Aragona M
Psychiatric Clinic, La Sapienza University, Rome, Italy.
Clin Neuropharmacol. 2000 Sep-Oct;23(5):281-3. doi: 10.1097/00002826-200009000-00008.
The imidazopyridine zolpidem is a short-acting hypnotic chemically distinct from benzodiazepines (BZs). According to its peculiar neuropharmacologic activity (selectivity for the omega 1-BZ receptors), zolpidem is expected to be a pure hypnotic, without the other effects of BZs. In particular, it has been stressed that zolpidem is well tolerated in adults and in the elderly, and that tolerance, abuse, dependence, rebound insomnia, and other withdrawal effects do not develop in relation to zolpidem administration. However, despite these assumptions, zolpidem abuse, dependence, and withdrawal effects have been recently discussed and reviewed herein. In addition, the case of a 43-year-old woman who had an epileptic attack after abrupt interruption of an abused, high dose of zolpidem (600 mg/d), is reported and discussed. At the clinical level, it is stressed that the subjective effects ofzolpidem are comparable to those of other BZs, and that abuse, dependence, and withdrawal seizures cannot be avoided simply shifting the regimen of a BZ abuser to zolpidem. At the pharmacologic level, it is important to note that zolpidem's clinical effects cannot be explained on the basis of the old distinction between omega I and 2 receptors because this distinction is no longer valid; the new classification ofGABAA receptor subtypes is reported and zolpidem activity at this level is discussed herein.
咪唑吡啶类药物唑吡坦是一种短效催眠药,其化学结构与苯二氮䓬类(BZs)不同。根据其独特的神经药理活性(对ω1-BZ受体的选择性),唑吡坦有望成为一种单纯的催眠药,而无BZs的其他作用。特别需要强调的是,唑吡坦在成人和老年人中耐受性良好,且与唑吡坦给药相关的耐受性、滥用、依赖性、反弹性失眠及其他戒断效应均不会出现。然而,尽管有这些假设,但唑吡坦的滥用、依赖性及戒断效应最近仍在此处被讨论和综述。此外,本文还报告并讨论了一名43岁女性在滥用高剂量唑吡坦(600mg/d)后突然停药而发生癫痫发作的病例。在临床层面,需强调唑吡坦的主观效应与其他BZs相当,且不能简单地将BZ滥用者的用药方案换成唑吡坦来避免滥用、依赖性及戒断性癫痫发作。在药理层面,需注意唑吡坦的临床效应无法基于ω1和ω2受体之间的旧有区分来解释,因为这种区分已不再有效;本文报告了GABAA受体亚型的新分类,并讨论了唑吡坦在此层面的活性。