臨床執(zhí)業(yè)醫(yī)師考試大綱復(fù)習(xí)藥理學(xué)名師輔導(dǎo)講義

1、臨床執(zhí)業(yè)醫(yī)師考試大綱復(fù)習(xí)藥理學(xué)名師輔導(dǎo)講義第六篇 藥 理 學(xué)第1章 藥物代謝動(dòng)力學(xué)與藥物效應(yīng)動(dòng)力學(xué)考綱要求藥物代謝動(dòng)力學(xué)：吸收（首過消除）。分布：血腦屏障，胎盤屏障。體內(nèi)藥量變化的時(shí)間過程：生物利用度。藥物消除動(dòng)力學(xué)：一級(jí)消除動(dòng)力學(xué)，零級(jí)消除動(dòng)力學(xué)。藥物效應(yīng)動(dòng)力學(xué)：不良反應(yīng)（副反應(yīng)，毒性反應(yīng)，后遺效應(yīng)，停藥反應(yīng)，變態(tài)反應(yīng)，特異質(zhì)反應(yīng)）。藥物劑量與效應(yīng)關(guān)系：半數(shù)有效量，治療指數(shù)。藥物與受體：激動(dòng)藥，拮抗藥。 復(fù)習(xí)要點(diǎn)一、藥物代謝動(dòng)力學(xué)藥物代謝動(dòng)力學(xué)是研究藥物的吸收、分布、代謝、排泄過程的學(xué)科，并運(yùn)用數(shù)學(xué)原理和方法闡釋藥物在機(jī)體內(nèi)的動(dòng)態(tài)規(guī)律。1吸收 （1）概念 藥物自用藥部

2、位進(jìn)入血液循環(huán)的過程稱為吸收。藥物只有經(jīng)吸收后才能發(fā)揮全身作用。有些用藥只要求產(chǎn)生局部作用，則不必吸收。不同給藥途徑有不同的藥物吸收過程和特點(diǎn)。（2）首過消除（首過代謝、首過效應(yīng)） 口服是最常用的給藥途徑。從胃腸道吸收入門靜脈系統(tǒng)的藥物在到達(dá)全身血循環(huán)前必先通過肝臟，如果肝臟對(duì)其代謝能力很強(qiáng)，或由于膽汁排泄的量大，則使進(jìn)入全身血循環(huán)內(nèi)的有效藥物量明顯減少，這種作用稱為首過清除。 首過清除高時(shí)，生物利用度則低，機(jī)體可利用的有效藥物量就少。要達(dá)到治療濃度，就必須加大用藥劑量，從而可能出現(xiàn)代謝產(chǎn)物的毒性反應(yīng)。2分布藥物被吸收進(jìn)入血循環(huán)后，便可能分布到機(jī)體的各個(gè)部位和組織。藥物吸收后從血循環(huán)達(dá)到機(jī)體各

3、個(gè)部位和組織的過稱，稱為分布。藥物在體內(nèi)的分布受很多因素的影響，包括藥物的脂溶度、毛細(xì)血管通透性、器官和組織的血流量、與血漿蛋白和組織蛋白的結(jié)合能力、藥物的pka和局部的ph值、藥物轉(zhuǎn)運(yùn)載體的數(shù)量和功能狀態(tài)、特殊組織膜的屏障作用等。3藥物消除動(dòng)力學(xué) （1）一級(jí)消除動(dòng)力學(xué)與零級(jí)消除動(dòng)力學(xué)的鑒別（2）一級(jí)消除動(dòng)力學(xué)的特點(diǎn)體內(nèi)藥物按瞬時(shí)血藥濃度（或體內(nèi)藥量）以恒定的百分比消除，但單位時(shí)間內(nèi)實(shí)際消除的藥量隨時(shí)間遞減。藥物消除半衰期恒定，與劑量或藥物濃度無關(guān)。絕大多數(shù)藥物都按一級(jí)動(dòng)力學(xué)消除，這些藥物在體內(nèi)經(jīng)過5個(gè)t1/2后，體內(nèi)藥物可基本消除干凈。每隔一個(gè)t1/2給藥一次，則體內(nèi)藥量（或血藥濃度）可逐漸

4、累積，經(jīng)過5個(gè)t1/2后，消除速度和給藥速度相等，達(dá)到穩(wěn)態(tài)。qcwa3ptgz7r4i30ka1dkaghn3xtkknbycudxqa7fhyi2chhi92tgkqcwa3ptgshls50clmtwn60eo8wgqv7xav2ohum32wgeauwydiawgmer4i30ka1dkaghn3xtkknbycudxqa7fhyi2chhi92tgkqcwa3ptgz7r4i30ka1dkagtgkqcwa3p tgz7r4i30ka1dkaghn3xtkknbycudxqa7fhyi2chhi92tgkqcwa3ptgshls50clmtwn60eo8wgqv7xav2ohum32w

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