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氯硝西泮:其药理学特性及在癫痫治疗中的疗效综述

Clonazepam: a review of its pharmacological properties and therapeutic efficacy in epilepsy.

作者信息

Pinder R M, Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1976 Nov;12(5):321-61. doi: 10.2165/00003495-197612050-00001.

Abstract

Clonazepam or 5-(2-chlorphenyl)-1, 3-dihydro-7-nitro-2H-1,4benzodiazepin-2-one, is a close structural and pharmacological relative of nitrazepam. It has a broad spectrum of activity against the various types of epilepsy, and is effective in many patients whose condition has proved resistant to other antiepileptic drugs. Its chief uses are in status epilepticus, in which intravenous clonazepam may replace diazepam as the drug of first choice, and in the minor motor seizures of childhood, particularly petit mal absences, the Lennox-Gastaut syndrome and infantile spasms. Clonazepam is also at least as effective as current treatment in psychomotor and myoclonic epilepsies, but seems unlikely to replace phenytoin and the barbiturates in the treatment of grand mal or focal motor seizures except in patients resistant to standard therapy. Initial success with clonazepam can be followed by loss of effect, but benefit can often be restored, at least initially, by temporary interruption and re-institution of treatment. Side-effects are common with clonazepam. Most patients experience drowsiness and fatigue, which are frequent causes of withdrawal, together with lesser incidences of ataxia, dystonia, hypotonia, and hyperactivity. These effects usually disappear with continued therapy, and are minimised by gradual introduction of the drug over 2-4 weeks. Hypersalivation and excessive bronchial secretion may be a problem in children and infants.

摘要

氯硝西泮,即5 -(2 - 氯苯基)-1,3 - 二氢 - 7 - 硝基 - 2H - 1,4 - 苯并二氮杂卓 - 2 - 酮,是硝西泮在结构和药理上的近亲。它对各种类型的癫痫都有广泛的活性,对许多已证明对其他抗癫痫药物耐药的患者有效。其主要用途是治疗癫痫持续状态,静脉注射氯硝西泮可替代地西泮作为首选药物;也用于治疗儿童的轻微运动性癫痫,特别是失神小发作、伦诺克斯 - 加斯东综合征和婴儿痉挛症。氯硝西泮在精神运动性癫痫和肌阵挛性癫痫的治疗中至少与目前的治疗方法一样有效,但除了对标准治疗耐药的患者外,在治疗大发作或局灶性运动性癫痫时似乎不太可能取代苯妥英钠和巴比妥类药物。使用氯硝西泮最初可能会取得成功,但随后可能会失效,但至少在最初,通过暂时中断治疗然后重新开始治疗,通常可以恢复疗效。氯硝西泮的副作用很常见。大多数患者会出现嗜睡和疲劳,这是停药的常见原因,共济失调、肌张力障碍、肌张力减退和多动的发生率较低。这些影响通常会随着持续治疗而消失,通过在2 - 4周内逐渐引入药物可将其降至最低。流涎过多和支气管分泌物过多可能是儿童和婴儿的一个问题。

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