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镇静催眠药的药代动力学及药物相互作用

Pharmacokinetics and drug interactions of the sedative hypnotics.

作者信息

Wang Jun-Sheng, DeVane C Lindsay

机构信息

Department of Psychiatry and Behavioral Sciences, Medical University of South Carolina, Charleston, South Carolina, USA.

出版信息

Psychopharmacol Bull. 2003 Winter;37(1):10-29.

Abstract

Sleep complaints are common among patients and may be associated with mild to severe clinical symptoms. The use of hypnotic agents to improve the onset and quality of sleep has a history dating back centuries. Currently, several benzodiazepines and nonbenzodiazepines are widely used as sedative hypnotic drugs. The pharmacokinetic and pharmacodynamic profiles of these agents vary substantially, allowing them to be chosen for different clinical situations and tailored to specific sleep complaints. The short-acting benzodiazepines and benzodiazepine agonists have become the most widely prescribed sedative hypnotics because of their short to ultrashort half-life, and low tendency to impair cognitive and psychomotor performance on the day following nighttime use. In the current review, we summarize the pharmacokinetic and drug interaction profiles of the Food and Drug Administration-approved benzodiazepine sedative hypnotics: estazolam, flurazepam, quazepam, temazepam, and triazolam. In addition, alprazolam is included because of its popularity for this use, and 2 benzodiazepine receptor agonists, zolpidem and zaleplon, are reviewed. The presented data will provide clinicians with insight into the pharmacokinetic profiles of several popular sedative hypnotic agents, and provide guidelines to help them recognize or avoid drug interactions.

摘要

睡眠问题在患者中很常见,可能与轻至重度临床症状相关。使用催眠药物改善睡眠的起始和质量已有数百年历史。目前,几种苯二氮䓬类药物和非苯二氮䓬类药物被广泛用作镇静催眠药。这些药物的药代动力学和药效学特征差异很大,使其能够针对不同临床情况进行选择,并根据特定的睡眠问题进行调整。短效苯二氮䓬类药物和苯二氮䓬类激动剂因其半衰期短至超短,且夜间使用后次日损害认知和精神运动功能的倾向较低,已成为处方最广泛的镇静催眠药。在本综述中,我们总结了美国食品药品监督管理局批准的苯二氮䓬类镇静催眠药(艾司唑仑、氟西泮、夸西泮、替马西泮和三唑仑)的药代动力学和药物相互作用特征。此外,阿普唑仑因其在此用途上的广泛应用而被纳入,并且对两种苯二氮䓬受体激动剂唑吡坦和扎来普隆进行了综述。所呈现的数据将为临床医生提供对几种常用镇静催眠药药代动力学特征的深入了解,并提供指导方针以帮助他们识别或避免药物相互作用。

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