Introduction to Pharmacology Pharmacology • the study of science of drugs Drug • any chemical that affects the processes of a living

organism I. Drug sources: a. b. c. d. II. Drug uses: • prevent diseases • treat diseases • diagnose diseases • prevent pregnancy • maintain health III. Drug names  Chemical name o the drug’s chemical composition and molecular structure o ex.( +/- ) – 2 – ( p-isobutylphenyl ) proponic acid  Generic Name ( Nonproprietary name ) o name given by the United States Adopted Name Council o universally accepted o ex.ibuprofen  Trade Name ( Brand name/ Proprietary name) o the drug has a registered trademark ; use of the name restricted by the drug’s owner o ex. Motrin IV. Drug Standards: • same drug name must have same strength, quality & purity • based on United States Pharmacopeia and National Formulary (USP-NF) V. Drug references: • American Hospital Formulary Service (AHFS) Drug Information • Physicians’ Desk Reference (PDR) • Package inserts • Drug Facts and Comparisons • Saunders/ Lipincott’s Nursing Drug Guide • Journals • Internet

plants animals minerals chemical synthesis/ biogenetic engineering

VI. Phases of Drug Development 1. Preclinical trial 2. Phase 1 3. Phase 2 4. Phase 3 5. Phase 4

VII. Legal Regulation A. Food and Drug Administration (FDA) Pregnancy Categories: Category A Category B Category C Category D Category X  no risk to fetus  no risk in animal fetus; no human studies available  adverse effects to animal fetus; no human studies available  possible fetal risk in humans reported  fetal abnormalities reported; + evidence of fetal risk in animal/& human studies.

B. Controlled Substances:  controlled substances  OTC drugs

 prescription drugs  orphan drugs  dependence Drug Enforcement Agency (DEA) Schedules of Controlled Substances: Schedule I Drugs • high potential for abuse • used for research only • ex. heroin, marijuana, lysergic acid diethylamide (LSD) Schedule II Drugs • high abuse potential • severe physical & psychologic dependence • acceptable medical use, with restrictions • ex. amphetamines, cocaine, mepiridine (Demerol) , morphine, anabolic steroids Schedule III Drugs • moderate potential for abuse • psychological dependence , low physical dependence • acceptable medical use, by prescription only • ex. secobarbital (Seconal), Tylenol with codeine Schedule IV • low potential for abuse • limited physical & psychological dependence • ex. diazepam (Valium), phenobarbital, chlordiazepoxide (Librium) Schedule V • low potential for abuse • acceptable medical use • OTC narcotic drugs, sold only by registered pharmacists: buyer must be 18yo • Ex. cough syrups with codeine eg. Guaifenesin, diphenoxylate HCL with atropine ( Lomotil)

Pharmacologic Principles I. Drug Action:  Pharmaceutics  Pharmacokinetics  Pharmacodynamics II. Drug Effect:  Pharmacotherapeutics Pharmaceutics • the study of how various drug forms influence pharmacokinetic and pharmacodynamic activities. o disintegration o dissolution Pharmacokinetics • the study of what the body does to the drug: o Absorption o Distribution o Metabolism or biotransformation o Excretion or elimination Pharmacodynamics • the study of what the drug does to the body : o the mechanism of drug action in living tissues. Pharmacotherapeutics • the use of drugs and the clinical indications for drugs to prevent and treat diseases. Pharmacognosy • the study of natural ( plant and animal ) drug sources. I. The 3 Phases of Drug Action: A. Pharmaceutic Phase 1. disintegration 2. dissolution  Rate limiting – time it takes for drug to disintegrate & dissolve to be absorbed by the body B. Pharmacokinetic Phase 1. Absorption:

• passage of a drug into the bloodstream from site of administration  Processes of drug absorption:  passive absorption  active absorption  pinocytosis  Drug absorption of Oral Preparations: Liquids, elixirs, syrups Fastest Suspension solutions Powders Capsules Tablets Coated tablets Enteric-coated tablets Slowest  The rate at which the drug leaves its site of administration, and the extent to which absorption occurs.  Bioavailability  Factors that affect absorption :  solubility of drug  food or fluids administered with the drug  dosage formulation  status of the absorptive surface  rate of blood flow to the small intestine  acidity of the stomach  status of GI motility  administration route of drug  Routes : • a drug’s route of administration affects the rate and extent of absorption of the drug. o Enteral o Parenteral o Topical  Enteral Route • drug is absorbed into the systemic circulation through the oral or gastric mucosa, the small intestine, or rectum. o oral o sublingual* o buccal o rectal  Parenteral Route • Intravenous * • Intramuscular • Subcutaneous • Intradermal

• Intrathecal • Intraarticular  Topical Route • skin ( including transdermal patches ) • eyes, ears & nose • lungs ( inhalation )* • vagina First – Pass Effect • the metabolism of a drug and its passage from the liver into the circulation.  A drug given via the oral route may be extensively metabolized by the liver before reaching the systemic circulation ( high first – pass effect ).  The same drug – given IV – bypasses the liver, preventing the first – pass effect from taking place, the more drug reaches the circulation. • Routes that bypass the liver : o sublingual o buccal o rectal* o intravenous o intranasal transdermal vaginal intramuscular subcutaneous inhalation

2. Distribution • transport of a drug by the bloodstream to its site of action  Factors affecting drug distribution: • protein-binding • water soluble vs fat soluble • areas of rapid distribution o heart, liver, kidneys, brain • areas of slow distribution o muscle, skin, fat 3. Metabolism or biotransformation • the transformation of a drug into an inactive metabolite, a more soluble compound or a more potent metabolite  liver*  others: kidneys, lungs, plasma ,intestinal mucosa  Factors that decrease metabolism: • cardiovascular problem • renal problem • starvation • liver problem • erythromycin or ketoconazole drug therapy

 Factors that increase metabolism: • nicotine • alcohol • barbiturates & glucocorticoids • rifampin therapy  Half-life o time it takes for one half of the original amount of a drug in the body to be removed. o a measure the rate at which drugs are removed from the body 4. Excretion • elimination of drugs from the body  kidneys*  others: lungs, exocrine glands (sweat, salivary or mammary glands), skin & intestinal tract C. Pharmacodynamics Phase  Onset of Action • time it takes for the drug to elicit a therapeutic response  minimum effective concentration (MEC)  Peak Action • time it takes for drug to reach its maximum therapeutic response  Duration of Action • the time a drug concentration is sufficient to produce its therapeutic response  Receptor Theory • most receptors are found on cell membrane • drug binding occurs on receptors • lock & key interaction :  Agonist & antagonist: Agonists • drugs that attracts to receptors  stimulate/ enhance a response • ex. Insulin, isoproterenol – stimulate beta 1 receptor Antagonists • drugs that attracts to receptors  block a response • ex. cimetidine – blocks H2 receptor  Nonspecific & Nonselective Drugs Nonspecific Drugs • affect various sites of the body

ex. Bethanecol  stim. cholinergic receptor  strengthen bladder contraction,increases HR, decreases BP, bronchiole & pupil constriction

Nonselective Drugs • affect various receptors • ex. Epinephrine  acts on alpha1, beta 1 & 2 receptors

 Categories of drug action: a. depress cellular activities b. stimulates cellular activities c. inhibit or kill organisms d. act as substitute for missing chemicals

 Therapeutic Index & therapeutic Range: Therapeutic Index (TI) • relationship bw the drug’s therapeutic effects & its adverse effects TI= LD50 ED50 • • High TI  wide margin of safety Low TI  narrow margin of safety

Therapeutic Range (therapeutic window) • drug concentration bw therapeutic effect & toxic effect • Ex. Digoxin = 0.5 to 2 ng/ml  Peak & Trough Level Peak drug level

• •

highest plasma concentration of drug at a specific time indicate rate of absorption

Trough level • lowest plasma concentration • indicate rate of elimination  Loading dose • large initial dose given for immediate response. • given to achieve a rapid minimum effective concentration. • Ex. Digoxin (digitalization)

II. Pharmacotherapeutics • use of drugs to treat disease. A. Types of Therapies: 1. acute therapy • px is critically ill & requires immediate intensive therapy 2. empiric therapy • based on practical experience rather than on pure scientific data 3. maintenance therapy • chronic conditions that don’t resolve 4. supplemental or replacement therapy • replenish or substitute missing substances in the body 5. supportive therapy • doesn’t treat the cause of disease but maintains other threatened body systems until the patient’s condition resolve. 6. palliative therapy • used for end-stage or terminal diseases to make the patient as comfortable as possible

Drug Effects:  Main effect • desired therapeutic effect • reason drug is administered  Side effects • physiologic effects that are not related to desired drug effects • expected, well-known reactions that result in little or no change in patient intervention

 Adverse Reactions • more severe than side effects • undesirable & unexpected effects occurring even at normal dose  Local vs Systemic drug effect  Placebo Effect • a therapeutic effect that results from a patient’s belief in the benefits of a medication

 Factors affecting Drug Effects: • Age • Size • Sex • Genetic factors • Disease conditions • Emotional conditions • Route of administration • Time of day • Drug taking history • Environmental conditions • Drug-interactions

Drug Interactions Drug interactions • occur bw drugs or bw drugs & foods I. Drug – Drug Interactions: 1. additive drug effect 2 drugs produce equivalent effects when either drug is given alone in higher doses. ex. diuretic & beta blocker aspirin & codeine 2. synergistic/potentiation – 2 drugs produce same effects but one drug enhances the effect of the other drug  greater effect ex. meperidine (Demerol) & promethazine alcohol & sedatives 3. antagonistic – combined effects of 2 drugs are less than the effect produced by the 2 individual drugs ex. tetracycline & antacid morphine & naloxone 4. Incompatibility – 2 drugs mixed together  chemically incompatible ex. ampicillin & gentamicin II. Drug – Food Interactions:

• tetracycline & dairy products • levodopa & high protein meals • monoamine oxidase inhibitor (MAO) inhibitor & tyramine-rich foods • nitrofurantoin • Metoprolol & food • lovastatin

Adverse Drug Reactions I. Dose- related adverse reactions: • Secondary effects • Hypersensitivity or hypersusceptibility • Overdose • Iatrogenic • Tolerance • Dependence Patient sensitivity-related adverse reactions • Allergic reaction • Idiosyncrasy I. Dose-related adverse reactions: a. Secondary effects ex. morphine antihistamine b. Hypersensitivity or hypersusceptibility • excessive therapeutic response even with usual therapeutic dose ex. anticholinergics  dry mouth, blurring of vision, urinary retention & constipation narcotic analgesic oral contraceptives digitalis aspirin c. Overdose & toxicity

II.

• excessive dose  exaggerated response • pediatric & elderly ex. CNS depressants digoxin d. Iatrogenic effects • adverse reactions that caused by drugs that are part of medical tx. • drug-induced diseases ex. antineoplastics, aspirin, corticosteroids  GI irritation & bleeding propanolol gentamicin e. tolerance • decrease response to drug over time ex. psychoactive drugs (e.g. benzodiazepines) propanolol cocaine morphine f. dependence • strong physical & psychological need for a certain drug  habituation  addiction

g. cumulation • body cannot metabolize & excrete one dose of a drug completely before the next dose. II. Patient sensitivity-related adverse reactions: • result from unusual & extreme sensitivity to a drug a. Allergic reaction • abnormal response due to antibodies against a certain drug ex. antibiotics (penicillin) , aspirin, sulfonamides 1. Types: Immediate allergic reaction :  Urticaria sxs: • skin rash with severe itching

• swelling  Anaphylaxis sxs: • dyspnea • extreme weakness • nausea & vomiting • cyanosis • hypotension • circulatory collapse 2. Delayed allergic reaction  Serum sickness Sxs. • itchy rash • fever • swollen & stiff joints Interventions: • notify prescriber & discontinue drugs • emergency tx for anaphylactic shock • Epinephrine • Antihistamines or topical corticosteroids • Cool environment b. Idiosyncratic reactions: • unique or strange responses to certain drugs thought to be caused by genetic factors ex. succinylcholine primaquine

III.

Other drug- related effects: a. Teratogenic • produce organ defects in developing fetus ex. marijuana/ cocaine alcohol aminoglycoside b. Carcinogenic • induce malignant changes in cells ex. estrogen therapy

antineoplastics for pediatric leukemias c. Mutagenic • produce genetic mutations

IV.

Drug-induced tissue & organ damage: A. Dermatological reactions: Sxs: • hives/ urticaria • rash • exfoliative dermatitis • Stevens- Johnson syndrome Ex. procainamide - butterfly- rash sulfonamide - Stevens-Johnson syndrome Tx: • frequent skin care • notify prescriber & discontinue drug • topical corticosteroids, antihistamine & emollients B. Stomatitis S/sxs: • swollen gums & tongue. • difficulty swallowing • bad breath • pain in mouth & throat ex. antineoplastic agents (eg fluorouracil) Tx: • frequent mouth care • frequent, small meals D. Gingival hyperplasia S/sxs: • red, & enlarged gums ex. phenytoin (anticonvulsant) E. Superinfections S/sxs: • fever • diarrhea • hairy tongue

• mucous membrane lesions • vaginal discharge ex. antibiotics F. Blood dyscrasias  agranulocytosis*  anemia  thrombocytopenia s/sxs: • fever & chills • extreme weakness • sore throat • high risk to infection • high risk for bleeding/hemorrhage ex. antineoplastics & antipsychotics antibiotics (eg. chloramphenicol, sulfonamides) anti-inflammatory (eg non-steroidal anti-inflammatory drugs (NSAID) tx. • monitor blood counts • protect from exposure to infection • avoid activities that result in injury or bleeding G. Hepatotoxicity s/sxs: • jaundice* • fever • nausea & vomiting • increase in liver enzymes (AST & ALT) • altered bilirubin ex. isoniazid (INH) acetaminophen H. Nephrotoxicity s/sxs • edema • increase Crea & BUN • decrease hematocrit • electrolyte imbalances ex. aminoglycosides (eg gentamicin) sulfonamide I. Ototoxicity

s/sxs • dzziness • ringing in ears • loss of balance • hearing problem ex. aminoglycoside (eg. Gentamicin) azithromycin, erythromycin aspirin quinidine J. Ocular toxicity s/sxs • burring of vision • color vision changes • blindness ex. chloroquine (anti-malarial ) K. Hypoglycemia s/sxs • headache • tremors • drowsiness • cold clammy skin • seizures/coma ex. antidiabetic agents (eg. Insulin, glipizide) L. Hyperglycemia s/sxs • polyphagia • polyuria • polydipsia • kussmaul’s respiration • fruity breath ex. ephedrine ( bronchodilator) M. Hypokalemia s/sxs • serum K • irregular, weak pulse • weakness & numbness of extremities • paralytic ileus o absent bowel sounds o abdominal distention ex. loop diuretics (eg, furosemide)

N. Hyperkalemia s/sxs • same as hypokalemia ex. potassium-sparing diuretics (eg. Spironolactone) antineoplastic drugs O. General CNS effects s/sx • anxiety • insomnia • nightmares ex. beta-blockers (eg. Metoprolol) P. Atropine- like (Cholinergic) effects s/sxs • dry mouth • constipation • urinary retention • decrease sweating, • hot dry skin ex. antidepressants (eg. TCA)

Q. Extrapyramidal reactions/ parkinson- like syndrome s/sxs • immobility (akinesia) • rigidity • muscular tremors • violent movement of head & arms (dystonia) • restlessness (akathisia) ex. antipsychotic drugs R. Neuroleptic Malignant syndrome s/sxs • extrapyramidal symptoms • hyperthermia ex. general anesthetics S. Photosensitivity s/sxs

• itching • scaling • reddening of skin Ex. sulfonamides, tetracycline T. Cough - ACE inhibitors U. Gray Baby Syndrome - chloramphenicol V. Osteoporosis – corticosteroids, heparin W. Pseudomembranous colitis – clindamycin X. Discolors teeth – tetracycline Y. Nasal stuffiness – reserpine Z. cervical cancer – estrogen hemorrhage – oral anticoagulants, heparin

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