2 第二章 药动学幻灯片.pptVIP

Chapter 2; Object;pharmacokinetics include:;drug;biomembrane structure;§1 Transmembrane transportation of drug ;I. Passive transport;Most drugs;Penicillin G sodium (青霉素G钠) penicillin - + Na +------water-solubility? ionization (解离型) ∴ Un-ionization (非解离型)------lipo-solubility ?;Un-ionization degree depend on: pKa (解离指数) of the drug pH of the environment ;by the Henderson-Hasselbalch equation: ;For example:;Clinical significance:;II. carrier-mediated transport;characteristics of facilitated diffusion :;§2 The process of drug in the body ;Routs of administration ;First pass elimination (首关消除) 药物经胃肠道吸收后第一次通过肝脏被代谢一部分,使进入血循环的有效药量减少,此作用称～. ;2. Parenteral administration (胃肠道外) 1) Inhalation (吸入) 2) Local administration include skin , ear, nose or eye drops…… s;2. Distribution;Factor affecting distribution:;D + P;distribution and redistribution (再分布);combine with tissue;extracellular fluid pH = 7.4;Barrier (屏障) phenomenon Blood-brain barrier（血脑屏障） BBB;Placenta barrier（胎盘屏障） The permeability of placenta barrier is not especial.;3. Biotransformation (metabolism);Phases of metabolic reactions;Enzymes for biotransformation:;Characteristics of the enzymes ;Enzyme revulsant (药酶诱导剂) some drugs ?? activity of certain enzyme ? ? metabolism (own or other drug ). e.g phenobarbital (苯巴比妥)…… Enzyme inhibitor (药酶抑制剂) some drugs ?? activity of certain enzyme ? ? metabolism of the other drug. e.g cimetidine (西米替丁)…… ;+药酶诱导剂;4. Excretion;①Renal excretion;Clinical significance:;② Biliary excretion（胆汁）;others;§3 Compartment model (房室模型);Two compartment open model ;§4 Elimination kinetics of drugs;§4 Elimination kinetics of drugs;§4 Elimination kinetics of drugs;I. First order elimination kinetics (一级消除动力学) 单位时间内药物消除的比例是恒定的.;T1/2;Half life (半衰期, t ? );II. zero order elimination kinetics (零级消除动力学) 单位时间内药物消除的量是恒定的.;III. mixed elimination kinetics