苯二氮䓬类催眠药的药代动力学特性。

Pharmacokinetic properties of benzodiazepine hypnotics.

作者信息

Greenblatt D J, Abernethy D R, Divoll M, Harmatz J S, Shader R I

出版信息

J Clin Psychopharmacol. 1983 Apr;3(2):129-32.

Abstract

The kinetic properties of three benzodiazepine hypnotics are reviewed. Flurazepam serves as a precursor for at least two rapidly appearing and rapidly cleared metabolites that may contribute to sleep induction and are nonaccumulating. The final metabolite of flurazepam (N-desalkylflurazepam), however, has a long half-life and accumulates during repeated dosage. Temazepam has a relatively slow rate of absorption and an intermediate half-life in the range of 10 to 20 hours. Triazolam has an intermediate rate of absorption; due to its ultrashort half-life (1.5 to 5 hours), triazolam is a non-accumulating hypnotic. Taken together with sleep laboratory studies and clinical trials, knowledge of the kinetic profile of benzodiazepine hypnotics can assist in evaluating their clinical benefits and disadvantages.

摘要

本文综述了三种苯二氮䓬类催眠药的动力学特性。氟西泮可转化为至少两种迅速出现并迅速清除的代谢产物，这些代谢产物可能有助于诱导睡眠且不会蓄积。然而，氟西泮的最终代谢产物（N-去烷基氟西泮）半衰期较长，在重复给药时会蓄积。替马西泮吸收相对较慢，半衰期中等，在10至20小时之间。三唑仑吸收速度中等；由于其超短半衰期（1.5至5小时），三唑仑是一种不会蓄积的催眠药。结合睡眠实验室研究和临床试验，了解苯二氮䓬类催眠药的动力学特征有助于评估其临床优缺点。