Chapter 2 Clinical Pharmacodynamics.pptVIP

Clinical Pharmacodynamics and Receptors Definition A subject on drug effects and mechanisms of action and their applications in clinical practice. Receptor and its related issues : core of clinical pharmacology. The discovery of receptor Paul Ehrlich( some organic agents , antiparasitic effects ) John Langley ( curare blocks muscle contraction induced by nicotine, not by electricity ) The actions and clinical uses of drugs related to receptors : (1) Receptors largely determine the quantitative relations between dose or concentration of drug and pharmacologic effects (affinity , total number of receptors ). Affinity determines the concentrations required to produce a certain extent of efficacy. The number of receptors determines the maximal efficacy. (2) Receptors are responsible for selectivity of drug action( molecular size, shape, and electrical charge of a drug ) What receptors to be selectively bound largely depends on molecular size, shape, and electrical charge of a drug. Distribution of receptors are heterogeneous. (3) Receptors mediate the actions of pharmacologic both agonists and antagonists Agonist: Many drugs are or similar to endogeneous substances to regulate the function after their binding to receptors. Antagonist: Some drugs block actions of agonists by preventing them from binding to the receptors. MACROMOLECULAR NATURE OF DRUG RECEPTORS regulatory proteins ( β-adrenoceptor) Enzymes( ACE ) transport proteins (calcium channel ) structural proteins( tubulin for colchicine)  In this chapter we are going to deal with Receptor function as determinants of the quantitative relation between the concentration of a drug and the pharmacologic response. Receptor function as key determinants of the therapeutic and toxic effects of drugs in patients. RELATION BETWEEN DRUG CONCENTRATION RESPONSE Concentration-Effect Curves Receptor Binding of AgonistsIn idealized or in vitro systems The curve of the equation Antagonist Recetptor antagonist C