Module I BASIC PRINCIPLES OF PHARMACOLOGY 1) The nature of drugs. 2) Characteristic (or properties) of drug molecule. 3) Drug reactivity and drug-receptor bonds. 4) Controlled clinical trial. 5) Definition and uses of . 6) Ways and means of the introduction medicine (routes of administration). 7) The absorption (permeation): mechanisms. Drug absorption from the intes- tine, factors affecting gastrointestinal absorption. 8) Transport medicinal material. 9) Pharmacologic role of the P-glycoprotein /permeability glycoprotein/ (multi- drug-resistance type 1 transporter). 10) and . 11) The effect (presystemic metabolism) of first-pass hepatic elimination: ex- traction ratio and the first-pass effect, alternative routes of administration and the first-pass effect. 12) Prodrugs: definition, pharmacological means, classification (types and subtypes), examples. 13) Distribution of the drugs (). 14) Drug principles: the ways of the elemination medicine from or- ganism.

15) Half-life period (t1/2) (probabilistic nature of half-life, formulae for half- life in exponential decay, half-life in non-exponential decay), pharmacologic role. 16) Drug accumulation (tapes; accumulation factors). 17) Mathematical modeling of the pharmacokinetic processes (single- compartment pharmacokinetic model, two-compartment model). 18) Metabolism of the drugs (drug biotransformation). The role of biotrans- formation in drug disposition.

19) Human liver P450 enzymes and cytochrome P450 cycle in drug oxidations. The mechanisms of the action inductor and inhibitor ferment metabolism. 20) Phases of drug-body interactions. 21) The types of the action medicine. 22) The repeated introduction of the drugs. 23) Receptor nomenclature. Receptor heterogeneity and subtypes. Macromo- lecular nature of drug receptors. 24) Types of drug-receptor interactions: definition of pharmacologic antagon- ist drugs, mimic drugs, receptor's affinity, drug-receptor complex, re- ceptor-effector systems, specific macromolecules, natural ligands, selective . 25) Drug antagonism.

26) Types of doses: median effective dose (ED50), median toxic dose (TD50),

(LD50), minimum lethal dose, medium therapeutic dose, , "no-effect" dose, , course dose, dayly dose, single dose, , therapeutic window. 27) The dose-concentration relationship (target concentration, maintenance dose, maintenance concentration). 28) Duration of drug action: immediate effects, delayed effects, cumulative effects. Variation in drug responsiveness: unusual or idiosyncratic drug re- sponse, hyporeactive or hyperreactive, hypersensitivity, desensitization, to- lerance, . 29) Side effects of the drugs: classification (cause, seriousness and severity, overall drug risk, location). Monitoring bodies. Examples of adverse effects associated with specific medications. 30) Special aspects of perinatal and pediatric pharmacology. Drug therapy in pregnancy: pharmacokinetics (lipid solubility, molecular weight and size, placental transporters, protein binding, placental and fetal ), (maternal drug actions, therapeutic drug actions in the fe- tus, predictable toxic drug actions in the fetus, teratogenic drug actions), tera- togenic agents, teratogenic mechanisms, defining a teratogen, counseling women about teratogenic risk, critical periods of human development, Wil- son's 6 principles (The Six Principles of Teratology). 31) General principles of drug therapy in infants and children: drug absorption (blood flow at the site of administration, gastrointestinal tract function), drug distribution, drug metabolism, drug . 32) Pediatric dosage forms and compliance. Drug use during lactation. Pedia- tric drug dosage: surface area, age and weight (calculations of dosage). 33) Special aspects of geriatric pharmacology. Pharmacologic changes asso- ciated with aging: effect of age on some physiologic functions, pharmacoki- netic changes (absorption, distribution, metabolism, elimination), pharmaco- dynamic changes, behavioral and lifestyle changes. Adverse drug reactions in the elderly. 34) Basic principles of drug discovery. Drug screening: the pharmacologic profile of the drug and screening procedure. Animal models of disease for the discovery of new therapeutic agents. Preclinical safety and testing (acute and chronic toxicity of the new drugs). Evaluations in humans (clinical trials of the new drugs). The placebo response. 35) General principles of rational prescribing and prescription writing. Ra- tional prescribing: rational steps. The prescription: a typical chart order, common form of outpatient prescription, elements of the prescription. Pre- scribing errors: omission of information, poor prescription writing, inappro- priate drug prescriptions. Compliance (adherence). Labeled and unlabeled uses of drugs.