Stone B M
Br J Clin Pharmacol. 1979;8(1):57S-16S.
The effects of diazepam 5, 10 and 15 mg and its hydroxylated metabolites, 3-hydroxydiazepam (temazepam) 10, 20 and 30 mg and 3-hydroxy, N-desmethyldiazepam (oxazepam) 15, 30 and 45 mg on sleep in healthy man were studied in young adulthood and in middle age. The effectiveness of the drugs for sleep during the day was also investigated. In young adults diazepam and temazepam reduced sleep onset latencies and awake activity and increased total sleep time, and temazepam also reduced drowsy sleep. The activity of oxazepam was similar to that of temazepam except that it had no effect on sleep onset latencies. In middle age the effects of diazepam and temazepam were less pronounced than would be expected from studies in young adulthood. Essentially they reduced awake activity. During the day diazepam increased total sleep time and reduced drowsy sleep in young adults, but temazepam and oxazepam had less activity than would be expected from their effect on night-time sleep. With temazepam there was no increase in total sleep time, although there was reduced awake activity and drowsy sleep, and with oxazepam total sleep time was increased without changes in awake activity and drowsy sleep. It is considered that these hypnotics provide a basis for the management of sleep disturbance in persons involved in skilled activity. In limited doses each drug has hypnotic activity without residual effects on performance.
研究了地西泮5毫克、10毫克和15毫克及其羟基化代谢产物，即3-羟基地西泮（替马西泮）10毫克、20毫克和30毫克以及3-羟基-N-去甲基地西泮（奥沙西泮）15毫克、30毫克和45毫克对年轻成年人及中年健康男性睡眠的影响。还研究了这些药物在白天对睡眠的有效性。在年轻成年人中，地西泮和替马西泮缩短了入睡潜伏期并减少了清醒活动，增加了总睡眠时间，且替马西泮还减少了浅睡眠。奥沙西泮的作用与替马西泮相似，只是对入睡潜伏期没有影响。在中年，地西泮和替马西泮的作用不如在年轻成年人中的研究所预期的那么明显。基本上它们减少了清醒活动。在白天，地西泮增加了年轻成年人的总睡眠时间并减少了浅睡眠，但替马西泮和奥沙西泮的作用比它们对夜间睡眠的影响所预期的要小。使用替马西泮时，总睡眠时间没有增加，尽管清醒活动和浅睡眠减少了，而使用奥沙西泮时，总睡眠时间增加了，清醒活动和浅睡眠没有变化。据认为，这些催眠药为管理从事熟练活动者的睡眠障碍提供了依据。在有限剂量下，每种药物都具有催眠活性且对表现没有残留影响。
