药理学PPT课件（南开大学）第三章 药物代谢动力学.ppt

第二章药物代谢动力学 Pharmacokinetics 南开大学医学院 张京玲 韩姗 Pharmacokinetics 目的 掌握药代动力学的基本概念及基本参数的计算。了解药代动力学的基本房室模型及血药浓度测定的临床意义。 Pharmacokinetics 内容 一级动力学与零级动力学衰减原理。药物的跨膜转运机理与影响因素。药物吸收途径，第一关卡消除，肝肠循环，生物利用度，血浆蛋白结合原理与意义，药物分布不均匀性的原因与意义，表观分布容积，药物体内转化过程及代谢产物，肝脏微粒体药物代谢酶（肝药酶及P450）的特性，诱导与抑制，药物作用的消除即代谢，排泄与储存。药物消除速率常数与药物消除率的概念。药物排泄途径与机理，药物时效关系曲线，药物血浆半衰期，连续用药时药物在体内的蓄积，稳态血浓度与首剂速效剂量。药物血浆浓度监测的应用。 Pharmacokinetics Disposition of drug ( ADME system ) Time-concentration relationship Elimination kinetics Disposition of drug Drug transport Absorption Distribution Metabolism or Biotransformation Excretion Drug transport Type Feature Influence factor Feature Feature Influence factor Handerson-Hasselbalch equation Absorption Concept Route Speed Degree Influence factor Distribution Concept Influence factor Metabolism Concept Phase Result Enzyme Enzyme induction Excretion Hepatoenteral circulation Milk Saliva Skin Lungs Time-concentration curve Time-concentration relationship Elimination kinetics Elimination kinetics Zero-order kinetics Concept Formula Ct = C0 – Kt ; 0.5C0 = C0 – Kt1/2 figure Feature Significance Elimination kinetics First-order kinetics Concept Formula Figure Feature significance Elimination kinetics Compartment model One-compartment model Two-compartment model Three-compartment model Elimination kinetics Parameters Bioavailability, (F) Absolute F Relative F Elimination kinetics Apparent volume of distribution, (Vd) Definition Formula： Clinical significance Elimination kinetics Elimination rate constant, (Ke) Half-life, (t1/2) Concept Formula Clinical significance Elimination kinetics Area under curve, (AUC) formula Clearance, (Cl) Definition Formula Clinical significance Elimination kinetics Steady state or Plateau, (Css) Cmax Tpeak Dose Loading dose (D1) Maintenance dose (DM) * * ①Con. gradient; ②carrier; energy; ③saturable; ④competitive inhibit; ① Filtration Passive ② Simple diffusion transport Carrier-mediated transpor