Central Nervous System

 Many drugs specifically target the CNS

 Many drugs cause undesired side effects or adverse effects in the CNS
 Some drugs are given for their CNS side effects

 Sedatives/Hypnotics (Inhibitory)
 Stimulants (Excitatory)

Sleep
 Transient, reversible, periodic state of rest, with decreased physical activity and level of
consciousness.
 Sleep Architecture
 REM and Non-REM
o Various drugs affect different stages
 REM Rebound

Neurotransmitters
 GABA-Gamma-aminobutyric acid
o Primary inhibitory neurotransmitter in the brain.
 Calms and quiets, or puts the breaks on the CNS
 Sed/Hyp mimic GABA in the CNS
 Sedative/Hypnotics

Sedatives
 Drugs that have an inhibitory (depressive) effect on the
CNS
 Reduce:
o Nervousness
o Excitability
o Irritability without causing sleep

Hypnotics
 Cause sleep
 REM-REM rebound

**A sedative can become a hypnotic if it is given in large enough doses

Sedative/Hypnotics
Three Main Types
 Benzodiazepines
 Miscellaneous or Non-benzos
 Barbiturates

Benzodiazepines: Valium - Prototype

epam/olam Action: not fully understood, Interactions and Contraindications
Long Acting mimics GABA  Other CNS depressants (alcohol,
diazepam, Indications: Anxiety, Insomnia opioids)
clonazepam Route: Oral, sub lingual,  Antacids
Intermediate IM(deep), IV(caution)  MAOIs (antidepressant)
Acting Alerts  Kava and Valerian
Lorazepam,  Lethal combos with other  Grapefruit juice, cardiac meds
alprazolam CNS depressants and antifungals increase action
Short Acting  Caution in Seniors  Reduces effectiveness of oral
midazolam  Schedule IV contraceptives
Side effects  Pregnancy and lactating moms
 Drowsiness  Alcohol abuse
 Decreased mental  Nonbenzodiazepine Hypnotics
alertness  The ZZZ’s
 Dizziness, Vertigo  Share many characteristics of
 BP drop benzodiazepines
 Lethargy  Used for
 Withdrawal o short term treatment of
 Fall hazard for elderly insomnia
persons o Sedation preop
 “Hangover” o Sedation pre EEG
effect/daytime sleepiness  Examples:
Toxicity and OD o Chloral hydrate, zalepion
 Confusion (Sonata), zolpidem
 Respiratory depression (Ambien), eszoplicone
 Coma (Lunesta), and ramelteon
 Diminished reflexes (Rozerem)
 Death o Eszoplicone and
extended-release zolpidem
 Flumazenil (Romazicon) only ones approved for
benzodiazepine antagonist long-term insomnia
antidote treatment

Nonbenzodiazepines
Action Adverse reactions Contraindicated in breast
 not fully known  N&V feeding
 Lose effectiveness by  Paradoxical rxn-  Use cautiously in older
end of week 2 agitation adults/lower dose
 Gastric irritation  Chloral hydrate
 Hangover o Bleeding risk with oral
anticoagulants
Barbituates: Phenobarbital sodium (Luminal)
Mechanism of Action Fallen out of favor Nursing concerns
 Acts on the brainstem area  Unfavorable safety  Assess anxiety
called reticular formation profile level prior to
 Depresses impulses to cerebral  Low Therapeutic administration
cortex Index  Caution with
 Effect is dose related  Benzos are safer driving or operating
machines
utol All cause drowsiness,  Dependency and
inal addiction, and respiratory tolerance
onal depression  Withdrawal
itol o Sweating,
 Ultrashort Acting vomiting, muscle
Drug Effects o Thiopental cramps, tremors
 Low doses: sedative effects  Short Acting convulsions
 High doses: hypnotic effects o Secobarbital  Monitor VS
respiratory depression, coma ---  Intermediate  May be crushed or mixed
death o Butabarbital with food
Uses:  Long Acting  Concomitant CNS
 Pre-op sedation and anesthesia  Phenobarbital depression use (opiates,
 Insomnia ETOH)
 Anxiety Side Effects
 Seizure disorders-most common  Vertigo
Route  N&V
 Oral, IV, NO IM  Constipation
Safety precautions!  Anxiety
 Always use an infusion pump  Irritability
for IV!  Spasm of the voice box
 Caustic to the vein  Hangover
 pain
 Resp depression

 Stevens Johnson
syndrome
o

CNS STIMULANTS = Go faster!

Neurotransmitters
 Primary Excitatory Neurons
o Dopamine, Norepinephrine and Serotonin

Indications:
 Narcolepsy
 Migraine headaches
 ADHD
 Anorexiant
 Analeptics
Major Chemical Classes
 Amphetamines
 Serotonin Agonists
 Sympathomimetics
 Xanthines

Major Therapeutic Classes

 Anti-attention Deficit
 Anti-narcoleptic
 Anorexient
 Anti-Migraine
 Analeptic

Drug Action
 Increase dopamine, norepinephrine, and serotonin effect
o Action and effects vary according to drug used
o Effects are often dose-related

In general they:
 Elevate mood
 Increase energy
 Increase alertness
 Decrease appetite
 Enhance task performance

High abuse potential!

Common adverse effects

 Too much of a good thing:
o Palpitations, tachycardia, hypertension, angina, dysrhythmias, nervousness,
restlessness, anxiety, insomnia, nausea, vomiting, diarrhea, dry mouth, increased
urinary frequency

Anti-Attention Deficit
 Amphetamines:
o Dextroamphetamine
o Amphetamine (Adderall)
o Lisdexamfetamine (Vyvanse)

 Non-amphetamines
o Methylphenidate (Concerta, Ritalin)
o Atomoxetine (Strattera)
Bought, sold and traded on college campuses
CNS Stimulants
 Obesity as a Medical Diagnosis?
 Anorexiants
o Supress the appetite centers in the brain
o Effectiveness not proven
 Phentermine (Lonamin)
 Benzphetamine (Didrex)
 Liraglutide (Saxenda, Victoza) also a DM drug
 orlistat (Xenical) not a CNS Stimulant-Lipase inhibitor
 sibutramine (Meridia) withdrawn due to safety concerns (MI, CVA,
Death)
o Adverse side effects:
 Dry mouth
 Headache
 Insomnia
 Constipation,
 Tachycardia
 Cardiac Dysrhythmias
 HTN
 Changes in mentation
 Changes in mood
 Seizures
 Anal leakage (oily)

Migraine
 Anti-migraine (serotonin agonists) the triptans
o almotriptan (Axert)
o eletriptan (Relpax)
o frovatriptan (Frova)
o naratriptan (Amerge)
o rizatriptan (Maxalt)
o sumatriptan (Imitrex)
o zolmitriptan (Zomig)

Contraindications
o Ergot Alkaloids:
 HTN
 Cerebral, Cardiac or PVD
 Dysrhythmias
 CAD
o Triptans :
 Allergy
 Cardiovascular disease
Adverse Effects
o Ergot Alkaloids:
 N/V, clammy, muscle pain, anxiety, bitter taste
Triptans:
o Vasoconstriction
o Local irritation (injection)
o Tingling, flushing
o Congested feeling
CNS Stimulants
 Analeptics
o Used less frequently
o Still used for neonatal apnea or drug induced resp depression
o Examples:
 doxapram (Dopram)
 Methylxanthines, such as aminophylline,
 theophylline
 caffeine
Caffeine
 Used in:
o Neonatal apnea
o Respiratory depression in adults
o Enhances effects of analgesics and migraine medications
o Stimulates CNS (NoDoz, Vivarin)
 Found in:
o Over-the-counter drugs
o Combination prescription drugs
o Foods and beverages
 Use with caution
o Recent myocardial infarction
o Dysrhythmias
o Peptic ulcer
Nursing Considerations: Stimulants
 Assess for:
o Potential contraindications
 abnormal cardiac rhythms, seizures, palpitations, liver problems
 MAO inhibitor use
 Monitor for:
o Side effects
o Dependency
o Drug diversion

Nursing Care : ADHD

Last daily dose should be given 4 to 6 hours before bedtime
 Take on an empty stomach, 30 to 45 minutes before meals
 For children
o Assess baseline height and weight
o Monitor child for continued physical growth, including height and weight
 Drug “holidays” may be ordered (let them go wild over Christmas!)