吗氯贝胺：演变、药效学及药代动力学特性
Moclobemide: evolution, pharmacodynamic, and pharmacokinetic properties.
作者信息
Bonnet Udo
机构信息
Rheinische Kliniken Essen, Department of Psychiatry and Psycotherapy, University of Essen, Essen, Germany.
出版信息
CNS Drug Rev. 2002 Fall;8(3):283-308. doi: 10.1111/j.1527-3458.2002.tb00229.x.
Abstract
The benzamide moclobemide is a reversible inhibitor of monoamine-oxidase-A (RIMA). It has been extensively evaluated in the treatment of a wide spectrum of depressive disorders and less extensively in anxiety disorders. While clinical aspects will be presented in a subsequent review, this article focuses primarily on moclobemide's evolution, pharmacodynamic and pharmacokinetic properties. In particular, the effects on neurotransmission and intracellular signal transduction, the neuroendocrine system, the tyramine pressure response and animal models of depression are surveyed. In addition, other CNS effects are reviewed with special respect to experimental serotonergic syndrome, anxiolytic and antinociceptive activity, sleep, cognition and driving performance, neuroprotection and seizures.
摘要
苯甲酰胺类药物吗氯贝胺是一种单胺氧化酶-A（RIMA）的可逆抑制剂。它已在多种抑郁症治疗中得到广泛评估，而在焦虑症治疗中的评估则相对较少。虽然临床方面将在后续综述中阐述，但本文主要关注吗氯贝胺的发展历程、药效学和药代动力学特性。特别对其在神经传递、细胞内信号转导、神经内分泌系统、酪胺升压反应及抑郁症动物模型等方面的作用进行了研究探讨。此外，还对其他中枢神经系统效应进行了综述，尤其涉及实验性血清素综合征、抗焦虑和抗伤害感受活性、睡眠、认知与驾驶性能、神经保护及癫痫发作等方面。
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