Kales A, Kales J D
J Clin Psychopharmacol. 1983 Apr;3(2):140-50. doi: 10.1097/00004714-198304000-00038.
Flurazepam, temazepam, and triazolam are compared in terms of initial and short term efficacy, effectiveness during intermediate and long term use, withdrawal effects, and general side effects. The usefulness of temazepam is considerably restricted since the drug is slowly absorbed; peak blood concentrations are not reached until 2 to 3 hours after ingestion. Consequently, while the majority of insomniac patients complain primarily of difficulty falling asleep, temazepam is not effective for this sleep complaint. Further, the drug has an intermediate elimination half-life and induces a significant degree of morning sleepiness (hang-over). Rebound insomnia of a moderate degree occurs with some frequency following withdrawal of temazepam. Triazolam is effective initially and with short term use both for inducing and maintaining sleep. However, much of this effectiveness is lost with continued nightly use over an intermediate period (2 weeks). The drug has a rapid elimination rate; during drug administration, sleep may worsen in the final hours of the night (early morning insomnia), and following drug withdrawal, rebound insomnia is frequent, immediate, and severe. Side effects are frequent and include some morning sleepiness (before tolerance develops) and significant memory impairment and even episodes of amnesia. Triazolam may have a narrow margin of safety in that serious behavioral symptoms have been reported even with a 1-mg dose. Flurazepam is effective both for initiating and maintaining sleep with initial and short term drug administration. Further, its efficacy is maintained not only with intermediate term use but with long term drug use (4 weeks). Flurazepam is a long elimination half-life drug, and there is significant daytime sedation during short term use; with continued use this effect diminishes. Rebound insomnia has not been noted following withdrawal of flurazepam; there is a carry-over effectiveness into the first and second nights of withdrawal, and any withdrawal sleep disturbance would be expected to be infrequent, delayed in appearance, and mild in degree.
对氟西泮、替马西泮和三唑仑在初始及短期疗效、中期和长期使用期间的有效性、戒断效应及一般副作用方面进行了比较。替马西泮的效用受到很大限制,因为该药物吸收缓慢;服药后2至3小时才会达到血药浓度峰值。因此,虽然大多数失眠患者主要抱怨难以入睡,但替马西泮对这种睡眠问题无效。此外,该药物的消除半衰期中等,会导致明显程度的晨起困倦(宿醉)。停用替马西泮后,中度反弹性失眠会经常出现。三唑仑在初始及短期使用时对诱导和维持睡眠均有效。然而,在中期(2周)持续每晚使用后,这种有效性会大幅丧失。该药物的消除速率很快;在用药期间,夜间最后几个小时睡眠可能会恶化(早醒性失眠),停药后,反弹性失眠很常见、出现迅速且严重。副作用很常见,包括一些晨起困倦(在产生耐受性之前)、明显的记忆损害甚至失忆发作。三唑仑的安全范围可能较窄,因为即使服用1毫克剂量也有严重行为症状的报告。氟西泮在初始及短期用药时对启动和维持睡眠均有效。此外,其疗效不仅在中期使用时得以维持,在长期用药(4周)时也能维持。氟西泮是一种消除半衰期长的药物,短期使用时有明显的日间镇静作用;持续使用后这种作用会减弱。停用氟西泮后未观察到反弹性失眠;停药后的第一晚和第二晚有延续性疗效,任何停药后的睡眠障碍预计都不常见、出现延迟且程度较轻。