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扎来普隆:一种用于治疗失眠的吡唑并嘧啶类镇静催眠药。

Zaleplon: a pyrazolopyrimidine sedative-hypnotic agent for the treatment of insomnia.

作者信息

Weitzel K W, Wickman J M, Augustin S G, Strom J G

机构信息

Department of Pharmacy Practice, Mercer University School of Pharmacy, Atlanta, Georgia, USA.

出版信息

Clin Ther. 2000 Nov;22(11):1254-67. doi: 10.1016/s0149-2918(00)83024-6.

DOI:10.1016/s0149-2918(00)83024-6
PMID:11117652
Abstract

BACKGROUND

Insomnia is the subjective complaint of poor sleep or an inadequate amount of sleep that adversely affects daily functioning. For the past 4 decades, treatment of insomnia has shifted away from the use of barbiturates toward the use of hypnotic agents of the benzodiazepine class. However, problems associated with the latter (eg, next-day sedation, rebound insomnia, dependence, and tolerance) have prompted development of other agents.

OBJECTIVE

This review describes the recently approved nonbenzodiazepine agent, zaleplon.

METHODS

Studies of zaleplon were identified through a search of English-language articles listed in MEDLINE and International Pharmaceutical Abstracts, with no limitation on year. These were supplemented by educational materials from conferences.

RESULTS

The efficacy and tolerability of zaleplon have been documented in the literature. Zaleplon has been shown to improve sleep variables in comparison with placebo. Like most hypnotic agents, zaleplon can be used for problems of sleep initiation at the beginning of the night, but its short duration of clinical effect may also allow patients to take it later in the night without residual effects the next morning. Zaleplon can be taken < or = 2 hours before awakening without "hangover" effects. It is generally well tolerated, with headache being the most commonly reported adverse event in clinical trials (15%-18%). Compared with flurazepam, a long-acting benzodiazepine sedative-hypnotic agent, zaleplon causes significantly less psychomotor and cognitive impairment (P < 0.001). Zaleplon has not been studied in pregnant women or children. The dose of zaleplon should be individualized; the recommended daily dose for most adults is 10 mg.

CONCLUSIONS

Insomnia has a substantial impact on daily functioning. If pharmacologic treatment is indicated for insomnia, the choice of an agent should be guided by individual patient characteristics.

摘要

背景

失眠是对睡眠质量差或睡眠时间不足的主观抱怨,会对日常功能产生不利影响。在过去40年里,失眠的治疗已从使用巴比妥类药物转向使用苯二氮䓬类催眠药。然而,与后者相关的问题(如次日镇静、反弹性失眠、依赖性和耐受性)促使了其他药物的研发。

目的

本综述介绍最近获批的非苯二氮䓬类药物扎来普隆。

方法

通过检索MEDLINE和《国际药学文摘》中列出的英文文章来确定扎来普隆的研究,对年份无限制。这些研究还得到了会议教育资料的补充。

结果

扎来普隆的疗效和耐受性已在文献中得到记载。与安慰剂相比,扎来普隆已被证明可改善睡眠变量。与大多数催眠药一样,扎来普隆可用于解决夜间开始时的入睡问题,但其临床作用持续时间短,也可让患者在夜间较晚时服用,且次日早晨无残留影响。扎来普隆可在醒来前≤2小时服用而无“宿醉”效应。它总体耐受性良好,头痛是临床试验中最常报告的不良事件(15%-18%)。与长效苯二氮䓬类镇静催眠药氟西泮相比,扎来普隆引起的精神运动和认知损害明显更少(P<0.001)。尚未在孕妇或儿童中对扎来普隆进行研究。扎来普隆的剂量应个体化;大多数成年人的推荐日剂量为10毫克。

结论

失眠对日常功能有重大影响。如果失眠需要药物治疗,药物的选择应根据患者个体特征来指导。

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Clin Ther. 2000 Nov;22(11):1254-67. doi: 10.1016/s0149-2918(00)83024-6.
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