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催眠药氟硝西泮和三唑仑在人体中的活性。

Activity of the hypnotics, flunitrazepam and triazolam, in man.

作者信息

Nicholson A N, Stone B M

出版信息

Br J Clin Pharmacol. 1980 Feb;9(2):187-94. doi: 10.1111/j.1365-2125.1980.tb05832.x.

Abstract

Effects of flunitrazepam and triazolam (0.25 and 0.5 mg) on sleep and on performance were studied in six healthy adult males. Sleep was assessed by electroencephalography and analogue scales, and performance by a visuo-motor coordination task. Over the same dose range triazolam had a more pronounced effect than flunitrazepam. Total sleep time was increased by 0.25 and 0.5 mg triazolam, and by 0.5 mg flunitrazepam. Both drugs decreased awake activity and drowsy sleep, though the effect of flunitrazepam was limited to the 0.5 mg dose and restricted to the first 6 h after sleep onset. There were no changes in slow wave sleep. Latency to the first period of rapid eye movement (REM) sleep was increased with 0.5 mg triazolam, and when doses were combined (0.25-0.5 mg) the latencies with both drugs were increased. Both doses of triazolam reduced the duration and percentage of REM sleep during the early part of the night, though the whole night duration of REM sleep was not changed. After the morning ingestion of 0.25 mg flunitrazepam performance was impaired for 2.0 h, but there were no residual effects when 0.25 or 0.5 mg were taken at night. With the morning ingestion of 0.25 mg triazolam performance was impaired from 0.5 to at least 5.0 h after ingestion. There were no residual effects with 0.25 mg overnight, but with 0.5 mg triazolam there was an effect on performance 10 h after ingestion with recovery within 1.5 h (11.5 h of ingestion). Triazolam (0.25 mg) and 0.5 mg flunitrazepam provide useful hypnotic activity when impaired performance the next day is to be avoided. The activity of 0.5 mg triazolam is accompanied by only limited residual sequelae compared with some other benzodiazepines of comparable efficacy, and so may prove to be useful when a more powerful effect is required.

摘要

在6名健康成年男性中研究了氟硝西泮和三唑仑(0.25毫克和0.5毫克)对睡眠和行为表现的影响。通过脑电图和模拟量表评估睡眠,通过视觉运动协调任务评估行为表现。在相同剂量范围内,三唑仑的作用比氟硝西泮更明显。0.25毫克和0.5毫克三唑仑以及0.5毫克氟硝西泮均可增加总睡眠时间。两种药物均减少清醒活动和昏昏欲睡的睡眠,尽管氟硝西泮的作用仅限于0.5毫克剂量且仅限于睡眠开始后的前6小时。慢波睡眠无变化。0.5毫克三唑仑可增加快速眼动(REM)睡眠第一阶段的潜伏期,当联合使用两种药物的剂量(0.25 - 0.5毫克)时,两种药物的潜伏期均增加。两种剂量的三唑仑均减少夜间早期REM睡眠的持续时间和百分比,尽管REM睡眠的整夜持续时间未改变。早晨服用0.25毫克氟硝西泮后,行为表现受损2.0小时,但晚上服用0.25毫克或0.5毫克时无残留影响。早晨服用0.25毫克三唑仑后,行为表现在服药后0.5至至少5.0小时受损。晚上服用0.25毫克无残留影响,但服用0.5毫克三唑仑后,服药后10小时对行为表现仍有影响,1.5小时内恢复(服药后11.5小时)。当要避免次日行为表现受损时,三唑仑(0.25毫克)和0.5毫克氟硝西泮可提供有效的催眠作用。与其他一些疗效相当的苯二氮䓬类药物相比,0.5毫克三唑仑的作用仅伴有有限的残留后遗症,因此当需要更强效的作用时可能证明是有用的。

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本文引用的文献

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