Diazepam and its hydroxylated metabolites: studies on sleep in healthy man

Abstract

1 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.

2 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.

3 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.

4 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.