The use of short‐ and long‐acting hypnotics in clinical medicine.

Abstract

1 Activity of short‐ and long‐acting benzodiazepines is reviewed with reference to pharmacokinetics and residual sequelae, and to efficacy and adverse effects. 2 Some benzodiazepines may not lead to obvious effects on performance, such as nordiazepam and clobazam, and the persistence of residual sequelae may not relate obviously to elimination half‐lives (as with diazepam and possibly flunitrazepam). However, benzodiazepines with mean half‐lives less than 8 h may have residual sequelae, whereas hypnotics with mean half‐lives greater than 16 h are likely to lead to impared performance and/or anxiolytic effects the next day. 3 Potassium chlorazepate 15 mg, with its long‐ acting metabolite nordiazepam, would seem to be the drug of choice for insomnia secondary to anxiety. For the insomniac without significant psychopathology, temazepam 10‐20 mg, triazolam 0.125‐0.25 mg and for occasional use, diazepam 5‐10 mg, provide the initial approach. Flurazepam hydrochloride 15‐30 mg, nitrazepam 5‐10 mg and flunitrazepam 1 mg and above, have persistent residual effects and should be reserved for refractory patients, and for those in whom some impairment of performance the next day would be acceptable. 4 There is little or no evidence to suggest that the proper use of the short‐acting hypnotics, triazolam and temazepam, leads to a worsening of sleep on withdrawal. However, some benzodiazepines may lead to disturbances of sleep and/or rebound insomnia, and nitrazepam and flunitrazepam may be implicated.

Drug-Alcohol Interactions on Psychomotor Skills: Zopiclone and Flunitrazepam

“…It is possible that 2 mg of flunitrazepam is slightly superior to 7.5 mg of zopiclone in hypnotic potency [29], Our results confirm the findings of earlier studies in which motor impairment and EEG changes characteristic of benzodiazepines have been measurable up to 12-18 h after 1 and 2 mg of flunitrazepam orally [3,8,15]. Similar results have been obtained for other benzodiazepines, especially for those with long elimination half-life or with long-acting active metabolites [3,[22][23][24], and even for those with rapid elimination rate, e.g.. triazo lam and temazepam [15][16][17], provided that fairly high doses are used. There is some evi dence that glutethimide and methaqualone, unless otherwise more harmful, could be safer in this respect [22], As to zopiclone, it had not residual effects in the present study at a dose of 7.5 mg. We think that this lack of hangover, although shown in healthy volunteers, is advanta geous, as residual effects can be serious for ambulant insomniacs who are active in skilled mental or physical work despite sug gestions that in practice the residual effects of hypnotics have no major importance and that chronic insomniacs suffer from hang over similarly after nights on placebo or longacting hypnotics [6], At least results concern ing late adverse effects of hypnotics on per formance of healthy volunteers may well be generalized to a majority of patients receiving hypnotics who may not suffer from severe insomnia [10].…”

The association between benzodiazepine use and sleep quality in residential aged care facilities: a cross-sectional study

“…Australian Therapeutic Guidelines recommend the use of PRN medication in both the treatment of insomnia and anxiety [32]. Historically, short-acting benzodiazepines have been attributed with lower rates of adverse events and lowered risk of residual next-day sequelae such as napping [34]. Clinician awareness of preventing adverse events is seen through prescribing habits and patterns.…”

Daytime Sleepiness and Antihistamines

“…Benzodiazepine hypnotics both induce and maintain sleep \vhether during the usual nighttime hours or during the day (5,6). They increase total sleep time while decreasing stage 1 and wake time.…”