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夸西泮:催眠疗效与副作用。

Quazepam: hypnotic efficacy and side effects.

作者信息

Kales A

机构信息

Sleep Research and Treatment Center, Hershey Medical Center, Hershey, PA 17033.

出版信息

Pharmacotherapy. 1990;10(1):1-10; discussion 10-2.

PMID:1969151
Abstract

Quazepam is a benzodiazepine hypnotic that can be useful in the adjunctive pharmacologic treatment of insomnia. It is slowly eliminated due to the long elimination half-lives of the parent compound and its two active metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam. This drug is recommended in doses of 15 mg for adults and 7.5 mg for geriatric patients. Sleep laboratory studies and clinical trials have shown that the 15 mg dose is quite efficacious for inducing and maintaining sleep not only with initial and short-term use but also with continued use. The 7.5 mg dose which has been studied less extensively has also been shown to be effective for inducing and maintaining sleep. There is considerable evidence of carryover effectiveness both during drug administration and after withdrawal. Thus, rebound phenomena are not observed during administration (early morning insomnia and daytime anxiety) and after withdrawal (rebound insomnia). Furthermore, certain behavioral side effects that have occurred with certain benzodiazepines (triazolam) have not been reported with quazepam. The only notable side effect seen with quazepam is a variable degree of daytime sedation, which can be minimized by intermittent use of the 15 mg dose when necessary and use of the 7.5 mg dose in the elderly. In comparison to triazolam and temazepam, quazepam is more effective with short-term use, and with continued use it maintains its efficacy in contrast to both of these drugs which show rapid development of tolerance. Most important, quazepam lacks the frequent and severe side effects increasingly reported with triazolam use or following its withdrawal.

摘要

夸西泮是一种苯二氮䓬类催眠药,可用于失眠的辅助药物治疗。由于母体化合物及其两种活性代谢物2-氧代夸西泮和N-去烷基-2-氧代夸西泮的消除半衰期较长,其消除缓慢。该药物推荐的成人剂量为15毫克,老年患者剂量为7.5毫克。睡眠实验室研究和临床试验表明,15毫克剂量不仅在初始和短期使用时,而且在持续使用时,对诱导和维持睡眠都非常有效。研究较少的7.5毫克剂量也已被证明对诱导和维持睡眠有效。有大量证据表明,在给药期间和停药后都有持续的疗效。因此,在给药期间(清晨失眠和日间焦虑)和停药后(反弹性失眠)均未观察到反跳现象。此外,某些苯二氮䓬类药物(三唑仑)出现的某些行为副作用在夸西泮中未被报道。夸西泮唯一值得注意的副作用是不同程度的日间镇静作用,必要时可通过间歇性使用15毫克剂量以及在老年人中使用7.5毫克剂量将其降至最低。与三唑仑和替马西泮相比,夸西泮在短期使用时更有效,并且在持续使用时能维持其疗效,而这两种药物都显示出快速产生耐受性。最重要的是,夸西泮没有三唑仑使用或停药后越来越多地报道的频繁和严重的副作用。

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