安徽医科大学国际教育学院教案与讲稿 Potency:The sensitivity of an organ or tissue to the drug Efficacy:The maximum effect RELATING DOSE TO EFFECT IN VIVO 4min Dose Effect site =Effect Concentration Pharmacokinetics Pharmacodynamics Age Tissue/organ sensitivity Absorption (receptor status) Distribution Elimination Drug interactions [MAJOR SOURCES OF VARIABILITY] 5min Compliance Age-neonates,children,elderly Physiology-gender,pregnancy Disease-Hepatic,renal,cardiovascular,respiratory Drug interactions Environmental influences on drug metabolism Genetic polymorphisms [PHARMACODYNAMIC MODELS] 2min Relation between concentration and the intensity of an effect The Emax and Sigmoid Emax Models Linear Models Relation between concentration and probability of occurrence of an effect Fixed-effect model [THE EMAX AND SIGMOID EMAX MODELS] 3min Models describing relations between intensity of an effect and drug concentrations at the site of action Can be used inin vivo PK/PD modelling when there exist a direct and immediate link between plasma concentrations and effect EMAX MODELI 5min Relation described by two parameters Emax:intrinsic activity,EFFICACY EC50:conc.Associated with half-maximal effect,POTENCY Empirical justifications The most simple mathematical description of the occurrence of a maximum effect Theoretical justifications Ligand-receptor interaction 3安徽医科大学国际教育学院教案与讲稿 3 Potency: The sensitivity of an organ or tissue to the drug Efficacy: The maximum effect [RELATING DOSE TO EFFECT IN VIVO] 4min [MAJOR SOURCES OF VARIABILITY] 5min Compliance Age- neonates, children, elderly Physiology- gender, pregnancy Disease- Hepatic, renal, cardiovascular, respiratory Drug interactions Environmental influences on drug metabolism Genetic polymorphisms [PHARMACODYNAMIC MODELS] 2min Relation between concentration and the intensity of an effect The Emax and Sigmoid Emax Models Linear Models Relation between concentration and probability of occurrence of an effect Fixed-effect model [THE EMAX AND SIGMOID EMAX MODELS] 3min Models describing relations between intensity of an effect and drug concentrations at the site of action Can be used in in vivo PK/PD modelling when there exist a direct and immediate link between plasma concentrations and effect [EMAX MODEL] 5min Relation described by two parameters Emax: intrinsic activity, EFFICACY EC50: conc. Associated with half-maximal effect, POTENCY Empirical justifications The most simple mathematical description of the occurrence of a maximum effect Theoretical justifications Ligand-receptor interaction