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短效和长效催眠药在临床医学中的应用。

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

作者信息

Nicholson A N

出版信息

Br J Clin Pharmacol. 1981;11 Suppl 1(Suppl 1):61S-69S. doi: 10.1111/j.1365-2125.1981.tb01841.x.

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.

摘要
  1. 本文参考药代动力学、残留后遗症、疗效及不良反应,对短效和长效苯二氮䓬类药物的活性进行了综述。2. 某些苯二氮䓬类药物可能对行为表现无明显影响,如去甲西泮和氯巴占,且残留后遗症的持续时间可能与消除半衰期无明显关联(如地西泮,氟硝西泮可能也是如此)。然而,平均半衰期小于8小时的苯二氮䓬类药物可能会有残留后遗症,而平均半衰期大于16小时的催眠药可能会导致次日行为表现受损和/或抗焦虑作用。3. 氯氮䓬钾15毫克及其长效代谢产物去甲西泮,似乎是治疗焦虑继发失眠的首选药物。对于无明显精神病理学问题的失眠患者,替马西泮10 - 20毫克、三唑仑0.125 - 0.25毫克,偶尔使用地西泮5 - 10毫克,可作为初始治疗方法。盐酸氟西泮15 - 30毫克、硝西泮5 - 10毫克及氟硝西泮1毫克及以上,有持续的残留效应,应留用于难治性患者,以及次日行为表现有一定受损可接受的患者。4. 几乎没有证据表明正确使用短效催眠药三唑仑和替马西泮会导致撤药时睡眠恶化。然而,某些苯二氮䓬类药物可能会导致睡眠障碍和/或反弹性失眠,硝西泮和氟硝西泮可能与此有关。

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本文引用的文献

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Five Weeks to Escape the Sleeping-pill Habit.五周摆脱安眠药成瘾
Br Med J. 1965 Nov 6;2(5470):1093-5. doi: 10.1136/bmj.2.5470.1093.
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Hypnotics: rebound insomnia and residual sequelae.催眠药:反弹性失眠和残留后遗症。
Br J Clin Pharmacol. 1980 Mar;9(3):223-5. doi: 10.1111/j.1365-2125.1980.tb04829.x.
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Activity of the hypnotics, flunitrazepam and triazolam, in man.
Br J Clin Pharmacol. 1980 Feb;9(2):187-94. doi: 10.1111/j.1365-2125.1980.tb05832.x.
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Residual effects of hypnotics.催眠药的残留效应。
Psychopharmacologia. 1972;25(2):117-32. doi: 10.1007/BF00423189.
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The residual effects of flurazepam.氟西泮的残留效应。
Psychopharmacologia. 1973 Sep 28;32(3):223-35. doi: 10.1007/BF00422145.
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Blood level profile in man following chronic oral administration of flurazepam hydrochloride.
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