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Pharmacology

Drug Fundamentals, Plus the Most Frequently Prescribed Drug Classifications—Including Indications, Reactions, Examples & More

definitions

pharmacokinetics

pharmacodynamics Study of the mechanisms of action of drugs within

the body and how drugs produce their effects in the body

pharmacogenetics Study of drug reactions in the body that are

unanticipated or unusual, and may have a hereditary basis for the response

pharmacokinetics Study of drug actions as they move through the

body; the way the body absorbs, distributes, metabolizes and excretes

drugs; mathematical study of drugs based on time and dose

pharmacology Study of biologically active compounds, how they react

in the body and how the body reacts to them

pharmacotherapeutics Study of drugs used to prevent, treat or

diagnose disease

pharmacy Preparation and dispensing of drugs

toxicology Study of harmful or poisonous effects of drugs

Routes drugs take to get into the body

• Enteral:

o Enters the body through the GI tract

o Taken by mouth, through the rectum, under the tongue or held in the cheeks

• Parenteral:

o Enters the body through a different means (i.e., other than the GI tract)

o Can be injected into the veins, arteries, muscles, spinal cord, or under

the skin; inhaled through the lungs; transdermally through the skin via

ointment or patch

Absorption

• Bioavailability Percent absorbed into systemic circulation after administration

o Bioavailability depends on route of administration as well as the

drug’s ability to cross membranes and reach its target

o First Pass Effect:

n Drugs absorbed through the stomach and small intestine must pass

through the liver before circulating systemically

n Liver can inactivate the drug, making less of the drug available to

reach the target organ

• Absorption at cellular level occurs through passive transport, active

transport, pinocytosis and facilitated diffusion

Distribution

• Influenced by several factors:

o Tissue permeability: Ability of drug to pass through the membranes

rapidly affects the extent to which the drug moves around in the body

o Blood flow: Once in the blood stream, will get to the organs and

tissues that are highly perfused

o Plasma proteins binding: Drug can bind to a protein that will render

the drug inactive; only an unbound drug can attach to the receptors

o Binding to subcellular components

o blood pH

Drug Storage Sites

• Adipose tissue Primary site; lipid-soluble; drugs tend to remain for long

periods of time due to low metabolic rates of drugs and poor blood

perfusion of tissue

• Bone Toxic agents like heavy metals

• Muscle Binding can cause muscle to store drugs

• Organs Liver and kidneys

Metabolism

• Biotransformation Chemical changes that occur in the drug following

administration

• Metabolite Altered version of the chemical compound

• Can have a higher or lower rate of activity than the original drug; if

higher, drug is given as an inactive or prodrug form

• Prodrug Requires metabolism or activation of drug in order for it to act

within the body

Excretion

• First order Rate of removal of drug from the body is proportional to the

concentration of the drug in the plasma

• Half-life Time required to decrease the blood levels of a drug by one-half

• A one-time drug dosage will be eliminated almost completely by 5

half-lives

• A drug given on a continuous dosage schedule will reach steady state

concentration after 5 half-lives

• Steady state Rate of drug administration is equal to the rate of drug excretion

• Organs that excrete drugs Kidneys, lungs, sweat glands, mammary

glands, salivary glands, skin and GI tract

drug names

DRUG

Chemical Name

Generic Name

Trade Name

Chemical Name: Scientific

name, describes the atomic

and molecular structure of

a drug

Generic Drug: Nonpro-

prietary name, abbreviation

of the chemical name

Brand Name: Trade

name, selected by the

pharmaceutical company

that made the drug

pharmacodynamics

Receptors

• Protein molecules with one or more binding sites, located on cell

membranes

• Receive a signal from the body’s chemicals: neurotransmitters,

hormones, enzymes

• Signal will cause a molecular event on the inside of the cell to occur

• Drugs Enhance ( agonist ), diminish ( partial agonist ) or block ( antagonist )

the generation, transmission or receiving of the signal

• Affinity Attraction between a drug and a receptor

• High affinity Drug will bind easily to the receptor

• Low affinity Requires a higher concentration of the drug to get a

therapeutic response

Drug Potency

• Amount of drug required to produce a therapeutic response

Dose Response Curve

• Effective Dose (ED) Amount of drug that produces a therapeutic

response in 50 % of the people taking it

• Toxic Dose (TD) Amount of drug that produces adverse effects in 50 %

of the people taking it

• Therapeutic Index (TI) Margin of safety; ratio between the TD and

the ED

• The higher the TI, the safer the drug is considered to be; in general,

nonprescription drugs have much higher TIs than prescription drugs

schedule drugs

Schedule Class

Characteristics

Examples (C-I to C-IV)

Schedule 1: C-1

Schedule 2: C-II

• High abuse potential; not legal; no acceptable medical use; no prescriptions available

• High abuse potential and severe dependence liability; current, accepted medical

use; prescription drug-signed; not stamped prescription; 30-day supply, no refills

• Less abuse potential; low-moderate physical dependence; high psychological

dependence; by prescription only, expires within 6 months; max. 5 refills on one

script

• Less abuse potential than C-III drugs; accepted medical use; limited physical and

psychological dependence; written or verbal prescription, expires in 6 months;

max. 5 refills on one script

• Limited abuse potential; accepted medical use; small amounts of narcotics used as

antitussives (cough medicine) or antidiarrheals; may not need a prescription but

must be recorded as a transaction

• Heroin, LSD, cocaine,

marijuana, methaqualone

• Opium, morphine, coca,

methadone

• Amphetamines, codeine,

barbiturates, Valium, Xanax,

anabolic steroids

• Chloral hydrate, meptro-

bamate, paraldehyde,

phenobarbital

Schedule 3: C-III

Schedule 4: C-IV

Schedule 5: C-V

Pharmaceutical Cllassiifiicatiions

adrenergics

Common drug examples:

• Doxazosin mesylate Cardura

• Prozosin hydrochloride Minipress

• Tamsulosin hydrochloride Flomax

• Terazosin hydrochloride Hytrin

Mimic naturally occurring catecholamines (epinephrine, norepinephrine

and dopamine) or stimulate the release of norepinephrine

Indications Alpha-adrenergic agonists used to treat hypotension

Common drug examples:

• Norepinephrine Lovophed

• Pseudoephedrine Cenafed, Dimetapp, Sudafed, Triaminic DM (OTC

used to treat other conditions)

Adverse reactions Orthostatic hypotension, headache, palpitations,

fatigue, nausea, weakness, dizziness, fainting

aminoglycosides

Adverse reactions: Increased blood pressure, AV block; other effects

include: nausea, vomiting, sweating, goose bumps, rebound miosis,

difficulty in urinating, headache, dilated pupils, photophobia, burning,

stinging and blurry eyes

Beta 1 adrenergic agonists Bradycardia, low cardiac output, paroxysmal

atrial or nodal tachycardia, ventricular fibrillation, cardiac output

Indications:

• Treat infections resistant to penicillin, septicemia, urinary tract

infections, infections of skin, soft tissue and bone, gram-negative

bacillary meningitis

• Used in combination with other antibiotics to treat staphylococcal

infections, endocarditis, tuberculosis, pelvic inflammatory disease

Common drug examples:

• Dobutamine hydrochloride Dobutrex

Common drug examples:

• Amikacin sulfate Amikin

• Gentamicin sulfate Cidonycin, Gentasol

• Neomycin sulfate Mycifradin

Adverse reactions Tachycardia, palpitations and other arrhythmias,

premature and ventricular contractions, tachyarrhythmias and

myocardial necrosis

Beta 2 adrenergic agonists Acute and chronic bronchial asthma,

emphysema, bronchitis, acute hypersensitive (allergic) reaction to drugs,

delays delivery in premature labor, dysmenorrhea

Adverse reactions Systemic ototoxicity and nephrotoxicity, skeletal

weakness and respiratory distress; oral meds can cause nausea,

vomiting, diarrhea; local injections can cause phlebitis and abscess

Common drug examples:

• Albuterol sulfate Proventil, Ventolin, Volmax

• Bitolterol mesylate Tornalate

• Metaproterenol sulfate Alupent

• Pirbuterol acetate Maxair

• Salmeterol xinafoate Serevent

• Terbutaline Brethine, Bricanyl

androgens

Testosterone used to promote maturation of male sex organs and

development of secondary sex characteristics; promotes retention of

calcium, nitrogen, phosphorus, sodium, and potassium; enhances anabolism

Indications Androgen deficiency resulting from testicular failure or

deficiency of pituitary origin, palliative for metastatic breast cancer,

postpartum breast engorgement, hereditary angioedema, endometriosis,

fibrocystic breast disease

Adverse reactions Nervousness, tremors, headaches, tachycardia,

palpitations, hypertension, nausea, vomiting, cough

Dopamine Improves blood flow to the kidneys; used in acute renal failure,

heart failure and shock

Common drug examples:

• Danazol Cyclomen, Danocrine

• Fluoxymesterone Halotestin

• Testosterone Testopel pellets

Common drug examples:

• Dopamine hydrochloride Intropin

Adverse reactions:

• Extensions of hormonal action

o Males: Frequent and prolonged erections, bladder irritability,

gynecomastia

o Females: Clitoral enlargement, deepening of the voice, facial or

body hair growth, unusual hair loss, irregular or absent menses

• Metabolic reactions Fluid and electrolyte retention, hypercalcemia,

decreased blood glucose level, increased serum cholesterol, hepatic

dysfunction

Adverse reactions Headaches, ectopic beats, tachycardia, hypoten-

sion, bradycardia, nausea, vomiting, hyperglycemia, asthma attacks,

anaphylactic reactions

adrenocorticoids

Glucocorticoids Regulate carbohydrate, lipid and protein metabolism;

block inflammation; regulate body’s immune response

Indications Asthma, advance pulmonary tuberculosis, pericarditis,

acute and chronic inflammation, adrenal insufficiency, antenatal use in

preterm labor, hypercalcemia, cerebral edema, acute SCI, MS, shock

Contraindicated Men with breast or prostatic cancer or symptomatic

prostrate hypertrophy, patients with severe cardiac, renal or hepatic

disease or with undiagnosed genital bleeding

Common drug examples:

• Betamethasone Beclovent, QVAR, Vanceril

• Hydrocortisone Cortet, Hycort

• Methylprednisone Medrol, Meprolone, Metacort

• Prednisone Apo-prednisone, Deltasone, Meticort, Orasone, Sterapred

• Triamcinolone Azmacort, Nasacort

angiotensin-converting enzyme iinhiibiitors

Indications Treat high blood pressure and heart failure

Common drug examples:

• Benazepril hydrochloride Lotensin

• Captopril Capoten

• Enalapril maleate Vasotec

• Fosinopril sodium Monopril

• Lisinopril Prinvil, Zestril

Adverse reactions Primarily a catabolic effect on muscle, bone,

ligament, tendon; suppression of hypothalamic-pituitary-adrenal

pathway; Cushingoid syndrome with long-term use; other effects

include euphoria, insomnia, psychotic behavior, pseudotumor, mental

changes, nervousness, restlessness, heart failure, hypertension, edema,

acute tendon ruptures, delayed wound healing

• Withdrawal symptoms if drugs stopped abruptly Fever, myalgias,

arthralgias, malaise, nausea, orthostatic hypotension, dizziness,

fainting, dyspnea, hypoglycemia

Mineralocorticoid Regulates electrolyte homeostasis

Adverse reactions Persistent dry cough, skin rash, loss of taste,

weakness, headaches, palpitations, fatigue, proteinuria, hyperkalemia

angiotensin II receptor antagoniists

Vasodilates arterioles by blocking the effects of angiotensin II, enhance

renal clearance of sodium and water

Indications Treatment of high blood pressure

Indications Adrenal insufficiency, orthostatic hypotension in diabetics

Common drug examples:

• Candesartan cilexetil Atacand

• Eprosartan mesylate Teveten

• Irbesartan Avapro

• Losartan potassium Cozaar

• Telmisartan Micardis

• Valsartan Diovan

Common drug examples

• Fludocortisone acetate Florinef

Adverse reactions Salt and water retention, hypertension, cardiac

hypertrophy, edema, heart failure, bruising, diaphoresis, urticaria, allergic

rash, hypokalemia

[ Note: All adrenocorticoid drugs have both glucocorticoid and mineralo-

corticoid properties to some extent]

Adverse reactions Dizziness, anxiety, confusion, cough, upper

respiratory infections, myalgia, insomnia, hypotension, visual

changes, GI/GU effects

alpha-adrenergic bllockers

anticholinergics

Lower blood pressure by dilating peripheral blood vessels, reducing

peripheral resistance

Indications:

• Spastic conditions including Parkinson’s disease, muscle dystonia,

muscle rigidity and extra-pyramidal disorders

Indications Raynaud’s disease, acrocyanosis, frostbite, phlebitis, diabetic

gangrene, hypertension, benign prostatic hyperplasia

Pharmaceutical Classifications ( continued )

• Prevent nausea and vomiting from motion sickness, adjunctive

treatment for peptic ulcers and other GI disorders, bronchospasms,

and GU tract disorders

• Treat poisoning from certain plants and pesticides

• Use preoperatively to decrease secretions and block cardiac reflexes

Common drug examples:

• Amobarbital Amytal

• Phenobarbital Bellatal, Solfoton

• Primidone Mysoline

• Secobarbital sodium Seconal

Common drug examples:

• Antiparkinsonians:

o Benztropine mesylate: cogentin

• Belladonna alkaloids:

o Scopolamine hydrobromide: IsoptoHyoscine, Scopace

• Synthetic quaternary anticholinergics:

o Glycopyrroltae: Robinul

• Tertiary synthetic and semisynthetic derivatives:

o Dicyclomine hydrochloride: Antispas, A-spas, Dibent, Dilomine,

Lomine, Ortyl

Adverse reactions Drowsiness, lethargy, vertigo, headaches and CNS

depression, hypersensitivity can occur (rash, fever)

• After hypnosis hangover effect, impaired judgment, mood distortion,

rebound insomnia

• Geriatric patients Confusion

• Pediatric patients Hyperactivity

benzodiazepines

Enhance/facilitate actions of the gamma-aminobutyric acid (GABA)

Indications Seizure disorders, anticonvulsants, anxiety, tension and

insomnia, surgical adjuncts for conscious sedation or amnesia,

skeletal muscle spasms or tremors, delirium, schizophrenia as an adjunct,

nausea and vomiting induced by chemotherapy, neonatal opiate withdrawal

Adverse reactions Dry mouth, decreased sweating, headache, dilated

pupils, blurred vision, dry skin, urinary hesitancy and urine retention,

constipation, palpitations and tachycardia; other peripheral effects

include dry mucous membranes, dysphasia, stupor, seizures,

hyperthermia, hypertension and increased respiration

• Toxic doses May cause disorientation, confusion, hallucinations,

delusions, anxiety, agitation and restlessness

Common drug examples:

• Alprazolam Alprazolam, Xanax

• Chlordiazepoxide Libritab

• Clonazepam Klonopin, Rivotril

• Clorazepate dipotassium Catapres, Dixarit

• Diazepam Valium, Zetran

• Estazolam ProSom

• Flurazepam Apo-Flurazepam, Dalmane

• Lorazepam Apo-Lorazepam, Ativan

• Midazolam Versed

• Oxazepam Apo-Oxazepam, Serax

• Temazepam Restoril

• Triazolam Halcion

anticoagulants

Indications Prevent clot formation in patients with DVTs and pulmonary

embolism, provide anticoagulation during hemodialysis, prevention of

postoperative clot formation after surgery, decrease risk of strokes,

decrease risk of MI in patients with atherosclerosis

Common drug examples:

• Danaparoid Orgaran

• Delteparin Fragmin

• Enoxaparin Lovenox

• Heparin Heparin Lock Flush, Hep-lock

• Tinzaparin Innohep

Adverse reactions Drowsiness and impaired motor function; constipa-

tion, diarrhea, vomiting, changes in appetite, urinary alterations,

nightmares, hallucinations, insomnia

• Toxic effects Visual disturbances, short-term memory loss, vertigo,

confusion, severe depression, shakiness, slurred speech, staggering,

bradycardia, difficulty breathing

Adverse reactions Insomnia, headache, dizziness, confusion, peripheral

edema, nausea, constipation, pain, fever, vomiting, joint pain, rash

antihistamines

beta bllockers

Indications Allergies, pruritis, vertigo, nausea and vomiting, sedation,

suppression of cough, dyskinesia

Reduce the workload of the heart by blocking the sympathetic conductance

at the beta receptors on the SA node and myocardial cells, thus decreasing

the force of contraction and causing a reduction in heart rate

Common drug examples:

• Allergies:

o Azelastine hydrochloride: Astelin, Optivar

o Chlopheniramine maleate: Aller-Chlor, Chlor-Trimeton, Chlor-Tripolon

o Clemastine fumarate: Tavist

o Diphenhydramine hydrochloride: Allergy DM, Benadryl, Diphen,

Dormin, Midol PM, Nytol, Sominex, Twilite

o Promethazine hydrochloride: Anergan 50, Phenergan

• Pruritus:

o Cyproheptadine hydrochloride: Periactin

o Hydroxyzine hydrochloride: Anxanil, Atarax, Multipax, Quiess, Vistacon

• Vertigo, nausea, vomiting:

o Cyclizine hydrochloride: Marezine

o Cyclizine lactate: Marezine, Marzine

o Dimenhydrinate: Dimetab, Hydrate, Triptone

o Meclizine hydrocholoride: Antivert, Antrizine, Bonine, Vergon

o Promethazine hydrochloride: Anergan, Phenergan

• Sedation:

o Diphenhydramine: Diphenhydramine syrup

• Cough suppression:

o Diphenhydramine syrup

• Dyskinesia:

o Diphenhydramine

Indications Hypertension, angina, arrhythmias, glaucoma, myocardial

infarction, migraine prophylaxis

Common drug examples:

• Beta 1 Blockers:

o Acebutolol: Sectral

o Atenolol: Tenormin

o Betaxolol hydrochloride: Betoptic, Kerlone

o Bisoprolol fumarate: Zebeta

o Esmolol: Brevibloc

o Metoprolol tartrate: Lopressor

• Beta 1 & 2 Blockers:

o Carteolol: Cartrol, Ocupress

o Carvedilol: Coreg

o Labetalol hydrochloride: Normodyne, Trandate

o Levobunolol hydrochloride: AKBeta, Betagen

o Metipranolol hydrochloride: Opti Pranolol

o Nadolol: Corgard

o Pindolol: Visken

o Propranolol: Inderal

o Sotalol: Betapace

o Timolol maleate: Blocarden, Timoptic

Adverse reactions Insomnia, nausea, fatigue, slow pulse, weakness,

increased cholesterol and blood glucose levels, bradycardia,

depression, hallucinations, sexual dysfunctions, skin hyperpigmentation

• Toxic effects Severe hypotension, bradycardia, heart failure,

bronchospasms

Adverse reactions Drowsiness and impaired motor function; anticholinergic

action will cause dry mouth and throat, blurred vision and constipation

• Toxic effects Sedation, reduced mental alertness, apnea, cardiovas-

cular collapse, hallucinations, tremors, seizures, dry mouth, flushed

skin, and fixed, dilated pupils; (reverses when drug is withdrawn)

bile aciid sequestrants

anxiolytic skeletal musclle rellaxant

Indications Lowering cholesterol

Indications Anxiety, muscle spasm, tetanus, acute alcohol withdrawal,

adjunct for epilepsy

Common drug examples:

• Cholestyramine Locholest, Prevalite, Questran

• Colesevelam Welchol

• Colestipol Colestid

Common drug examples:

• Diazepam Apo-Diazepam, Valium

Adverse reactions Drowsiness, slurred speech, tremor, fatigue,

ataxia, headache, insomnia, hypotension, bradycardia, nausea,

constipation, joint pain, physical or psychological dependence

Adverse reactions Headache, anxiety, vertigo, dizziness, insomnia,

fatigue, syncope, tinnitus, constipation, nausea, vomiting, anemia,

muscle and joint pain

barbiturates

calcium channell bllockers

Indications Seizure disorders (tonic-clonic and partial seizures),

sedation, hypnosis, preanesthesia sedation, psychiatric use

Relaxes smooth muscle to provide vasodilation and affects cardiac muscle

to reduce HR and SV

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