najARRIETA, RN, RM, CTN, MANc, DRDMc

Pharmacology Review
Pharmacology
• Study of biological effects of
chemicals

DRUGS!!!
Pharmaco-kinetics

• Absorption
– Consider: FIRST
PASS EFFECT
• Distribution
• Biotransformation/
Metabolism
– Liver!!
• Excretion
Computations!
• Parenteral Drugs
– Consider the quantity/diluent
– Modify the available as needed

Remember PA-Q
Drug Administration
• Oral
– Pills
– Tablets
– Capsules
– Caplets
– Liquids
• Take note of presence of food!
• NPO – nil per os
Drug Administration
• Parenteral
– ID
• Create wheal, and mark borders!
– Subcutaneous
• No greater than 1 mL!
• Insulin – Rotate sites – prevent lipodystrophy!
– IM (may use Z-track)
• No greater than 3 mL!
• Aspirate for 5 to 10 seconds!
• 10 secs/mL in injecting!
Subcutaneous
Drug Administration
• IV
– Disinfect Y-Port!
– Kink tubing nearest the patient first and
aspirate for more fluid (if possible)
– Kink tubing farthest when injecting
– SLOW push!
– Do not mix IV medications! Unless allowed
Drug Administration
• Respiratory
– Nebulization
– Metered-Dose Inhaler
• Topical
– Slowest to be absorbed!
– Clean area and don gloves
– Do NOT touch droppers/tube tips
Mini-Quiz
• The physician orders for Cefalexin
1000mg, there are 250mg caplets. How
many caplets will the nurse prepare?
Mini-Quiz
• The physician prescribes Paracetamol 200
mg, the available is 300mg/mL in a 2 mL
ampoule. How many mL will the nurse
prepare?
Mini-Quiz
• The physician orders Hydrocortisone 4mg.
The nurse reads that the vial containing 8
mg needs to be added 1.5 mL to make a
2mL solution. How many mL will the nurse
prepare?
Mini-Quiz
• The physician orders IV for an adult client.
Started IVF with PNSS 1 L to run for 10
hours
– How many drops per minute is the regulation?
– How many mL is infused per hour?
– If the IVF started at 9AM, what level is the IVF
at 12NN?
Pharmacodynamics
• Mechanisms by which drugs produce
biochemical and physiologic changes
in the body
– Additive (1 + 1 = 2)
• ie ibuprofen + acetaminophen = pain relief
– Synergistic (1 + 1 = 3)
• ie promethazine + codeine = greater pain relief
– Antagonistic (1 + 1 = 0)
• Morphine + Naloxone = No Effect
Chemotherapeutic Agents

• Anti-infectives/Antibacterials
• Antiviral
• Antifungal
• Antiprotozoal
• Antihelminthic
• Antineoplastic
Aminoglycosides

• Ends in –cin
• Examples:
– Amikacin
– Gentamicin (P)
– Kanamycin
– Streptomycin
– Tobramycin
• Bactericidal; inhibits protein synthesis
Macrolides

• Ends in –thromycin
• Examples:
– Erythromycin (P)
– Clarithryomycin
– Azithromycin
• Interferes with protein synthesis
Lincosamides

• Ends in –mycin; with “lin”

• Examples:
– Clindamycin (P)
– Lincomycin
• Similar to macrolides; interferes with protein
synthesis
Tetracyclines

• Ends in –cycline
• Examples:
– Demeclocycline
– Doxycycline
– Minocycline
– Tetracycline (P)
• Inhibits protein synthesis
Fluoroquinolones

• Ends in –floxacin
• Examples:
– Ciprofloxacin (P)
– Gemifloxacin
– Levofloxacin
– Moxifloxacin
– Norfloxacin
– Ofloxacin
• Interfere with DNA replication
Penicillins

• Ends in –cillin
• Examples:
– Penicillin
– Amoxicillin
– Ampicillin
– Carbenicillin
– Ticarcillin
– Nafcillin
– Oxacillin
• Prevents cell wall synthesis
Cephalosporin (4 Generations)

• Starts with cef- or ceph-

• Examples:
– Cefazolin
– Cephalexin
– Cefaclor (P)
– Cefuroxime
– Cefotaxime
– Ceftriaxone
– Cefepime
• Same as penicillins, interferes with cell wall
synthesis
Monobactam antibiotic

• Aztreonam
• Disrupts bacterial cell wall synthesis
Sulfonamides

• Starts with sulf-

• Examples:
– Sulfadiazine
– Sulfisoxazole
– Sulfasalazine (P)
– Sulfamethoxazole
• Inhibits PABA, prevents synthesis of folic acid
SUMMARY

Drug Groups Action

Aminoglycosides Inhibits protein synthesis

Macrolides
Lincosamides
Penicillin Prevents bacterial cell wall
Cephalosporin synthesis
Monobactam
Fluoroquinolone Inhibits DNA

Sulfonamide Prevents folic acid synthesis

Antimycobacterial - antituberculosis

• Rifampicin
• Isoniazid
• Pyrazinamide
• Ethambutol
• Streptomycin
• Capreomycin
• Cycloserine
Antimycobacterials – Leprostatic drugs

• Dapsone
• Clofazamine
• Rifampicin
Antivirals

• Agents for Influenza

– Amantadine
– Rimantadine
– Oseltamivir (Tamifllu)
– Ribavirin
• Agents for Herpes and Cytomegalovirus
– Acyclovir
– Ganciclovir
– Valacyclovir
– Valganciclovir
Antivirals

• Agents for HIV and AIDS

– Reverse Transcriptase Inhibitors
• Bind to HIV reverse transcriptase
– Protease Inhibitors
• Blocks protease activity in the HIV
– Nucleosides
• Interferes with HIV replication
– Fusion Inhibitors (new)
• Prevents HIV from binding to the cell membrane
Antivirals

• Agents for Hepatitis B

– Prevents viral replication
– Adefovir
– Entacavir
Antifungals

• Systemic Antifungals
– Amphotericin B (IV)
– Caspofungin
– Micafungin
– Flucytosine Action:
– Griseofulvin Alters cellular
permeability
• The “Azoles”
– Ketoconazole
– Fluconazole
Antiprotozoals

• Antimalarials
– Prevents protein synthesis of plasmodium
– Chloroquine (P)
– Primaquine
– Quinine
– Mefloquine
– Pyrimethamine
– Artemeter-Lumefantrine**
Antiprotozoals

• These drugs inhibit DNA synthesis in

susceptible protozoa
• For giardiasis, amebiasis, trichomoniasis
– Metronidazole
– Tinidazole
• For PCP
– Atavaquone
– Pentamidine
Antihelminthic Agents

• Prevents glucose uptake by helminths

• Mebendazole (P)
• Albendazole
• Thiabendazole
• Pyrantel
• Praziquantel
Cell Cycle: Understanding Oncology
Antineoplastic

Drug Class and Mechanism of Cell Cycle Common Side

Examples Action Specificity Effects

Alkylating Agents Alter DNA Cell cycle- Bone marrow

>Busulfan, structure by nonspecific suppression,
carboplatin, misreading DNA vomiting, cystitis
chlorambucil, code, initiating (cyclophosphamid
cisplatin, breaks in the e, ifosfamide),
cyclophosphamide, DNA molecule, stomatitis,
dacarbazine, cross-linking alopecia, gonadal
hexamethul, DNA strands suppression, renal
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Nitrosureas Similar to Cell cycle- Delayed and

>Carmustine alkylating agents; nonspecific cumulative
(BCNU), cross the blood- myelosuppression
lomustine brain barrier , especially
(CCNU), thrombocytopenia;
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Topoisomerase I Induce breaks in Cell cycle- Bone marrow

Inhibitors the DNA strand specific (S suppression,
>Irinotecan, by binding to Phase) diarrhea, nausea,
topotecan topoisomerase I, vomiting,
preventing cells hepatotoxicity
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Antimetabolites Interfere with the Cell cycle- Nausea,

>5-Azacytadine, biosynthesis of specific (S vomiting,
capecitabine, metabolites or phase) diarrhea, bone
cytarabine, nucleic acids marrow
edatrexate necessary for suppression,
fludarabine, 5- RNA and DNA proctitis,
flourouracil (5- synthesis stomatitis, renal
FU), FUDR, toxicity
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Antitumor Interfere with Cell cycle- Bone marrow

Antibiotics DNA synthesis nonspecific suppression,
>Bleomycin, by binding DNA; nausea,
dactinomycin, prevent RNA vomiting,
daunorubicin, synthesis alopecia,
doxorubicin anorexia, cardiac
(Adriamycin), toxicity
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Mitotic Spindle      
Poisons      
>Plant alkaloids: Arrest Cell cycle- Bone marrow
etoposide, metaphase by specific (M suppression
teniposide, inhibiting tubular Phase) (mild with VCR)
vinblastine, formation; inhibit   neuropathies
vincristine (VCR), DNA and protein   (VCR), stomatitis
vindesine, synthesis    
vinorelbine    
 Arrest    
Drug Class and Mechanism of Cell Cycle Common Side
Examples Action Specificity Effects

Hormonal Bind to hormone Cell cycle- Hypercalcemia,

Agents receptor sites nonspecific jaundice,
>Androgens and that alter cellular increased
antiandrogens, growth; block appetite,
estrogens and binding of masculinization,
antiestrogens, estrogens to feminization,
progestins and receptor sites sodium and fluid
antiprogestins, (antiestrogens); retention,
aromatase inhibit RNA nausea,
Drugs Acting on the Immune System

• Anti-inflammatory Agents
• Vaccines and Sera
Anti-inflammatory Agents

• Salicylates
– Aspirin (P)
• NSAIDs
– Ibuprofen (P)
– Celecoxib
– Ketorolac
– Diclofenac
– Mefenamic acid
Vaccines and Sera

• Active immunity versus passive immunity

• Natural versus artificial immunity
• Vaccines are immunization containing
weakened or altered protein antigens
• Immune sera contains antibodies to specific
bacteria or viruses
• Antitoxin or antivenin are immune sera that
contain antibodies against toxins or venom
Drugs Acting on the Central and
Peripheral Nervous System

• Anxiolytic and Hypnotic Agents

• Antidepressants
• Psychotherapeutic Agents
• Antiepileptic Agents
• Antiparkinsonism Agents
• Narcotics and Antimigraine
Anxiolytics and Hypnotic Agents

• Benzodiazepines (Ends in –lam or –pam)

– Potentiate GABA, a neural inhibitor
– Diazepam (P)
– Alprazolam
– Clonazepam
– Lorazepam
– Midazolam
• Barbiturates (ends in –bartbital)
– Depresses the CNS
– Phenobarbital (P)
– Pentobarbital
– Secobarbital
Other Anxiolytics

• Buspirone (BuSpar) does not cause sedation

• Diphendydramine (Benadryl) and Hydroxyzine
(Iterax) are antihistamines
Antidepressants

• Monoamine Oxidase Inhibitors (PaNaMa)

– Tranylcypromine (Parnate)
– Phenelzine (Nardil)
– Isocarboxazid (Marplan)
• Special Note:
– Do not give with tyramine rich-foods (eg. Aged
cheese, fermented meat, brewer’s yeast, fava
beans, red wines)
– Interaction: Hypertensive crisis – treat with
Phentolamine
Antidepressants

• Tricyclic Antidepressants (Ends in –triptyline or

–pramine)
– Prevents reuptake of NE and 5HT
– Clomipramine (Anafranil)
– Imipramine (Tofranil)
– Nortrptyline (Pamelor)
– Doxepin (Sinequan)
– Protriptyline (Vivactil)
– Desipramine (Norpramin)
– Trimipramine (Surmontil)
– Nortriptyline (Aventyl)
Antidepressants

• Selective Serotonin Reuptake Inhibitors

– Sprecifically block the reuptake of 5HT
– Fluoxetine (Prozac)
– Duloxetine (Cymbalta)
– Citalopram (Celexa)
– Fluvoxamine (Luvox)
– Paroxetine (Paxil)
– Sertraline (Zoloft)
– Escitalopram (Lexapro)
Psychotherapeutics

• Typical Antipsychotics (-zine)

– Chlorpromazine (P)
– Fluphenazine
– Perphenazine
– Thioridazine
– Thiothexene
– Haloperidol
– Molindone
• Blocks dopamine receptors
Psychotherapeutics

• Atypical Antipsychotics (-zapine, -done)

– Clozapine (P)
– Olanzapine
– Quetiapine
– Risperidone
– Ziprasidone
• Blocks both dopamine and serotonin receptors
Adverse Effects of Antipsychotics

• Extrapyramidal signs and symptoms

– Dystonia
– Akathisia
– Pseudoparkinsonism
– Tardive Dyskinesia
– Neuroleptic Malignant Syndrome
Antimanic Drugs

• Lithium as Lithotabs or Lithobid

• Maintain therapeutic levels of 0.6 to 1.2 mEq/L
• Caution on AR if blood levels reachers ≥1.5
mEq/L
– Lethargy, slurred speech, muscle weakness,
tremors, polyuria, ataxia, hyperreflexia, hypotension
CNS Stimulants

• Dextroamphetamine (Dexedrine)
• Dexmethylphenidate (Focalin)
• Metylphenidate (Concerta, Ritalin)
• Modafinil (Provigil)

• Increase release of catecholamines,

increasing stimulation of postsynaptic neurons
Antiepileptic Agents

• Hydantoins (ends in –toin)

– Stabilizes nerve membranes, manipulates Na-K
ions
– Phenytoin (P)
• Barbiturates (ends in –barbital)
• Benzodiazepines (ends in –lam or pam)
• Succinimides (ends in –suximide)
– Modulate GABA
– Ethosuximide (P)
– Methsuximide
Antiparkinsonism Agents

• Anticholinergics
– Benztropine (Cogentin)
– Biperiden (P) (Akineton)
– Diphenhydramine (Benadryl)
– Trihexyphenidyl (Artane)
– Procyclidine (Kemadrin)
• Blocks the action of acetycholine in the CNS to
normalize ACH-Dopa imblance
Antiparkinsonism

• Dopaminergics
– Pramipexole (Mirapex)
– Carbidopa
– Entacapone (Comtan)
– Apomorphine (Apokyn)
– Bromocriptine (Parlodel)
– Pergolide (Permax)
– Selegiline (Eldepryl)
– Levodopa (P)
– Amantadine (Symmetrel)
Narcotics and Antimigraines

• Narcotics
– Reacts with opioid receptors to cause analgesia
– Codeine
– Fentanyl
– Hydrocodone
– Meperidine
– Methadone
– Morphine (P)
– Opium
– Oxycodone
• Narcotic Antagonist
– Binds to opioid receptors but does not activate
them
– Nalmefene
– Naloxone (P)
– Naltrexone
Antimigraine

• Causes vasoconstriction of cranial vessels

• Ergot Derivatives
– Ergotamine
– Dihydroergotamine
• Triptans
– Sumatriptan (P)
– Almotriptan
– Eletriptan
– Naratriptan
– Rizatriptan
Drugs Acting on the Autonomic Nervous
System
• Adrenergic Agents
• Adrenergic Blocking Agents
• Cholinergic Agents
• Anticholinergic Agents
Sympathetic System

• Alpha1 Receptors
– Vasoconstriction
– Increased peripheral resistance
– Pupil dilation
– Thickened salivary secretion
– Closure of urinary sphincter
– Male sexual emission
• Alpha2 Receptors
– Negative feedback control of norepinephrine
– Moderation of insulin release from pancrease
Sympathetic System

• Beta1 Receptors
– Increased heart rate
– Increased myocardial contraction
– Lipolysis in peripheral tissue
• Beta2 Receptors
– Bronchial dilation
– Vasodilation
– Relaxation of uterine muscles
– Decreased GI peristalsis and secretions
– Relaxation of urinary bladder detrusor muscle
Parasympathetic System

• Muscarinic Receptors
– Pupil constriction
– Decreased heart rate
– Increased GI motility and secretions
– Increased urinary bladder contraction
– Male erection
• Nicotinic Receptors
– Muscle contraction
– Release of NE from adrenal medulla
Adrenergic agents

• Alpha and Beta Adrenergic Agonists

– Vasopressor
– Dobutamine
– Dopamine (P)
– Ephedrine
– Epinephrine
• Alpha-Specific Adrenergic Agonists
– Clonidine (Alpha2)
– Phenylephrine
• Beta-Specific Adrenergic Agonists
– Causes bronchodilation
– Albuterol
– Isoproterenol
– Salmeterol
– Terbutaline
Adrenergic Blocking Agents

• Alpha and Beta Adrenergic Blocking Agents

– Amiadarone
– Carvedilol
– Labetalol (P)
• Alpha Adrenergic Blocking Agent
– Phentolamine (P)
• Alpha1 Selective Adrenergic Blocking Agents
– Alfuzosin
– Doxazosin
– Prazosin
• Beta Adrenergic Blocking Agents
– Nadolol
– Pindolol
– Propanolol
– Timolol
• Beta1 Selective Adrenergic Blocking Agents
– Atenolol (P)
– Bisoprolol
– Metroprolol
– Esmolol
Cholinergic Agents

• Direct-Acting Cholinergic Agonists

– Act at cholinergic receptors in the PNS to mimic
effects of ACh- slowed heart rate, decreased
myocardial contractility, vasodilation,
bronchoconstriction, increased GI and urinary
activity, pupil constriction
– Bethanechol (P)
– Carbachol
– Cevimeline
– Pilocarpine
• Indirect-acting Cholinergic Agonists
– Blocks acetylcholinesterase- increases ACh
– For Myasthenia Gravis
• Ambenonium (Mytelase)
• Edrophonium (Tensilon)
• Neostigmine (Prostigmine)
• Pyridostigmine (Mestinon) (P)
– For Alzheimer’s Disease
• Donepezil (Aricept) (P)
• Galantamine (Razadyne)
• Rivastignmine (Exelon)
• Tacrine (Cognex)
• Myasthenic Crisis vs. Cholinergic Crisis
– For myasthenic crisis, give cholinergics
• Give edrophonium, patient gets well
– For cholinergic crisis, withdraw the drug
• Give edrophonium, the patient worsens
• Treat with atropine

• Pralidoxine is an antidote to irreversible

anticholinesterase
Anticholinergic Agents

• Anticholinergics/Parasympatholytics
– Competitively blocks the acetylcholine at the
muscarinic cholinergic receptors to cause
mydriasis, decreased salivation,
– Atropine (P) derived from belladona
– Dicyclomine
– Scopalamine
– Propantheline
• Physostigmine is the antidote for atropine
toxicity
Drugs Acting on the Endocrine System

• Hypothalamic and Pituitary Agents

• Adrenocortical Agents
• Thyroid and Parathyroid Agents
• Antidiabetic Agents
Summary of Hormones

Hypothalamus Anterior Pituitary Target Organ Response

Hormones Hormones
Corticotropin-Releasing Adrenocorticotropic Adrenal corticosteroid
Hormone Hormone hormone
Thyroid-Releasing Thyroid-Stimulating Thyroid hormone
Hormone Hormone
Growth Hormone- Growth Hormone Cell growth
Releasing Hormone
Gonadotropin-Releasing LH and FSH Estrogen and
Hormone Progesterone,
Prolactin-Releasing Prolactin Testosterone
Milk Production
Hormone
Somatostatin Stops GH

Prolactin-Inhibiting Stops Prolactin

Anterior Pituitary Hormones

• Chorionic gonadotropin for male

hypogonadism, induction of ovulation
• Menotropins (Pergonal) stimulate ovulation
and spermatogenesis
• Somatropin** for children with growth failure or
hypopituitarism
Growth Hormone Antagonist

• Inhibits GH release; for hyperpituitarism,

gigantism, acromegaly
• Bromocriptine mesylate
• Octreotide
• Pegvisomant
Posterior Pituitary Hormones

• Antidiuretic Hormone
– Decreases urine production
– For Diabetes insipidus
– Desmopressin
– Vasopressin (P)
Adrenocortical Agents

• Glucocorticoids (ends in –one)

– Mainly anti-inflammatory and for use in adrenal
insufficiency
– Beclomethasone
– Cortisone
– Hydrocortisone
– Prednisone (P)
– Budesonide
– Triamcinolone
• Mineralocorticoids
– Increase sodium reabsorption in renal tubules,
increases potassium and hydrogen excretion
– Fludicortisone (P)
– Cortisone
– Hydrocortisone
• Special Note: Taper the dose gradually
Thyroid Hormone

• Thyroid Replacement Hormones

– Replaces deficient thyroid hormones
– Levothyroxine (P)
– Liothyronine
– Iotrix
• Antithyroid Agents
– Thioamides prevent the formation of thyroid
hormones within thyroid cells
– Propylthiouracil (P) may be given to mothers
– Methimazole
• Iodine Solutions
– Oversaturates iodine and may destroy thyroid cells
– Sodium iodide (I131)
– Lugol’s solution
– Do not give to pregnant women
Parathyroid Hormone

• Antihypocalcemic Agents
– Vitamin D stimulate calcium absorption from the
intestine to restore calcium levels
– Calcitriol (P)
– Dihydrotachysterol
Antihypercalcemic Agents

• Biphosphanates (ends in –dronate)

– slow normal and abnormal bone resorption
– For Paget’s disease and postmenopausal
osteoporosis
– Alendronate (P)
– Etidronate
– Ibandronate
– Pamidronate
– Tiludronate
– WOF esophageal erosion
• Calcitonins
– Inhibit bone resorption; lowers calcium levels;
increases excretion of phosphates, calcium, and
sodium
– Calcitonin (Human; Salmon)
Antidiabetic Agents

• Replacement Insulin
– Given Subcutaneously; Regular insulin may be
given intravenously
– Measure correct dose
– Rotate sites
– Monitor blood glucose level

Time Course Agent Onset Peak Duration

Short-Acting Regular 1 2 4
Intermediate NPH 4 8 16
Long-Acting Ultralente 8 16 32
• Sulfonylureas
– Stimulate beta cells to secrete insulin
– Chlorpropramide (P)
– Tolazamide
– Tolbutamide

– Glimepiride
– Glipizide
– Glyburide (P)
• Biguanide
– Decreases intestinal absorption of glucose
– Decreases hepatic glucose production
– Increases peripheral uptake of glucose
– Metformin (P)
– Does not cause hypoglycemia
• Alpha-Glucosidase Inhibitors
– Delay absorption of glucose
– Miglitol
– Acarbose
• Thiazolidinediones (Ends in –glitazone)
– Increase insulin receptor sensitivity
– Pioglitazone
– Rosiglitazone
• Meglitinides (Ends in –glinide)
– Stimulate insulin release
– Nateglinide
– Repaglinide
New Antidiabetics

• Amylinomimetic Agent
– Delays gastric emptying time
– Pramlintide (Symlyn)
• Incretin
– Enhances insulin secretions; suppresses glucagon
secretion; delays gastric emptying; reduces
appetite
– Exanitide (Byetta) GLP-1
– Sitagliptin (Januvia) Dipeptidyl Peptidase-4 Inhibitor
Drugs Acting on the Reproductive System

• Drugs Affecting the Female Reproductive

System
• Drugs Affecting the Male Reproductive System
Estrogens

• For hormone replacement; palliation of

menopause; also for contraception
• Estradiol (P)
• Conjugated Estrogen
• Estropipate
Progestins

• Used for contraception; prevents FSH and LH

• Medroxyprogesterone (Provera)
• Norethindrone (P)
• Norgestrel
Fertility Drugs

• Induces ovulation
• Clomiphene (P) (Clomid)
• Menotropins (Pergonal)
• Follitropin
• Urofollitropin

• Increased chance of multiple births

Oxytocics

• Stimulates uterine contraction

• Ergonovine (Ergotrate)
• Methyergonovine (Methergine)
• Oxytocin (Pitocin)
• Check BP prior to administration
Tocolytics

• Relaxes uterine smooth muscle

• Ritrodrine (Yutopar)
• Terbutaline
Androgens

• Forms of testosterone; for hypogonadism and

treatment of some breast cancers
• Blocks FSH and LH in women
• Testosterone (P)
• Testolactone
• Donazol
Anabolic Steroid

• Analogs of testosterone; tissue-building

• For muscle wasting; anemia
• Oxandrolone (P)
• Nandrolone
• Oxymetholone
Drugs for Treating Erectile Dysfunction

• Alprostadil acts locally to increase blood flow

to the penis
• Phosphodiesterase-5 inhibitors increase
nitrous oxide levels
– Sildenafil (Viagra)
– Tadalafil (Cialis)
– Verdenafil (Levitra)
Drugs Acting on the Cardiovascular
System
• Drugs Affecting Blood Pressure
• Cardiotonic Agents
• Antiarrhythmic Agents
• Antianginal Agents
• Lipid-lowering Agents
• Drugs Affecting Blood Coagulation
• Drugs to Treat Anemias
Drugs Affecting Blood Pressure

• ACE Inhibitors (Ends in –pril)

– Captopril (P)
– Enalapril
• Angiotensin II Receptor Blockers (Ends in –
sartan)
– Losartan (P)
– Olmesartan
– Valsartan
• Calcium-channel Blockers (Ends in –dipine)
– Diltiazem (P)
– Amlodipine
– Felodipine
– Nicardipine
– Nifedipine
– Verapamil
• Vasodilators
– Hydralazine
– Nitroprusside (P)
Cardiotonic Agents

• Cardiac Glycoside
– Derived from foxglove; increases myocardial
contractility (positive inotropic effect); slows heart
rate (negative chronotropic effect)
– Digoxin (Lanoxin)

– Toxicity: Halos, GI upset, anorexia

– Treat with digoxin immune Fab (Digibind)
Heart Contraction

• Phase 0 – Depolarization
• Phase 1 – Sodium is equal inside and outside
the cell
• Phase 2 – Calcium enters the cell;
Repolarization
• Phase 3 – Potassium flows out of the cell
• Phase 4 – The cell comes to rest
Antiarrhythmics

• Class I (A, B, C) – depress phase 0

– Lidocaine (P)
– Procainamide
• Class II are beta-adrenergic blocking agents –
depress phase 4
– Acebutolol
– Esmolol
– Propanolol
• Class III blocks potassium channels in phase 3
– Amiodarone
– Sotalol (P)
– Bretylium
• Class IV are calcium channel blockers;
prolongs Phase 1 and 2 repolarization
– Verapamil
– Diltiazem (P)
Antianginal

• Nitrates act directly on the smooth muscle to

cause relaxation
– Nitroglycerin (P)
– Isosorbide mononitrate or dinatrate
• Beta-Blockers
• Calcium Channel Blockers
New Drug for Hypertension

• Renin Inhibitor
– Directly inhibits renin which stops the RAAS
pathway
– Aliskiren (P) (Tekturna)
Lipid-Lowering Agents

• Bile acid sequestrans bind with bile acids and

is excreted in the feces.
– Cholestyramine (P)
• HMG-CoA Reductase Inhibitors (Statins)
– Atorvastatin (P) (Lipitor)
– Fuvastatin
– Rosuvastatin
– Simvastatin
• Others: Fenofibrate, Gemfibrozil, Niacin
– Stimulate breakdown of lipoproteins and removal
from plasma
Anticoagulants

• Antiplatelet Drugs
– Inhibit platelet adhesion and aggregation by
blocking receptor sites on the platelet membrane
– Aspirin (P)
– Cilostazol
– Clopidogrel
– Dipyridamole
• Anticoagulants
– Warfarin interferes with Vitamin-K dependent
clotting factors
• Treat toxicity with Vitamin K
– Heparin inhibits conversion of prothrombin to
thrombin and fibrinogen to fibrin
• Treat toxicity with protamine sulfate
– Low-Molecular-Weight Heparin inhibits thrombus
and clot formation by blocking Xa and IIa
Thrombolytics (Ends in –kinase or –plase)

• Activates plasminogen to plasmin – breaks

fibrin threads to dissolve a formed clot
• Give within 6 hours of clot formation
• Urokinase
• Streptokinase
• Alteplase
• Reteplase
• Tenecteplase
Systemic Hemostatic Agents

• Inhibits plasminogen-activating substances

• Aminocaproic Acid
• Tranexamic Acid
Drugs Used to Treat Anemias

• Erythropoietin (for renal failure)

– Stimulate RBC production
– Epoetin alfa (P) (Epogen)
– Darbepoetin alfa
• Iron preparations
– Elevate serum iron concentrations
– Ferrous sulfate (P)
– Ferrous fumarate
– Ferrous gluconate
– Give via Z-Track
• Folic Acid and Vitamin B12
– Essential for cell growth and division RBC
– Folic acid and leucovorin for megaloblastic anemia
– Hycroxycobalamin and cyanocobalamin for
pernicious anemia
Drugs Acting on the Renal System

• Diuretic Agents
• Drugs Affecting the Urinary Tract and Bladder
Diuretic Agents

• Thiazide Diuretic (Mild)

– Blocks chloride pump along with sodium
– Hydrochlorothiazide (P)
• Loop Diuretic (High-ceiling)
– Blocks chloride pump in the Loop of Henle
– Furosemide (P)
– Bumetanide
– Torsemide

• Given for edema states (CHF, hypertension)

• Carbonic Anhydrase Inhibitors
– Blocks carbonic anhydrase; slows production of
aqueous humor
– For glaucoma
– Acetazolamide (P)
– Methazolamide
• Potassium-Sparing Diuretics
– Acts as aldosterone antagonist
– Retains potassium
– Amiloride
– Spirolonactone (P)
– Triamterene
– Avoid high-potassium foods
• Osmotic Diuretics
– Mannitol (P)
– Hyperosmotic volumes
Drugs Acting on the Respiratory System

• Drugs Acting on the Upper Respiratory Tract

• Drugs used to Treat Obstructive Pulmonary
Disorders
Sympathomimetic Decongestants

• Stimulate the alpha-adrenergic receptors of

the nasal mucous membranes, causing
vasoconstriction.
• Ephedrine
• Epinephrine
• Phenylephrine
• Naphazoline
• Oxymetazoline
• Tetrahydrozoline
Antihistamines

• AKA H-1 receptor antagonists, are chemical

agents that react by competing with the
allergy-liberated histmaine for H-1 receptor
sites in the patient’s arterioles, capillaries, and
secretory glands in mucous membranes.
• Take as scheduled
• Sedation is a common side effect.
Antihistamines

Sedating Non-Sedating
• Diphenhydramine • Fexofenadine
• Cyproheptadine • Loratadine
• Clemastine • Desloratadine
• Doxylamine
Mast Cell Stabilizer

• Cromolyn Sodium
• Inhibits the release of histamine and other
mediators of inflammation.
• Used for rhinitis, bronchospasm, and asthma
• Take before being exposed to allergens
• Treat blocked nasal passages first
Expectorants

• Liquefy mucus by stimulating the secretion of

natural lubricant fluids from the serous glands
• Guaifenesin
• Potassium Iodide
• Increase fluid intake
• Humidify the air
Antitussives

• Action: suppresses cough center in the brain

• Examples:
– Codeine – may cause respiratory depression and
constipation
– Dextromethorphan
– Benzonatate
– Diphenhydramine
– Butamirate citrate
Mucolytics

• Dissolves chemical bonds within the mucus

itself, causing it to separate and liquefy,
thereby reducing viscosity
• Acetylcysteine
• Assess breath sounds
• Perform CPT
Beta-Adrenergic Bronchodilating Agents

• Action: Stimulates the beta receptors in the

smooth muscle of the tracheobronchial tree to
relax
• Albuterol
• Salbutamol
• Salmeterol
Anticholinergic Bronchodilating Agent

• Produces bronchodilation by inhibiting

cholinergic receptors on bronchial smooth
muscles blocking the bronchoconstriction
action of vagal effector impulses
• Ipratropium
• Tiotropium
• Do not use if with close-angle glaucoma
• Instruct use of MDI
Xanthine Derivatives

• Act directly on the smooth muscle of the

tracheobronchial tree to dilate the bronchi
• Aminophylline
• Theophylline – monitor blood levels ( 10 – 20
mg/L)
Corticosteroids

• Action: Directly affects smooth muscle

relaxation; enhances the effect of beta-
adrenergic bronchodilators and inhibit
inflammation
• Beclomethasone
• Budesonide
• Fluticasone
• Do not give if with active infections (fungal)
Antileukotriene Agents

• Action: selective and competitive receptor

antagonist of the cysteinyl leukotriene receptor
• Montelukast
• Zafirlukast
• Not used for acute episodes
Immunomodulator Agent

• Omalizumab binds to circulating IgE

• Do not give to children below 12 years
• Administer as ordered
• Caution: Anaphylaxis is possible
Drugs Acting on the Gastrointestinal
System
• Drugs Affecting Gastrointestinal Secretions
• Laxative and Antidiarrheal Agents
• Emetic and Antiemetic Agents
Antacids

• Lowers the acidity of gastric secretions by

buffering hydrochloric acid – buffers acidity
• Aluminum hydroxide – causes constipation
• Magnesium hydroxide – causes diarrhea
• Calcium carbonate
Histamine-2 Receptor Antagonists (Ends
in –tidine)
• Blocks H2 receptors on the surface of gastric
parietal cells resulting in decreased volume of
acid secreted
• Cimetidine
• Ranitidine
• Famotidine
• Nizatidine
• Best taken before eating
Proton Pump Inhibitors (Ends in –prazole)

• Inhibits gastric acid secretion by inhibiting the

gastric acid pump of the stomach’s parietal
cells
• Omeprazole
• Lansoprazole
• Esomeprazole
• Pantoprazole
• Rabeprazole
• Best taken before meals
• Capsules and tablets are swallowed whole
Gastrointestinal Prostaglandins

• Inhibits gastric acid and pepsin secretion to

protect the stomach and duodenal lining
against ulceration
• Caution: may stimulate uterine contraction
• Illegally used as an abortifacient
• Misoprostol (Cytotec)
Antipeptics (Coating agents)

• Sucralfate forms a complex that adheres to the

crater of an ulcer, protecting it from
aggravators such as acid, pepsin, and bile
salts.
• Give 1 tablet before each meal and at bedtime
Prokinetic Agents

• Metoclopramide is a gastric stimulant that

strengthens the lower esophageal sphincter
pressure; increases peristalsis; relaxes the
pyloric sphincter
• Also an antiemetic which block dopamine and
serotonin in the chemoreceptor trigger zone
• May cause EPS, treat wit diphenhydramine
Antispasmodics

• Are anticholinergics
• Decreases peristalsis and secretions of
hydrochloric acid, pepsin, and bile
• Examples:
– Atropine, belladona, dicyclomine, scopalamine,
methscopalamine
• Check for other diseases (asthma, prostatic
enlargement, glaucoma)
• Administer with food or milk
Dopamine Antagonists

• Phenothiazines, butyrophenones, and

metoclopramide – inhibit dopamine receptors
that are part of the pathway to the vomiting
center
• May cause EPS
• Examples:
– Phenothiazines (chlorpromazine, promethazine,
prochlorperazine)
– Butyrophenones (haloperidol, droperidol,
trimethobenzamide)
Serotonin Antagonists

• Blocks serotonin receptors (5-HT3 type in the

CTZ and GIT)
• Dolasetron
• Granisetron
• Ondansetron
• Palonosetron
Anticholinergic Agents

• Counters acetylcholine at the CTZ and VC by

cholinergic nerves receiving impulses from the
vestibular network.
• Cyclizine
• Diphenhydramine
• Hydroxyzine
• Meclizine
Corticosteroids

• Dexamethasone and methylprednisolone can

be effective antiemetics
• Do not use long-term
Benzodiazepines

• Acts through: sedation, reduction in anxiety,

possible depression of the vomiting center,
and amnesic
• Lorazepam
• Midazolam
• Diazepam
Cannabinoids

• Active ingredient: Tetrahydrocannabinol

• Acts by inhibiting pathways to the VC
– Dronabinol (CIII)
– Nabilone (CII)
– Levonantradol
• Potential for abuse
Neurokinin-1 Receptor Antagonists

• Substance P is a neuropeptide is found in high

concentrations in the area of the CNS
responsible for vomiting, and it coexists with
serotonin in the enterochromaffin cells and
vagal afferent nerves of the GIT
• Aprepitant, is a selective NK1 antagonist that
blocks the effects of substance P
Emetic

• Syrup of Ipecac stimulates the CTZ and

induces vomiting within 20 minutes
• Given to children who may have ingested
poisons
Constipation

• a symptom-based disorder of unsatisfactory

defecation and is characterized by infrequent
stools, difficult stool passage, or both.
• Chronic constipation – 3 months
• Caused by improper diet, too little residue or
too little fluid, lack of exercise and sedentary
habits, failure to respond to defecation
impulses, colon muscle weakness, anemia,
hypothyroidism, medicines, tumors, rectal
diseases
Management of Constipation

• I – Increased…
• T – Tubig
• E – Exercise
• L – Lamon ng high fiber

• Laxative
Diarrhea

• Is the increase in the frequency or fluid content

of bowel movements
• Caused by intestinal infections; spicy or fatty
foods; enzyme deficiencies; excessive use of
laxatives; drug therapy; emotional stress;
hyperthyroidism; inflammatory bowel disease;
surgical bypass of the intestine
Management of Diarrhea

• B – Banana
• R – Rice
• A – Applesauce
• T – Toast
• Y - Yogurt
Stimulant Laxatives

• Acts directly on the intestine, causing irritation

that promotes peristalsis and evacuation
• Bisacodyl
• Sennosides
Osmotic Laxatives

• Are hypertonic compounds that draw water

into the intestines from surrounding tissue
• Lactulose
• Sorbitol
• Polyethylene glycol
• Glycerin
Saline Laxatives

• Are hypertonic compounds that draw water

into the intestine from surrounding tissue
• Magnesium hydroxide, magnesium sulfate,
magnesium citrate, sodium phosphates
Lubricant Laxatives

• Lubricate the intestinal wall and soften the

stool
• Mineral oil
Bulk-Forming Laxative

• Causes water to be retained within the stool,

thus increasing bulk
• Psyllium
• Calcium polycarbophil
• Methylcellulose
• Wheat bran
Stool Softeners

• AKA wetting agents

• Draws water into the stool, causing it to soften
• Docusate calcium
• Docusate sodium
Opioid Antagonist

• Mythylnaltrexone is a mu-opioid receptor

antagonist that binds to opioid receptors in the
GIT, inhibiting the constipation producing
effects of opioid drugs
Locally-Acting Antidiarrheal

• Acticated charcoal, pectin, and psyllium

absorb excess water to cause a formed stool
and to adsorb irritants or bacteria that are
causing the diarrhea
• Bismuth subsalicylate acts to stop secretion of
fluids into the GIT; also has antimicrobial
properties
Systemic Antidiarrheal Agents

• Acts through the autonomic nervous system to

reduce peristalsis and motility of the GIT
• Diphenoxylate
• Loperamide
• Difenoxin with atropine
• Opium
Probiotics As Antidiarrheals

• Lactobacillus acidophilus
Recolonizes the GIT to counter the presence of
pathogenic microorganisms