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咪达唑仑和三唑仑:单次睡前剂量后的催眠作用及残留效应

Midazolam and triazolam: hypnotic action and residual effects after a single bedtime dose.

作者信息

Borbély A A, Loepfe M, Mattmann P, Tobler I

出版信息

Arzneimittelforschung. 1983;33(10):1500-2.

PMID:6140018
Abstract

The hypnotic action and residual effects of a single bedtime dose of 8-chloro-6(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine (midazolam, Ro 21-3981, Dormicum) (7.5 or 15 mg) or 8-chloro-6(o-chlorophenyl)-1-methyl-4H-S-triazolo[4,3-a] [1,4]benzodiazepine (triazolam) (0.25 or 0.5 mg) were investigated in young, healthy adults. Motor activity was continuously recorded by a wrist-worn activity monitor. In comparison to placebo, all compounds reduced night-time motor activity in the first half, but not in the second half of the night. Subjects rated their sleep as more quiet. Neither the spontaneous daytime motor activity nor the self-rated state in the morning and at noon was affected by drug intake in the preceding night. Performance in the morning as measured by a psychomotor test was significantly impaired only after triazolam 0.5 mg. There was no evidence for rebound insomnia in the 3 nights following drug intake. The results indicate that midazolam 15 mg and triazolam 0.25 mg have a reliable hypnotic action without significant residual sequelae.

摘要

对年轻健康成年人研究了单剂量睡前服用8-氯-6-(2-氟苯基)-1-甲基-4H-咪唑并[1,5-a][1,4]苯二氮䓬(咪达唑仑,Ro 21-3981,多美康)(7.5或15毫克)或8-氯-6-(邻氯苯基)-1-甲基-4H-三唑并[4,3-a][1,4]苯二氮䓬(三唑仑)(0.25或0.5毫克)的催眠作用及残留效应。通过佩戴在手腕上的活动监测器持续记录运动活动。与安慰剂相比,所有化合物在前半夜均降低了夜间运动活动,但在后半夜未降低。受试者将他们的睡眠评价为更安静。前一晚服药对白天的自发运动活动以及上午和中午的自我评定状态均无影响。仅在服用0.5毫克三唑仑后,通过精神运动测试测得的上午表现才受到显著损害。在服药后的3个晚上没有反弹性失眠的证据。结果表明,15毫克咪达唑仑和0.25毫克三唑仑具有可靠的催眠作用且无明显残留后遗症。

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