hallucination drowsiness, and they
D2, D3and D4 parkinsonssynd ,dystonic should avoid driving or
receptors and the 5- rome ,patient reactions , operating machinery till
HT7 receptor ,it also with a history dizziness or the full effects of drug
a hERG blocker. of cardiac vertigo are known.
arrhythmias , ,weakness ,
excessive

27
sweating, body
temperature
dysregulation
,headache
,EEGchanges
,increased
incidence of
epileptic seizure
Autonomic – Urge patient to have
Dry mouth periodic eye examination
,blurred vision ,
difficulty with
accommodation,
urinary retention,
and urinary
Cardiovascular - - Monitor blood pressure
Hypotension lying and standing
,tachycardia ,and frequently document and
fluctuation in report significant
blood pressure changes.
-Instruct the patent to
rise slowly from a lying
or sitting position
Endocrine – -Patients should be
Hyperprolactine advised to speak to a
mia, amenorrhea healthcare provider if
and impotence pregnant, intend to
become pregnant, or are
breastfeeding.
Miscellaneous – -Monitor respiratory rate
urticarial , fever , asses any sign and
asthma distress and be ready for
obstructive prompt action,
jaundice , blood -Monitor vital sign and
dyscrasis , sign of any breathing
leukopenia , difficulty. Complete
dermatitis blood count before and
acnieformedema periodically during
, treatment.

28
 PENFLURIDOL

Trade Name
Semap ,Micefal , longoperidol, Uridol, flump, flumap

Classification
Diphenylbutylpiperidine antipsychotic

Dose
PO initial: 20 – 60 mg/wk.

Mechanism of Indication Contraindi Side effect Nursing responsibility

action cation management of side effect
Penfluridol binds Chronic Pre existing Central nervous -Assess therapeutic response.
to the dopamine schizophre central system – Monitoring for side effects,
receptor (D1, nia, neurons Epilepsy in including mental state
D2, and D3 & paranoid system, people with low assessment.
D4). It exerts its symptomat depression threshold for -Patients must not drive or
antipsychotic ology or coma seizures, operate machinery until they
activity by marked liver agitation, know how this drug affects them.
blocking the impairment anxiety, -Alcohol can add to the
dopamine depression and drowsiness caused by this drug.
projections in the emotion. Inform patients that it may take
limbic system several weeks to benefit from the
and in full therapeutic effects. Patients
mesocortical should not stop taking penfluridol
area. suddenly without taking medical
Peripherally and advice.
centrally it acts Gastrointestinal during therapy .take fluid orally
as a competitive – Constipation, prevent dehydration ,apply
Dopamine diarrhea, loss of glycerin on lips to prevent dry lip

29
antagonist. appetite, dry -Chew xylitol chewing gum
mouth, nausea chewing gum .
and vomiting. -Increase water intake and fibre
content in diet .eat moist food
such fruit vegetable and soup
.electrolyte intake to avoid
dehydration.
Metabolic – -Eat small, frequent meals rather
Weight gain, than larger meals three times, Eat
increased saliva low sugar, low acid food, chew
and decrease in low sugar candy.
blood sugar.

Genitourinary – -These changes are due to raised

Increased risk of levels of a hormone called
breast cancer, prolactine, and it can be very
absence of distressing
menstrual cycle
and retention of
urine.
Respiratory – -Monitor respiratory rate asses
Asthma. any sign and distress and be ready
for prompt action, monitor vital
sign and sign of any breathing
difficulty.
Liver – Jaundice. -Liver test and serum level to
assess liver dysfunction
Miscellaneous – - Monitor blood pressure lying
Skin rash, low and standing frequently document
blood pressure and report significant changes.
and movement Instruct the patent to rise slowly
disorders. from a lying or sitting position

Potentially Fatal -Check CBC level.

– Blood disorder,
severe heart
disease and brain
tumor.

30
 MOLINDONE

Trade Name
Moban concentrate

Classification
Dihydroindolone derivative

Dose
Initial :5omg to 75mg daily in divided dose three or four times a daily ,doses increased to 100mg
daily in 3 to 4 days as needed. Maintenance : mild psychosis 5 to 15 mg TDS or QID daily , for
moderate psychosis 10 to 25 mg TDS or QID daily , for severe psychosis 225 mg in divided dose
daily .

Mechanism of Indication Contraindication Side effect Nursing

action responsibility
management
of side effect
Act as Used to treat Patient who are in Drowsiness, dizziness -Get up slowly
occupying mental / mood coma or in a state ,blurred vision, euphoria , when rising
(antagonizing) disorder such of severe CNS Extra pyramidal symptoms from a sitting
dopamine d2 as depression (eg , tardive dyskinesia or lying
receptor sites schizophrenia, overdose of Stiff muscles ,severe position.
in reticular reduce alcohol , muscles spasm ,twisting Avoid to use
limbic system aggressive barbiturates , neck , arching back ,eyes marijuana aura
in the brain , behaviour, narcotics , etc) rolling ,tremor ,drooling alcohol can
thus decrease brain tumor ,a ,mask like expression of make more
decreasing hallucination, high prolactine the face , Depression dizzy drowsy.
dopamine balance of level , very low ,fainting

31
activity .this certain natural level granulocytes CV – ORTHOSTATIC -Advice patient
leads to a substances , low level of HYPOTENSION, to rise slowly
reduction of dopamine in white blood cell tachycardia , unstable from lying or
spontaneous the brain. ,liver problem, Blood pressure. sitting position
locomotion muscles rigidity to minimize
and and confusion , orthostatic
aggressiveness blockage of the hypotension .
, suppression stomach or -Drug should
of conditioned intestine , also be used
response , cautiously in
antagonism of patient with
stereotyped cardiovascular
behaviour and disease.
hyperactivity
induced by Eye – blinking or eyelid -Give oral
amphetamines spasm , blurred vision ,dry solution
mouth , inability to moves undiluted or
eyes . mixed with
water,
GI –constipation , nausea carbonated
beverages ,
fruit juice or
milk .give fiber
diet and plenty
of fluid ,enema
if needed.

Rare but serious side effect -Liver function

- fever ,persistence sore test done for
throat ,sign of liver check liver
problem problem and
impairment
-Advise to
monitor
temperature
and sign of
infection

HEME – -Monitor CBC

agranulocytosis,leukopenia often during
, neutropenia first few
months, if
history of low
WBC count.

32
 LOXAPINE

Trade name
LAXITANE , ADASUVE, loxapac , loxitane c , loxitaneIM

Classification
Dibenzoxapine derivative

Dose
Laxitane capsule 5mg to 10 mg twice a daily, increased over 7days . Maintenance15mg to 25mg
twice daily to four times daily , maximum 250 mg daily
Adasuve – aerosol powder 10mg
I/M – 12.5 to 50 mg every 4 to 6 hr or longer maximum: 250 mg daily.

Mechanism of Indication Contraindication Side effect Nursing responsibility

action management of side effect
Treat psychotic Treatment of Blood dyscrasias CNS side effect -Assess sign of tardive
disorder by schizophrenia ,bone marrow Dizziness,faintn dyskinesia including
blocking . depression ess ,staggering involuntary protrusion of
dopamine at ,cerebrovascular gait ,shuffling tongue and chewing
postsynaptic disease ,coma , gait ,muscle movements. these signs may
receptors in coronary ,artery twitching , appear month or year after
brain .with disease , weakness loxapine therapy.
prolonged use , hypersensitivity to insomnia seizor
loxapine loxapine or its , agitation , -Observe extrapyramidal
enhances component , slurred speech , reaction or parkinsonian
antipsychotic impaired hepatic neuroleptic symptoms such as excessive
effect by function , severe malingnant salivation ,mask like face
causing drug induced CNS syndrome . ,rigidity and tremor ,
depolarization depression ,severe dystonia , especially in 1st few days of
blocked of hypertension or pseudoparkinso treatment
dopamine tracts hypotension . n
,resulting in
decreased

33
dopamine CVS – Advise to patient change
neurotransmissi orthostatic position slowly to minimize
on. hypotension orthostatic hypotension.

EENT – blurred Urge patient to have periodic

vision , dry eye examination during
mouth therapy .take fluid orally
prevent dehydration ,apply
glycerin on lips to prevent
dry lip
Chew xylitol chewing gum.

GI – .Instruct the patient to dilute

constipation , loxapine oral solution with
ileus , nausea , orange and grape fruit juice
vomiting weight just before taking .tell patient
gain not to take antacids and
antidiarrheal within 3 hrs of
loxapine .caution patient to
avoid alcohol while taking
loxapine
SKIN – Advise patient to avoid
photosensitivity prolonged sun exposure and
(mild) rash. to use sunscreen to minimize
risk of photosensitivity.

GU – menstrual These changes are due to

irregularity , raised levels of a hormone
sexual called prolactin, and it can be
dysfunction , very distressing
urine retention

CLOZAPINE

34
Trade Name
Clozaril ,Fazaclo , Versacloz

Classification
Dibenzidiazepine derivative

Dose
Initial: 12.5mg once or twice daily .increased by 25 to 50 mg daily to 300 to 450 mg daily in divided
doses by the end of 2wk .dosage titration shouldn’t exceed 100mg twice per wk. Maximum: 900mg
daily

Mechanism of Indicatio Contraindic Side effect Nursing responsibility

action n ation management of side effect
Produce To treat Angle – CNS – Agitation, Analyses of post marketing
antipsychotic severe clouser , anxiety , ataxia , safety databases suggest that
effects by schizophr glaucoma , confusion , clozapine is associated with an
interfering with enia coma , depression , increased risk of fatal
dopamine unrespons history of dizziness , myocaeditis, especially during,
binding to ive to dozapine – drowsiness , but not limited to, the first
dopamine – standard induced dystonia , fatigue month of therapy, in patients in
especially D4 – drugs; to agranulocytos , fever, headache , whom myocarditis is suspected,
receptors in the reduce is or severe , insomnia , clozapine treatment should be
limbic region of sisk of granulocytop myoclonic jerk , promptly discontinued.
the brain and by recurrent enia , seizur Seizures have been associated
antagonizing suicidal hypersensitivi with the use of clozapine. Dose
adrenergic, behaviour ty ,to appears to be an important
cholinergic, in dozapine or predictor of seizures, with a
histaminic, and schizophr its greater likelihood at higher
serotoninergic enia or components , clozapine doses. Caution should
receptors. schizoaffe myloprolifera be used when administering
ctive tive disorder , clozapine to patients having a
disorder. severe CNS history of seizures or other
depression , predisposing factors. Patients
uncontrolled should be advised not to engage
epilepsy in any activity where sudden loss
,WBC count of consciousness could cause
below serious risk to the themselves or
3,500/mm others.
CV – cardiac -Advice patient to rise slowly
arrest, arterial and from lying or sitting position to
ventricular minimize orthostatic
fibrillation , chest hypotension .drug should also be
pain , DVT , used cautiously in patient with
orthostatic cardiovascular disease or a
hypotension family history of prolonged QT
,tachycardia . syndrome because clozapine
therapy may increase the QT
interval

35
EENT –blurred Instruct patient to peel foil back
vision, dry mouth to remove tablet and then to
, increase nasal immediately place tablet in
congestion , mouth and it dissolve before
increase swallowing .explain that no
salivation . water is needed.

ENDO : -Check blood glucose level

ketoacidosis , during therapy.
severe -Done LFT , abdominal
hyperglycemia . examination , check blood
GI –abdominal glucose level , advise to take
discomfort , acute fiber diet and plenty of water
pancreatitis ,
anorexia ,
constipation ,
diarrhea ,
heartburn
,jaundice , nausea
,vomiting
HEME : elevated -Inform patient that he’ll need
hemoglobine , blood test .Review evidence of
thrombocytopenia dyscrasias (fatigue , fever , sore
, thrombocytosis throat , weakness ) develop mild
leukopenia or granulocytopnia
check count twice weekly until
normal

MS – backpack, -Monitor patient and be alert for

leg pain ,muscles complaint of neck spasm , which
spasm, sometimes may progress to
myasthenia throat tightness , trouble
syndrome swallowing or breathing ,and
RESP- dysnea, tongue protrusion
LRTI, pleural
effusion,
respiratory arrest
SKIN – -Urge the patient to avoid
photosensitivity exposure to sunlight and any
,purities , rash , condition that may cause
Stevens Johnson dehydration or overheating
syndrome, because they may increase the
urticaria risk of heat stroke

36
 RISPERIDONE

Trade Name
Sizodon

Classification
Atypical antipsychotic—serotonin dopamine antagonists

Dose
Oral: 0.5-6 mg/day

Mechanism of Indication Contraindi Side effect Nursing responsibility

action cation management of side effect
Antiserotonergic, Positive and Hypersensiti acute renal -Before beginning risperidone
antiadrenergic negative vity, heart failure, Liver therapy assesses or blood urea
and symptoms of diseases, dysfunction nitrogen levels and serum
anthistaminergic schizophrenia, epilepsy, alkaline phosphate
actions. It has other hyperprolact , bllirubin, Creatinine, renal and
less action as Psychosis, inemia, hepatic functions. liver function
anadopaminergic schizoaffectiv parkinsonis test result
, e symptoms m, renal and
especially D2 hepatic CNS: -Assess for behavioral and
receptors impairment Somnolence, emotional status Instruct the
seizures, patient to change positions
headache, slowly to minimize the drugs
dizziness hypotensive effects.

-Urge the patient to avoid

alcohol during risperidone
therapy

37
CVS: -The elderly are more
Orthostatic susceptible to orthostatic
hypotension, hypotension. They may require
dizziness, a dosage adjustment because of
tachycardia age-related renal or hepatic
and syncope, impairment.
irregular pulse
or blood -Monitor patients BP, heart
pressure, rate, and weight gain
tachycardia,
diaphoresis,
cardiac
arrhythmias

Other adverse -Fiberdiet, take measure to

reactions: reduce constipation.
weight gain, -Urge the patient to notify the
constipation, physician if he or she
erectile experiences altered gait,
dysfunction, difficulty in breathing
vomiting rash, palpations, pain or swelling in
abdominal breasts

Rare reactions -Observe t he patient for fine

include: tongue movements, which may
tardive be the first sign of irreversible
dyskinesia tradive dyskinesia
(characterized
by tongue -Monitor patient or neuorleptic
protrusion, malignant syndrome., severe
putting of the dizziness or fainting, trembling
cheeks fingers, unusual movements,
chewing or rash or visual changes.
puckering of Inform the patient that
the mouth risperidone may cause
muscle dizziness.
rigidity,
change in -Warn the patient to avoid tasks
mental status that require mental alertness or
motor skills until his response
to the drug has been
established.

38
 OLANZAPINE

Trade Name
Zyprexa

Classification
Atypical antipsychotic—serotonin dopamine antagonists

Dose
Oral: 5-t0 mg/day.

Mechanism of Indication Contraindic Side effect Nursing responsibility management of

action ation side effect
Antagonize Positive and Narrow Central -Assess the patient’s behaviour and
alpha- negative angle nervous emotional status. the day to reduce
adrenergic, manifestations glaucoma, system:
dopamine of paralytic Somnolence, -Administer or instruct patient to take
histamine schizophrenia, ileus, agitation, drug early in Insomnia,
muscarinic and schizoaffectiv urinary out insomnia,
serotonin e disorders, flow headache,
receptor bipolar mania obstruction nervousness,
anticholinergic, . hostility.
histaminic and Other adverse Instruct to avoid caffeinated drinks or
CNS reaction: food. Warm the patient to avoid tasks
depressant rare reactions requiring mental alertness or monitor
effects Include skills until his response to the drug
seizures, has been established
neuroleptic Causation the patient against abruptly
malignant discontinuing the
syndrome, drug or increasing the dosage.
EPS. Inform the patient that drowsiness
generally subsides with continued
therapy.

39
Impaired liver -Obtain liver function test results, as
function ordered before beginning olanzapine
treatment. Use olanzapine cautiously
in patient with a hepatic impairment,
cerebrovascular

Cardiovascula -Hypersentivity disease,

r system: cardiovascular disease, history of
Orthostatic seizures and conditions predisposing
hypotension. patients to hypotension such as
Tachycardia, dehydration, hypovolemia, use of
syncope, antihypertensive.
dizziness.
-Monitor the patient for blood pressure
instruct the patient to take olanzapine
as ordered.

-Caution the patient to notify the

physician, if she becomes pregnant or
intends to become pregnant during
olanzapine therapy

Weight gain, -Advise the patient to avoid

constipation dehydration, particularly during
,dry mouth , exercise exposure to extreme heat; and
concurrent use of medication that
cause dry mouth or other drying
effects.
-Suggest taking sips of tepid water and
chewing sugarless gum to help relieve
dry mouth.
-Instruct the patient to maintain a
healthy diet and exercise program to
prevent weight gain.

40
 QUETIAPINE

Trade Name
Serequel

Dose
Children and adolescents 100-350 mg/day, Adults-300 to 400 mg in 2-3 divided doses in a day.

Classification
Atypical antipsychotic agent, Dibenzothiazepine

Mechanism of Indication Contraindication Side effect Nursing responsibility

action management of side
effect
Exact mechanism Treatment of Use with caution in Headache, -Monitor for side effects
of action is schizophreni patients with depression Instruct the patient
unknown, it has a, Parkinson's disease, somnolence, To take medication
been proposed that schizoaffecti hemodynamic dizziness, along with the food,
this drugs ve disorders, instability, prior dystonia regularly on same time,
antipsychotic mania, myocardial ,extrapyramidal -Urge the family
activity is bipolar infarction, reaction member and care giver
mediated through disorders, hypercholesterolem ,hypertonia to watch
a combination of autism, ia, thyroid disease, ,hyperthermia patients closely for
dopamine type psychosis Seizures, hepatic ,lethargy suicidal tendency when
2(D2) and impairment, renal ,amnesia therapy stats or dosage
serotonin type 2 or respiratory ,suicidal changes ,
(5-HT2) diseases. Should ideation ,tardive
antagonism not be used for dyskinesia -Do not suddenly stop
patients with the medicine
hypersensivity to Drug may cause
quetiapine, bone drowsiness avoid
marrow blood driving, doing other
dyscrasias, Severe activities until you see
hepatic aisease or how this medicine

41
coma. Marrow affects you
suppression, Avoid alcohol, take
plenty of oral fluids.

CV – -Use quetiapine
cardiomyopathy cautiously in patient who
,hypercholester have history of
olemia cardiovascular disease ,
,orthostatic -Advise to patient
hypotension change position slowly
,palpitation , to minimize orthostatic
hypotension .
Encourage patient on
long term therapy to
have regular eye
EENT - dry examination so that
mouth ,nasal cataract can be detected
congestion .advise to patient
,rhinitis improve fluid intake
,pharyngitis and take electrolyes for
prevention from
dehydration.
andhypovolemia.
ENDO – *assess patient for
galactorrhea hypothyroidism because
,hyperglycaemi drug can cause dose-
a ,inappropriate dependent decrease in
ADH secretion total and free
, thyroxin(T4) levels ..
*monitor patients blood
glucose and lipid level
routinely ,as order
because drug increase
risk of hyperglycaemia
and
hypercholesterolemia
MS- dysarthria Monitor patient for
,muscles abnormal muscle
weakness , contraction during few
rhabdomyolysis days of drug therapy

42
 HEME – check CBC first few
agranulocytosis months of
,decrease therapy,asorderd, in
platelet ,count patient with low WBC
,neutropenia , count or a history of
leukope drug induced
haematological problem
.If count drop or patient
develop fever or other
sign if infection ,notify
and discontinue drug
therapy ,and provide
supportive care
GI – Instruct patient to take
constipation drug with food to reduce
,indigestion stomach upset , advise to
,anorexia take plenty of water
,pancreatitis ,take small meal diet.
*caution patient to avoid
consuming alcoholic
beverages because they
can increase dizziness
and drowsiness.

ZIPERASIDONE

Trade name
Zeldex, Ziperasidone Hydrochloride, Ziperasidone Mesylate

Classification
Atypical Antipsychotic D (3) dopamine receptor antagonist.

43
Dose
Adult- 20-100 mg twice daily orally, intramuscular injection 10 mg in every 2 hours or 20 mg in
every 4 hours.

Mechanism of action Indication Contraindication Side effect Nursing responsibility

management of side
effect
Ziprasidone's Schizophrenia Hypersensitivity to Somnolence, Monitor serum
antipsychotic activity , acute mania, ziprasidone, recent headache, potassium and
is likely due to a bipolar myocardial nausea, magnesium levels
combination of its affective infarction, history hypertension, Potential for
antagonistic function disorder, also of arrhythmias, postural extrapyramidal
at D2 used for heart failure, use of hypotension, symptoms, fever,
receptors in the depression, antiarrhythmic. Use extrapyramida confusion, stiffness
mesolimbic pathways anxiety, with caution in l symptoms, should be promptly
and at 5H12A aggression patients with rash evaluated for
receptors in the dementia, seizures. dysmenorrhoe neuroleptic malignant
frontal cortex. attention al, syndrome
Alleviation of deficit constipation, Drug should not be
positive hyperactivity abdominal administered to a
symptoms is due to disorder, pain patient who recently
antagonism at D2 obsessive had heart attack or
receptors in the compulsive congestive heart
frontal cortex. disorder, failure
Alleviation of autism, post-
positive traumatic
symptoms is due to stress disorder
antagonism at D2
receptors while relief
of negative symptoms
is due to 5HT2A
antagonism.

RESERPINE

44
Trade Name
Novoreserpine ,Reserfia , serpalan , serpasil

Classification
Rauwolfia alkaloid

Dose
Adult: 0.1 to 0.25 mg daily
Children: 0.005 to 0.02 mg/kg daily once daily or in divided doses twice a daily

Mechanism of action Indicatio Contraindi Side effect Nursing responsibility

n cation management of side effect
Reserpine reduce blood To treat Active CNS – anxiety -If patient has a history of
pressure by decreasing hypertensi peptic ulcer depression depression use reserpine
norepinephrine store in ve ,electroconv ,dizziness, cautiously because it may
presynaptic sympathetic ulsive drowsiness , cause depression masked as
neurons. Nerve impulse therapy , headache , somatic complaints.
activates a sympathetic hyper nightmare ,sleep
neuron, the nerve ending sensitivity disturbance , -Caution patient about
release norepinephrine to reserpine nervousness possible drowsiness and
which stimulate alpha and or its ,syncope advise him to avoid
beta receptors on target component ,weakness potentially hazardous
cell membrane ,mental activities until drugs ‘s
,stimulation of alpha may depression , CNS effects are known
produce vasoconstriction ulcerative
CV - Arrhythmias -Monitor blood pressure
,stimulation of beta colitis
, such as frequently during drug
receptor may increase
bradycardia , therapy.
heart rate & force of
chest pain
myocardial contraction
,peripheral edema
,which circulatory
instability even if GI – abdominal -Instruct to patient to take
withhold before cramp or pain , drug with food or milk to
procedure . anorexia , diarrhea minimize stomach upset
, increase gastric
secretion , melena
, nausea ,
vomiting

45
 ARIPIPRAZOLE

Trade Name
Aripiprex

Classification
psychotropic drug—atypical antipsychotic, dopamine, serotonin agonist and antagonist

Dose
Available forms
Tablets: 10, 15, 20, 30 mg
Adults: 10-15 mg/day PO
pediatric patients: Safety and efficacy not established

Mechanism of Indication Contraindica Side effect Nursing responsibility

action tion management of side effect
Produce Used in the Contraindicat CNS – abnormal *watch patient closely for
antipsychotic treatment of ed in the gait , agitation , suicidal tendencies ,
effect through schizophrenia, presence of akathisia, anxiety particularly when therapy
partial agonist bipolar allergy to , conative and started because depression
and antagonist disorder, aripiprazol, motor impairement may worsen temporarily
actions. major during , depression , during these time .use
aripiprazole acts depressive lactation dizziness, dystonia cautiously in elderly patient
as a partial disorder (as an period. Use , fatigue , fever , because cerebrovascular
agonist at add on cautiously in hallucination, effect , such as stroke and
dopamine treatment), tic the presence headache , transient ischemic attack
especially D2 disorders, and of suicidal intracranial .advice the patient to get up
receptors and irritability ideation, hemarrage, mania , from bed and chair slowly.
serotonin associated pregnancy, neuroleptic avoid driving because of
especially 5HT with autism. breast feeding malingnanat , dizziness, advise to patient
1A receptors .the . cerebral paranoia, to not to consume alcohol
drug acts as an vascular schizophrenia , during therapy
antagonist at 5- disease, seizure
HT2A serotonin known
receptor . cardiovascular
disease,

46
 seizures Cardiovascular – -Use cautiously in patient
disorders, bradycardia, chest with CV disease.
patients with pain ,
Alzheimer's cardiopulmonary -Advice the patient to get up
disease, arrest , DVT from bed and chair slowly ,
dysphasia ,HYPERTENSIO monitor blood pressure and
(risk for N ,orthostatic documentation.
aspiration hypotension
pneumonia
GI – abdominal -Monitor patient for
discomfort , difficulty in swallowing or
constipation , excessive somnolence ,
decrease appetite which could predisposing to
difficulty accidental injury or
swallowing GI aspiration
bleeding , nausea ,
vomiting

AMISULPRIDE

Trade name
Amgrace, Cyme, Bipo Life, Zonapride, Zulpride, Solian

Classification
Second generation atypical antipsychotics

Dose
It comes as a tablet to take by mouth on an empty stomach, IM injection should be given into large muscle. For adult less than
15 years, the recommended dose 400-800 mg/day in divided doses PO. Maximum dose is 1.2 g/day. Intramuscular
injection the recommended dose is 400mg/day.

47
Mechanism of action Indication Contraindication Side effect Nursing responsibility
management of side
effect
Amisulpride, a substituted For the Caution should be CNS – -Watch patient closely for
benzarnide derivative is a treatment of exercised in Extrapyrami extrapyramidal symptoms,
second-generation schizophrenia, patients with dal particularly when therapy
(atypical) antipsychotic. schizoaffectiv history of diabetes, symptoms started.
AmisuliPhide binds e disorders, epilepsy, brain ,insomnia, Caution should be exercised in
selectively to D2 bipolar damage, anxiety patients with history of
dopaminergic receptors affective Parkinson's agitation, sugar, epilepsy, brain
and D3 receptors, but does disorders and disease, heart dizziness, damage, Parkinson's
not have any affinity for other disease, stroke, restlessness dementia, heart disease,
,
pl, adrenergic cholinergic, psychotic dementia, high abnormal heart rhythm,
serotonergic or Hi disorders. blood pressure, disturbances in blood
(histaminergic receptors). alcoholism, electrolytes level, stroke,
It shows greater affinity elderly, pregnancy Dementia, high blood
for limbic doparminergic and lactationon period. pressure, smoking habit,
receptors than for striatal - It should not be alcoholism, elderly, and
structures suggesting better used in following during pregnancy .
neurological tolerability patients: Who are -Advice the patient to get
compared with classical allergic to up from bed and chair
neuroleptics which block amisulpride, breast slowly. avoid driving
all dopamine receptors cancer, tumor on , because of dizziness
equally. High their adrenal gland -Advise to patient to not
doses (400-800 mg) inhibit (prolactine to consume alcohol during
hyperdopaminergic dependent therapy
s
ymptomatology and tumors), taking Cardiovasc Use cautiously in patient
control psychotic levodapa ular – with CV disease. .
symptom% low medicines, during bradycardia advicethe patient to get up
doses (50-300 mg) have pregnancy and ,chest pain from bed and chair slowly
an effect on negative lactation period, , , monitor blood pressure
symptoms. children before the cardiopulm and documentation.
onset of puberty. onary
Pharmacokinetics arrest ,
Amisuipride is absorbed DVT
rapidly, within 3-4 hours ,HYPERT
of oral administration. ENSION
Drug is excreted through. ,orthostatic
urine mainly as unchanged hypotensio
drug, the elimination half- n
life is approximately 12
hours, plasma protein GI – Monitor patient for
binding is low. abdominal difficulty in swallowing or
discomfort excessive somnolence ,
,constipatio which could predisposing
n ,decrease to accidental injury or
appetite aspiration
,nausea
,vomiting

48
ANTIDEPRESSANT DRUG

49
 ANTIDEPRESSANT

Antidepressants are those drugs, which are used for the treatment of depressive illness. It
relieves symptoms of depression, social anxiety disorders and anxiety disorders, seasonal anxiety
disorder and dysthymia, or mild chronic depression as well as other conditions.
They aim to correct chemical imbalance of neurotransmitters in the brain that are believe to be
responsible for changes in mood and behaviour. These are also called as mood elevators or
thymoleptics.

HISTORY OF ANTIDEPRESSANT
Antidepressants were first developed in the 1950s. Their use has become progressively more
common in the last 20 years.
Imipramine was the first discovered antidepressant.
iproniazid and antitubereulosis medications were found to have antidepressant effects.

INDICATIONS FOR ANTIDEPRESSANT

DEPRESSION:
 Depressive episode
 Dysthymia
 Reactive depression
 Secondary depression
 Abnormal grief reaction.

CHILDHOOD PSYCHIATRIC DISORDERS:

 Enuresis
 Separation anxiety disorder
 Somnambulis
 School phobia
 Night terrors.

OTHER PSYCHIATRIC DISORDERS:

 Panic attack
 Generalized anxiety disorder
 Agoraphobia, social phobia
 OCD with or without depression
 Eating disorder
 Borderline personality disorder
 Post-traumatic stress disorder
 Depersonalization syndrome.

50
CONTRAINDICATIONSFOR ANTIDEPRESSANT
Antidepressants are contraindicated in individuals with hypersensitivity and also
following conditions.
 Recent myocardial infarction or cardiac disease.
 Severe renal or hepatic impairment.
 Angle-closure glaucoma.

PHARMACOKINETICS
Antidepressants are highly lipophilic and protein-bound. The half-life is long and usually
more than 24hours. It is predominantly metabolized in the liver.

MECHANISM OF ACTION
These drugs elevate mood and alleviate other symptoms associated with moderate-to
severe depression. These drugs ultimately work to increase the concentration of norepinaphrine,
serotonin and dopamine in the body. This is accomplishedby the brain by blocking the reuptake
of these neurotransmitters by the neurons (trycles, tetracyclics, SSRI, etc). It also occurs when an
enzyme, monoamine oxidase that is known to inactivate norepinephrine, serotonin and dopamine
is inhibited at various sites in the nervous system (MAOLI).

TYPES OF ANTIDEPRESSANT
 First generation antidepressants or tricyclic antidepressants (TCA) – drug of choice for
severe depression.
 Second generation antidepressants or selective serotonin reuptake inhibitors (SSRI) –
drug or choice for mild to moderate depression.
 Serotonin norepinephrine reuptake inhibitors (SNRI).
 Monoamine oxidase inhibitors (MAOI)
 Atypical antidepressants.

TRICYCLIC ANTIDEPRESSANTS (TCAs)

Tricyclic antidepressants are a class of medications that are used primarilyas
antidepressants. TCAs were discovered in the early 1950s and were marketed later in the decade.
They are named after their chemical structure, which contains three rings of atoms are a
closely related group of antidepressant compounds.

EXAMPLES OF DRUGS:
 Imipramine
 Amitriptyline
 Clomipramine

51
 1. IMIPRAMINE:

Trade Name
Antidep, tofranil

Classification
Tertiarytricyclic antidepressant drugs

Dose for depression

Adult: 75-100mg/day orally, maximum 300 mg/day.
Child: 1.5 mg/kg/day, may increase by 1 mg/kg/day

Mechanism of Indication Contraindications Side Effects Nursing

Action Management
The tricyclic  Depressive Cardiac disorders,  Autonomic: Dry  Monitor for HR
antidepressants episodes, acute recovery mouth, and BP
are also called as depression with period after MI, constipation, frequently.
monoamino psychotic use within 14 days urinary  Monitor for
reuptake symptoms, of MAOIs. retention, potential signs of
inhibitors dysthymia,  Severe renal or mydriasis, toxicity- QRS
(MARIS). Their reactive hepatic orthostatic prolongation,
main modes of depression, impairment hypotension, arrhythmias,,
action are: secondary importence, hyptension etc.
 Blocking the depression due to delirium,  During first 2 wks
reuptake of hypothyroidism, blurred vision, of therapy , older
norepinephrine cushing’s urinary adults may
(NE) and syndrome, hesitancy. develop confusion
serotonin (5-HT) abnormal grief  CNS: , restlessness. Etc
at the nerve reaction. sedation, tramors,  Weigth patient
terminals, thus  Childhood withdrawal under standard
increasing NE psychiatric syndrome, conditions
and 5-HT level at disorders, seizures. biweekly.
receptor site. enuresis, phobia,  CVS:  Monitor diabetic
 Regulation of the separation tachycardia,
52
beta adrenergic anxiety, arrhythmias, patients for loss of
receptors. somnambulism, direct myocardial glycemic control.
night terrors. depression.  Don not drive or
 Other psychiatric  Allergic: engage in other
disorders like Agranulocytosis, potentially
panic attacks, cholestatic hazardiousactivity
agophobia, social jaundice. .
phobia,  Other  Avoid exposure to
obsessive reactions: Weight strong sunlight.
compulsive gain, tiredness,  Do not breast
disorder, drowsiness, feed while taking
aggression in insomnia, acute this drug without
elderly, post- organic consulting
traumatic stress syndrome. physician.
disorder,
depersonalizatio
n.
 Medical
disorders:
chronic pain,
migraine, peptic
ulcer.

2. AMITRIPTYLINE

Trade Name
Elavil, Endep, Levate

Classification
Tertiary Tricyclic antidepressant drugs

53
 Dosage
30-100mg per day orally, may increase up to 150-300 mg/day.

Mechanism of Indications Contraindication Side Effects Nursing Management

Action
A tricyclic Depression, relief Cardiac disorders, Dizziness, Take drug exactly as
antidepressant that of neuropathic acute recovery somnolence, dry prescribed; do not stop
blocks the pain, such as period after MI, mouth, abruptly or without
reuptake of experienced by use within 14 days orthostatic consulting health care
neurotransmitters, patients with of MAOIs. hypotension, provider.
such as diabetic headache,  Avoid using
norepinephrine neuropathy or increased alcohol, other sleep-
and serotonin at post therapeutic appetite, weight inducing drugs, OTC
CNS presynaptic neuralgia, gain, nausea, drugs.
membranes, treatment of unusual fatigue,  Avoid
increasing their bulimia nervosa. unpleasant taste, prolonged exposure to
availability at blurred vision, sunlight or sunlamps;
postsynaptic confusion, use a sunscreen or
receptor sites. constipation, protective garments.
arrhythmias, fine  You may
muscle tremors, experience these side
anxiety, diarrhea, effects: Headache,
diaphoresis, dizziness, drowsiness,
heartburn, weakness, blurred
insomnia. vision (reversible; if
severe, avoid driving
and tasks requiring
alertness while these
persist); nausea,
vomiting, loss of
appetite, dry mouth (eat
frequent small meals;
use frequent mouth
care and suck on
sugarless candies);
nightmares, inability to
concentrate, confusion;
changes in sexual
function.
 Report dry
mouth, difficulty in
urination, excessive
sedation.

54
 3. CLOMIPRAMINE

Trade Name
Anafranil

Classification:
Tertiary Tricyclic antidepressant drugs.

Dosage
25 mg, 50 mg, 75 mg
Dose considerations for OCD:
Adult: 25mg orally once /day, gradually increase 100mg /day, may increase further upto 250
mg /day
Pediatric: 10 yrs and older 25 mg once /day, increase to max. 3mg/kg/day

Mechanism of Indications Contraindications Side effects Nursing

Action management

A tricyclic Obsessive-  Cardiac Somnolence,  Use with

antidepressant compulsive disorders, acute fatigue, dry mouth, caution during
that blocks the disorder, recovery period blurred vision, pregnancy, if benefit
reuptake of depression, after MI, use within constipation, overweigh risk.
neurotransmitte phobias, pain 14 days of MAOIs. sexual dysfunction,  Its distributed
rs, such as disorder.  Should be ejaculatory failure, in breast milk so
norepinephrine avoided during impotence, weight advice to do not
and serotonin at pregnancy, the drug gain, delayed nurse.
CNS should be given micturition,  Monitor for
presynaptic cautiously in orthostatic, suizers
membranes, patients with hypotension,  Monitor for
increasing their hepatic and renal diaphoresis, and report the signs
availability at disease. impaired of neurolpetic
postsynaptic concentration,
55
receptor sites. increased appetite, malignant syndrome.
urine retention, GI  Look for
disturbances, sedation and vertigo.
seizures,  Notify
orthostatic physician for fever
hypotension, and sore throat .
dizziness,  Mens should
tachycardia, be acknowledge that
palpitation and the durg may cause
arrhythmias and impotence or
hyperpyrexia. ejaculation failure.

4. DOTHIEPIN

Trade Name:
Prothiaden, others

Classification:
TCA

Dosage:
25mg, 50mg, 100mg, 150 mg
Adult: PO start at 50 mg, bid or tid , may increase on third day to 100mg tid
Geriatric:PO 25mg hs,may increase to 50-150mgmg/day, max. 300mg/day

Mechanism of Indications Contraindicati Side effects Nursing

action ons management
The Clinical effect Depression of  Epilepsy  Drowsiness  Supervise
is due to any aetiology. as it canlowe  Extrapyramidal patient closely
potentiation of Psychogenic the seizure symptoms during therapy for

56
adrenergic facial pain. threshold.  Tremor suicidal ideation and
synapses by  TCAs  Disorientation potential serious
blocking uptake of should not be  Dizziness adverse effects.
norepinephrine at used  Paresthesias  Report
nerve endings. concomitantly  Alterations immidiately for
Also block uptake or within 14 to ECG patterns signs for neuroleptic
of serotonin. days of  Dry mouth malignant
treatment with  Sweating syndrome, fever ,
monoamine sweating .
 Urinary retention
oxidase  Monitor
 Hypotension
inhibitors due to weight at weekly
 Postural
the risk for
hypotension  Minimize
serotonin alcohol intake.
 Tachycardia
syndrome.  Rinse mouth
 Acute  Palpitations
frequently with clear
recovery phase  Arrhythmias
water, especially
following  Conduction after eating , to
mycocardial defects relieve mouth
infarction as  Increased or dryness.
TCAs may decreased libido  Do not take
produce  Nausea any prescription or
conducation  Vomiting OTC drugs .
defects and  Constipation  Consult to
arrhythmias.  Blurred vision physician regarding
LESS COMMON breast feed.
ADVERSE
EFFECTS:-
 Disturbed
concentration
 Delusions
 Hallucinations
 Anxiety
 Fatigue
 Headaches
 Restlessness
 Excitement
 Insomnia
 Hypomania
 Nightmares
 Peripheral
neuropathy
 Ataxia
 Incoordination
 Seizures

57
 SELECTIVE SEROTONIN REUPTAKE INHIBITION [SSRI]:
Selective serotonin reuptake inhibitors (SSRIS) are a class of drug they are typically used
as antidepressants in the treatment of major depressive disorder and anxiety disorders.

EXAMPLE OF DRUGS:
 Fluoxetine
 Sertraline

1. FLUOXETINE

Trade Name:
Auscap, Fluohexal, Lovan, Novo-Fluoxetine, Prozac.

Classification
Antidepressant – Serotonin – Specific reuptake inhibitors .

Dosage
Initially, 20 mg each morning. If therapeutic improvement does not occur after 2 weeks,
gradually increase to a maximum of 80 mg/day in two equally divided doses in morning and at
noon.

Mechanism Indications Contraindication Side Effects Nursing management

of Action

Selectively Depression Hypersensitivity, Headache, Notify physician of intent

inhibits obsessive- severe hepatic or nervousness, to become pregnant.
serotonin compulsive renal impairment, insomnia, Notify physician of any
uptake in the disorder, panic pregnancy, lactation drowsiness, rash; possible sign of a
CNS, disorder and and history of anxiety, serious group of adverse
enhancing other anxiety seizures. seizures, rarely effects.

58
serotonergic disorder, EPS, apathy, Do not drive or engage in
function. bulimia anorexia, potentially hazardous
nervosa, nausea, activities until responseto
premenstrual diarrhea, drug is known; especially
dysphonic dyspepsia, and if dizziness noted.
disorder, sexual Monitor blood glucose
treatment of dysfunction. for loss of glycemic
hot flashes. control if diabetic.
Note: Drug may increase
seizure activity in those
with history of seizure.
Do not breast feed while
taking this drug without
consulting physician

2. SERTRALINE

Trade Name
Zoloft

Classification
Antidepressant – Serotonin – Sepcific reuptake inhibitors

Dosage
50-200mg

Mechanism of Indications Contraindication Side Effects Nursing

Action managemnent
Selectively inhibits Depression Hypersensitivity, Headache,  Supervise
serotonin uptake in obsessive- severe hepatic or nervousness, patients at risk for
the CNS, enhancing compulsive renal impairment, insomnia, suicide closely
serotonergic disorder, panic pregnancy, lactation drowsiness, during initial therapy.
59
function. It blocks disorder and and history of anxiety,  Monitor for
the reuptake of the other anxiety seizures. seizures, rarely worsening of
neurotransmitter disorder, EPS, apathy, depression or
serotonin at CNS bulimia anorexia, emergence of
neuronal nervosa, nausea, suicidal ideation.
presynaptic premenstrual diarrhea,  Monitor older
membranes, dysphonic dyspepsia, and adults for fluid and
increasing its disorder, sexual sodium imbalances.
availability at treatment of hot dysfunction.  Monitor
postsynaptic flashes. patients with a
receptor sites history of a seizure
disorder closely.
 Lab tests:
Monitor PT and INR
with patients
receiving concurrent
warfarin therapy

SEROTONIN NOREPINEPHRINE REUPTAKE INHIBITORS (SNRI):

Serotonin norepinephrine reuptake inhibitors are a class of antidepressant drugs that treat major
depressive disorder, anxiety disorders, obsessive-compulsive disorder, social phobia, attention-
deficit hyperactivity disorder, chronic neuropathic pain, fibromyalgia syndrome, and menopausal
symptoms.

Example of Drug
VENLAFAXIN
1) VENLAFAXIN

60
 Trade Name:
EFFEXOR

Classification:
antidepressant-serotonin norepinephrine reuptake inhibitors

Dose:
75-225mg

Mechanism of Action Indications Contraindication Side Effects Nursing

Managemnent
It works by blocking the Major High cholesterol, low Nausea,  Monitor for
transporter “reuptake” depressive amount of sodium in vomiting, worsening of
proteins for key disorder, the blood manic diarrhea, depression or
neurotransmitters afferting generalized behaviour, lever change in emergence of
mood, thereby leaving anxiety, social problem moderate to appetite or suicidal ideation.
more active anxiety, panic sever kidney weight, dry  Monitor
neurotransmitters in the disorder. impairment seizures mouth, cardiovascular
synapse. yawning, status periodically
The neurotransmitters dizziness, with
affected are serotonin and headache, measurements of
norepinephrine. tremors or HR and BP.
shaking, sleep  Lab tests:
problems Periodic lipid
(insomnia), profile.
strange  Monitor
dreams, tired neurologic status
feeling and report
excessive anxiety,
nervousness, and
insomnia.
 Monitor
weight
periodically and
report excess
weight loss.
 Assess
safety, as dizziness
and sedation are
common

61
 MONOAMINE OXIDASE INHIBITORS (MAOI):
Monoamine oxidase inhibitors (maois) are a class of drugs that inhibit the activity of one or both
monoamine oxidase enzymes: monoamine oxidase A and monoamine oxidase B. They are best
known as powerful antidepressants, as well as effective therapeutic agents for panic disorder and
social phobia.

EXAMPLE:
TRAZODONE
TRANYLCYPROMINE
ISOCARBOXAZID

1) TRAZODONE

Trade Name: (DesyrelDividose)

Dosage: oral 150mg/day.

Classification: antidepressant-monoamine oxidase inhibitors:

Mechanism of Indications Contraindication Side Effects Nursing

Action managemnent

inhibits the Treatment of Contraindicated CNS: Anger,  Monitor

presynaptic reuptake depression in with hostility, pulse rate and
of the inpatient and hypersensitivity to agitation, regularity before
neurotransmitter outpatient setting and trazodone, recent nightmares administration if
serotonin and for depressed patients MI. hallucinations, patient has
potentiates the with and without Use cautiously with delusions, preexisting cardiac

62
behavioural effects anxiety unlabeled preexisting cardiac hypomania, disease.
of the serotonin uses: treatment of disease confusion,  Note:
precursor; the aggressive behaviour, (arrhythmias, disorientation. Adverse effects
relation of these cocaine withdrawal, including CV: generally are mild
effects to clinical insomnia, alcoholism, ventricular Hypertension, and tend to
efficacy is unknown. panic disorders, tachycardia, may be shortness of decrease and
schizophrenic more likely), breath, disappear after the
disorders, drugs- lactation, syncope, first few weeks of
induced dyskinesias. pregnancy. tachycardia, treatment.
palpitations.  Observe
GI: increased patient's level of
appetite, bad activity. If it
taste in mouth, appears to be
dry mouth, increasing toward
nausea, sleeplessness and
vomiting, agitation with
diarrhea, changes in reality
constipation. orientation, report
GU: Decreased to physician.
libido, Manic episodes
impotence, have been
priapism. reported.
Musculo  Male
skeletal: patient should
musculoskeletal report
aches and inappropriate or
pains. prolonged penile
erections. The
drug may be
discontinued.

2) TRANYLCYPROMINE

63
 Trade name:parnate

Dosage: 10-60mg/day

Classification: antidepressants-monoamine oxidase inhibitors.

Mechanism of Indications Contraindication Side Effects Nursing

Action managemnent

An MAOI that Depression congestive heart Frequently:  Assess

inhibits the activity refractory to or failure (CHF), Orthostatic mental status,
of the enzyme intolerant of children younger hypotension, mood changes, and
monoamine the therapy. than 16 year, restlessness, GI upset, anxiety level
oxidase at CNS pheochromocytoma, insomnia, dizziness, frequently. Assess
storage sites, severe hepatic or lethargy, weakness, dry for suicidal
leading to renal impairment, mouth, peripheral tendencies,
increased levels of uncontrolled edema. especially during
the hypertension. Occasional: Flushing, early therapy.
neurotransmitters diaphoresis, rash, Restrict amount of
epinephrine, urinary frequency, drug available to
norepinephrine, increased appetite, patient.
serotonin and transient impotence.  Monitor
dopamine at Serious reactions: BP and pulse rate
neuronal receptor Hypertensive crisis before and
sites. occurs rarely and is frequently during
marked by severe therapy. Report
hypertension, occipital significant changes
headache radiating promptly.
frontally, neck stiffness  Monitor
or soreness, nausea, intake and output
vomiting, diaphoresis, ratios and daily
fever or chills, clammy weight. Assess
skin, dilated pupils, patient for
palpitations, peripheral edema
tachycardia and and urinary
constricting chest pain. retention.

64
 3. ISOCARBOXAZID

Trade Name:-Marplan

Dosage:- PO (Adults): 10 mg twice daily; may be increased every 2– 4 days by 10 mg, up to 40

mg/day by the end of the first wk, then may increase by up to 20 mg every wk, up to 60 mg/day
in 2– 4 divided doses. After optimal response is obtained, dose should be slowly decreased to
lowest effective amount (40 mg/day or less).

Classification:-
Therapeutic: antidepressants
Pharmacologic:monamine oxidase (MAO) inhibitors

Mechanism of Indications Contraindication Side Effects Nursing management

Action

Inhibits the Treatment of Hypersensitivity; CNS: SEIZURES, Monitor BP and pulse

enzyme depression Liver disease; dizziness, rate before and
monoamine (usually reserved Severe renal headache, frequently during
oxidase, for patients who disease; akathisia, anxiety, therapy. Report
resulting in an do not tolerate or Cerebrovascular ataxia, drowsiness, significant changes
accumulation respond to other disease; euphoria, promptly.
of various modes of therapy Cardiovascular insomnia,
neurotransmitt [e.g.tricyclic disease; restlessness, Monitor intake and
ers (dopamine, antidepressants, Uncontrolled weakness. output ratios and daily
epinephrine, SSRIs, SSNRIs or hypertension; EENT:blurred weight. Assess patient for
norepinephrine electroconvulsive Pheochromocytom vision. urinary retention.
, and therapy]). a; History of CV:
serotonin) in severe or frequent HYPERTENSIVE May cause dizziness or
the body. headaches CRISIS, drowsiness.
Therapeutic orthostatic Caution patient to avoid
Effects: hypotension. driving and other

65
Improved GI: nausea, black activities requiring
mood in tongue, alertness until response
depressed constipation, to medication is known.
patients. diarrhea, dry
mouth. Caution patient to change
GU:dysuria, sexual positions slowly to
dysfunction, minimize orthostatic
urinary hypotension. Geriatric
incontinence, patients are at increased
urinary retention. risk for this side effect.
Derm:
photosensitivity. Instruct patient to consult
with health care
professional before
taking any new
prescription, OTC, or
herbal product.

Advise patient to notify

health care professional
if dry mouth, urinary
retention, or constipation
occurs. Frequent rinses,
good oral hygiene, and
sugarless candy orgum
may diminish dry mouth.
An increase in fluid
intake, fiber, and exercise
may prevent constipation

ATYPICAL ANTIDEPRESSANTS:
Atypical antidepressants are not typical — they don't fit into other classes of antidepressants.
They are each unique medications that work in different ways from one another.
Atypical antidepressants ease depression by affecting chemical messengers (neurotransmitters)
used to communicate between brain cells. Like most antidepressants, atypical antidepressants
work by ultimately effecting changes in brain chemistry and communication in brain nerve cell
circuitry known to regulate mood, to help relieve depression

EXAMPLE
1) MIRTAZAPINE
2) MIANSERIN
3) AMINEPTINE

66
 1) MIRTAZAPINE

Trade Name: Remeron

Dosage
15mg, 30mg, 45mg,45mg tablets , and orally disintegrating tablets.

Classification: antidepressants-atypical antidepressants.

Mechanism of Indications Contraindications Side Effects Nursing

Action management
MOA unknown; relief of contraindicated with CNS:  Patient
appears to act symptoms hypersensitivity to any hallucinations, should be
similarly to TCAs, of tricyclic or tetracyclic disorientation, monitored for
which inhibit the depression drugs; concomitant CV: Orthostatic worsening o
presynaptic (endogenous therapy with an MAOI; hypotension, fdepression or
reuptake of the depression recent MI; myelography hypertension, emergence of
neurotransmitters, most within previous 24hr or syncope, suicidality.
norepinephrine and responsive) scheduled within 48 hr tachycardia,  Assess fr
serotonin; pregnancy ( limb Palpitations, MI, weight gain and if
anticholinergic at reduction abnormalities arrhythmias, heart yes then notify .
CNS and peripheral reported); lactation use block, precipitation  Monitor
receptors; sedating; cautiously with ECT: of chf, stroke those with history
relation of these pre-existing CV ENDOCRINE: of increased
effects to clinical. disorders Elevated or intraocularr
depressed blood pressure or
sugar; elevated urinary retention.
prolactin levels;  Monitor
inappropriate ADH those with history
secretion of seizuersfor
GI: Dry mouth, lowering of
constipation, seizure
paralytic ileus, threashold..
nausea

67
 GU: urinary
retention.

2. MIANSERIN

Trade Name:Tolvon, others

Other Names:Mianserin hydrochloride

Dosage:
Adult: Initially, 30-40 mg daily gradually increased if necessary. Maintenance: 30-90 mg daily
as a single dose at night or in divided doses. Max: 200 mg/day.
Elderly: Initially, 30 mg slowly increased if necessary.

Classification:Atypical antidepressant

Mechanism of Indications Contraindic Side Effects Nursing management

Action ations
Description: Depression lactation, Nervousness, Before Administration
Mianserin is a porphyria irritability, insomnia,  Check for drug or
structural analogue anxiety, dizziness, herbal interactions
of serotonin (5-HT) nausea, sweating,  Check for
with antagonistic tremors and allergies
effects at 5-HT2A, headache. These  Assess baseline
5-HT2C and 5-HT3 symptoms can mental status
receptors. resolve within a few  Assess for
Mianserin also weeks of taking the suicidal tendencies
blocks the medication on a After Administration
inhibitory α2- daily basis. The two  Monitor for
receptors, thus most disturbing side effectiveness as exhibited
leading to an effects of SSRIs are by a decrease in
increase in weight gain and symptoms
noradrenaline sexual dysfunction  Monitor for side
68
release effects and serotonin
syndrome
 Remember that a
lot of these drugs can
cause dizziness in the
first few weeks of taking
so take safety precautions

3. AMINEPTINE

Trade Name: Survector

Dosage: 100mg/day, 200 mg/day

Classification: Atypical Antidepressant

Mechanism of Indications Contraindications Side Effects Nursing
Action management
It prevents the Depression. Lactating women, Sleepiness, Advise patients
reabsorption of This medicine individual suffering Increased heart rate, not to drink
dopamine very is also used to from severe liver Blurred vision, alcohol with
effectively and treat cronic damage, cardiac Constipation, medicines.
norepinephrine to pain such as arrhythmias and Orthostatic. Avoid
some extent, headache severe manic Breastfeeding,
thereby providing caused by disease. Adverse Effect:- Dry consult doctor in
a sound migraine, Mouth sedation, problem case of
antidepressant tension, panic during urination, blurred pregnancy.
result. Since it is attacks, joint vision, excessive swetting,
an antidepressant pain, arthritis sexual dysfunction, abrupt
it encourages and weightgain, increased
neurotransmission. neuropathy. appetite, enlargement of
testicles in males,
convulsions, blood
disorders and fever.

69
MOOD STABILIZING DRUGS

70
 MOOD STABLIZER
Mood stabilizing drug are typically used to control the symptoms of mania and once controlled,
to prevent its recurrence. It’s also treating the mood disorder such as bipolar disorder and
depression. In recent year several other medications also used in combination or alone for these
disorders. Some commonly used stabilizers as follows are

 Lithium (eskalistis , lithone)

 Carbamazepine (tegretol)
 Sodium valporate (depakene)

Other anticonvulsant drugs notably gabapentin (neurontin) have come into use both as mood
stabilizers in their own right and as antidepressant augmenting agents.
Mood stabilizer drugs are

MOOD
STABILIZER

Lithium Sodium
Carbamazepine
(eskalistis , valporate
(tegretol)
lithone) (depakene)

71
 LITHIUM

Lithium carbonate
TRADE NAME:-Carbolith (can), Duralith (can),
Eskalith, Eskalith CR, Lithane,
Lithizine (can), Lithobid, Lithonate,
Lithotabs

Lithium citrate
TRADE NAME:-Cibalith-S
Class and Category
Chemical class: Alkaline metal, monovalent
Cation
Therapeutic class: Antidepressant, antimanic

DOSAGE:-
Lithium carbonate: - 300 mg tablets (e.g. licab); 400mg sustained released tablets (e.g.
lithosum-SR)
Lithium citrate: - 300mg/5ml liquid
The usual range of dose per day in acute mania is 900-1200 mg given in 2-3 divided doses. The
treatment is started after serial lithium estimation is done after a loading dose of 600mg or 900
mg of lithium to determine the pharmokinectics.

MECHANIS INDICATION CONTRAINDIC SIDE EFFECT NURSING RESPONSIBILITY

M OF ATION
ACTION
Mechanism Acute mania Cardiac, renal, Neurological:- -Ensure the client does not
of action is Prophylaxis for thyroid or Tremors, motor participate in activities that
not fully bipolar and neurological hyperactivity, require alertness for example
understood unipolar mood dysfunctional. muscular driving.
but may disorder Presence of blood weakness,
enhance Schizoaffective dyscrasis cogwheel
72
reuptake of disorder During first rigidity,
norepinephri Cyclothymia trimester of seizures,
ne and Impulsivity and pregnancy and neurotoxicity
serotonin, aggression lactation (delirium,
decreasing Other disorders:- Severe abnormal
the levels in \premenstrual dehydration involuntary
the body, dysphonic Hypothyroidism movements,
resulting disorder History of seizures, coma)
decreased seizures.
hyperactivity Bulimia nervosa Renal:-
may take 1-3 Borderline Polydipsia,poly Provide instruction to reduced
weeks for personality uria,tubular caloric diet.
symptoms to disorder enlargement, Emphasize importance of
subside Episodes of nephritic maintaining adequate intake of
binge drinking syndrome sodium’
Trichotillomania Ensure that patient’s fluid and
Cluster sodium
headaches Intake is adequate during
treatment.

Cardiovascular: Monitor daily intake output and

- T wave weight
depression -Monitor skin turgor daily.
Monitor vital sign twice or trice a
Gastrointestinal day
:- Nausea,
vomiting, -Administer medication with
diarrhea, meals to minimise GI upset report
abdominal pain physician, who may decrease
and metallic doses.
taste.
Endocrine:-
Abnormal
thyroid
function, goitre,
and weight gain
Dermatological:
- Acneiform
eruptions,
popular
eruptions and
exacerbation of
psoriasis.
Pregnancy and
lactation:-
Incidence of

73
 Ebistein's
anomaly
(distortion in
downward
displacement of
tricuspid valve
in right -Expect to monitor blood lithium
ventricle) when level two or three times weekly
taken in first during first month, and then
trimester. weekly to monthly during
Secreted in milk maintenance therapy and when
and can cause starting or Stopping NSAID
toxicity in therapy.
infant -In uncomplicated cases, plan to
- Lithium monitor lithium level every 2 to 3
toxicity:- : months
Toxicity occurs -Weigh patient daily to detect
when serum sudden
lithium level Weight changes.
>2.0 mEq/L -Monitor blood glucose level
(Box 5.3). OK often in
5.3: Signs and Diabetic patient because lithium
symptoms of alters Glucose tolerance.
lithium toxicity -Palpate thyroid gland to detect
(serum lithium enlargement because drug may
level >2.0 cause
mEq/L) goiter.

Lithium toxicity:-lithium toxicity means when serum level >2.0meq/L IS CALLED

TOXICITY

MILD MODRATE SEVERE >2.5

Mild 1.0-1.5 Impaired Moderate 1.6-2.5 Severe Impaired
concentration, lethargy., Disorientation, confusion, consciousness (with
irritability, muscle weakness, drowsiness, rest-lessness, progression to coma),
tremor, slurred speech, and unsteady gait, coarsc tremor, delirium, ataxia, generalized
nausea dysarthria, muscle fasciculation, extra pyramidal
fasciculation’s, and vomiting symptoms, convulsions, and
impaired renal function

74
MANGEMENT OF LITHIUM TOXICITY
 Discontinue the drug immediately
 For significant short-term ingestions, residual gastric content should be removed
by induction of emesis, gastric lavage and adsorption with activated charcoal
 If possible, instruct the patient to ingest fluids
 Assess serum lithium levels, serum electrolytes’, renal functions, ECG as soon as
possible
 Maintenance of fluid and electrolyte balance
 In a patient with serious manifestations of lithium toxicity, haemodialysis should
be initiated.
There is no specific antidote for Li. intoxication, and treatment is supportive.
> Dialysis is the most effective means of removing the ion from the body and is
necessary in severe poisonings, i.e., in patients exhibiting symptoms of toxicity or
patients with serum Li+ concentrations greater than 4 mEq/L in acute overdoses or
greater than 1.5 mEq/L in chronic overdoses.

NURSE’S RESPONSIBILITIES

Before drug -History and physical examination.

-Vital and blood investigation should be carried out like B.P
temp. Weight
investigation like blood HB,ESR,blood count, and thyroid, sugar
and cast, electrolytes, urea, serum, creatinine, urine for protein,
sugar and cast, pregnancy test,ECG, thyroid function test.
-History clearfully taken may be sure about patient is not taking
thiazide diuretic.
After starting -Lithium should be taken daily basis, same time daily doses
which are prescribed by the physician. It may be begin and
continues with two doses 12 hours.
Example: the patient taking lithium on tads as by the physician,
and he/she is forget to take a dose of medicine than he /she
should wait for the next dose and do not take twice the amount
at one time because it lead to drug toxicity.
Prophylaxis drug begin with 750-1000mg per day in divided
doses. Than blood serum level evaluation is important so blood
test should be done for lithium estimation every week. For
prophylaxis a lithium level of 0.4 to 0.8 mmol/l (in a sample
taken 12 hours after the last dose) may be adequate, if this is not
effective the high range of 0.7 to1.2 mmol/l should be used.
When the therapy start mild side effects such as hand tremors,
excess trust and urination, nausea, anorexia etc.
Some are serious side effect like vomiting, extreme hand
tremors, sedation, muscle weakness and vertigo. Those serious

75
 side effect occurs than discontinue the drug and inform the
psychiatrics.
Follow up and Told patient about follow up in every six month, blood should be
evaluation taken for investigation.
Special care should be taken before starting haloperidol or any
other drugs, ECT and anesthesia.
As per prescriptions the lithium may be given at least a year and
may be continue for more than five year. When lithium
withdrawn suddenly some patient become irritable and
emotionally labile, and a few relapse into mania. It is prudent to
withdraw lithium gradually.

CARBAMAZEPINE (TEGRETSAL)

Trade name
Tegretol, mazetol, zeptol, and Zen retard

Classification
Anticonvulsant, Mood stabilizing drug

Dose
Daily dose- 600-1800 mg orally in divided doses.
The therapeutic blood levels are 6-12 ug/ml.
Toxic level – more than 15 ug/ml

76
MECHANIS INDICATION CONTRAIND SIDE EFFECT NURSE’S
M OF ICATION RESPONSIBILITY
ACTION
Abortion by GI seizures-complex Hypersensitivit Nausea/vomiting/dia May give with food and
tract partial seizures, y, glaucoma, rrhoea/dry meal to reduce GI upset
distribution GTCS, Seizures due liver-renal mouth/abdominal
corsses blood to alcohol withdrawn disease, pain
and placental Psychiatric lactation
barrier, and disorders-rapid caution in
excreted in cycling bipolar elderly liver-
breast milk disorders, acute renal disease
metabolism in depression, impulse and pregnancy.
liver and control disorders
excreted by acute depression,
kidney aggression psychosis
with epilepsy,
schizoaffective
disorders broad line
personality disorder,
cocaine withdrawn
syndrome.
Paroxysmal pain
syndrome –
trigeminal neuralgia
and phantom limb
pain.

Drowsiness/dizzines -Ensure the client does

s/confusion/headach not operate dangerous
e machinery or such
activities.

Others side effect Other nursing

are responsibilities are
Hypertension, -Advice patient not to
arrhythmias skin consume alcohol when he
rashes, Steven is on the durg.advice for
Johnson syndrome, regular follow-up visits
jaundice, hepatitis, and periodic examination
oliguria, leukopenia, of blood count and
thrombocytopenia, monitoring of cardiac,
bone marrow renal hepatic and bone
depression leading marrow function.
to aplastic anaemia.

77
 SODIUM VALPORATE

Trade name
Encorate, Chrono, Epilex, Epival

Classification
Mood stabilizer

Dose
Dose is 15mg/kg/day
Maximum dose is 60 mg/kg/day orally

MECHANISM INDICATION CONTRAINDICA SIDE NURSE’S

OF ACTION TION EFFECT RESPONSIBILITY
The drug act on acute mania, Hypersensitivity, Prolonged Ensure patient to advise to
gamma amino prophylactic Glaucoma, liver- bleeding avoid situation which may
butyric acid treatment of renal disease, time, cause bleeding.
(GABA) an bipolar 1 disorder Lactation caution in Thrombocyt Advise to use soft brush and
inhibitory amino Schizoaffective elderly liver-renal openia, nonabrasive toothpaste to
acid disorder disease and platelet reduce risk for gum injury
neurotransmitter. Seizures pregnancy. dysfunction.
GABA receptor Other disorder
activation serves like bulimia Advice the patient to take
in reduce neuronal nervosa, drug or medicine after food
excitability. obsessive to reduce GI irritation.
compulsive
disorder, agitation Ensure the client does not
and PTSD nausea, participate in activities that
vomiting, require alertness for

78
diarrhoea, example driving.

Advice regular check up or

follow up and periodically
Sedation, examination of blood count,
ataxia, and hepatic function and thyroid
dysrrthimas. function. Therapeutic serum
Tremor, level of valporic acid is 50-
weight gain, 100 mg/ml.
loss of hair, Monitor the spontaneous
bleeding or brushing.

79
ANTIPARKINSONIAN
DRUGS

80
 Antiparkinsonian drugs

Introduction:
Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the
dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic
antagonists.

CLASSIFICATION OF ANTIPARKINSONIAN DRUGS

I. Drugs acting on dopaminergic system:

Dopamine precursors — Levodopa (1-dopa)
Peripheral decarboxylase inhibitors — carbidopa and benserazide
Dopaminergic agonists: Bromocriptyne, Ropinirole and Pramipexole
MAO-B(monoamine oxidase B) inhibitors — Selegiline, Rasagiline
COMT (catechol-o-methyltransferase) inhibitors — Entacapone, Tolcapone
Dopamine facilitator - Amantadine

2. Drugs acting on cholinergic system

Central ticholinergics — Teihexyphenidyl (Benzhexol), Procyclidine, Biperiden
Antihistaminics — Orphenadrine, Promethazine

LEVODOPA /CARBIDOPA

81
 Trade name
Atamet,Sinemet

Classification
Dopamineric antiparkinsonian

Dose
Immediate-release including Oral disintegrating tablets: Initial dose: 25 mg-100 mg orally three
times a day or 10 mg-100 mg orally 3 or 4 times a day -Increase by 1 tablet every day or every
other day as needed until a dose of 8 tablets is reached; may use a combination of tablets from
both ratios (1:4 or 1:10) to provide the optimum dose.

Conversion from LEVODOPA:

-Levodopa should be discontinued at least 12 hours before starting carbidopa-levodopa; initiate
with approximately 25% of the previous levodopa dose.
-Suggested dose for patients receiving less than levodopa 1500 mg per day: 25 mg-100 mg
orally 3 or 4 times a day.
-Suggested dose for patients receiving more than levodopa 1500 mg per day: 25 mg-250 mg
orally 3 or 4 times a day.

MECHANISM INDICATION CONTRAINDI SIDE EFFECT NURSE’S

OF ACTION CATION RESPONSIBILITY
1. Because which is nowadays malignant Abnormal - Assess therapeutic
dopamine does always combined melanoma, a thinking: holding response.
not cross the with a type of skin false beliefs that - Monitoring for side-
blood-brain decarboxylase cancer, cannot be changed effects, including mental
barrier inhibitor, is the diabetes, mental by fact, agitation state assessment and
levodopa, the most efficient drug problems from , anxiety, blood pressure
precursor of for the treatment of taking the drug, clenching or measurement.
dopamine, is Parkinson's disease. psychotic grinding of teeth, - Care should be taken
given It is irrelevant disorder, clumsiness or to avoid confusion with
instead. which of the two suicidal unsteadiness, the antihypertensive
2. Levodopa is decarboxylase thought, signs confusion, medication methyldopa.
formed L- inhibitors is used. or symptoms of difficulty - Levodopa can cause
tyrosine and is Levodopa treatment neurosis, swallowing , false results in urine
an is normally started depression, dizziness,excessiv tests for sugar and
intermediate in when wide-angle e watering of ketones.
the synthesis of anticholinergic glaucoma, mouth, false sense
catecholamines. agents and closed angle of well being, PATIENT TEACHING
3. Levodopa amantadin do not glaucoma, a feeling faint, - Inform patients of the
itself has suffice any longer, heart attack, general feeling of possibility of a sudden
minimal or when the patients abnormal heart discomfort or onset
pharmacologic are severely rhythm, a illness, of excessive daytime
82
activity, hindered in their disease of the hallucinations sleepiness.
in contrast to its daily activities or lung , a stomach (seeing, hearing, or - Patients must not drive
decarboxylated social contacts. At ulcer feeling things that or operate machinery
product, the beginning are not there), until they know how this
dopamine. over 75% of the an ulcer of the hand tremor, drug affects them.
4. Levodopa is patients respond to duodenum, an increased, nausea - Alcohol can add to the
rapidly levodopa treatment. ulcer from too or vomiting, drowsiness caused by
decarboxylated The combination much stomach numbness, unusual this drug.
in the with other acid, liver and uncontrolled - Inform patients that it
gastrointestinal Parkinsonian drugs problems, movements of the may take several weeks
tract. (especially with bleeding of the body, including to benefit from the full
Prior to the bromocriptine or stomach or the face, tongue, therapeutic effects.
advent of selegilin) makes it intestines, arms, hands, head, - Patients should not
decarboxylase possible to reduce seizures, a type and upper body, stop taking levodopa
inhibitors the dose and of abnormal unusual tiredness suddenly without taking
(carbidopa), therefore also the movement or weakness medical advice.
large oral side-effects. The disorder called Nurses should refer to
doses of efficacy of dyskinesia, an Less common manufacturer’s
levodopa were levodopa usually inability to Blurred vision, summary of product
required; thus, diminishes through completely difficult urination, characteristics and to
toxicity from the years. After two empty the difficulty opening appropriate local
dopamine was a to five years of bladder mouth ,dilated guidelines
limiting factor therapy the (large) pupils,
complications Allergies: dizziness or
slowly mutliply Carbidopa/Levo lightheadedness
(dyskinesias, dopa when getting up
fluctuation of the from a lying or
effect). In advanced sitting position,
stages, the double vision
physicians' efforts
concentrate on the
reduction of side-
effects.
Parkinsonism
induced by drugs
cannot

83
 2.TRIHEXYPHENIDYL

Trade name:
Artane, Parkin, Pacitane, Hexymer, Trihexane, Trihexy

Classification
Antiparkinsons

Dose:
1-2 mg/day orally initially ,maximum dose up to 15 mg/day in divided doses.

Mechanism of action Indication Contraindicatio Side effect Nursing management

n
It acts by increasing the Drug ARTANE Dizziness, Assess parkinsonism and
release of dopamine from induced (trihexyphenidyl nervousness extrapyramidal symptoms.
presynaptic vesicles, parkinsonism ) is , Medication should be
blocking reuptake of Adjunct in contraindicated drowsiness, tapered gradually.
dopamine into presynaptic the in patients weakness, Periodic eye examination
nerve terminals or by management with hypersensiti headache, should be done
exerting an agonist effect of vity to confusion,
on post synaptic dopamine parkinsonism trihexyphenidyl
receptors HCl or to any of
.Trihexyphexyphenidyl the tablet or blurred Caution patient to make
reaches peak plasma elixir vision, position changes to slowly
concentration in 2-3 hours ingredients. mydriasis, to minimize orthostatic
after oral administration Artane tachycardia hypotension.
and has duration of action (trihexyphenidyl Instruct the patient about
up to 12 hours. ) is also frequent rinsing of mouth
contraindicated and good oral hygiene.
in patients with orthostatic
84
 narrow hypotension
angle glaucoma. , Caution patient that this
Blindness after medication decrease
long-term use perspiration and over
due to narrow heating may occur during
angle glaucoma hot weather.
has been
reported. dry mouth,
nausea,
constipation
, vomiting,

urinary
retention,
and
decreased
sweating.

BENZTROPINE

Trade name:
Cogentin

Classification
Antiparkinson

Dose:
Adult: Postencephalitic parkinsonism: 1-2 mg/day (range, 0.5-6 mg/day)
orally/intravenously/intramuscularly at bedtime or divided every 6-12 hours; may consider lower
dose or 0.5 mg at bedtime in highly sensitive patients; not to exceed 6 mg/day

85
 Idiopathic parkinsonism: 0.5-1 mg at bedtime initially; titrate dose in 0.5-mg increments every 5-
6 days (range 0.5-6 mg daily; some patients may need 4-6 mg/day); not to exceed 6 mg/day
Geriatric:
0.5 mg orally once daily or every 12 hours; titrate dose in 0.5-mg increments every 5-6 days; not
to exceed 4 mg/day
Drug-Induced Extrapyramidal Disorders
Adult: 1-2 mg intravenously/intramuscularly/orally every 8-12 hours; reevaluate after 1-2 weeks
Acute dystonia: 1-2 mg intravenously (IV), then 1-2 mg orally once or twice daily for 7-28 days
to prevent recurrence
Children over 3 years: 0.02-0.05 mg/kg intravenously/intramuscularly/orally once daily or every
12 hours
Children under 3 years: Not recommended

Mechanism of action Indication Contraindica Side effect Nursing management

tion
In Parkinson's there is For the treatment hypersensivity Nausea, Monitor for constipation,
an imbalance between of parkinsonism o . Benztropine, vomiting, abdominal pain,
levels of dopamine r Parkinson's closed- abdominal distention, or absence of
and acetylcholine disease, including angle glauco distension,cons bowel sounds. Monitor
neurotransmitters. Ben tremor due to the ma because tipation, dry intake and output ratios
ztropine helps restore disease. the drug can mouth and assess patient for
balance by blocking For the treatment induce urinary retention
the action of of drug- cycloplegia (dysuria, ... Patients with
acetylcholine in the induced extrapyra and mydriasis, mental illness are at risk
central nervous system midal symptoms. resulting in of developing
(brain and spinal For the treatment increased exaggerated symptoms
cord).s Benztropine w of chronic intraocular of their disorder during
as approved by the sialorrhea† pressure. early therapy
U.S. Food and (chronic drooling) with benztropine.
Administration (FDA) in
in 1954. developmentally- Assess clients behaviour
disabled patients. and doMSE

Nursing Implications.
rapid heart Assessment & Drug
rate, Effects. Assess
confusion, therapeutic effectiveness.
memory Clinical improvement may
problems, not be evident for 2–3 d
visual after oral drug is started.
hallucinations,

86
 BIPERIDEN

Trade name:
Akineton

Classification
Antiparkinson

Dose:
2 mg orally 3 to 4 times a day; the dose may be titrated up to a maximum of 16 mg per 24 hours
Usual Adult Dose for Extrapyramidal Reaction
Neuroleptic-induced: 2 mg orally 1 to 3 times a day

Mechanism of Indication Contraindication Side effect Nursing management

action
The mechanism of Biperiden is It should not be Dry mouth, Advise patient to take
action of centrally used to treat the used in people nose throat, sips of water frequently.
active stiffness, with a bowel nausea
anticholinergic drugs tremors, spasms, obstruction or vomiting. Assessment & Drug
such as AKINETON and poor muscle glaucoma. It is decreased Effects. Monitor BP and
(biperiden) is control of unclear if use in sweating pulse after IV
considered to relate Parkinson's pregnancy or administration.
to competitive disease. It is breastfeeding is
antagonism of also used to safe. Biperiden is Periodic eye examination
acetylcholine at treat and in the should be done.
cholinergic receptors prevent these anticholinergic
in the corpus same muscular family of blurred vision, Assess patient,s
striatum, which then conditions when medication. drowsiness, behaviour and MSE.
restores the balance. they are caused Mysthenia
by drugs such as gravis,pyloric or
chlorpromazine duodenal
(Thorazine), obstruction. euphoria, or Advise patient to make
fluphenazine disorientation, position changes
(Prolixin), agitation, slowly ...
perphenazine disturbed

87
 (Trilafon), and behaviour
others. urinary Advise patient to avoid
retention, driving or other activities
dizziness when that require alertness
standing up, until response to the drug
difficulty or is known. Caution patient
painful to change positions
urination, slowly to minimize
involuntary orthostatic hypotension.
movements,
slow heart rate.

BROMOCRIPTINE

Trade name:
Parlodel and Cycloset. Bromocriptine comes in two forms: an oral tablet and an oral capsule.

Doses:
Initial dose: 1.25 to 2.5 mg orally once a day
-Increase in increments of 2.5 mg every 2 to 7 days as tolerated until optimal response is
achieved
Maintenance dose: 2.5 to 15 mg orally once a day

Mechanism of Indication Contraindicati Side effect Nursing

action on management
Bromocriptine It is used to psychotic Low blood Assessment &
is unique in treat acromegaly disorder pressure (hypotension) Drug Effects.
that it does not and conditions high blood Headache Monitor vital
have a specific associated with pressure signs closely
receptor that hyperprolactine significant during the first

88
mediates mia like uncontrolled few days and
its action on amenorrhea, high blood periodically
glucose and infertility, and pressure throughout
lipid hypogonadism, coronary artery therapy.
metabolism. prolactin- disease
Rather, its secreting a stroke
effects are adenomas; it is low blood Abdominal cramps
mediated via also used to pressure Loss of appetite
resetting of prevent ovarian liver problems Constipation
dopaminergic hyperstimulation a mother who is Indigestion
and syndrome. It is producing milk Trouble swallowing
sympathetic also used to treat and Stomach/abdominal
tone within the Parkinson's breastfeeding pain or discomfort
CNS. disease. Allergies:
Ergot Alkaloids
Amine Ergot
Alkaloid Gastrointestinal bleedin
Hydrogenated g
Ergot Alkaloid
Semi-Synthetic
Ergot Alkaloid Vomiting
Dopamine nausea Watch for signs
Receptor of bleeding.
Agonist

Drowsiness Tell patient to

dizziness take each dose
Fatigue with a meal or
Faintness snack to
Visual hallucinations minimize nausea.
Sleep problems Avoid
(insomnia) hazardeous
Lightheadedness activities until
Nightmares drug effect are
Paranoia known.
Psychosis Bed should be in
Seizures low position with
Spinning sensation (vert side rails up.
igo)
Irregular heartbeats
(arrhythmias)
Slow heart rate Assess for
High blood hypotension
pressure (hypertension) when therapy
Heart attach starts and
(myocardial infarction) hypertension (2

89
 Mottled skin nd week).
Dizziness on standing
Vasospasm
Palpitations
Pericardial effusions
Raynaud's syndrome ex
acerbation
Fainting
Eyelid twitching or
closing
BUN increased
Burning discomfort of
the eye
Double vision
Facial pallor
Leg cramps
Nasal congestion
Rash Assess MSE
Hives during therapy.
Depression
Tired feeling
Diarrhea
Cold feeling or
numbness in your
fingers
Dry mouth
Stuffy nose

SELEGILINE

90
 Trade name:
Eldepryl and Emsam

Dose:
Conventional
5 mg PO at breakfast & 5 mg at lunch (10 mg/day)
After 2-3 days of selegeline therapy, can begin to taper levadopa dose by 10-30% as tolerated;
continue to taper based upon patient response
Not to exceed 10 mg/day
Orally-disintegrating (with levodopa/carbidopa)
Initial 1.25 mg PO qDay, may increase after 6 weeks if inadequate response, no more than 2.5
mg/day
Do not take food or liquid for 5 minutes after dose

Mechanis Indication Contraindication Side effect Nursing

m of managemen
action t
Selegiline i Adjunct to Selegiline is Dizziness, abdomin Find patient
sa levodopa/carbidop contraindicated in al pain, trouble medical
selective a in Parkinsonism. patients with a sleeping, and information
inhibitor of Adult: 5mg at known hypersensitivity t headache may occur. for Selegiline
MAO-B, breakfast and at o this drug. Selegiline is If any of these including
irreversibly lunch; max contraindicated for use effects persist or its uses, side
inhibiting it 10mg/day. ... with meperidine worsen, notify your effects and
by binding (DEMEROL & other doctor or pharmacist safety,
to it trade names). This promptly. If you are interactions,
covalently. contraindication is often also taking levodopa, pictures,
It exerts extended to other opioids you may experience warnings and
effects by more side effects user ratings.
blocking from the levodopa
the when taking
breakdown selegiline.
of Advise
dopamine, nausea stomach patient to
thus upset, take Small
increasing sips of water
its activity. frequently

91
ANTAABUSE DRUGS
(ALCOHOL DETERRENT THERAPY)

92
 ANTAABUSE DRUGS(ALCOHOL DETERRENT THERAPY)
Introduction:
Deterent agents are those which are given to desensitize the individual to the effects of alcohol
amd maintain anstinence. The most commonly used drug is disulfiram(tetra ethylthiuram
disulfide) or antabuse.

DISULFIRAM

Trade name
Diluxram, Disiram, Antawell

Dose:
Alcoholism
Only administer after the patient has abstained from ethanol for at least 12 hr
Use ONLY as adjunct to supportive & psychotherapeutic treatment; in motivated patient
500 mg PO qDay initially for 1-2 weeks; not to exceed 500 mg/day
Maintenance: 250 mg PO qDay (125-500 mg range); continue therapy until a bases for self-
control has been established; patient may continue to take drug therapy for months or even years

Mechanism of action Indication Contraindicat Side effect Nursing management

ion
Disulfiram is an aldehyde Disulfiram is an Pulmonary and Fatigue, 1.An informed consent
dehydrogenase inhibitor that aid in the cardiovascular dermatitis, must be taken before
interfares with the management of diseases. impotence, starting treatment.
metabolism of alcohol and selected should be be optic 2.Ensure that atleast
produces a marked increase chronic alcohol p used with neuritis, 12 hours have elapsed
in blood acetaldehyde levels atients who want caution in mental since the last ingestion
.The accumulation of to remain in a patients with changes, of alcohol before

93
acetaldehyde produces a state of enforced nephritis, brain acute administering the
wide variety of unpleasant sobriety so that damage, polyneurop drug.
reaction called the supportive and hypothyroidis athy, and 3.Caution the patient
disulfiram ethanol psychotherapeuti m, diabetes, hepatic against taking CNS
reaction(DER),characterized c treatment may hepatic damage. depressent or any over
by nausea, be applied to diseases, the counter medication
throbbing,headache, best advantage. seizures, during disulfiram
vomiting, hypotension, Disulfiram is not abnormal ECG therapy.
flushing, sweating ,thirst, a cure 4.Instruct the patient
dyspnea, tachycardia, chest for alcoholism. to avoid driving or
pain, vertigo, blurred vision, other activities
and a sense of impending requiring alertness
doom associated with severe until response to drug
anxiety.The reaction occurs is known
almost immediately after the 5.Patient shold warned
ingestion of even one that disulfiram alcohol
alcoholic drink and may reaction may continue
lasts up to 30 minutes. for as long as 1 to 2
weeks after the last
dose of drug
.6.Emphasizes on
follow up visits to
monitor progress of
therapy.

94
 ANTICRAVING DRUGS

Craving is sometime define as a “subjectively experienced” desire or urge to approach and

consume a particular substance.
The withdrawal symptoms of a particular type of drug such as an opiate are managed as the
toxins from the drug are removed from the body. However, removing the drug from the body
will also be accompanied by cravings in some cases both physical, psychological and emotional.
A number of stimuli can set off a craving response within the brain. Anti-craving drugs seem to
work by blocking the receptors associated with cues that set off relapse. However, some cues are
not effected by the blocking of these reward receptors.

Usage of Anti-Craving medicines:

To date, several different addictions are being treated with the use of anti-craving medications
after detox. These include alcoholism, opiate addiction, nicotine addiction, and cocaine
addiction. These drugs are used to help prevent relapse both during the detox phase and in early
recovery.
Types of Anti-Craving Drugs
NALOXONE
BACLOFEN
NALTREXONE
ACAMPROSATE CALCIUM
TOPIRAMATE
GABAPENTIN
NALOXONE

Naloxone used to block the effects of opioids. It is commonly used for decreased breathing in
opioid overdose. Naloxone may also be combined with an opioid (in the same pill) to decrease
the risk of opioid misuse. When given intravenously, naloxone works within two minutes, and
when injected into a muscle, it works within five minutes; it may also be sprayed into the nose.
The effects of naloxone last about half an hour to an hour. Multiple doses may be required, as the
duration of action of most opioids is greater than that of naloxone.

Trade Name:
Narcan, Evzio, others

95
 Dosage:
Postoperative Opioid-Induced Respiratory Depression
IV (Adults): 0.02– 0.2 mg q 2– 3 min until response obtained; repeat q 1– 2 hr if needed.
IV (Children): 0.01 mg/kg; may repeat q 2– 3 min until response obtained. Additional doses
may be given q 1– 2 hr if needed.
IM, IV, Subcut (Neonates): 0.01 mg/kg; may repeat q 2– 3 min until response obtained.
Additional doses may be given q 1– 2 hr if needed.
Opioid-Induced Respiratory Depression During Chronic (1 wk) Opioid Use
IV, IM, Subcut (Adults >40 kg): 20– 40 mcg (0.02– 0.04 mg) given as small, frequent (q min)
boluses or as an infusion titrated to improve respiratory function without reversing analgesia.
IV, IM, Subcut (Adults and Children <40 kg): 0.005– 0.02 mg/dose given as small, frequent (q
min) boluses or as an infusion titrated to improve respiratory function without reversing
analgesia.
Overdose of Opioids
IV, IM, Subcut (Adults): Patients not suspected of being opioid dependent—0.4 mg (10
mcg/kg); may repeat q 2– 3 min (IV route is preferred). Some patients may require up to 2 mg.
Patients suspected to be opioid dependent—Initial dose should be decrease to 0.1– 0.2 mg q 2– 3
min. May also be given by IV infusion at rate adjusted to patient’s response.
IV, IM, Subcut (Children >5 yr or > 20 kg): 2 mg/dose, may repeat q 2– 3 min.
IV, IM, Subcut (Infants up to 5 yr or 20 kg): 0.1 mg/kg, may repeat q 2– 3 min.
Opioid-Induced Pruritus
IV (Children): 2 mcg/kg/hr continuous infusion, may increase by 0.5 mcg/kg/hr every few hours
if pruritus continues

Classification:
Therapeutic: antidotes (for opioids)
Pharmacologic: opioid antagonists

Mechanism of Indications Contraindicatio Side Effects Nursing management

Action ns
While the Reversal of Contraindicated CV: -Monitor respiratory rate,
mechanism of CNS in VENTRICUL rhythm, and depth; pulse,
action of naloxone depression Hypersensitivity. AR ECG, BP; and level of
is not fully and Use Cautiously ARRHYTHM consciousness frequently for
understood, the respiratory in:Cardiovascula IAS, 3– 4 hr after the expected peak
preponderance of depression r disease; hypertension, of blood concentrations. After
evidence suggests because of Patients hypotension. a moderate overdose of a short
that naloxone suspected physically GI: nausea, half-life opioid, physical
antagonizes the opioid dependent on vomiting. stimulation may be enough to
opioid effects by overdose. opioids (may Interactions prevent significant
competing for the Unlabeled precipitate Drug-Drug: hypoventilation. The effects of
same receptor sites, Use: Opioid- severe Can some opioids may last longer
especially the mu- induced withdrawal); precipitate than the effects of naloxone,
opioid receptor. pruritus (low OB: May cause withdrawal in and repeat doses may be
Recently, naloxone dose IV acute withdrawal patients necessary.

96
has been shown to infusion). syndrome in physically -Patients who have been
bind all three Management mother and fetus dependent on receiving opioids for 1 wk are
opioid receptors of refractory if mother is opioid extremely sensitive to the
(mu, kappa and circulatory opioid analgesics. effects of naloxone. Dilute and
gamma) but the shock. dependent; Larger doses administer carefully.
strongest binding is Lactation:Safety may be
to the mu receptor. not established; required to -Assess patient for level of
Pedi:May cause reverse the pain after administration when
acute withdrawal effects of used to treat postoperative
syndrome in buprenorphine respiratory depression.
neonates of , butorphanol,
opioid- nalbuphine, or -Naloxone decreases
dependent pentazocine. respiratory depression but also
mothers. Antagonizes reverses analgesia.
postoperative Assess patient for signs and
opioid symptoms of opioid
analgesics. withdrawal (vomiting,
restlessness, abdominal
cramps, increased BP, and
temperature). Symptoms may
occur within a few minutes to
2 hr. Severity depends on dose
of naloxone, the opioid
involved, and degree of
physical dependence.
Lack of significant
improvement indicates that
symptoms are caused by a
disease process or other non-
opioid CNS depressants not
affected by naloxone.

-Toxicity and Overdose:

Naloxone is a pure antagonist
with no agonist properties and
minimal toxicity.

97
 BACLOFEN

Trade Name:
Gablofen, Lioresal

Dosage:
PO (Adults): 5 mg 3 times daily. May increase q 3 days by 5 mg/dose up to 80 mg/ day (some
patients may have a better response to 4 divided doses).
PO (Children >8 yr): 30– 40 mg daily divided q 8 hr; titrate to a maximum of 120 mg/day.
PO (Children 2– 7 yr): 20– 30 mg daily divided q 8 hr; titrate to a maximum of 60 mg/day.
PO (Children <2 yr): 10– 20 mg daily divided q 8 hr; titrate to a maximum of 40 mg/day.
IT (Adults): 100– 800 mcg/day infusion; dose is determined by response during screening
phase.
IT (Children >4 yr): 25– 1200 mcg/day infusion (average 275 mcg/day); dose is determined by
response during screening phase.

Classification:
Therapeutic: antispasticity agents, skeletal muscle relaxants (centrally acting)

Mechanism of Indications Contraindications Side Effects Nursing

Action management
Inhibits reflexes PO: Treatment Contraindicated in CNS:SEIZURES(I -Assess muscle
at the spinal of reversible Hypersensitivity. T), dizziness, spasticity before and
level. spasticity due to Use Cautiously in: drowsiness, periodically during
Therapeutic multiple Patients in whom fatigue, weakness, therapy.
Effects: sclerosis or spasticity maintains confusion, -Observe patient for
Decreased spinal cord posture and balance; depression, drowsiness,
muscle lesions. IT: Patients with epilepsy headache, dizziness, or ataxia.
spasticity; Treatment of (maypseizure insomnia. EENT: May be alleviated by
bowel and severe spasticity threshold); Renal nasal congestion, a change in dose.
bladder of cerebral or impairment (pdose tinnitus. -IT: Monitor patient
function may spinal origin may be required); OB, CV:edema, closely during test
also be (should be Lactation:Safety not hypotension. GI: dose and titration. -

98
improved. reserved for established; Pedi: nausea, Resuscitative
patients who do Children 4 yr constipation. GU: equipment should be
not respond or (intrathecal) (safety frequency. Derm: immediately
are intolerant to not established); Geri: pruritus, rash. available for life-
oral baclofen) Geriatric patients are Metab:hyperglyce threatening or
(should wait at atqrisk of CNS side mia, weight gain. intolerable side
least one year in effects. Neuro: ataxia. effects.
patients with Misc: -Lab Test
traumatic brain hypersensitivity Considerations: May
injury before reactions, causeqin serum
considering sweating. glucose, alkaline
therapy).Unlabel phosphatase, AST,
edUse:Managem and ALT levels.
ent of pain in
trigeminal
neuralgia.

NALTREXONE

Trade Name:
Contrave

Dosage:
PO (Adults):Week 1– one tablet in the morning; week 2– one tablet in the morning and one
tablet in the evening; week 3– two tablets in the morning and one tablet in the evening; week 4
and onward– two tablets in the morning and two tablets in the evening; concurrent use of
CYP2B6 inhibitors– dose should not exceed one tablet twice daily.
Renal Impairment
PO (Adults) Moderate to severe renal impairment– dose should not exceed one tablet in the
morning and one tablet in the evening.Hepatic Impairment
PO (Adults) Dose should not exceed one tablet in the morning.

Classification:
aminoketones, opioid antagonists

99
Mechanism of Indications Contraindications Side Effects Nursing
Action management
Bupropion– an Adjunct to Contraindicated in: CNS: HOMICIDAL Administer in the
antidepressant calorie-reduced Known hypersensitivity THOUGHTS/BEHA morning and
that acts as a diet and to bupropion or VIOR, SEIZURES, evening according
weak inhibitor increased naltrexone; SUICIDAL to dose escalation
of neuronal physical Uncontrolled THOUGHTS/BEHA schedule. Swallow
reuptake of activity for hypertension; VIOR, headache, tablets whole; do
dopamine and chronic weight End-stage renal disease; aggression, agitation, not break, crush,
norepinephrine. management in Seizure disorders; anxiety, delusions, or chew. Do not
Naltrexone– obese patients Anorexia or bulimia; depression, dizziness, administer with a
acts as an (BMI ≥30 During withdrawal from hallucinations, high-fat meal; may
opioid kg/m2 ) or or discontinuation of hostility, insomnia, increase risk of
antagonist. overweight alcohol, mania, panic, seizures.
In combination patients (BMI benzodiazepines, paranoia, psychosis;
they affect two ≥27 kg/m2 ) barbiturates or CV: hypertension,
different brain with at least antiepileptics; tachycardia; EENT:
areas involved one other Chronic opioid/opiate angle-closure
in food intake: comorbidity agonist or partial agonist glaucoma
the (hypertension, use or acute opiate (bupropion), tinnitus;
hypothalamic type 2 withdrawal; GI: nausea,
appetite diabetes, or During/within 14 days constipation,
regulatory dyslipidemia). of MAOIs; vomiting, abdominal
center and Concurrent use of pain, diarrhea, dry
mesolimbic CYP2B6 inducers; mouth, dysgeusia,
dopamine Concurrent use of other hepatotoxicity
circuit reward bupropion-containing (naltrexone); Derm:
system. medications; hot flush, sweating;
Therapeutic OB: Pregnancy (may Neuro: tremor; Misc:
Effect(s): cause fetal harm); ALLERGIC
Decreased Lactation: Discontinue REACTIONS
appetite with bupropion/naltrexone or INCLUDING
associated discontinue breast ANAPHYLAXIS/AN
weight loss. feeding; APHYLACTOID
Pedi: Not recommended REACTIONS
for use in children.

Use Cautiously in:

History of suicidal
behavior/ideation;
History of seizure risk
(avoid administration
with a high-fat meal,
adhere to recommended
dose);
History of

100
 cardiac/cerebrovascular
disease;
History of angle-closure
glaucoma;
Diabetes mellitus
(weight loss may result
in hypoglycemia if
treatment is not
adjusted);
Concurrent use of drugs
that ↓ seizure threshold;
Moderate to severe renal
impairment (use lower
dose);
Hepatic impairment (use
lower dose);
Geri: Elderly may be ↑
sensitive to adverse
CNS reactions and ↓
renal elimination

ACAMPROSATE CALCIUM

Trade Name:
Campral

Dosage:
PO (Adults): Two 333-mg tablets (666 mg/dose) 3 times daily. Lower doses may be effective
in some patients.
Renal Impairment
PO (Adults): CCr 30– 50 ml/min—One 333-mg tablet 3 times daily.

Classification:
Therapeutic: alcohol abuse therapy adjuncts

101
 Pharmacologic: gamma aminobutyric acid (GABA) analogues

Mechanism of Indications Contraindicati Side Effects Nursing

Action ons management
Interacts with Maintenance of alcohol Contraindicated CNS: abnormal -Instruct patient to
and restores abstinence; part of a in thinking, anxiety, take medication as
balance to CNS comprehensive alcohol Hypersensitivit depression, directed, even if
glutamate and abstinence program. y; CCr 30 drowsiness, relapse occurs.
GABA mL/min. headache. -Advise patient to
neurotransmitte Use Cautiously EENT: abnormal discuss any
r systems. in:CCr 30– 50 vision. Resp:cough, renewed drinking
Therapeutic mL/min dyspnea, pharyngitis, with health care
Effects: (dosepnecessary rhinitis. professional.
Continued ); History of CV: palpitations, May cause
alcohol depression or peripheral edema, dizziness and
abstinence. suicide attempt; syncope, changes in vision.
OB: Use only if vasodilation. -Caution patients
potential GI: abdominal pain, to avoid driving
maternal benefit anorexia, and other activities
outweighs fetal constipation, requiring alertness
risk; diarrhea, until response to
Lactation:Pedi: flatulence,qappetite, medication is
Safety not nausea, taste known.
established. perversion, vomiting. -Advise female
GU: plibido, erectile patients to notify
dysfunction. Derm: health care
rash. Metab: weight professional if
gain. MS: arthralgia, pregnancy is
back pain, mylagia. planned or
Neuro: tremor. suspected or if
breast feeding.
Encourage patient
to continue active
counselling and
support.
Acamprosate helps
maintain
abstinence only
when used as part
of a
comprehensive
psychosocial
treatment program.

102
 TOPIRAMATE

Trade Name:
Topamax, Trokendi XR

Dosage:-
Epilepsy (monotherapy)
PO (Adults and children > 10 yr): Immediate-release—25 mg twice daily initially, gradually
increase at weekly intervals to 200 mg twice daily over a 6– wk period; Extended-release—50
mg once daily initially, gradually increase at weekly intervals to 400 mg once daily over a 6– wk
period.
PO (Children 2–<10 yr and <11 kg): Immediate-release—25 mg once daily in the evening
initially, gradually increase at weekly intervals to 75 mg twice daily over a 5-7– wk period; if
needed may continue to titrate dose on a weekly basis up to 125 mg twice daily.
PO (Children 2–< 10 yr and 12– 22 kg): Immediate-release—25 mg once daily in the evening
initially, gradually increase at weekly intervals to 100 mg twice daily over a 5-7– wk period; if
needed may continue to titrate dose on a weekly basis up to 150 mg twice daily.
PO (Children 2–< 10 yr and 23– 31 kg): Immediate-release—25 mg once daily in the evening
initially, gradually increase at weekly intervals to 100 mg twice daily over a 5-7– wk period; if
needed may continue to titrate dose on a weekly basis up to 175 mg twice daily.
PO (Children 2–< 10 yr and 32– 38 kg): Immediate-release—25 mg once daily in the evening
initially, gradually increase at weekly intervals to 125 mg twice daily over a 5-7– wk period; if
needed may continue to titrate dose on a weekly basis up to 175 mg twice daily.
PO (Children 2–< 10 yr and >38 kg): Immediate-release—25 mg once daily in the evening
initially, gradually increase at weekly intervals to 125 mg twice daily over a 5- 7– wk period; if
needed may continue to titrate dose on a weekly basis up to 200 mg twice daily.

Renal Impairment
PO (Adults): CCr70 ml/min— decrease in dose by 50%.

Migraine prevention
PO (Adults): 25 mg at night initially, increase by 25 mg/day at weekly intervals up to target dose
of 100 mg/day in 2 divided doses.

Classification:-
103
 Therapeutic: anticonvulsants, mood stabilizers

Mechanism of Indications Contraindications Side Effects Nursing management

Action
Action may be Seizures Contraindicated in CNS: Increase in -Monitor closely for notable
due to: including: Hypersensitivity; SEIZURES, changes in behavior that
Blockade of partial-onset, Recent alcohol use SUICIDAL could indicate the emergence
sodium primary (within 6 hr before THOUGHTS, or worsening of suicidal
channels in generalized and after use of dizziness, thoughts or behavior or
neurons, tonic-clonic, extended-release drowsiness, depression.
Enhancement of seizures due to product); fatigue, impaired -Seizures: Assess location,
gamma- Lennox- Metabolic acidosis concentration/me duration, and characteristics
aminobutyrate Gastaut (on metformin) mory, of seizure activity.
(GABA), an syndrome. (with extended- nervousness, -Migraines: Assess pain
inhibitory Prevention of release product psychomotor location, intensity, duration,
neurotransmitte migraine only); slowing, speech and associated symptoms
r, Prevention of headache in Lactation:Lactatio problems, (photophobia, phonophobia,
activation of adults n. sedation, nausea, vomiting) during
excitatory (immediaterele Use Cautiously in: aggressive migraine attack. Monitor
receptors. ase only). All patients reaction, frequency and intensity of
Therapeutic Unlabeled Use: (mayqrisk of agitation, pain on pain scale.
Effects: Adjunct in suicidal anxiety, Bipolar Disorder: Assess
Decreased treatment of thoughts/behaviors cognitive mental status (mood,
incidence of bipolar ); Renal disorders, orientation, behavior) and
seizures. disorder. impairment (dose confusion, cognitive abilities before and
Decreased Infantile reduction depression, periodically during therapy.
incidence/severi spasms. recommended if malaise, mood -Lab Test Considerations:
ty of migraine CCr 70 problems. Monitor CBC with
headache. mL/min/1.73 m2); EENT: abnormal differential and platelet count
Hepatic vision, diplopia, before therapy to determine
impairment; nystagmus, acute baseline levels and
Dehydration; myopia/secondar periodically during therapy.
Patients y angle closure Frequently causes anemia.
predisposed to glaucoma. GI: -Hepatic function should be
metabolic acidosis; nausea, monitored periodically
Patients allergic to abdominal pain, throughout therapy. May
sulfa; anorexia, cause increase AST and ALT
OB:Mayqrisk for constipation, dry levels.
cleft palate and/or mouth, -Evaluate serum bicarbonate
cleft lip in infants encephalopathy, prior to and periodically
exposed during hyperammonemi during therapy. If metabolic
pregnancy; use a. GU: kidney acidosis occurs, dosing taper
only if maternal stones. or discontinuation may be
benefit outweighs Derm:oligohydro necessary.
fetal risk; Pedi: sis (increase in -Instruct patient to take
Children are more children). F and topiramate exactly as

104
prone to E: directed. Take missed doses
oligohydrosis and hyperchloremic as soon as possible but not
hyperthermia; metabolic just before next dose; do not
safety in children 2 acidosis. Hemat: double doses. Notify health
yr (immediate- leukopenia. care professional if more
release) and 6 yr Metab: weight than 1 dose is missed. -
(extended-release) loss, Medication should be
not established; hyperthermia gradually discontinued to
Geri: Consider (increase in prevent seizures and status
age-related children). Neuro: epilepticus.
decrease in ataxia, - Instruct patient to read the
renal/hepatic paresthesia, Medication Guide before
impairment, tremor.Misc: starting and with each Rx
concurrent disease fever. refill, changes may occur.
states and drug May cause decreased
therapy. sweating and increased body
temperature. Advise patients,
especially parents of
pediatric patients, to provide
adequate hydration and
monitoring, especially during
hot weather.
-May cause dizziness,
drowsiness, confusion, and
difficulty concentrating.
Caution patients to avoid
driving or other activities
requiring alertness until
response to medication is
known.

GABAPENTIN

105
Trade Name:-Gralise, Horizant, Neurontin.

Dosage:-
The sustained/extended-release formulations should not be interchanged with the immediate-
release products.
Epilepsy
PO (Adults and Children >12 yr): 300 mg 3 times daily initially. Titration may be continued until
desired (range is 900– 1800 mg/day in 3 divided doses; doses should not be more than 12 hr
apart). Doses up to 2400– 3600 mg/day have been well tolerated.
PO (Children >5–12 yr): 10– 15 mg/kg/day in 3 divided doses initially titrated upward over 3
days to 25– 35 mg/kg/day in 3 divided doses; dosage interval should not exceed 12 hr (doses up
to 50 mg/kg/day have been used).
PO (Children 3–4 yrs): 10– 15 mg/kg/day in 3 divided doses initially titrated upward over 3 days
to 40 mg/kg/day in 3 divided doses; dosage interval should not exceed 12 hr (doses up to 50
mg/kg/day have been used).

Renal Impairment
PO (Adults and Children >12 yr):CCr 30– 59 mL/min—200– 700 mg twice
daily; CCr 15– 29 mL/min—200– 700 mg once daily; CCr 15 mL/min—100–
300 mg once daily; CCr<15 mL/min—Reduce daily dose in proportion to CCr.

Post-Herpetic Neuralgia
PO (Adults): Immediate-release– 300 mg once daily on first day, then 300 mg 2 times daily on
second day, then 300 mg 3 times/day on day 3, may then be titrated upward as needed up to 600
mg 3 times/day; Sustained-release (Gralise)—300 mg once daily on first day, then 600 mg once
daily on second day, then 900 mg once daily on days 3– 6, then 1200 mg once daily on days 7–
10, then 1500 mg once daily on days 11– 14, then 1800 mg once daily thereafter; Extended-
release (Horizant)—600 mg once daily in the morning on days 1– 3, then 600 mg twice daily
thereafter.

Restless Legs Syndrome

PO (Adults): Extended-release (Horizant)—600 mg once daily at 5 pm.
Renal Impairment
(Adults):CCr 30– 59 mL/min—300 mg once daily at 5 pm; may increase to 600 mg once daily
at 5 pm as needed ; CCr 15– 29 mL/min—300 mg once daily at 5 pm; CCr 15 mL/min—300 mg
every other day; CCr 15 mL/min (on hemodialysis)—Not recommended.

Neuropathic Pain (unlabeled use)

PO (Adults): 100 mg 3 times daily initially. Titrate weekly by 300 mg/day up to 900–2400
mg/day (maximum: 3600 mg/day).
PO (Children): 5 mg/kg/dose at bedtime initially then increase to 5 mg/kg BID on day 2 and 5
mg/kg TID on day 3. Titrate to effect up to 8– 35 mg/kg/day in 3 divided doses.

106
 Classification:-Therapeutic: analgesic adjuncts, therapeutic, anticonvulsants, mood stabilizers.

Mechanism of Indications Contraindications Side Effects Nursing management

Action
Mechanism of Anticonvulsant. Contraindicated in CNS:  Monitor closely
action is not Postherpetic Hypersensitivity. SUICIDAL for notable changes in
known. May neuralgia. Use Cautiously in: THOUGHTS, behavior that could
affect transport Unlabeled All patients (may confusion, indicate the emergence or
of amino acids Use:Chronicpain increase risk of depression, worsening of suicidal
across and ,prevention suicidal dizziness, thoughts or behavior or
stabilize ofmigraine thoughts/behaviors) drowsiness, depression.
neuronal headache. ; Renal sedation,  Seizures: Assess
membranes. Bipolar disorder, insufficiency anxiety, location, duration, and
Therapeutic anxiety. (decrease in dose concentration characteristics of seizure
Effects: and/or increase in difficulties activity.
Decreased dosing interval if (children),  Post-herpetic
incidence of CCr<60 mL/min); emotional Neuralgia &
seizures. OB: Pregnancy; lability Neuropathic Pain:
Decreased post- Pedi: Children <18 (children), Assess location,
herpetic pain. yr (sustained- hostility, characteristics, and
Decreased leg /extended-release) hyperkinesia intensity of pain
restlessness. or <3 yr (children), periodically during
(immediate-release) malaise, vertigo, therapy.
(safety not weakness.  Migraine
established); EENT: Prophylaxis: Monitor
Lactation: abnormal vision, frequency and intensity of
Discontinue drug or nystagmus. CV: pain on pain scale.
bottle-feed; Geri: hypertension.  Restless Leg
May be more GI: weight gain, Syndrome: Assess
susceptible to anorexia, frequency and intensity of
toxicity due to age- flatulence, restless leg syndrome
relatedpin renal gingivitis. MS: prior to and periodically
function. RHABDOMYO during therapy.
LYSIS,  Lab Test
arthralgia,qcreati Considerations: May
ne kinase. cause false-positive
Neuro: ataxia, readings when testing for
altered reflexes, urinary protein with Ames
hyperkinesia, N-Multistix SG dipstick
paresthesia. test; use sulfosalicylic
Misc: MULTI- acid precipitation
ORGAN procedure.
HYPERSENSIT
 May cause
IVITY leukopenia.
REACTIONS,
 Advise patient and
facial edema.
family to notify health
107
care professional if
thoughts about suicide or
dying, attempts to commit
suicide; new or worse
depression; new or worse
anxiety; feeling very
agitated or restless; panic
attacks; trouble sleeping;
new or worse irritability;
acting aggressive; being
angry or violent; acting on
dangerous impulses; an
extreme increase in
activity and talking, other
unusual changes in
behavior or mood occur.
 Instruct patient to
notify health care
professional of medication
regimen before treatment
or surgery.
 Advise female
patient to notify health
care professional if
pregnancy is planned or
suspected or if breast
feeding.
 Advise patient to
carry identification
describing disease process
and medication regimen at
all times.

108
ANTIEPILEPTIC DRUGS

109
 ANTIEPILECTIC DRUGS

Introduction
Antiepileptic Drug
• A drug which decreases the frequency and/or severity of seizures in people with epilepsy
• Treats the symptom of seizures, not the underlying epileptic condition
• Goal—maximizes quality of life by minimizing seizures and adverse drug effects

Classification of AEDs
Phenytoin Phenobarbital Primidone Carbamazepine Ethosuximide Valproate (valproic acid)
Trimethadione (not current in use)
amotrigine Felbamate Topiramate Gabapentin Tiagabine Vigabatrin Oxycarbazepine
Levetiracetam Fosphenytoin
In general. The newer AEDs have less consosedating effects than the classical AEDs
History-of Antiepileptic Drug Therapy in the U.S.
• 1857 – Bromides
• 1912 - Phenobarbital
• 1937 – Phenytoin
• 1954 – Primidone
• 1960 - Ethosuximide
• 1974 - Carbamazepine
• 1975 – Clonazepam (benzodiazapine)
• 1978 – Valproate
• 1993 - Felbamate, Gabapentin
• 1995 - Lamotrigine
• 1999 – Levetiracetam
• 2000 - Oxcarbazepine, Zonisamide
• Vigabatrin—not approved in US

LAMOTRIGINE

110
 Trade Name
Lamictal

Classification
Central nervous system agent; anticonvulsant

Dose
Available forms-25 mg 100 mg, 150 mg. 200 mg tablets; 2 mg. 5 mg, 25 mg chewable tablets.
Adults-25-200 mg/day PO in two divided doses
Paediatric patients-Safety and efficacy not established

MECHANISM OF INDICATION CONTRAINDIC SIDE EFFECT NURSE’S RESPONSIBILITY

ACTION ATION
The exact Adjuvant Contraindicated Skin rash, -Monitor patient for any sign of
mechanism of therapy in the with Steven skin rash; discontinue
action is unknown; treatment of  allergy Johnson lamotrigine immediately if rash
thought to act by partial seizures to drug, syndrome, appear.
inhibiting the in adults with  lactation Toxic
release of epilepsy and epidermal -Monitor renal and hepatic
glutamate, an Monotherapy pregnan necrolysis with function before and during
excitatory in adults with cy multiorgan therapy
neurotransmitter, at partial seizures  Use failure,
voltage-sensitive Generalized cautious -Advice the patient for periodic
sodium channels. tonic-clonic, ly with dizziness ophthalmologic examination
Stabilizing the absence, or impaired insomnia, with long-term use.
neuronal membrane myoclonic hepatic, headache,
and modulating seizures in renal or somnolence, -Do not discontinue drug
calcium-dependent adults, cardiac ataxia, abruptly or change the dosage
presynaptic release treatment of function diplopia, without medical advice.
of excitatory amino bipolar : blurred vision,
acids disorder patients nausea, -Taper drug slowly over a two
Pharmacokinetics <16 year vomiting week period when discontinuing.
Usual
administration is -Advise the patient not to breast
oral route. feed while taking drug.
Metabolized in the
liver, may cross
placenta; may pass
into breast
milk, it excretes
through urine.

111
 OXCARBAZEPINE

Trade name
Trileptal, Oxtellar XR

Classification
Antiepileptic

Dose
Usual preparations —Tablet 150,300, 600 mg oral suspension —60mg/m1
Usual dosages —Starting dose - 300 mg/day (5mg/kg/day), which may be increased by weekly
increment of 300 mg/week Maintenance - 900-1800
mg/day (20-45 mg/kg/day)
Dosing frequency— 2 times/day

112
MECHANI INDICATI CONTRAINDICA SIDE EFFECT NURSE’S
SM OF ON TION RESPONSIBILITY
ACTION
Mechanism Primary TRILEPTAL is Fatigue, asthenia, -Restrict more water intake
of action Indications indicated for use as peripheral and instruct low sodium diet.
Blockade of Adjunctive monotherapy or edema,generalized
voltage gated therapy or adjunctive therapy edema, chest pain,
Na channels monotherap in the treatment of weight gain.
and N and P y for partial partial seizures in Hypotension,
type calcium and adults and as Lymphadenopathy
channels. secondary monotherapy in the Hyponatremia.
generalized treatment of partial Muscle weakness.
seizures. - seizures in -Advice the patient to tale
Also useful paediatric patients drug or medicine after food
to treat• aged 4 years and to reduce GI irritation.
primary above with epilepsy, Nausea, vomiting,
generalized and as adjunctive abdominal
tonic clonic therapy in paediatric pain, diarrhea,
seizures not patients aged 2 years dyspepsia, -Ensure the client does not
associated and above with constipation, gastritis, participate in activities that
with partial seizures anorexia, dry mouth. require alertness for example
absence driving.
and Headache, dizziness,
myoclonic somnolence, ataxia,
seizures nystagmus, abnormal
gait, insomnia, tremor,
nervousness, agitation,
abnormal
coordination, speech -Monitor patient for any sign
disorder, confusion, of skin rash inform
abnormal thinking, phyisician.
aggravate convulsions,
emotional lability. -Advice the patient for
periodic ophthalmologic
Rhinitis, cough, examination with long-term
bronchitis, use.
pharyngitis. -Add antibiotics for infection
according to physician order.
Acne, hot flushes, -Monitor for and report Sign
purpura, Stevens- & Symptom of
Johnson Hyponatremia (e.g., nausea,
syndrome, toxic malaise, headache, lethargy,
epidermal necrolysis. confusion); CNS impairment
(e.g., somnolence, excessive

113
Diplopia, vertigo, fatigue, cognitive deficits,
abnormal and speech or language
vision, abnormal problems, in coordination,
accommodation, taste gait disturbances).
perversion, ear ache -Monitor phenytoin levels
when administered
Urinary tract infection, concurrently.
micturition frequency, -Lab tests: Periodic serum
vaginitis. sodium, T4 level; when
oxcarbazepine is used as
adjunctive therapy, closely
monitor plasma level of the
concomitant antiepileptic
drug during titration of the
oxcarbazepine dose.
Patient & Family Education
-Notify physician of the
following: Dizziness, excess
drowsiness, frequent
headaches, malaise, double
vision, lack of coordination,
or persistent nausea.
-Exercise special caution
with concurrent use of
alcohol or CNS depressants.
-Use caution with potentially
hazardous activities and
driving until response to drug
is known.
-Use or add contraceptive
since drug may render
hormonal methods
ineffective.
-Do not breast feed while
taking this drug.

114
ANXIOLYTICS (ANTI ANXIETY DRUGS)
& HYPNOSEDATIVES

115
 ANXIOLYTICS (ANTI ANXIETY DRUGS) &
HYPNOSEDATIVES

INTRODUCTION
Anxiolytics, sedatives and hypnotics are medicines that work on the central nervous system to
relieve anxiety, aid sleep, or have a calming effect.
Anxiolytics are also known as minor tranquilizers. The term is less common in modern texts
and was originally derived from a dichotomy with major tranquilizers, also known
as neuroleptics or antipsychotics.

Types of Anxiolytics, and hypnosedatives

ANXIOLYTICS

NON-
BARBITURATES BENZODIAZEPINE
BARBITURATES

Barbiturates
Barbiturates exert an anxiolytic effect linked to the sedation they cause. The risk of abuse and
addiction is high. Many experts consider these drugs obsolete for treating anxiety but valuable
for the short-term treatment of severe insomnia, though only after benzodiazepines or non-
benzodiazepines have failed.

116
Non-benzodiazepines
Non-benzodiazepine such as zolpidem, zopiclone and zaleplon, demonstrate hypnotic efficacy
similar to that of benzodiazepines along with excellent safety profiles. Non
benzodiazepines generally cause less disruption of normal sleep architecture
than benzodiazepines.

Benzodiazepines
Benzodiazepines are prescribed for short-term and long-term relief of severe and disabling
anxiety. Benzodiazepines may also be indicated to cover the latent periods associated with the
medications prescribed to treat an underlying anxiety disorder. They are used to treat a wide
variety of conditions and symptoms and are usually a first choice when short-
term CNS sedation is needed. If benzodiazepines are discontinued rapidly after being taken
daily for two or more weeks there is some risk of benzodiazepine withdrawal and rebound
syndrome, which varies by the specific drug. Tolerance and dependence may also occur, but
may be clinically acceptable,] also the risk of abuse is significantly smaller than in case of
barbiturates. Cognitive and behavioral adverse effects are possible. Benzodiazepines include:
• Alprazolam (Xanax)
• Bromazepam (Lectopam, Lexotan)
• Chlordiazepoxide (Librium)
• Clonazepam (Klonopin, Rivotril)
• Clorazepate (Tranxene)
• Diazepam (Valium)
• Flurazepam (Dalmane)
• Lorazepam (Ativan)
• Oxazepam (Serax, Serapax)
• Temazepam (Restoril)
• Triazolam (Halcion)
Benzodiazepines exert their anxiolytic properties at moderate dosage. At higher
dosage hypnotic properties occur.
ALPRAZOLAM

117
 Trade Name
Alptax, Apo-Alpraz, Novo-Alprazol

Classification
Antianxiety agents, sedatives/hypnotics—benzodiazepines

Dose
Oral: Adults-0.25-0.5 mg, 2 to 3 times daily

MECHANISM INDICATI CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION ON ATION EFFECT
Antianxiety agents Anxiety Acute alcohol CNS -Inform the patient about side effect
may increase the disorders, intoxication with Ataxia, of the drug.
inhibiting effects of panic disorder, depressed vital signs, light- -Assess the patient for motor
gamma premenstrual acute angle closure headedness, responses, such as agitation, tension
aminobutyric acid syndrome, glaucoma, transient and trembling, and autonomic
(GABA), an insomnia, myasthenia gravis, mild responses, such as cold, clammy hands
inhibitory irritable bowel severe chronic somnolence, and diaphoresis
neurotransmitter. syndrome. obstructive slurred - Caution the patient to avoid tasks that
Benzodiazepines pulmonary disease speech. require mental alertness or motor skills
reduce anxiety by (COPD), Confusion, until his response to the drug has been
stimulating the action hypersensitivity, depression, established.
of the inhibitory pregnancy and headache -Avoid activity that require alertness
neurotransmitter lactation.
GABA in the limbic CVS:- - Monitor vital sign every shift
system. The limbic Tachycardia -Check potassium level
system plays an to - Observe for symptoms of dizziness,
important role in the Cardiovascu palpitations, syncope or
regulation of human lar collapse Weakness
behavior. Dysfunction
of GABA G.I.: - - Provide the patient with sugarless,
neurotransmission in Dry mouth candy or gum, ice and frequent sips of
the limbic system may nausea. water
be linked to the - Ensure that the client practices strict
development of oral hygiene
certain anxiety
disorders. Constipatio - Order food high in fibers
n - Encourage increase in physical
activity and fluid intake if not contra
indicated
-Administer with food to minimize
gastric irritation
Occular:- -Explain that symptoms will most likely
Blurred subside after a few weeks.
vision, -Advise the client not to drive a vehicle
until vision clears

118
Skin:- - Reports the appearance of any rash on
Rash, skin to the physician
Photosensitivi - Avoid spilling any of the liquid
ty concentrate skin
-Ensure that client wears protective sun
screens, clothing and sunglasses while
spending the outdoor
Metabolic:- -Weight the client every day
Changes in - Order a caloric controlled diet
weight -Provide diet and exercise

Physical & -Advice the patient do not abrupt the

Psychologic drug suddenly after long term uses.
al -Advice the patient to maintain
Dependence: follow-up check up routinely.
- Abrupt or -Urge the patient to avoid alcohol
too-rapid during therapy
withdrawal -Encourage the patient to stop
may result in smoking because smoking reduces
pronounced alprazolam's effectiveness
restlessness, -Urge the female patient on long-term
irritability, therapy to use effective contraception
insomnia, during therapy and notify the physician
hand immediately if she becomes or even
tremors, suspects to be pregnant
abdominal -Inform the patient that drowsiness
and muscle usually disappears with continued
cramps, therapy
diaphoresis, - Closely observe clients with history of
vomiting and seizures
seizures. - Discuss with the physician the
Overdose possibility of administering the
results in drug at bed time
somnolence, - Discuss with the physician the
confusion, possible decrease in dosage or
diminished order for less sedating
reflexes and -Advice the patient to stop the drug
coma. gradually.
-Report the physician if withdrawal
symptoms are more serious
-Provide information about Chronic use
of alprazolam during pregnancy may
produce withdrawal symptoms in the
patient and CNS depression in the
neonate

119
 CHLORDIAZEPDXIDE

Trade Name
librium, Novopoxide

Classification
Antianxiety agents, sedatives/hypnotics—benzodiazepin

Dose
Oral: 15-100 mg per day in 3-4 divided doses. Parental: 25- 50 mg IV or IM

MECHANISM INDICATI CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION ON ATION EFFECT
Antianxiety agents alcohol Comatose patients, CNS -Inform the patient about side effect
may increase the withdrawal pre-existing CNS Ataxia, of the drug.
inhibiting effects of symptoms, depression, dizziness, -Assist the patient with ambulation if he
gamma anxiety, panic uncontrolled severe somnolence, experiences ataxia or drowsiness
aminobutyric acid disorder, tension pain, narrow angle Confusion, -Assess the patient's BP, pulse rate and
(GABA), an headache, glaucoma, acute respiratory rate, rhythm and depth
inhibitory tremors. alcohol intoxication. immediately before giving
neurotransmitter. chlordiazepoxide
Benzodiazepines - Caution the patient to avoid tasks that
reduce anxiety by require mental alertness or motor skills
stimulating the action until his response to the drug has been
of the inhibitory established.
neurotransmitter -Avoid activity that require alertness
GABA in the limbic

120
system. The limbic G.I. -Administer with food to minimize
system plays an Disturbanc gastric irritation
important role in the es -Gives sips of water frequently
regulation of human - Order food high in fibers
behavior. Dysfunction - Encourage increase in physical
of GABA activity and fluid intake if not contra
neurotransmission in indicated
the limbic system may
be linked to the CVS:- - Monitor vital sign every shift
development of Tachycardia -Check potassium level
certain anxiety to - Observe for symptoms of dizziness,
disorders. Cardiovascu palpitations, syncope or
lar collapse weakness

Pain at IM -Inform the patient that intramuscular (IM)

injection injection may produce discomfort
site -Keep the patient recumbent for up to 3
hours after Parenteral administration to
reduce the drug's hypotensive effect
Dermatolog - Reports the appearance of any rash on
ic: Skin skin to the physician
Rash - Avoid spilling any of the liquid
concentrate skin Photo sensitivity

Thrombop -Give IV injection slowly.

hlebitis & -Avoid exacerbation from the site of
Carpel injection
tunnel -Change the intracath timely.
syndrom -Keep the patient recumbent for up to 3
hours after Parenteral administration to
reduce the drug's hypotensive effect

hysical & -Advice the patient do not abrupt the

Psychologic drug suddenly after long term uses.
al -Advice the patient to maintain
Dependence: follow-up check up routinely.
- Abrupt or -Urge the patient to avoid alcohol
too-rapid during therapy
withdrawal -Inform the patient that drowsiness
may result in usually disappears with continued
pronounced therapy
restlessness, - Closely observe clients with history of

121
 irritability, seizures
insomnia, - Discuss with the physician the
hand possibility of administering the
tremors, drug at bed time
abdominal - Discuss with the physician the
and muscle possible decrease in dosage or
cramps, order for less sedating
diaphoresis, -Advice the patient to stop the drug
vomiting and gradually.
seizures. -Report the physician if withdrawal
Overdose symptoms are more serious
results in
somnolence,
confusion,
diminished
reflexes and
coma.

DIAZEPAM

Trade Name
Valium, valpam

Classification
Antianxiety agents, sedatives/hypnotics—benzodiazepines.

Dose
Oral: 2-10 mg, 2-4 times a day. Parental: 2-10 mg, may repeat in 3 to 4 hours if needed

122
MECHANISM INDICATI CONTRAINDIC SIDE NURSING RESPONSIBILITY
OF ACTION ON ATION EFFECT
May potentiate the Anxiety, Angle closure CNS -Assess the patient's BP, pulse rate and
effects of gamma- skeletal glaucoma, coma, pre- Dizziness, respiratory rate, rhythm and depth
aminobutyric acid muscle existing CNS drowsiness, immediately before giving diazepam
(GABA) and other relaxation, depression, lethargy, -Inform the patient that drowsiness
inhibitory preanesthesia, respiratory hangover, usually disappears with continued
neurotransmitters by alcohol depression, severe paradoxical therapy
binding to specific withdrawal, uncontrolled pain. excitation, -Instruct the patient to change positions
benzodiazepine status mental slowly from recumbent to sitting, before
receptors in the epilepticus, depression, standing to prevent dizziness
limbic and cortical control of headache, -Inform the patient about side effect
areas of the central increased hypotension of the drug.
nervous system seizure activity -Assess the patient for motor
(CNS). GABA inhibits in patients with responses, such as agitation, tension
excitatory stimulation refractory and trembling, and autonomic
which helps control epilepsy who responses, such as cold, clammy hands
emotional behavior. are on stable and diaphoresis
Diazepam suppresses regimens of - Caution the patient to avoid tasks that
the spread of seizure anti_ require mental alertness or motor skills
activity caused by convulsants, until his response to the drug has been
seizure-producing treatment of established.
foci in the cortex, panic disorder, -Avoid activity that require alertness
thalamus and limbic tension -Avoid other CNS depressants drugs
structures. headache, along with diazepam
tremors. CVS: -Assess the patient’s BP, pulse rate
Hypotensio before giving diazepam.
n -Keep the patient in recumbent
position after parentral administration
to reduce drug’s hypertensive effect

Respirator -Monitor respiratory rate, depth and

y: rhythm before giving diazepam
Respiratory
depressin

G.I.: - - Provide the patient with sugarless,

Nausea, candy or gum, ice and frequent sips of
Vomiting water
- Ensure that the client practices strict
oral hygiene
- Order food high in fibers
Constipatio - Encourage increase in physical
n activity and fluid intake if not contra
indicated
-Administer with food to minimize
gastric irritation

123
Occular:- -Explain that symptoms will most likely
Blurred subside after a few weeks.
vision, -Advise the client not to drive a vehicle
until vision clears

Skin:- - Reports the appearance of any rash on

Rashes skin to the physician
- Avoid spilling any of the liquid
concentrate skin

Metabolic:- -Weight the client every day

Changes in - Order a caloric controlled diet
weight -Provide diet and exercise

Venous -If intramuscular (IM) administration is

Thrombosi preferred give deep IM
s& -For iv administration do not mix with
Phlebitis any other drug. Give slow as
respiratory or cardiac arrest can occure;
-monitor vital signs during IV
administration. Prevent extravasations,
since it can cause phlebitis venous
thrombosis.
-Keep the patient recumbent for up to 3
hours after parenteral administration to
reduce the drug's hypotensive effect

Psychologic -Advice the patient do not abrupt the

al drug suddenly after long term use.
Dependence: -Advice the patient to maintain
follow-up check up routinely.
-Urge the patient to avoid alcohol
during therapy
- Discuss with the physician the
possibility of administering the
drug at bed time
- Discuss with the physician the
possible decrease in dosage or
order for less sedating
-Advice the patient to stop the drug
gradually.
-Report the physician if withdrawal
symptoms are more serious

124
 PHENBARBITONE

Trade Name
Oral preparations: Bellatal, Solfoton
Parenteral: Luminal Sodium

Classification
Barbiturates- Anticonvulsant, sedative-hypnotic

Dose
Preoperative: 1 to 3 mg/kg.
1. Daytime sedative: 30 to 120 mg daily in 2 to 3 divided doses.
2. Bedtime hypnotic: 100 to 320 mg.
3. Anticonvulsant: 50 to 100 mg 2 to 3 times daily.

MECHANISM INDICATI CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION ON ATION EFFECT
Phenobarbital acts on the treatment Hepatic disease; Nervous -Inform the patient about side effect
GABAA receptors, of all types of history of addiction system: Agi of the drug.
increasing synaptic seizures, to hypnotics or tation, -Assess the patient for motor
inhibition. This has except absence sedatives; confusion, responses, such as agitation, tension
the effect of seizures ,tremo hypersensitivity to hyperkinesia and trembling, and autonomic
elevating seizure rs and seizures phenobarbital, other , ataxia, CN responses, such as cold, clammy hands
threshold and associated barbiturates, or their S depression and diaphoresis
reducing the spread with abrupt components; , - Caution the patient to avoid tasks that
of seizure activity withdrawal nephritis; porphyria; nightmares, require mental alertness or motor skills
from a seizure focus. from severe nervousness, until his response to the drug has been
Phenobarbital may benzodiazepin respiratory disease psychiatric established.
also inhibit calcium es, insomnia, with airway disturbance, -Avoid activity that require alertness

125
channels, resulting in preanesthesia obstruction hallucinatio -Advice the patient to avoid driving or
a decrease in or dyspnea ns, insomnia handling heavy machinary
excitatory transmitter , anxiety,
release. The dizziness,
sedative-hypnotic thinking
effects of abnormality
phenobarbital are CVS: -During I.V. use, monitor blood
likely the result of its Hypotensio pressure, respiratory rate, and heart rate
effect on the n, sinus and rhythm.
polysynaptic bradycardia -Anticipate increased risk of
midbrain reticular hypotension, even at recommended rate.
formation, which Keep resuscitation equipment readily
controls CNS available.
arousal. RESP: -Monitor respiratory rate, depth and
Bronchospa rhythm
sm, -
respiratory
depression
G.I.: - - Provide the patient with sugarless,
Dry mouth candy or gum, ice and frequent sips of
nausea. water
- Ensure that the client practices strict
oral hygiene

Constipatio - Order food high in fibers

n - Encourage increase in physical
activity and fluid intake if not contra
indicated
-Administer with food to minimize
gastric irritation
Skin:- - Reports the appearance of any rash on
Dermatitis, skin to the physician
photosensiti - Avoid spilling any of the liquid
vity, rash, concentrate skin Photo sensitivity --
urticaria -Ensure that client wears protective sun
screens, clothing and sunglasses while
spending the outdoor
Metabolic:- -Weight the client every day
Changes in - Order a caloric controlled diet
weight -Provide diet and exercise

Physical & -Advice the patient do not abrupt the

Psychologic drug suddenly after long term use.
al -Advice the patient to maintain
Dependence: follow-up check up routinely.
- The patient should be warned against
increasing the dose of the drug without
consulting a physician.
-Urge the patient to avoid alcohol

126
 during therapy
- Discuss with the physician the
possibility of administering the
drug at bed time
- Discuss with the physician the
possible decrease in dosage or
order for less sedating
-Advice the patient to stop the drug
gradually.
-Report the physician if withdrawal
symptoms are more serious
-Do not take this drug longer than 2
weeks (for insomnia), and do not
increase the dosage without consulting
health care provider.
Do not reduce the dosage or
discontinue this drug (when used for
epilepsy); abrupt discontinuation could
result in a serious increase in seizures.

THIOPENTONE

Trade Name
Sodium Pentothal, thiopental, trapanal

Classification
Barbiturates, Anticonvulsant, sedative-hypnotic

127
 Dose
IV Induction of anesth As 2.5 or 5% soln: 100-150 mg, repeat every 30-60 sec if needed. Max:
500 mg. Max in pregnant women: 250 mg.
Status epilepticus With assisted ventilation: As 2.5% soln: 75-125 mg. Reduction of raised
intracranial pressure Intermittent bolus inj of 1.5-3.5 mg/kg, if adequate ventilation is
provided.

MECHANISM INDICATIO CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION N ATION EFFECT
Depresses the CNS Status Porphyria; dyspnoea CNS -Inform the patient about side effect of
and may inhibit epileptus, or respiratory Agitation, the drug.
ascending Phobia, obstruction. anxiety, -Avoid activity that require alertness
transmission of Convulsion, seizures Advise patient to use caution when
impulses in the Reduction of Special precaution driving or performing tasks that require
reticular formation. raised the patient with alertness for at least 24 hours after
Thiopental may intracranial Hypovolaemia; receiving thiopental.
enhance pressure, history of severe - Instruct patient not to consume alcohol
or mimic inhibitory Induction of asthma, severe or other CNS depressants for at least
action of anaesthesia cardiac disease, 24 hours after thiopental administration
gammaaminobutyric severe anaemia, (unless prescribed) because they increase
acid, thereby causing hyperkalaemia, the effects of thiopental.
anticonvulsant toxaemia, -In patient with a history of seizures,
effect and producing myasthenia gravis, institute seizure precautions according to
sedation myxoedema; severe facility protocol.
and hypnosis. renal or hepatic
Thiopental may disease; muscular CVS: -If patient has a history of CV disease or
reduce ICP by dystrophies, Bradycardia, hypotension, monitor her for CV
increasing cerebral adrenocortical hypotension, depressant effects, such as bradycardia,
vascular resistance, insufficiency; shock, hypotension, or shock.
which increased tachycardia,
decreases cerebral intracranial pressure; thrombophle
blood flow and elderly, pregnancy, bitis
volume. actation. Avoid Respiratory -Monitor respiratory rate, rhythm, and
Onset: IV: 30 sec. extravasation or : Apnea, quality for signs of respiratory
Rectal: 8-10 min. intra-arterial bronchospas depression in debilitated patient or one
Distribution: Crosse administration. IV m, cough, with a history of respiratory disease.
s the placenta and inj of concentrated laryngospas
enters breast milk. thiopental solution m,
Protein-binding: 80% e.g. 5% may cause respiratory
Metabolism: Hepatic thrombophloebitis. depression,
; mostly converted to wheezing
inactive metabolites. G.I.: - - Provide the patient with sugarless,
Excretion: Eliminati Dry mouth candy or gum, ice and frequent sips of
on half-life: 10-12 hr nausea. water
(adults); 6 hr - Ensure that the client practices strict
(childn); 26-28 hr oral hygiene
(obese and pregnant Constipatio
patients). n - Order food high in fibers
- Encourage increase in physical activity

128
 and fluid intake if not contra indicated
-Administer with food to minimize
gastric irritation
Dermatolog - Reports the appearance of any rash on
ic:- Skin skin to the physician
Rash - Avoid spilling any of the liquid
concentrate skin Photo sensitivity

ETHANOL

Trade name
Ethylic alcohol, Ethyl alcohol, Ethylol

Dose
Loading dose
600 mg/kg IV (ie, 7.6 mL/kg of 10% EtOH solution)
600-700 mg/kg PO/NG using a 95% solution diluted to ≤ 20% with water or juice
Maintenance dose
65-155 mg/kg/hr depending on alcohol consumption status (lower for nondrinker)
Oral maintenance = 1.5 mL/kg/hr (IV = 1.4 mL/kg/hr) 10% ethanol
Chronic alcoholics and hemodialysis patients need increased dose; increased maintainence by
50%; non-users may need less
Maintain serum ethanol of 100-150 mg/dL [21.7-32.55 mmol/

Classification
Non- Barbiturates, anxiolytics

MECHANISM INDICATIO CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION N ATION EFFECT
Ethanol affects the Severe pain; brain operation, CNS: -Inform the patient about side effect of
brain’s neurons in Chronic pain; coma in a diabetic Headache, the drug.
several ways. It alters Trigeminal patient, dizziness, - Caution the patient to avoid tasks that
their membranes as neuralgia, diabetes tremor, require mental alertness or motor skills
well as their ion anxiety porphyria, lethargy, until his response to the drug has been
channels, enzymes, alcoholism, amnesia, established.
and receptors. low blood pressure, stupor, -Avoid activity that require alertness
Alcohol also binds liver problems, coma, loss -Advice the patient to avoid drive and
directly to the severe renal of handling of heavy machinery.
receptors for impairment, judgement, - Discuss with the physician the
acetylcholine, urinary tract emotional possibility of administering the
serotonin, GABA, infection, lability, drug at bed time
and the NMDA heavy bleeding after slurred - Discuss with the physician the possible
receptors for the delivery of a speech, decrease in dosage or
glutamate. The baby, ataxia, order for less sedating
sedative effects of seizures dysarthia. -Advice the patient to stop the drug
129
ethanol are mediated Pregnancy and gradually.
through binding to lactation.
ABA receptors and
glycine receptors
(alpha 1 and alpha 2 CVS:- - Assess the patient’s BP, pulse rate,
subunits). It also Cardiomyop rhythms
inhibits NMDA athy, -Check potassium level
receptor functioning. hypotension, -Instruct the patient report immediately
In its role as an anti- HTN, CV if any restlessness occur.
infective, ethanol acts collapse
as an osmolyte or
dehydrating agent G.I.: - - Provide the patient with sugarless,
that disrupts the Vomiting, candy or gum, ice and frequent sips of
osmotic balance nausea. water
across cell - Ensure that the client practices strict
membranes. oral hygiene
-Administer with food to minimize
gastric irritation
Resp: Resp -Monitor respiration rate and depth
depression. before and after giving medicine
Endocrine: -Monitor sugar level periodically
Hypoglycae -Advice the patient to take sugar candy
mia. with him every time
Musculoske -close observation regarding muscle
letal: Muscl incoordination.
e -Report the physician.
incoordinati
on.
Ophthalmol -Examine both eye every follow-up
ogic: Visual checkup.
impairment, -Advise the client not to drive a vehicle
nystagmus. until vision clears

Monitoring Monitor blood ethanol levels 1-2 hrly

until steady state (100-150 mg/L) is
reached, then 2-4 hourly thereafter.
Monitor for signs and symptoms of CNS
and respiratory depression. Monitor for
methanol/ethylene glycol blood levels,
blood glucose, arterial pH, blood gases,
heart rate, and BP.

130
 MEDAZOLAM

Trade name
Seizalam, Versed (DSC) Dormicum, Hypnovel, Versed,

Classification
Antianxiety Agents; Anxiolytics, Benzodiazepines

Dose
PO Short-term management of insomnia 7.5-15 mg at bedtime.
Oral syrup: 2mg/ml (generic)
Injectable solution:
 1mg/ml (generic)
 5mg/ml (generic, Seizalam)

MECHANISM INDICATIO CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION N ATION EFFECT
Midazolam are Seizures elderly, during CNS: -Inform the patient about side effect of
mediated through the status pregnancy, in Headache, the drug.
inhibitory epilepticus , children, in alcohol- dizziness, - Caution the patient to avoid tasks that
neurotransmitter acute or other drug- tremor, require mental alertness or motor skills
gamma-aminobutyric management dependent lethargy, until his response to the drug has been
acid (GABA), which of schizophreni individuals comorbid amnesia, established.
is one of the major a, psychiatric loss of -Avoid activity that require alertness
inhibitory disorders. judgement, -Advice the patient to avoid drive and
neurotransmitters in Procedural hypersensitivity, slurred handling of heavy machinery.
the central nervous sedation, acute narrow-angle speech, - Discuss with the physician the
system. Agitation, glaucoma, shock, ataxia, possibility of administering the
Benzodiazepines continuous hypotension, or head unusual drug at bed time
increase the activity deep sedation injury. Kidney or drowsiness, - Discuss with the physician the possible
of GABA, thereby therapy, liver impairments dullness, decrease in dosage or
producing a sedating tiredness, order for less sedating

131
effect, relaxing myoclonus, weakness, or -Advice the patient to stop the drug
skeletal muscles, and restlessness or feeling of gradually. Instruct the patient to change
inducing sleep, anxietyEnd of sluggishness positions slowly from recumbent to
anesthesia, and life care sitting, before standing to prevent
amnesia. dizziness
Benzodiazepines -Urge the patient to avoid alcohol
bind to the during therapy
benzodiazepine site CVS:- - Monitor vital sign every shift
on GABA-A Hypotension - Instruct the client in rise slowly from
receptors, which , lying or sitting position
potentiates the effects - Monitor blood pressure (lying &
of GABA by Standing)
increasing the
frequency of chloride G.I.: - - Provide the patient with sugarless,
channel opening. Vomiting, candy or gum, ice and frequent sips of
These receptors have nausea. water
been identified in - Ensure that the client practices strict
different body tissues oral hygiene
including the heart -Administer with food to minimize
and skeletal muscle, gastric irritation
although mainly Resp: Resp -Assess the paient’s respiratory rate and
appear to be present depression. depth before giving the medication
in the central nervous -Explain that symptoms will most likely
system. subside after a few weeks.

Endocrine: -Weight the client every day

weight gain -Order a caloric controlled diet
-Provide diet and exercise
Ophthalmol -Examine both eye every follow-up
ogic: blurred checkup.
vision -Advise the client not to drive a vehicle
until vision clears

Tolerance, -Advise the patient to take medication

dependence exactly as directed. Abrupt withdrawal
, and may cause insomnia, irritability and
withdrawal sometimes even seizures
irritability, -Advice the patient does not increase or
abnormal ref decrease the drug of daily doses.
lexes, tremo -Discuss about the tolerance, dependence
rs, clonus, h and withdrawal symptoms to the patient
ypertonicity,
delirium an
d seizures, n
ausea, vomit
ing, diarrhea
, tachycardia
,and tachypn
ea.

132
 CLONAZEPAM

Brand Name
Klonopin

Classification
Antianxiety Agents; Anxiolytics, Benzodiazepines; Anticonvulsants, Benzodiazepine

Dose
Intravenous
Emergency management of status epilepticus
Adult: 1 mg via slow IV inj or infusion over at least 2 minutes, repeated if necessary. Max: 10
mg.
Child: 500 mcg by slow IV inj over at least 2 minutes or by infusion.

Oral
Panic disorder
Adult: Initially, 0.25 mg bid, increased after 3 days up to 1 mg/day. Max: 4 mg/day.

Oral
Epilepsy
Adult: Initially, 1 mg given at night for 4 days, gradually increased over 2-4 wk. Maintenance: 4-
8 mg/day. Max: 20 mg/day.
Child: ≤10 yr or ≤30 kg: Initially, 0.01-0.03 mg/kg/day but not to exceed 0.05 mg/kg/day given
in 2 or 3 divided doses. May be increased by no more than 0.25-0.5 mg every 3rd day until
seizure control is achieved. Maintenance: 0.1-0.2 mg/kg/day divided 3 times daily. Max: 0.2
mg/kg/day.
Elderly: Initially, 0.5 mg at night for 4 days.

133
MECHANISM INDICATIO CONTRAINDIC SIDE NURSING RESPONSIBILITY
OF ACTION N ATION EFFECT
lonazepam reduces Seizures, Patient with acute CNS: -Inform the patient about side effect of
the nerve Panic disorders, angle closure Drowsiness the drug.
transmission in the episodic glaucoma, acute or sedation, - Caution the patient to avoid tasks that
motor cortex which epileptus pulmonary fatigue, require mental alertness or motor skills
suppresses the spike insufficiency, severe muscular until his response to the drug has been
and wave discharge respiratory hypotonia, established.
in absence seizures. insufficiency, behavioural -Avoid activity that require alertness
Its mechanism is myasthenia gravis, disturbances -Advice the patient to avoid drive and
believed to be related sleep apnoea including handling of heavy machinery.
to its ability to syndrome. aggressivene - Discuss with the physician the
enhance the activity Special precaution in ss, agitation, possibility of administering the
of GABA. Clinically, chronic pulmonary hyperkinesis drug at bed time
it improves focal insufficiency, and - Discuss with the physician the possible
epilepsy and porphyria, spinal or irritability; decrease in dosage or
generalised seizures. cerebellar ataxia, order for less sedating
history of alcohol or -Advice the patient to stop the drug
drug addiction, and gradually.
depression and/or
suicide attempts.
Increased risk of CVS:- - Monitor vital sign every shift
suicidal behaviour Hypotension - Instruct the client in rise slowly from
and ideation. Avoid , lying or sitting position
abrupt withdrawal. - Monitor blood pressure (lying &
Renal and hepatic Standing)
impairment. Elderly
or debilitated G.I.: - - Provide the patient with sugarless,
patient. Pregnancy Dry mouth, candy or gum, ice and frequent sips of
and lactation. Vomiting, water
nausea. - Ensure that the client practices strict
oral hygiene
-Administer with food to minimize
gastric irritation
Resp: Resp -Explain that symptoms will most likely
depression. subside after a few weeks.

Endocrine: -Weight the client every day

weight gain -Order a caloric controlled diet
or loss -Provide diet and exercise
Ophthalmol -Examine both eye every follow-up
ogic: visual checkup.
disturbances -Advise the client not to drive a vehicle
until vision clears

Urinary - Monitor Intake and output

retention, dy -Instruct the client to report any
suria, difficulty urinating
enuresis,

134
 Dermatologi -Reports the appearance of any rash on
cal: Skin skin to the physician dermatitis
rashes, Hair - Avoid spilling any of the liquid
loss concentrate skin

DIPHENHYDRAMINE

Trade name
Benadryl, Unisom, Sominex, Benadrex, Benaxil, Bexil, Hyphen, Medryl

Classification
Antihistamines & Antiallergics

Dose
Oral
Allergic conditions, Treatment and prophylaxis of motion sickness
Adult: 25-50 mg 3-4 times daily. For prevention of motion sickness, admin 30 min before
exposure to motion. Max: 300 mg daily.
Child: 2 to <6 yr 6.25 mg 4-6 hrly; 6-12 yr 12.5-25 mg 4-6 hrly. For prevention of motion
sickness, admin 30 min before exposure to motion.

Oral
Parkinson's disease
Adult: Initially, 25 mg tid, may increase to 50 mg 4 times daily if necessary.

135
 Oral
Short-term management of insomnia
Adult: 50 mg 30 min before bedtime as needed.

Parenteral
Allergic conditions, Treatment and prophylaxis of motion sickness
Adult: As 1% or 5% soln: 10-50 mg by deep IM or IV inj, up to 100 mg may be used if needed.
Max: 400 mg daily.
Child: 5 mg/kg daily in 4 divided doses by deep IM or IV inj. Max: 300 mg daily.

Parenteral
Parkinson's disease
Adult: As 1% or 5% soln: 10-50 mg by deep IM or IV inj, up to 100 mg may be used if needed.
Max: 400 mg daily

MECHANISM INDICATIO CONTRAINDI SIDE NURSING RESPONSIBILITY

OF ACTION N CATION EFFECT
Diphenhydramine is Diphenhydram Asthma, narrow CNS: -Assess level of sedation after
an antihistamine with ine is a first- angle glaucoma, ataxia, chills, administration
anticholinergic and generation prostatic confusion, -Assess the patient for motor
sedative effects. It antihistamine hypertrophy, dizziness, responses, such as agitation, tension
competes with used to treat a stenosing peptic drowsiness, and trembling, and autonomic
histamine for H1- number of ulcer, euphoria, responses, such as cold, clammy
receptor sites on conditions pyloroduodenal excitement, hands and diaphoresis
effector cells in the including aller obstruction or fatigue, -Inform the patient about side effect
GI tract, blood gic symptoms bladder neck headache, of the drug.
vessels and and itchiness, obstruction, insomnia, - Caution the patient to avoid tasks that
respiratory tract. the common porphyria. irritability, require mental alertness or motor skills
Pharmacokinetics: cold, insomnia, Neonates or nervousness, until his response to the drug has been
Absorption: Well motion premature infants. neuritis, established.
absorbed from the GI sickness, Lactation. paraesthesia, -Avoid activity that require alertness
tract. Time to peak and extrapyra paradoxical -Advice the patient to avoid drive
plasma midal excitation, and handling of heavy machinery.
concentration: symptoms, restlessness, - Discuss with the physician the
Approx 1-4 hr. Nausea sedation, possibility of administering the
Distribution: Widely Parkinson's seizure, vertigo; drug at bed time
distributed disease diaphoresis - Discuss with the physician the
throughout the body possible decrease in dosage or
including CNS. order for less sedating
Crosses the placenta, -Urge the patient to avoid alcohol
enters breast milk. during therapy
Plasma protein - Caution the patient to avoid alcohol
binding: High. or any other CNS depressants along
Metabolism: Extensi with this drug; also instruct him not to
vely hepatic. take any over-the-counter (OTC)
Excretion: Via urine, medications
mainly as metabolites
and unchanged drug CVS:- - Monitor vital sign every shift

136
in small amounts. Hypotension, - Instruct the client in rise slowly from
Elimination half-life: lying or sitting position
2.4-9.3 hr. - Monitor blood pressure (lying &
Standing)

G.I.: - - Provide the patient with sugarless,

anorexia, candy or gum, ice and frequent sips of
constipation, water
diarrhoea - Ensure that the client practices strict
oral hygiene
-Administer with food to minimize
gastric irritation
Respiratory: co -Assess the respiratory rate, depth and
nstriction of rhythm before giving the drug
pharynx, nasal -Explain that symptoms will most
congestion, likely subside after a few weeks.
thickening of
bronchial
secretions, ,
wheezing
Hematological: -Perform timely blood examination to
agranulocytosis, review any deviation
haemolytic -Report physician if any blood
anaemia, abnormalities occurs.
thrombocytopen
ia
Ophthalmologic -Examine both eye every follow-up
: Blurred vision checkup.
-Advise the client not to drive a
vehicle until vision clears

Renal: -Instruct the client to report any

difficulty in difficulty in urination
micturition, - Monitor Intake and output
urinary -Report the physician
frequency,
urinary retention

Dermatological -Reports the appearance of any rash

: on skin to the physician dermatitis
photosensitivity - Avoid spilling any of the liquid
, rash, urticaria concentrate skin
(topical) -
Reproductive -Inform the patient about menstrual
menstrual irregularities
disease

137
 FLURAZEPAM

Trade Name
Dalmane, Dalmadorm, Fluzepam

Classification
Hypnotics & Sedatives

Dose
Adult : PO 15-30 mg at night.

MECHANISM INDICATIO CONTRAINDIC SIDE NURSING RESPONSIBILITY

OF ACTION N ATION EFFECT
Flurazepam is a Flurazepam is Patient w/ pre- CNS: -Inform the patient about side effect of
long-acting officially existing CNS Increased the drug.
benzodiazepine indicated for depression or coma, risk of - Caution the patient to avoid tasks that
which binds to mild to resp depression, hazardous require mental alertness or motor skills
stereospecific moderate acute pulmonary sleep-related until his response to the drug has been
benzodiazepine insomnia and insufficiency, activities established.
receptors on the as such it is myasthenia gravis, (e.g. sleep- -Avoid activity that require alertness
postsynaptic GABA used for short- sleep apnoea, driving), -Advice the patient to avoid drive and
neuron w/in the CNS, term treatment chronic psychosis or drowsiness, handling of heavy machinery.
including the limbic of patients obsessional states. light- - Discuss with the physician the
system, reticular with mild to Pregnancy. headedness, possibility of administering the
formation. It moderate inso dizziness, drug at bed time
enhances the mnia such as Special precaution: confusion, - Discuss with the physician the possible
inhibitory effect of difficulty Patient w/ chronic anterograde decrease in dosage or order for less
GABA on neuronal falling asleep, pulmonary amnesia, sedating
excitability by frequent insufficiency, headache, -Urge the patient to avoid alcohol
increasing neuronal awakening, personality disorder, fatigue, during therapy
membrane early depression, resp reduced - Caution the patient to avoid alcohol or
permeability to Cl awakenings or disease, impaired alertness, any other CNS depressants along with
138
ions, thus resulting in a combination gag reflex, history of numbed this drug; also instruct him not to take
hyperpolarisation and of each. alcohol or drug emotions, , any over-the-counter (OTC)
stabilisation. Flurazepam is addiction. Renal and ataxia, medications -
Onset: Hypnotic: 15- a long-acting hepatic impairment. slurred
20 min. benzodiazepin Childn (<15 yr), speech
Duration: 7-8 hr. e and is elderly or debilitated
Pharmacokinetics: sometimes patient, Lactation. CVS:- - Monitor BP , pulse rate of the patient
Absorption: Readily used in Hypotension frequently
absorbed from the GI patients who - Instruct the client in rise slowly from
tract. Time to peak have difficulty lying or sitting position
plasma in maintaining - Monitor blood pressure (lying &
concentration: sleep. Standing)
Approx 30-60 min.
Distribution: Crosse G.I.: - - Provide the patient with sugarless,
s the placenta. GI candy or gum, ice and frequent sips of
Volume of disturbances water
distribution: 3.4 - Ensure that the client practices strict
L/kg. Plasma protein oral hygiene
binding: Approx -Administer with food to minimize
97%. gastric irritation
Metabolism: Underg Resp: -Monitor respiratory rate, depth and
oes hepatic apnoea, rhythm of the patient frequently
metabolism to N- dyspnoea, -If any abnormality arises inform the
desalkyl flurazepam physician
(active) and N- Endocrine: -Explain the patient about side effect of
hydroxyethylflurazep ecessive excessive salivation before giving the
am. salivation drug
Excretion: Via urine
(mainly as Ophthalmol -Examine both eye every follow-up
conjugated ogic: checkup.
metabolites). double -Advise the client not to drive a vehicle
Elimination half-life: vision until vision clears
2.3 hr (parent drug).
Urinary -Instruct the client to report any
retention difficulty urinating
- Monitor Intake and output

Dermatologi -Reports the appearance of any rash on

cal: Skin skin to the physician dermatitis
rashes - Avoid spilling any of the liquid
concentrate skin

139
 LORAZEPAM

Trade name
Ativan, Tavor, Temesta

Classification
lorazepamBelongs to the class of benzodiazepine derivatives anxiolytics

Dose
Adult: PO Anxiety 1-4 mg daily in divided doses for 2-4 weeks.
Insomnia associated with anxiety 1-2 mg at bedtime.
Premedication in surgery 2-3 mg given the night before the operation followed by 2-4 mg 1-2
hours before the procedure. IV/IM Premedication in surgery 0.05 mg/kg given 30-45 minutes
before surgery via IV or 60-90 minutes before surgery via IM.
Acute anxiety 0.025-0.03 mg/kg, may be repeated 6 hourly.
IV Status epilepticus 4 mg as single dose, may be repeated once after 10-15 minutes.

MECHANISM OF INDICAT CONTRAINDIC SIDE NURSING RESPONSIBILITY

ACTION ION ATION EFFECT
Lorazepam is a short- Anxiety, Acute pulmonary CNS: -Inform the patient about side effect of
acting benzodiazepine. Insomnia insufficiency, Drowsiness, the drug.
It binds to stereospecific associated respiratory sedation, - Caution the patient to avoid tasks that
benzodiazepine with depression, sleep dizziness, require mental alertness or motor skills
receptors on the anxiety, apnoea, acute unsteadiness until his response to the drug has been
postsynaptic GABA Premedicati narrow-angle , Asthenia, established.
neuron at several sites on in glaucoma, fatigue, -Avoid activity that require alertness
within the CNS surgery , obsessional state, ataxia -Advice the patient to avoid drive and
(including the limbic Status myasthenia gravis. handling of heavy machinery.
system, reticular epilepticus Severe hepatic - Discuss with the physician the
formation). Increased impairment. possibility of administering the
neuronal membrane Pregnancy (planning drug at bed time
permeability to chloride a pregnancy, 1st or - Discuss with the physician the possible
ions enhances the 3rd trimester). decrease in dosage or order for less
inhibitory effects of Special precaution sedating

140
GABA thereby resulting Patients with -Urge the patient to avoid alcohol
to hyperpolarisation and respiratory disease during therapy
stabilisation. (e.g. COPD), history - Caution the patient to avoid alcohol or
Onset: Anticonvulsant: of alcoholism or any other CNS depressants along with
Within 10 minutes (IV); drug abuse, this drug; also instruct him not to take
hypnosis: 20-30 minutes psychiatric or any over-the-counter (OTC)
(IM); sedation: within 2- personality medications -
3 minutes (IV). disorders; at risk of
Duration: Anaesthesia falls. Debilitated CVS:- - Monitor BP , pulse rate of the patient
premedication: Approx patients. Renal and Hypotension frequently
6-8 hours (IV, IM). mild to moderate - Instruct the client in rise slowly from
Absorption: Readily hepatic impairment. lying or sitting position
absorbed from the Children and elderly. - Monitor blood pressure (lying &
gastrointestinal tract Pregnancy (2nd Standing)
after oral administration; trimester) and
rapidly and completely lactation. Not Blood -Perform CBC, LFT, LDH (prolonged
absorbed after IM indicated for primary dyscrasia use) to know any blood related disorders
administration. treatment of (e.g.
Bioavailability: 90% psychotic illness or agranulocyt
(oral). Time to peak depressive disorders. osis,
plasma concentrations: leucopenia,
Approx 2 hours (oral); thrombocyto
within 3 hours (IM). penia,
Distribution: Crosses pancytopeni
placenta and blood-brain a)
barrier; enters Resp: -Monitor respiratory rate, depth and
breastmilk. Volume of apnoea, rhythm of the patient frequently
distribution: 1.3 L/kg. dyspnoea, -If any abnormality arises inform the
Plasma protein binding: physician
Approx 85%.
Metabolism: Metabolis Ophthalmol -Examine both eye every follow-up
ed in the liver, ogic: checkup.
conjugated to lorazepam double -Advise the client not to drive a vehicle
glucuronide (inactive vision until vision clears
metabolite).
Excretion: Via urine
(approx 88%; Dermatologi -Reports the appearance of any rash on
predominantly as cal: Skin skin to the physician dermatitis
inactive metabolites), rashes - Avoid spilling any of the liquid
faeces (approx 7%). concentrate skin
Elimination half-life:
Approx 12 hours (oral);
Physical -Enhanced sedative effects with alcohol.
approx 14 hours (IV);
and -Reduced sedative and anxiolytic effects
approx 13-18 hours
psychologic with caffeine.
(IM).
al -Increased plasma concentrations with
dependence, grapefruit juice.
withdrawal -Avoid abrupt withdrawal.
symptoms -Avoid prolong use of this drug

141
Drugs Use For Child Psychiatric
Disorders

142
 Drugs Use For Child Psychiatric Disorders
Introduction
Medication can be an effective part of the treatment for several psychiatric disorders of
childhood and adolescence. A doctor's recommendation to use medication often raises many
concerns and questions in both the parents and the youngster. The physician who recommends
medication should have experience treating psychiatric illnesses in children and adolescents.
Before recommending any medication, the child and adolescent psychiatrist interviews the
youngster and makes a thorough diagnostic evaluation. In some cases, the evaluation may
include a physical exam, psychological testing, laboratory tests, other medical tests such as an
electrocardiogram (EKG) or electroencephalogram (EEG), and consultation with other medical
specialists.

Indications

1. Bedwetting-if it persists regularly after age 5 and causes serious problems in low self-
esteem and social interaction.
2. Anxiety (school refusal, phobias, separation or social fears, generalized anxiety, or
posttraumatic stress disorders)
3. Attention-deficit/hyperactivity disorder (ADHD)-marked by a short attention span,
trouble concentrating, and restlessness.
4. Obsessive-compulsive disorder (OCD)
5. Depression-
6. Eating disorder-either self-starvation (anorexia nervosa), binge eating and vomiting
(bulimia), or a combination of the two.
7. Bipolar (manic-depressive) disorder.
8. Psychosis-symptoms include irrational beliefs, paranoia, hallucinations (seeing things or
hearing sounds that don't exist), social withdrawal. Psychosis may be seen in
developmental disorders, severe depression, schizoaffective disorder, or schizophrenia.
9. Autism spectrum disorders-characterized by severe deficits in social interactions,
language, and/or thinking or ability to learn, and usually diagnosed in early childhood.
10. Severe aggression-which may include assaultive behavior, excessive property damage,
or prolonged self-abuse, such as head-banging or cutting.
11. Sleep problems-symptoms can include insomnia, night terrors, sleep walking, fear of
separation, or anxiety.

Types of Medication

1. ADHD Medications: a)Stimulants include: Dextroamphetamine (Dexedrine, Adderal) and

Methylphenidate (Ritalin, Metadate, Concerta).
b)Non-stimulant medications include Atomoxetine (Strattera).

2. Antidepressant Medications: a)Serotonin reuptake inhibitors (SRI's) include: Fluoxetine

(Prozac), Sertraline (Zoloft), Paroxetine (Paxil), Fluvoxamine (Luvox),
143
b)Atypical antidepressants include: Bupropion (Wellbutrin), Nefazodone (Serzone),
c)Examples of tricyclic antidepressants (TCA's) include: Amitriptyline (Elavil), Clomipramine
(Anafranil), Imipramine (Tofranil), and Nortriptyline (Pamelor).
d)Examples of monoamine oxidase inhibitors (MAOI's) include: Phenelzine (Nardil), and
Tranylcypromine (Parnate).

3.Antipsychotic Medications: a)Examples of first generation antipsychotic medications include:

Chlorpromazine (Thorazine), Thioridazine (Mellaril), Fluphenazine (Prolixin),
b)Second generation antipsychotic medications (also known as atypical or novel) include:
Clozapine (Clozaril), Risperidone (Risperdal), Quetiapine (Seroquel), Olanzapine

4. Anticonvulsant Medications: Lithium (lithium carbonate, Eskalith), Valproic Acid

(Depakote, Depakene), Carbamazepine (Tegretol), Gabapentin (Neurontin), Lamotrigine

5. Anti-anxiety Medications: a)Benzodiazepines include: Alprazolam (Xanax), lorazepam

(Ativan), Diazepam (Valium),and Clonazepam (Klonopin).
b)Examples of antihistamines include: Diphenhydramine (Benadryl), and Hydroxizine (Vistaril).
c) Examples of atypical anti-anxiety medications include: Buspirone (BuSpar), and Zolpidem
(Ambien).

6. Sleep Medications: Trazodone (Desyrel), Zolpidem (Ambien), Zaleplon (Sonata) and

Diphenhydramine (Benadryl).

7. Miscellaneous Medications: Other medications are also being used to treat a variety of
symptoms. For example: clonidine (Catapres) may be used to treat the severe impulsiveness in
some children with ADHD .

Before starting a medication, the clinician prescribing the medication should discuss the
following with parents:

 Results of the assessment (your child's diagnosis)

 Target symptoms
 Risks of the illness if untreated
 Potential benefits of the medication
 Known risks, side effects, and/or Food and Drug Administration (FDA) warnings
 Whether the medication is being prescribed on-label or off-label (whether the medication
has been approved for children and adolescents for the condition for which it is being
prescribed).

144
 1. METHYLPHENIDATE

Trade Name
Ritalin, Concerta, Methylin, Daytrana, Metadate CD, Quillivant XR, Ritalin, Ritalin-LA,
Ritalin SR (CAN), Ritalin-SR

Classification -
Chemical class: Piperidine derivative
Therapeutic class: CNS stimulant
Pregnancy category: C
Controlled substance schedule: II

Dose
1. Capsules, E.R. Tablets, Oral Solution, S.R. Tablets, Tablets
Adults and adolescents- 5 to 20 mg twice daily or three times daily. Maximum: 90 mg daily.
Children ages 6 to 12- 5 mg twice daily before breakfast and lunch; increased by 5 to 10 mg
daily at 1-wk intervals. Maximum: 60 mg daily.

2. Extended release oral suspension (quillivant xr)

Adults and children ages 6 and older. Initially, 20 mg once daily in morning; increased weekly in
increments of 10 to 20 mg, as needed. Maximum: 60 mg daily.

3. Extended release once-daily tablets (concerta)

Adults and adolescents- 18 mg daily; increased in 18-mg increments at 1-wk intervals.
Maximum: 72 mg daily, not to exceed 2 mg/kg daily.
Children ages 6 to 12. 18 mg daily. Maximum: 54 mg daily.

4. Extended release once-daily capsules (metadate cd)

Children age 6 and over- 20 mg daily. Dosage titrated to 40 or 60 mg daily based on individual
response. Maximum: 60 mg daily.

145
 5.Transdermal Patch (Daytrana)
Adolescents ages 13 to 17, children ages 6 to 12.
Initial: 10-mg (12.5-cm2) patch worn 9 hr daily; after 1 wk, increased to 15-mg (18.75-cm2)
patch worn 9 hr daily; after 1 more wk, increased to 20-mg (25-cm2) patch worn 9 hr daily; after
1 more wk, increased to 30-mg (37.5-cm2) patch worn 9 hr daily. Maximum: 30-mg (37.5-cm2)
patch worn 9 hr daily.

Mechanism of Action Indication Contraindication Side effects Nursing

Responsibility
1.Methylphenidate 1.Used to •Angina pectoris, 1.CNS: •Monitor children and
primarily acts as treat •Agitation, adolescents for
a norepinephrine– attention •Cardiac •aggressiveness, firsttime psychotic or
dopamine reuptake deficit arrhythmias, •anxiety, manic symptoms. If
inhibitor (NDRI). problem •confusion, present, notify
with1 hyper •Heart failure, •depression, prescriber and expect
activity •dizziness, drug to be
2.Methylphenidate is •Recent MI, •hallucinations, discontinued.
a psychostimulant and •headache, •Watch closely
increases the activity of 2.Narco- •Severe •hyperactivity, (especially children,
the central nervous lepsy. hypertension, •insomnia, , adolescents, and young
system through •ischemic adults), for suicidal
inhibition on reuptake •Anxiety, •neurologic tendencies, particularly
of the neurotransmitters defects when therapy starts and
norepinephrine •Severe agitation, (reversible), dosage changes,
and dopamine. mania, migraine, because depression
•Depression, •obsessive- may worsen
compulsive temporarily during
3.As models of ADHD •Glaucoma, disorder, these times, possibly
suggest, it is associated •psychosis, leading to suicidal
with functional •Motor tics, •sedation, ideation.
impairments in some of •seizures,
the brain's •Tourette’s •stroke, •Monitor blood
neurotransmitter syndrome or •suicidal ideation. pressure and pulse rate
particularly those family history of to detect hypertension
involving dopamine it 2.Cardiovascula- and excessive
inthe mesocortical and r system stimulation.
mesolimbic pathways •Fructose - •Angina, •Notify prescriber if
intolerance, •arrhythmias, present. For patient
and norepinephrine in
•bradycardia, with hypertension,
the prefrontal
•Glucose- •cardiac arrest, expect to increase
cortex and locus
galactose •chest pain, antihypertensive
coeruleus. Psychosti- malabsorption, •extrasystoles, dosage or add another
mulants like hypertension, antihypertensive to
methylphenidate and •Sucrase- •hypotension, regimen.
amphetamine may be isomaltase •MI,
effective in treating insufficiency, •palpitations, •Advice patient to rinse
ADHD because they
146
increase •peripheral mouth and use hard
neurotransmitter vasculopathy candy for dry mouth.
activity in these including Advice patient to
systems. When •Hyperthyroidism tachycardia inform seriousness of
reuptake of those vision impairement.
neurotransmitters is •Thyrotoxicosis, 3.EENT: -
halted, its concentration •Accommodation
and effects in •Use of abnormality,
the synapse increase halogenated •blurred vision,
and last longer, anesthetics. •diplopia, •Monitor growth in
respectively. •dry mouth or children. Report failure
•Use within •throat•mydriasis, to grow or gain weight,
14 days of a •pharyngitis, and expect to stop drug.
MAO inhibitor. •rhinitis,
4.Therefore, •vision changes •Advice patient to take
methylphenidate is •Hypersensitivity fiber rich diet.
called a to 4.ENDO: •Advice for small and
norepinephrine– methylphenidate •Dysmenorrhea, frequrnt meal.
dopamine reuptake or its •growth •Monitor liver function
inhibitor. By increasing components, suppression in test periodically.
the effects of children with
norepinephrine and long-term use
dopamine,
methylphenidate 5.GI:
increased the activity of •Abdominal pain, •Warn male patients
the central nervous •anorexia, and parents of male
system and produced •constipation, child that painful
effects such as •diarrhea, penile erections may
increased alertness, •dyspepsia, occur while taking the
combated fatigue, and •hepatotoxicity, drug, after a dosage
improved attention. •nausea, increase or during
•vomiting period of drug
withdrawal medical
6.GU: attention should be
•Decreased libido, sought
•priapism •Monitor any sign of
bleeding.
7.HEME: •Periodic assessment of
•Anemia, complete blood profile.
•decreased
platelet count,
•leukopenia,
•pancytopenia,
•thrombocytopeni •Provide rest and give
a,thrombocytope- analgesic if prescribed.
nic, purpura •Use diversion therapy

147
 to childern to minimize
8.MS: pain.
•Arthralgia,
•myalgia, •Monitor respiratory
•muscle tightness rate assess for any sign
or twitching of distress and be ready
for prompt action.
9.RESP:
•Increased cough, •Caution patient to
•upper respiratory avoid applying patch to
tract infection skin that’s oily,
damaged, or irritated
10.SKIN: and to avoid the
•Allergic contact waistline, where
dermatitis, clothing may dislodge
• alopecia, the patch. •Tell patient
application-site to rotate application
reactions sites between hips.
(transdermal
patch), •Monitor transdermal
•diaphoresis, patch application site
•erythema for erythema. If more
•multiforme, intense reactions
exfoliative determine presence of
dermatitis, allergic contact
•pruritus, dermatitis.
•rash,
•urticaria

11.Other:•Anaph
ylaxis,
•angioedema

148
 2.ClONIDINE

Trade name
Catapres, Kapvay, Clonidine ER, Catapres-TTS Drug class(es):

Classification
Chemical class: Imidazoline derivative
Therapeutic class: Analgesic, antihypertensive centrally acting alpha-agonist hypotensive agents
Pregnancy category: C

Dose
1. Usual Pediatric Dose for Attention Deficit Disorder
Extended release:
6 years and older:
-Initial dose: 0.1 mg orally at bedtime
-Titration: Increase in 0.1 mg/day increments every 7 days until desired response; doses should
be administered twice daily (either split equally or with the higher split dosage given at bedtime)
-Maximum dose: 0.4 mg/day in 2 divided doses

2. Usual Adult Dose for Hypertension

Oral:
-Initial dose: 0.1 mg orally 2 times a day (morning and bedtime)
-Titration: Increments of 0.1 mg orally per day may be made at weekly intervals to desired
response
-Maintenance dose: 0.2 to 0.6 mg orally per day in divided doses
-Maximum dose: 2.4 mg orally per day in divided doses
3. Usual Adult Dose for Pain
149
 Epidural infusion:
-Initial dose: 30 mcg/hr as a continuous infusion
-Titration: May be titrated up or down depending on pain relief and occurrence of adverse events
Maximum dose 40 mcg/hr as a continuous infusion.

Note
-May be taken with or without food.
-If a dose is missed, that dose should be skipped and take the next dose as scheduled.
-Tablets should be swallowed whole, and not crushed, chewed, or broken to avoid increasing the
rate of drug release.
-When discontinuing therapy, taper daily dose by no more than 0.1 mg every 3 to 7 days.

Mechanism of Indication Contraindication Side effects Nursing management

action
1.Stimulates 1.To manage •Anticoagulant 1.CNS: •As drug stop abruptly can
peripheral hypertension. therapy (epidural •Agitation, elevate serum
alpha-adrenergic infusion); •delusional catecholamine levels and
receptors in the bleeding •perception, cause such withdrawal
CNS to produce 2.To treat diathesis; •depression, symptoms so the dosage
transient severe •dizziness, should be decreased by
vasoconstriction hypertension •drowsiness, 0.1 mg every 3 to 7 days
and then stimulates •Hypersensitivity •fatigue, when it is being
central to clonidine or its •hallucinations, discontinued.
alpha-adrenergic 3.To treat components, •headache,
receptors in the attention including •malaise,
brain stem to deficit adhesive used in •nervousness,
reduce peripheral hyperactivity transdermal •paresthesia,
vascular resistance disorder patch; •sedation,
and systolic and (ADHD) injection-site •syncope,
diastolic blood alone or as infection •weakness,
pressure. adjunct (epidural •tremor
therapy with infusion)
2.In ADHD stimulant 2.CV: • Monitor blood pressure
clonidine's drugs •Arrhythmias, and heart rate often during
molecular •AV block, clonidine therapy
mechanism of •bradycardia •If severe bradycardia
action occurs due 4.As adjunct (severe), occurs, be prepared to
to its agonism at to relieve •chest pain, administer IV atropine or
the alpha-2A severe pain •congestive isoproterneol and assist
adrenergic (in cancer heart failure, with insertion of
receptorthat is patients) that •orthostatic temporary cardiac pacing.
most principally isn’t hypotension, •Tell patient to rise slowly
found in the brain adequately •Raynaud’s to avoid hypotensive
within prefrontal relieved by phenomenon effects.

150
cortex(PFC) opioid
clonidine's analgesics
agonism on alpha- alone. 3.EENT: •Assessment of vision.
2A adrenergic •Accommodatio Inform patient who wears
receptors in the 5.Clonidine -n disorder, contact lenses that
PFC inhibits the also has •blurred vision, clonidine may cause dry
action of several off- •burning eyes, eyes.
downstream label uses, •decreased •Prescribe any lacrimal
neurons by and has been lacrimation, eye drop for the patient.
preventing the prescribed to •dry eyes and •Advice patient to drink
secretion of reduce mouth, more water.To minimize
norepinephrine psychiatric •salivary gland these effects, suggest
clonidine's disorders pain taking most of dosage at
inhibition of PFC including bedtime.
neurons helps to stress, sleep
eliminate disorders, 4.GI: •Advice patient for fiber
irrelevant attention and •Constipation, rich diet.
(and subsequent hyperarousal •hepatitis, •Monitoring of lab test
behaviors), caused by •elevated liver and inform doctor for
improving the posttrauma function test further management.
person's focus and disorder, and •nausea,
correcting deficits other anxiety vomiting •Advise men that libido
in attention disorders. may decrease before
5.GU: giving medication so that
3.May produce 5. Clonidine •Decreased they would be mentally
analgesia by is also a libido, prepare.
preventing mild sedativ •erectile
transmission of dysfunction, •Monitor for any bleeding.
e, and can be
pain signals to the •nocturia. •Assessment of blood test
used
brain at result.
as premedica
presynaptic and 6.HEME:
postjunctional tion before Thrombocytope
alpha2-adrenorece surgery or -nia •Tell patient to rotate
ptors in the spinal procedures transdermal sites.
cord. With • Instruct patient to
epidural 7.SKIN: remove patch and place a
administration, Angioneurotic fresh one on another site if
clonidine produces edema, pruritus, skin irritation, redness, or
analgesia in body rash, urticaria rash develops at patch
areas innervated site.
by the spinal cord •Assessment of weight
segments in which Other: Weight daily.
the drug gain, •Monitor early signs of
concentrates. withdrawal withdrawal.
symptoms

151
DRUGS USED IN DEMENTIA OF
ALZHEMER’S TYPE

152
 DRUGS USED IN DEMENTIA OF ALZHEMER’S TYPE
Dementia
Dementia is a syndrome in which there is deterioration in memory, thinking, behaviour and the
ability to perform everyday activities. Although dementia mainly affects older people, it is not a
normal part of ageing.

Alzheimer's disease
Alzheimer's disease is a progressive disorder that causes brain cells to waste away (degenerate)
and dies. Alzheimer's disease is the most common cause of dementia — a continuous decline in
thinking, behavioral and social skills that disrupts a person's ability to function independently.

DONEPEZIL

Brand Name
Aricept

Classification
Acetylcholinesterase inhibitor

Dose
5-10 mg per day.

153
MECHANISM OF INDICATI CONTRAINDIC SIDE NURSE’S
ACTION ON ATION EFFECT RESPONSIBILITY
The precise mechanism of Treatment of Donepezil should CNS: -Emphasize the importance of
action of donepezil in mild to not be used for Headache, taking the medication every
patients with Alzheimer's moderate people who are fatigue, day
disease is not fully dementia of allergic to dizziness, - Explain family members that
understood. In Alzheimer's the ingredients in vivid donepezil may cause dizziness
disease, there is a substantial Alzheimer's donepezil or to dreams, and the patient may need to
loss of the elements of the type. another piperidine aggression, take medication before going
cliolinergic system and it is derivates, use with agitation, to bed
generally accepted that the caution in people anorexia, - Patient Counselling This drug
symptoms of Alzheimer's with cardiac dizziness, may cause dizziness, do not
disease are related to this disease, chronic hallucinatio drive or operate machinery.
cholinergic deficit, obstructive ns, - Explain patient not to take
particularly in cerebral cortex pulmonary disease, alcohol, other medicines like
and other areas of the brain. In asthma, severe sedatives, tranquilizers, mood
normal function, cardiac stabilizer
acetylcholine is an essential arrhythmias,
neurotransmitter and plays an patients with
important role in cognitive gastrointestinal CVS: -Monitor heart rate as
function, including memory disorders and Bradycardia, bradycardia may occur
storage and retrieval. Loss of seizures. -Instruct the patient to avoid
cholinergic neurons of the heavy work
central nervous system has
been found to correlate with
the severity of cognitive G.I. -Advise small frequent meals,
impairment. Donepezil nausea, frequent mouth care, sucking hard
inhibits vomiting, candy or chewing gum may help
acetylcholinesterase, an diarrhoea, to reduce nausea
enzyme responsible for the anorexia, - Monitor body weight, and
destruction of one weight loss, symptoms of gastrointestinal
neurotransmitter, decreased intolerance.
acetylcholine. This leads to appetite - Emphasize to take medicine
increased concentrations of along with food and drinking
acetylcholine in the brain, plenty of liquids
and the increased
concentrations are believed Gastrointe -Monitor pain level through
to be responsible for the stinal rating scale
improvement seen during disorders: -Provide pain relief medicine
treatment with donepezil. Abdominal according to prescription
Cholinesterase inhibitors do pain, -Provide antacids according to
not alter Alzheimer's disease dyspepsia prescribed order
but may stabilize the elder at
the current level of dementia Dermatolog - Reports the appearance of any
or lessen the symptoms. ical: rash on skin to the physician
Pharrnacokinetics Skin rashes, - Avoid spilling any of the
It has an oral bioavailability pruritis liquid concentrate skin
of 100% and easily crosses

154
the blood-brain-barrier. Renal: -Educate the patient about side
Biological half-life is about increased effect of the dug
70 hours. Excretes through frequency of -Give the reassurance about the
urine. urination. symptoms
-report the physician

RIVASTIGMINE

Trade name
Exelon

Classification
Anticholinesterases, Neurodegenerative Disease Drugs

Dose
Adult: PO Mild to moderately severe dementia in Alzheimer's disease; Mild to moderately
severe dementia associated with Parkinson's disease As rivastigmine hydrogen tartrate: Initial:
1.5 mg bid, increased in increments of 1.5 mg bid at intervals of at least 2 wk, according to
response and tolerance. Usual dose: 3-6 mg bid. Max: 6 mg bid. Retitrate from 1.5 mg bid, if
treatment is interrupted for several days.

Transdermal Mild to moderately severe dementia in Alzheimer's disease; Mild to moderate

dementia associated with Parkinson's disease Initial: 4.6 mg/24 hr, increased after at least 4 wk,

155
 if tolerated to 9.5 mg/24 hr for Min 6 mth. Then, may increase to 13.3 mg/24 hr, according to
response. Retitrate from 4.6 mg/24 hr, if treatment is interrupted for more than 3 days. Apply
patch to dry, clean, and hairless skin on the upper or lower back, upper arm or chest. Place patch
on different area each day allowing 14 days to elapse before using the same area.

MECHANISM OF INDICATION CONTRAINDI SIDE NURSE’S RESPONSIBILITY

ACTION CATION EFFECT
Rivastigmine Alzheimer's Special precaution CNS: -Emphasize the importance of taking
increases dementia, with th Patient CNS the medication every day
acetylcholine present Dementia with sick sinus depression, - Explain family members that
in CNS by reversibly associated with syndrome, extrapyram rivastigmine may cause dizziness
inhibiting hydrolysis Parkinson's bradycardia, or idal and the patient may need to take
of acetylcholine by disease, conduction symptoms, medication before going to bed
cholinesterases. treatment of defects; risk of Dizziness, - Patient Counselling This drug may
Duration: Approx 10 mild to ulcer disease; headache, impair physical and mental abilities, if
hours. moderate Alzhei respiratory tremor, affected, do not drive or operate
Absorption: Readily mer's diseases (e.g. drowsiness, machinery.
and completely disease and Park COPD, asthma); agitation, - Monitor cognitive function
absorbed from the inson's. history of seizure seizures. Ps periodically
gastrointestinal tract. disorder; bladder ychiatric -Report the physician if extrapyramidal
Food delays outlet obstruction, disorders: I symptoms occur.
absorption. prostatic nsomnia, -Provide calm and Peaceful
Bioavailability: 36%. hyperplasia; body confusion, environment for sleeping
Time to peak plasma weight <50 kg. depression.
concentration: Approx Mild to moderate
1 hour (oral); 8 to 16 hepatic CVS: -Monitor BP regularly.
hours (transdermal). impairment. Bradycard -Instruct the patient to avoid heavy
Distribution: Widely Pregnancy and ia, heart work
distributed in the lactation. block
body. Readily crosses G.I. -Should be taken with food.
the blood-brain nausea, - Monitor body weight, and symptoms
barrier. Volume of vomiting, of gastrointestinal intolerance.
distribution: 1.8 to 2.7 diarrhoea, - Provide the patient with sugarless,
L/kg. Plasma protein- anorexia, candy or gum, ice and frequent sips of
binding: Approx 40%. weight water
Metabolism: Rapidly loss,
and extensively decreased
metabolised in the appetite
brain via Gastroint -Monitor pain level through rating
cholinesterase- estinal scale
mediated hydrolysis disorders: -Provide pain relief medicine
to weakly active Abdominal according to prescription
decarbamylated pain, -Provide antacids according to
metabolite; further dyspepsia prescribed order

156
metabolised in the Skin: - Reports the appearance of any rash
liver via N- Allergic on skin to the physician
demethylation and/or dermatitis - Avoid spilling any of the liquid
sulphate conjugation. (patch) concentrate skin
Excretion: Mainly
via urine (97% as
metabolites); faeces
(0.4%). Half-life
elimination: 1.5 hours
(oral); approx 3 hours
(transdermal).

MEMANTINE

Trade Name
Axura, Ebixa, Namenda

Classification
Anti-dementia drugs, Neurodegenerative Disease Drugs

Dose
PO Initial: 5 mg once daily for the 1st wk, increased in wkly increments of 5 mg. Max: 20
mg/day.

157
MECHANISM OF INDICATI CONTRAIND SIDE NURSE’S RESPONSIBILITY
ACTION ON ICATION EFFECT
Memantine, a Moderate to Special CNS: -Emphasize the importance of taking
derivative of severe precaution Headache, the medication every day
amantadine, is a dementia in Patient with CV dizziness, , - Explain family members that
noncompetitive N- Alzheimer's disease, somnolence, memantine may cause dizziness and
methyl-D-aspartate disease. epilepsy, history anxiety, the patient may need to take
(NMDA)-receptor of convulsions confusion, medication before going to bed
antagonist which or those with hallucinations, - Patient Counselling This drug may
binds preferentially to predisposing fatigue, impair physical and mental abilities, if
NMDA-receptor- factors for abnormal gait, affected, do not drive or operate
operated cation epilepsy. hypertonia machinery.
channels. It blocks the Conditions that suicidal ideation -provide psychological support
action of glutamate, may increase -Instruct the family member do not
the principal urinary pH (e.g. allow the patient lonely
excitatory drastic dietary
neurotransmitter in changes).
the CNS. Glutamate Moderate to CVS: -Monitor BP in every shift.
may contribute to the severe renal and Hypertension, -Instruct the patient to avoid heavy
pathogenesis of severe hepatic CHF work
Alzheimer's disease impairment. -Report the physician if BP arises
by overstimulating Pregnancy and consistentlly
various glutamate lactation. G.I. vomiting, - Provide the patient with sugarless,
receptors resulting in constipation candy or gum, ice and frequent sips of
excitotoxicity and water
neuronal cell death. -Provide high fiber diet
Absorption: Well -Advice the patient to drink more
absorbed. Absolute water
bioavailability:
Approx 100%. Time Hematological:
to peak plasma thromboembolis -Perform periodically blood
concentration: Approx m, increased examination to identify initially blood
3-8 hr. libido, psychotic diseases.
Distribution: Volume reactions, -Close observation on blood
of distribution: 9-11 pancreatitis,agra examination
L/kg. Plasma protein nulocytosis, -Report the physician if any significant
binding: Approx 45%. leucopenia occurs.
Metabolism: Underg (including
oes partial hepatic neutropenia),thr
metabolism to main ombocytopenia,
metabolites pancytopenia,
including N-3,5- thrombotic
dimethyl-gludantan thrombocytopen
and 1-nitroso-3,5- ic, purpura
dimethyl-adamantane.
Excretion: Mainly
via urine (approx 57-
82% as unchanged
drug). Terminal half-
life: 60-100 hr.

158
 Hepatic & -Perform periodically LFT &RFT
renal- blood examination
hepatitis, , acute -Inform the patient about the side
renal failure effect
(including -Report the physician
increased
creatinine and
renal
impairment),
Skin: -Perform close observation related to
Stevens-Johnson skin diseases.
syndrome. -Instruct the client report if any kind
of skin reactions seen
-Educate the patient about side effect
of the drug
-Report the physician if the patient
shows steven Johnson syndrome
related symptoms

GALANTAMINE

Trade Name
Razadyne, Reminyl

Classification
Anticholinesterases, Neurodegenerative Disease Drugs

159
 Dose
PO For symptomatic treatment of mild to moderately severe cases: As conventional tab/oral
suspension : Initially, 4 mg bid for 4 weeks, increase to 8 mg bid for at least 4 weeks, if tolerated.
May further increase to 12 mg bid according to individual response and tolerability. As
modified-release cap: Initially, 8 mg once daily, preferably in the morning for 4 weeks, increase
to 16 mg once daily for at least 4 weeks. May further increase to 24 mg once daily according to
individual response and tolerability.

MECHANISM OF INDICATI CONTRAINDI SIDE NURSE’S RESPONSIBILITY

ACTION ON CATION EFFECT
Galantamine is a Moderate to Severe renal and CNS: -Emphasize the importance of taking
selective, competitive severe hepatic CNS the medication every day
and reversible dementia in impairment. depression, - Explain family members that
centrally-acting Alzheimer's seizures, memantine may cause dizziness and
acetylcholinesterase disease. Special Headache, the patient may need to take
inhibitor. It elevates Precautions the dizziness, medication before going to bed
acetylcholine in the Patient with CV somnolence, - Patient Counselling This drug may
cerebral cortex by disease (e.g. syncope, impair physical and mental abilities, if
slowing its immediate post- tremor. affected, do not drive or operate
degradation. It also MI period, new- Psychiatric machinery.
increases onset atrial disorders: Depr -provide psychological support
acetylcholine from fibrillation, 2nd ession, -Instruct the family member do not
surviving presynaptic degree heart block hallucination allow the patient lonely
terminals by or greater, -Instruct the patient do not take any
modulating the unstable angina OTC drug during the treatment
nicotinic acetylcholine pectoris, CHF, regimen
receptors. Glutamate sick sinus
and serotonin levels syndrome,
may also be increased. bradycardia, or CVS: -Monitor BP periodically.
Absorption: Well other Hypertension,f -Instruct the patient to avoid heavy
absorbed from the supraventricular lushing Palpitat work
gastrointestinal tract. cardiac conduction ions -Report the physician if BP arises
Food delays rate of abnormalities); vagotonic consistently
absorption. uncorrected effects on heart -Instruct the client for routinely follow
Bioavailability: electrolyte rate (e.g. up checkup
Approx 90%. Time to disturbances (e.g. bradycardia,atri
peak plasma hyper- or oventricular
concentration: Approx hypokalaemia); node block)
1 hour (immediate- history of seizure G.I. disorders : -Monitor body weight daily
release); approx 4.5-5 disorders; increase gastric -Medicine should be taken with food.
hours (modified- Parkinson's acid secretion, - Provide the patient with sugarless,
release). disease; asthma, Nausea, candy or gum, ice and frequent sips of
Distribution: Volume COPD, active vomiting, water
of distribution: 175 L. pulmonary abdominal
Plasma protein infections (e.g. pain, diarrhoea,
binding: 18%. pneumonia); dyspepsia -Monitor abdominal pain through pain
Metabolism: Metabol bladder outlet scale.
ised in the liver obstruction or -provide pain relief medicine
according to physician’s order
160
mainly by CYP2D6 prostatic Eye -Explain the side effect of the drug
isoenzyme and hyperplasia; disorders: -Advice the patient do not drive a car
CYP3A4 isoenzyme gastrointestinal Blurred vision. in blurred vision
to O-desmethyl- obstruction or
galantamine, and recovering from Skin & -Perform close observation related to
galantamine-N-oxide gastrointestinal subcutaneous skin diseases.
metabolites, surgery; risk tissue -Instruct the client report if any kind
respectively. factors for ulcer disorder: of skin reactions seen
Excretion: Via urine disease (e.g. Hyperhidrosis, -Educate the patient about side effect
(approx 20-30% as history of ulcer, Serious skin of the drug
unchanged drug); concomitant reactions (e.g. -Report the physician if the patient
faeces (approx 6%). NSAID use). Stevens- shows steven Johnson syndrome
Elimination half-life: Moderate renal Johnson related symptoms
Approx 7 hours. and mild to syndrome, -Steven- Johnson syndrome patient
moderate hepatic acute should be managed in a single room.
impairment. generalised
Elderly. exanthematous
Pregnancy and pustulosis,
lactation. CYP2D erythema
6 poor multiforme)
metabolisers. Ear and -Perform close ear examination
labyrinth -Report the physician
disorders:
Tinnitus

161
OTHER DRUGS

162
 THIAMINE HYDROCHLORIDE

Thiamine Hydrochloride is the hydrochloride salt form of thiamine, a vitamin essential for
aerobic metabolism, cell growth, transmission of nerve impulses and acteylcholine synthesis.

Trade name
Betalin

Classification
Vitamin B1

Dose
1.Usual Adult Dose for Beriberi
10 to 20 mg IM three times daily for up to 2 weeks. Thereafter, use an oral therapeutic
multivitamin preparation containing 5 to 10 mg thiamine daily for one month. A complete and
balanced diet should follow.

2. Neuritis of pregnancy:
If vomiting severe to preclude oral therapy, give 5 to 10 mg IM daily.
3.Usual Adult Dose for Thiamine Deficiency
If dextrose administered: to patients with marginal thiamine status, give 100 mg in each of the
first few liters of IV fluid to avoid precipitating heart failure.

4. Usual Adult Dose for Vitamin/Mineral Supplementation

50 to 100 mg orally once a day

5. Usual Adult Dose for Wernicke's Encephalopathy

163
 100 mg IV as an initial dose followed by 50 to 100 mg/day IM or IV until the patient is on a
regular, balanced, diet.

6. Usual Pediatric Dose for Beriberi

10 to 25 mg IM or IV daily (if critically ill), or 10 to 50 mg orally every day for 2 weeks, then 5
to 10 mg orally daily for 1 month. If collapse occurs: 25 mg IV. Administer with caution.

7.Usual Pediatric Dose for Thiamine Deficiency

If dextrose administered: to patients with marginal thiamine status, give 100 mg in each of the
first few liters of IV fluid to avoid precipitating heart failure.

8. Usual Pediatric Dose for Vitamin/Mineral Supplementation

Infants: 0.3 to 0.5 mg orally once a day; children: 0.5 to 1 mg orally once a day.

Mechanism of Indication Contraindication Side effect Nursing

action management
1.Thiamine 1.Metabolic 1.Conditions: •Restlessness •Assesment prior to
combines with disorders. Taking Systemic medication for any
adenosine thiamine mytocytosis allergy to vitamine
triphosphate (ATP) by mouth helps supplement.
in the liver, correct certain 2.Allergies
kidneys, and inherited metabolic Vitamine B
leukocytes to disorders,1 including •Assessment of
produce thiamine Leigh's 3.Do not give intra patient for swelling
diphosphate. disease, maple syrup arterial •Rapid swelling
urine disease, and •Ulcers •Monitor the
2.Thiamine others. •Pruritus injection site
diphosphate acts as continuously.
a coenzyme in 2.Thiamine •Escape of blood
carbohydrate deficiency. Taking from a ruptured
metabolism, in thiamine by mouth blood vessel •Assessment for any
trans -ketolation helps prevent and hypersensitivity
reactions, and in treat thiamine reaction
the utilization of deficiency. •Skin rash
hexose in the Cyanosis
hexose- 3.Cardiovascular Nausea
monophosphate manifestations •Do not left the
shunt. Without include peripheral patient during
adequate thiamine, vasodilation, medication,
pyruvic acid does biventricular failure, continuously
not undergo and edema. •Heart failure assessment of vital
conversion to signs. Make sure for
acetyl-CoA and 4..Brain disorder due the arrangements of
cannot enter the to thiamine any cardiac
Krebs cycle. deficiency emegency
3.Pyruvic acid (Wernicke-

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accumulates in the Korsakoff
blood and is syndrome).
subsequently Thiamine helps
converted to lactic decrease the risk and
acid, with the symptoms of a
potential specific brain
development of disorder called
lactic acidosis. Wernicke-Korsakoff
Diminished syndrome (WKS).
production of This brain disorder is
NADH in the Krebs related to low levels
cycle also results in of thiamine. It is
lactic acid often seen in
production through alcoholics. Giving
facilitation of thiamine shots seems
anaerobic to help decrease the
glycolysis. risk of developing
WKS and decrease
symptoms of WKS
during alcohol
withdrawal.
5.Possible other uses
a) Cataracts.

b)Painful
menstruation

TRAMADOL

Trade name
Ultram Ultram ER, Ryzolt, ConZip

Classification
 Chemical class: Cyclohexanol
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  Therapeutic class: Analgesic
 Pregnancy category: C
 Controlled substance schedule: IV

Dose
ADULTS
 Patients who require rapid analgesic effect: 50–100 mg PO q 4–6 hr; do not exceed 400
mg/day.
 Patients with moderate to moderately severe chronic pain: Initiate at 25 mg/day in the
morning and titrate in 25-mg increments q 3 days to reach 100 mg/day. Then, increase in 50
mg-increments q 3 days to reach 200 mg/day. After titration, 50–100 mg q 4–6 hr; do not
exceed 400 mg/day.
 Patients with cirrhosis: 50 mg q 12 hr.
 Patients with creatinine clearance < 30 ml/min: 50–100 mg PO q 12 hr. Maximum 200
mg/day

PEDIATRIC PATIENTS
Safety and efficacy not established.

GERIATRIC PATIENTS OR PATIENTS WITH HEPATIC OR RENAL IMPAIRMENT

more than 75 years: Do not exceed 300 mg/day.

Mechanism of Indication Contraindication Side effects Nursing responsibility

action
1.Tramadol Relief of •Hypersensitiviy 1.CNS: •Assess patient for evidence
inhibits moderate Tto tramadol or •Agitation, of dependence or abuse
reuptake of to opioids. •anxiety before giving first dose of
norepinephrine moderately •Known or •asthenia, tramadol.
,serotonin and severe pain suspected gastroin •depression, •Avoid giving drug to
enhances testinal obstructio •dizziness, patients with a history of
serotonin n, •emotional dependence on other opioids.
release. including paralyti lability, •Use tramadol cautiously in
2.It alters c ileus. •euphoria, patients who are taking
perception and •Concurrent use •fatigue, tranquilizers or
response to of monoamine •fever, antidepressant drugs and in
pain by binding oxidase inhibitors •hallucinations, patients who use alcohol in
to mu-opiate (MAOIs) or use •headache, excess or who suffer from
receptors in the within last 14 •hypertonia, emotional disturbance or
CNS. days. •hypoesthesia, depression
3.Tramadol •Suicidal patients, •insomnia, •Monitor patient closely for
works by acute alcoholism; •lethargy, evidence of suicidal thinking
changing how head injuries; •nervousness, or behavior, especially when
your brain raised intracranial •paresthesia, therapy starts or dosage
senses pain. pressure; •restlessness, changes
4.Tramadol is severe renal •rigors, •Provide patient

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similar to impairment; •seizures, psychotherapy according to
substances in lactation. •serotonin the need.
your brain •syndrome, Take precautions for
called •somnolence, seizures.
endorphins. •suicidal •Provide harmless
Endorphins ideation, enviornment.
bind to •tremor,
receptors. The •vertigo,
receptors then •weakness •Monitor blood pressure
decrease the frequently.
pain messages 2.CV: •Advice patient to rise
that your body •Chest pain, slowly.
sends to your •orthostatic
brain. •hypotension,
•vasodilation •Instruct the patient about
visionary side effect in
3.EENT: advance and educate them to
•Blurred vision, inform immediately if it may
•dry mouth, worsen.
•nasal or sinus •Advice patient to rinse
congestion, mouth and use hard candy.
•sore
throat•vision
changes
•Avoid giving tramadol to
patients with acute
4.ENDO: Hot abdominal conditions
flashes because it may mask
evidence and disrupt
5.GI: assessment of the abdomen.
•Abdominal
pain,
•anorexia,
•constipation, •Monitor and maintain intake
•diarrhea, output chart.
•indigestion,
•nausea,
vomiting
•Provide rest to the patient.
5.GU:
•Urinary
frequency,
•urine retention
• Assess respiratory status
6.MS: often if patient has increased
•Arthralgia; intracranial pressure or head

167
 •back, limb, or injury because of possible
neck pain increased carbon dioxide
retention and CSF pressure,
either of which may cause
7.RESP: respiratory depression.
•Cough, dyspnea

SKIN: •After patient receives first

•Diaphoresis, tramadol dose, watch for
•dermatitis, allergic reactions if any
•flushing, allergic reaction occurs stop
•pruritus, the drug and notify
•rash physician.

Other:
Flulike illness,
physical and
psychological
dependence

PHENERGAN

Generic name
Promethazine hydrochloride

Trade name
Phenergan Anergan 25, Anergan 50, Antinaus 50, Histantil (CAN), Pentazine, Phenazine 50

Classification
Chemical class: Phenothiazine derivative
Therapeutic class: Antiemetic, antihistamine, antivertigo, sedative-hypnotic
Pregnancy category: C

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 Dose
1. To prevent or treat motion sickness -syrup, tablets
Adults and adolescents. 25 mg 30 to 60 min before travel and repeated 8 to 12 hr later, if needed.
Maximum: 150 mg daily.

2. To treat vertigo -syrup, tablets

Adults and adolescents. 25 mg twice daily, as needed. Maximum: 150 mg daily.

3. To treat signs and symptoms of allergic response -syrup, tablets

Adults and adolescents. 10 to 12.5 mg four times a daybefore meals and at bedtime, as needed.
Or, 25 mg at bedtime, as needed. Maximum: 150 mg daily.

4. To provide nighttime, preoperative, or postoperative sedation -syrup, tablets

Adults and adolescents. 25 to 50 mg as a single dose. Maximum: 150 mg daily.

5. To provide obstetric sedation -i.v. or i.m. injection

Adults and adolescents. 50 mg for early stages of labor, followed by 1 or 2 doses of 25 to 75 mg
after labor is established, repeated every 4 hr during normal labor.

Mechanism Indication Contraindi Side-Effects Nursing Management

Of Action cation
1. Competes 1. To •Angle- CNS: •Urge patient to avoid
with prevent or closure •Akathisia, alcohol and other CNS
histamine for treat glaucoma •CNS stimulation, depressants during
H1-receptor motion •confusion, therapy.
sites, thereby sickness. •Benign •dizziness, •drowsiness, Assessment of mental
antagonizing prostatic •dystonia, status before and after
many 2. To treat hyperplasia •euphoria, administration of drug.
histamine vertigo. •excitation, • Instruct patient to
effects and •Bladder •fatigue, •hallucinations, avoid hazardous
reducing 3. To neck •hysteria, •incoordination, activities until drug’s
allergy signs prevent or obstruction •insomnia, •irritability, CNS effects are known.
and treat nausea •nervousness,

169
symptoms. and •Bone CV: •Monitor patient for
vomiting in marrow •Bradycardia, evidence of neuroleptic
2. certain depression •hypertension•hypotension malignant syndrome,
Promethazine types of •tachycardia such as fever,
also prevents anesthesia •Breastfeedi hypertension or
motion and ng EENT: hypotension,
sickness, surgery. •Blurred vision•diplopia involuntary motor
nausea by •Children •dry mouth, activity, mental
blocking H1 4. To treat under age 2 nose, and throat changes, muscle
receptor and signs and •nasal congestion•tinnitus rigidity, tachycardia,
vertigo by symptoms •Coma •vision changes and tachypnea.Be
acting of allergic prepared to provide
centrally on response. •Hypersensit ENDO: •Hyperglycemia supportive treatment
medullary ivity or and drug therapy, as
chemorecepti 5. To history of GI: prescribed.
ve trigger provide idiosyncrati •Anorexia, •vomiting
zone and by nighttime, c reaction to •dry mouth • Suggest rinsing and
decreasing preoperativ promethazin use of sugarless gum or
vestibular e, or e. GU: hard candy to relieve
stimulation postoperati •Dysuria dry mouth.
and ve sedation.
labyrinthine HEME:•Agranulocytosis,
function in 6. To •leukopenia, • Monitor patient’s
the inner ear. relieve •thrombocytopenia, hematologic status as
3. It also apprehensio ordered because
promotes n and RESP: Apnea, •respiratory promethazine may
sedation and promote depression, •tenacious cause bone marrow
relieves sleep the bronchial secretions depression.
anxiety by night •Assess patient for
blocking before SKIN: Dermatitis, signs and symptoms of
receptor sites surgery. diaphoresis, jaundice, infection or bleeding.
in CNS, photosensitivity, rash,
directly urticaria •Monitor vital signs and
reducing Other:•Angioedema, sign of any breathing
stimuli to the 7. To paradoxical reactions difficulty. Provide
brain. provide Decongestant.
obstetric
sedation. Monitor for any allergic
reaction.
Advice patient to avoid
excessive sun
exposureand to use
sunscreen when
outdoors.

170
 BIBLIORAPHY

1. Sreevani, R. (2016). A Guide to health and psychiatric nursing. (4th ed). New Delhi.
Jaypee brothers, medical publishers (p) ltd.

2. Neeraja. K.P. (2008). Essential of mental health nursing.(1 st ed). New Delhi. Jaypee
brothers medical publishers (p) ltd.

3. Lalitha, K. (2007). Mental Health and Psychiatric Nursing – An Indian Perspective. New
Delhi. Satish Kumar Jain. CBS & Distributers.

4. www.mims.com

5. Learing, J. & k. (2015). Nurse’s Drug Handbook. (14th ed). United State of America.
Online book seller .Jones & Bartlett Learning 5 Wall Street Burlington.

6. Anbu, T. (2010). Textbook of Psychiatric Nursing. (1 st ed). Banglore. Manjunath S.

Heede. Emmess Medical Publishers.

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