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诺米芬辛:其药理特性及对抑郁症治疗效果的综述

Nomifensine: A review of its pharmacological properties and therapeutic efficacy in depressive illness.

作者信息

Brogden R N, Heel R C, Speight T M, Avery G S

出版信息

Drugs. 1979 Jul;18(1):1-24. doi: 10.2165/00003495-197918010-00001.

Abstract

Nomifensine is a tetrahydoisoquinoline antidepressant which is chemically unrelated to the tricyclic or tetracyclic antidepressants, the monoamine oxidase inhibitors or the recently introduced agents. Nomifensine resembles the tricyclic antidepressants in many of its pharmacological effects in animal models of depressive illness, but differs from them in that it strongly inhibits the re-uptake of dopamine as well as noradrenaline and is a relatively weak inhibitor of serotonin uptake. It has an overall efficacy comparable with that of imipramine and amitriptyline in depressive illness, but at dosages which have achieved a similar overall clinical improvement, nomifensine causes little or no sedation, fewer and milder anticholinergic side effects, and also appears less likely than these drugs to cause serious cardiotoxicity on overdosage. Nomifensine may aggravate the psychopathology of patients with schizo-affective disorders and intensification of the psychosis may require neuroleptic therapy. Nomifensine also has antianxiety activity, but its role in treating anxiety associated with primary depression has still to be clarified. Nomifensine appears to be well tolerated by the elderly.

摘要

诺米芬辛是一种四氢异喹啉类抗抑郁药,其化学结构与三环或四环抗抑郁药、单胺氧化酶抑制剂或最近推出的药物无关。在抑郁疾病动物模型中,诺米芬辛在许多药理作用上类似于三环抗抑郁药,但不同之处在于它强烈抑制多巴胺以及去甲肾上腺素的再摄取,并且是一种相对较弱的5-羟色胺摄取抑制剂。在抑郁疾病中,它的总体疗效与丙咪嗪和阿米替林相当,但在达到类似总体临床改善的剂量下,诺米芬辛几乎不引起或不引起镇静作用,抗胆碱能副作用较少且较轻,并且在过量用药时似乎比这些药物引起严重心脏毒性的可能性更小。诺米芬辛可能会加重分裂情感性障碍患者的精神病理学症状,精神病症状加重可能需要使用抗精神病药物治疗。诺米芬辛也具有抗焦虑活性,但其在治疗与原发性抑郁症相关的焦虑症中的作用仍有待阐明。诺米芬辛似乎在老年人中耐受性良好。

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