临床执业医师考试大纲复习药理学名师辅导讲义

1、临床执业医师考试大纲复习药理学名师辅导讲义第六篇 药 理 学第1章 药物代谢动力学与药物效应动力学考纲要求药物代谢动力学：吸收（首过消除）。分布：血脑屏障，胎盘屏障。体内药量变化的时间过程：生物利用度。药物消除动力学：一级消除动力学，零级消除动力学。药物效应动力学：不良反应（副反应，毒性反应，后遗效应，停药反应，变态反应，特异质反应）。药物剂量与效应关系：半数有效量，治疗指数。药物与受体：激动药，拮抗药。 复习要点一、药物代谢动力学药物代谢动力学是研究药物的吸收、分布、代谢、排泄过程的学科，并运用数学原理和方法阐释药物在机体内的动态规律。1吸收 （1）概念 药物自用药部

2、位进入血液循环的过程称为吸收。药物只有经吸收后才能发挥全身作用。有些用药只要求产生局部作用，则不必吸收。不同给药途径有不同的药物吸收过程和特点。（2）首过消除（首过代谢、首过效应） 口服是最常用的给药途径。从胃肠道吸收入门静脉系统的药物在到达全身血循环前必先通过肝脏，如果肝脏对其代谢能力很强，或由于胆汁排泄的量大，则使进入全身血循环内的有效药物量明显减少，这种作用称为首过清除。 首过清除高时，生物利用度则低，机体可利用的有效药物量就少。要达到治疗浓度，就必须加大用药剂量，从而可能出现代谢产物的毒性反应。2分布药物被吸收进入血循环后，便可能分布到机体的各个部位和组织。药物吸收后从血循环达到机体各

3、个部位和组织的过称，称为分布。药物在体内的分布受很多因素的影响，包括药物的脂溶度、毛细血管通透性、器官和组织的血流量、与血浆蛋白和组织蛋白的结合能力、药物的pka和局部的ph值、药物转运载体的数量和功能状态、特殊组织膜的屏障作用等。3药物消除动力学 （1）一级消除动力学与零级消除动力学的鉴别（2）一级消除动力学的特点体内药物按瞬时血药浓度（或体内药量）以恒定的百分比消除，但单位时间内实际消除的药量随时间递减。药物消除半衰期恒定，与剂量或药物浓度无关。绝大多数药物都按一级动力学消除，这些药物在体内经过5个t1/2后，体内药物可基本消除干净。每隔一个t1/2给药一次，则体内药量（或血药浓度）可逐渐

4、累积，经过5个t1/2后，消除速度和给药速度相等，达到稳态。hi92tgkqcwa3ptgshls50clmtwn60eo8wgqv7xav2ohum32wgeauwydiawgmer4i30ka1dkaghn3xtkknbycudxqa7fhyi2chhi92tgkqcwa3ptgz7r4i30ka1dkagtgkqcwa3p tgz7r4i30ka1dkaghn3xtkknbycudxqa7fhyi2chhi92tgkqcwa3ptgshls50clmtwn60eo8wgqv7xav2ohum32wgeauwydiawgmer4i30ka1dkaghn3xtkknbycudxqa7fhyi

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