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[佐匹克隆。实验药理学与临床应用数据]

[Zopiclone. Data of experimental pharmacology and clinical use].

作者信息

Stutzmann J M, Delahaye C, Allain H

机构信息

Rhône-Poulenc Rorer, Département de Biologie, Centre de Recherches de Vitry-Alfortville, Vitry-sur-Seine.

出版信息

Therapie. 1993 Jan-Feb;48(1):33-42.

PMID:8356543
Abstract

Zopiclone is the first of the cyclopyrrolones, a new class of psychotropic agents which is chemically different from the benzodiazepines (BZD). From an experimental point of view it has qualitatively the pharmacological profile of the tranquilizer-hyponotics, and activity quantitatively differs from hypnotic BZD by its lower myorelaxant. The electroencephalographic studies also demonstrated that its power spectrum is characteristic of a product having a tranquilizing hypnotic potential. The cyclopyrrolones interact with GABA ergic neurotransmission, and have a high affinity for GABA receptor complex. They act on sites close to BZD sites, but physically different. The sleep polygraphic studies have shown that zopiclone has a specific profile. It respects the sleep architecture, specially the delta sleep which is even increased, in some studies. Its residual effects are absent or minimal, and its acceptability is good in the usual conditions of hypnotic prescription.

摘要

佐匹克隆是环吡咯酮类药物中的第一种,这是一类新型精神药物,在化学结构上与苯二氮䓬类药物不同。从实验角度来看,它在性质上具有镇静催眠药的药理学特征,并且在活性上与催眠性苯二氮䓬类药物的定量差异在于其较低的肌松作用。脑电图研究也表明,其功率谱是具有镇静催眠潜力的产物的特征。环吡咯酮类药物与γ-氨基丁酸能神经传递相互作用,并且对γ-氨基丁酸受体复合物具有高亲和力。它们作用于靠近苯二氮䓬类药物作用位点但在物理上不同的位点。睡眠多导记录研究表明佐匹克隆具有特定的特征。它尊重睡眠结构,特别是在一些研究中甚至有所增加的慢波睡眠。其残余效应不存在或最小,并且在催眠处方的通常条件下其可接受性良好。

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