第三章：药物代谢动力学.ppt

Chapter 3 Object 掌握药物的体内过程及其影响因素， 掌握血浆半衰期、生物利用度、零级动力学、一级动力学的概念及意义。 熟悉 药动学概念，药物的转运方式，时量关系和时效关系，血药稳态浓度的实现及维持。 了解 时量曲线的有关参数及意义。 §1 Transmembrane transportation of drug I. Passive transport characteristics of simple diffusion: 1. Depend on concentration gradient (浓度梯度) 2. Need not carrier (载体) and energy 3. lie on lipid-solubility(脂溶性) of drug Clinical significance: Overdosage toxicosis （过量中毒）of weak acids------use basic drug to basify （碱化） blood or urine→ ionization↑，absorption↓，excretion↑. For example: phenobarbital （苯巴比妥） toxicosis use sodium bicarbonate （碳酸氢钠） iv. gtt. II. carrier-mediated transport characteristics of active transport: 1. converses concentration gradient 2. Need carrier (载体) and energy 3. Saturable (饱和性) 4. Competitive inhibition characteristics of facilitated diffusion : 1. Obedients concentration gradient(顺浓度） 2. Need carrier 3. Saturable 4. Competitive inhibition §2 The process of drug in the body 1. Absorption What’s absorption? A process of the drug traverse the cellular membrane and get into the circulation. Routs of administration 1. Gastrointestinal tract (胃肠道) 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 What’s the distribution? A transporting process of drug to all organs through circulation. Factor affecting distribution: ① Plasma protein binding ratio ② Blood flow ③ combine with tissue ④ pKa and pH ⑤ Barrier distribution and redistribution (再分布) combine with tissue Significance： ★ relationship with therapeutic action e.g iodin(碘) ----- thyroid (甲状腺) chloroquine ----- infective RBC ★ relationship with adverse reaction e.g gentamicin ----- deaf (耳聋) Placenta barrier（胎盘屏障） The