1. TOPICS TO DISCUSS
1. Pharmacodynamics. Definition (pharmacological effects, mechanisms of drug action, localization of drug action).
2. The main molecular targets for drug action.
3. Specific receptors: the main properties and functions. Membrane and intracellular receptors. Division of membrane receptors according to transduction mechanism. Characteristics and examples of each receptor type.
4. G-proteins. The role in transduction mechanisms. Mechanism of amplification. Types of G-proteins (Gs, Gi, Gq). Interaction with enzymes and ion channels.
5. Adenylate cyclase/cAMP system. Phospholipase C/IP3 system. The chains of cellular responses in cardiomyocytes and smooth muscle cells.
6. Drug-receptor binding (types of bonds, reversible and irreversible binding). Affinity. The quantitative characteristics of affinity: dissociation constant (Kd).
7. Intrinsic activity. Agonists (full, partial). Antagonists. Inverse agonists.
8. Graded dose-response curve. Efficacy. Potency. The characteristics of efficacy and potency: E
J r j max
and ED50.
9. Combined drug administration (synergism, po-tentiation, additive effect, antagonism). Pharmacological antagonism (competitive and non-competitive antagonism).
10. Changes in drug action as a result of continuous or repeated drug administration.
11. Tolerance. The mechanisms of tolerance: de-sensitization of receptors, loss of receptors, depletion of neurotransmitters, etc.
12. Drug dependence (definition, types, and characteristics of drug dependence).
13. Adverse and toxic effects of drugs.
14. Drug allergy. Idiosyncrasy.
15. Mutagenicity, carcinogenicity, teratogenicity of drug.
16. Quantal dose-response curve. Measure of drug safety: therapeutic index (TI).