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唑吡坦、三唑仑和替马西泮:对正常志愿者的行为及主观评定影响

Zolpidem, triazolam, and temazepam: behavioral and subject-rated effects in normal volunteers.

作者信息

Rush C R, Griffiths R R

机构信息

Department of Psychiatry, Johns Hopkins University School of Medicine, Baltimore, MD 21224, USA.

出版信息

J Clin Psychopharmacol. 1996 Apr;16(2):146-57. doi: 10.1097/00004714-199604000-00007.

Abstract

Zolpidem is an imidazopyridine hypnotic that is biochemically distinct from classic benzodiazepine agonists in that it may be selective for the BZ1 receptor subtype and shows a different pattern of distribution of binding sites. The present study compared the learning, recall, performance, subject-rated and observer-rated effects of zolpidem, triazolam, and temazepam in 11 healthy humans. Placebo, zolpidem (5, 10, and 20 mg/70 kg), triazolam (0.125, 0.25, and 0.50 mg/70 kg), and temazepam (15, 30, and 60 mg/70 kg) were administered orally in a randomized, double-blind, cross-over design. Zolpidem, triazolam, and temazepam produced orderly dose- and time-related impairment of learning, recall, and performance, and increased subject- and observer-rated estimates of strength of drug effect. The absolute magnitude of these effects at peak effect were comparable across the three compounds. The time to maximal drug effect was faster with zolpidem (0.5-1.0 hours) than with triazolam (1.5-2.0 hours) or temazepam (2-3 hours). These results suggest that despite the somewhat unique benzodiazepine receptor-binding profile of zolpidem, its behavioral and subject-rated effects are similar to those of benzodiazepine hypnotics (i.e., triazolam and temazepam).

摘要

唑吡坦是一种咪唑并吡啶类催眠药,在生化特性上与经典苯二氮䓬类激动剂不同,它可能对BZ1受体亚型具有选择性,并且显示出不同的结合位点分布模式。本研究比较了唑吡坦、三唑仑和替马西泮对11名健康人的学习、记忆、表现、受试者自评和观察者评定的影响。安慰剂、唑吡坦(5、10和20mg/70kg)、三唑仑(0.125、0.25和0.50mg/70kg)以及替马西泮(15、30和60mg/70kg)以随机、双盲、交叉设计口服给药。唑吡坦、三唑仑和替马西泮产生了与剂量和时间相关的学习、记忆和表现损害,并增加了受试者和观察者评定的药物效应强度估计值。这三种化合物在效应峰值时这些效应的绝对幅度相当。唑吡坦达到最大药物效应的时间(0.5 - 1.0小时)比三唑仑(1.5 - 2.0小时)或替马西泮(2 - 3小时)更快。这些结果表明,尽管唑吡坦具有某种独特的苯二氮䓬受体结合特征,但其行为和受试者评定的效应与苯二氮䓬类催眠药(即三唑仑和替马西泮)相似。

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