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Introduction to Pharmacology September 5, 2007 •Frank F. Vincenzi E-419, HSB •206-543-1993 •[email protected] •*Assignment*: If you have not already done so, send me an email message in response to my email to you. If you did not get a message from me, pay special attention. YOUR EMAILS WILL BE USED TO CREATE THE UNIQUE CLASS & MAILING LIST. Please tell me a little bit about yourself and what you hope/expect to learn in pharmacology - whatever you are comfortable sharing. Food for thought • The Food & Drug Administration (FDA) approves about 30 new drugs/year • Most MDs prescribe drugs that were not known when they graduated • About 2/3 of all physician visits lead to a prescription • More than half of drug advertising $$ goes to ‘detailing’ MDs (about $5000/yr/MD) Objectives of HuBio 543 •Impart a specific body of knowledge •Develop an ability to use the knowledge •Develop a systematic approach to critically evaluate pharmacological information •Develop motivation to add the knowledge base on a life-long basis Roadmap for Autumn Quarter • Basic Principles of Pharmacology • Peripheral Nervous System (somatic & ANS) • Cardiovascular • Chemotherapy • Disease, Syndrome & Patient-oriented Sessions Evaluation • Zero to three NO HARM quizzes AND/OR Final examination (if a quiz is not taken, or if the percentage score is less than the percentage on the Final Examination, then the quiz is simply dropped) • One take home quiz • One quiz mainly on peripheral NS • One quiz on CV and chemotherapy 100 points 100 points 100 points • Final Examination (comprehensive) 300 points Example of overall course average calculation for a hypothetical student • Quiz # 1 (take home) • Quiz # 2 (ANS) • Quiz # 3 (CV and chemo) (Autumn flu) • Final examination - comprehensive (68%) • (quiz 2 and quiz 3 dropped (< 68%) • (90 + 204)/400 = 0.735, (i.e., 73.5% … pass) points 90/100 60/100 -204/300 EXAMINATION FORMATS & GRADING • Multiple choice • Calculations • Short answer/essay • >= 70% overall average, guaranteed pass • >=90% overall average, guaranteed honors Sources of Information • Syllabus and Lectures & handouts • Textbook: Goodman & Gilman’s The Pharmacological Basis of Therapeutics, printed or online (Now in its11th edition) • Course Web Site https://courses.washington.edu/chat543/ – Schedule, objectives, grading, etc. – Drug List – Web Site for CV & ANS Pharmacology https://courses.washington.edu/chat543/cvans/index.html • Books & CD-ROMS, Internet resouces Katzung, Brody’s Human Pharmacology Physician’s Desk Reference (PDR) (Lippincott’s Board Review) Most common sources of drug information - clinically PDA ePocrates CP on Hand Physician’s Drug Handbook, Your Local Pharmacist !! Internet…… PDR Learning objectives for this session Introductory understanding of: • • • • • • • Pharmacology Drug Receptor Agonist Antagonist Pharmacodynamics Pharmacokinetics • • • • • • Toxicology Silent receptor Drug action Drug effect Chirality Why most drugs have MWs >100 and < 1000 Pharmacology is the science of drug action • Related disciplines: – Pharmacognosy - the study of drugs from natural sources – Toxicology - That branch of pharmacology which systematically studies the adverse effects of drugs on living systems • Related professions: – Pharmacy - the art and science of compounding and dispensing - and, increasingly, drug information... – Clinical pharmacology - the art and science of evaluating and optimizing the use of drugs in humans Drug • Noun – Any agent that, by virtue of its chemical properties, alters the structure or function of biological systems (pharmacologist’s view). – Any agent approved by the Food and Drug Administration for the treatment or prevention of disease (legal view). – Any agent taken by some, but disapproved by others (societal view). Receptor • Noun – Those molecules (or parts of molecules) with which a drug must interact in order to produce a given action in a biological system Macromolecules (especially proteins) as receptors • • • • • G Protein coupled receptors (GPCRs) (e.g., beta adrenoceptor) Ligand-gated ion channels (e.g., NAChR) Cytokine receptors (e.g., erythropoietin) Structural proteins (e.g., tubulin) Transmembrane enzymes – ion pumps (Na/K pump ATPase) – receptor tyrosine kinases (insulin receptor) Human genomic proteins as receptors Silent Receptor • Those molecules or parts of molecules with which a drug interacts without producing an action - a site of binding. – e.g., warfarin binding to serum albumin Chirality of drugs (stereoisomerism) • D-epinephrine is essentially inactive • L-epinephrine is extremely potent (halfmaximal effects at nanomolar concentrations) – Simplest interpretation is that L-epinephrine makes a three point contact with its receptors Drugs: molecular weight considerations Biological Systems: Interactions Through Differentiated Aspects of the Whole • • • • • • • Society Community Organism Organ system Organ Tissue Cell • • • • • • • Subcellular organelles Molecular systems Molecules Functional groups Atoms Subatomic particles Quarks Molecules are a LOT smaller than cells Two equally and clinically important aspects of pharmacology • Pharmacodynamics – Systematic study of the effects of drugs on living systems • Pharmacokinetics – Systematic study of the effects of living systems on drugs Agonist • Noun – A drug molecule which, when it interacts with a given receptor, produces a stimulus which results in a change in the biological system beyond the level of that receptor • e.g., epinephrine Partial Agonist • Noun – A drug molecule which, when it interacts with a given receptor, produces a stimulus for change beyond the level of that receptor, but the stimulus is less than the maximum characteristic of that receptor • e.g., buprenorphine Competitive Antagonist • Noun – A drug molecule which, when it interacts with a given receptor, does not directly produce a stimulus for change beyond the level of that receptor • e.g., atropine Sources of Drugs • Natural sources (mainly plants) – Atropa belladonna (deadly nightshade), Ginkgo biloba (Ginkgo), Hypericum perforatum (St. John’s Wort), etc. • Pure compounds derived from plants, molds, etc. – digoxin, vinblastine, penicillin G • Synthetic chemistry – Sulfanilamide, acetaminophen, zafirlukast • Biotechnology – Smallpox vaccine, rhGH, ... Alkaloids (basic nitrogenous compounds of plant origin that are pharmacologically active) • • • • • • • • • morphine (Papaver somniferum) quinine (Cinchona succirubra) atropine (Atropa belladonna) cocaine (Erythroxylum coca) colchicine (Colchicum autumnale) papaverine (Papaver somniferum) ephedrine (Ephedra sinensis) strychnine (Strychnos nux vomica) tubocurarine (Chondodendron tomentosum) Alkaloids (cont.) • • • • • • • • • nicotine (Nicotiana tabacum) reserpine (Rauwolfia serpentina) vinblastine (Cantharanthus roseus) physostigmine (Physostigma venenosum) ergonovine (Claviceps purpurea) pilocarpine (Pilocarpus jaborandi) mescaline (Lophophora williamsii) caffeine (Coffea arabica) theophylline (Camellia sinensis) Non-alkaloid plant substances as drugs • salicin (Salix purpurea and related species.) • tetrahydrocannabinol (Cannabis sativa) • digoxin (Digitalis lanata) Drug Nomenclature • The endings... – – – – – – – – ‘…ine’ often (but not always) signifies an alkaloid ‘…olol’; beta-blockers ‘…opril’; ACE inhibitors ‘…dipine’; dihydropyridine Ca channel blockers ‘…cillin’; penicillins ‘…tidine’; chemically related histamine antagonists ‘…sartan; antagonists of aldosterone ‘…statin; inhibitors of HMG CoA reductase Drug names: a hint to identity • Dihydropyridines: (one class of Ca channel blockers) – nifedipine, nisoldipine, niludipine,nimodipine • Local anesthetics – cocaine, procaine, bupivacaine, lidocaine, benzocaine • ACE inhibitors – captopril, enalapril, fosinopril • Beta blockers: – propranolol, metoprolol, nadolol, timolol, atenolol Drug names: a hint to identity (cont) • Penicillins – penicillin G, methicillin, amoxicillin, ticarcillin • Cephalosporins – cephalothin, cefaclor, cefotaxime, cefepime • Macrolide antibiotics – erythromycin, clarithromycin, azithromycin • Antifungals – ketoconazole, itraconazole, fluconazole, clotrimazole Generic and Trade names: Rx drugs • • • • • lanoxin, Dixogin® ciprofloxacin hydrochloride, Cipro® fluticasone propionate, Flonase® ipratropium bromide, Atrovent® nifedipine, Adalat®, Procardia® Generic and trade names: combination drugs • • • • fluticasone propionate-salmeterol (Advair®) imipenem-cilastin sodium, Primaxin® losartan potassium-hydrochlorothiazide, Hyzaar® trimethoprim-sulfamethoxazole, Bactrim®, Septra® • lidocaine hydrochloride-epinephrine, Xylocaine® with epinephrine What to learn about drugs on the ‘drug list’ • Generic name (Trade name only if it helps recognition) • Site of action • Mechanism of action • ...(and for clinically used drugs) • Indications and contraindications • Major effects, limitations and adverse reactions • Major interactions NOTE: Drug list items in the last chapter of the syllabus: ‘Simplified Table of Pharmacokinetic Values’ Questions? (& reminder) • Assignment: If you have not already done so, confirm your UW email address to [email protected]. • Your confirmations are used to build the unique mailing list for the course. • Please add some personal background and expectations/hopes for the course - whatever you are comfortable sharing. • Thank you.