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曲唑酮:对其药理特性及在抑郁和焦虑治疗中的应用综述

Trazodone: a review of its pharmacological properties and therapeutic use in depression and anxiety.

作者信息

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

出版信息

Drugs. 1981 Jun;21(6):401-29. doi: 10.2165/00003495-198121060-00001.

Abstract

Trazodone is a triazolopyridine derivative with antidepressant activity, that is chemically unrelated to other currently available antidepressants. Its pharmacological properties differ from those of most other antidepressants. Trazodone exhibits antiserotonin activity in animal studies, but its mechanism of action in depressive illness in humans is not clear. It has an overall therapeutic efficacy comparable with imipramine and amitriptyline in depressive illness but, at dosages which have achieved a similar overall clinical improvement, trazodone causes fewer anticholinergic side effects than the tricyclic antidepressants. Trazodone appears also to have activity against the concomitant anxiety in depressed patients and in limited studies was comparable with diazepam and chlordiazepoxide in anxiety neurosis. Trazodone has been reported to be of value in tremors and chronic alcoholism. Studies in animals, limited human studies and the low incidence of cardiovascular side effects in controlled therapeutic trials, suggest that trazodone is less likely than imipramine to cause cardiotoxicity at therapeutic doses, but the effects of overdosage are not known at present. Trazodone appears to be well tolerated by the elderly, seldom aggravates psychotic symptoms and does not produce neurological side effects.

摘要

曲唑酮是一种具有抗抑郁活性的三唑并吡啶衍生物,在化学结构上与目前其他可用的抗抑郁药无关。其药理特性与大多数其他抗抑郁药不同。在动物研究中,曲唑酮表现出抗血清素活性,但其在人类抑郁症中的作用机制尚不清楚。在抑郁症中,它的总体治疗效果与丙咪嗪和阿米替林相当,但在达到相似总体临床改善效果的剂量下,曲唑酮引起的抗胆碱能副作用比三环类抗抑郁药少。曲唑酮似乎对抑郁症患者伴发的焦虑也有作用,在有限的研究中,其在焦虑症中的效果与地西泮和氯氮卓相当。据报道,曲唑酮在震颤和慢性酒精中毒方面有一定价值。动物研究、有限的人体研究以及对照治疗试验中心血管副作用的低发生率表明,在治疗剂量下,曲唑酮比丙咪嗪引起心脏毒性的可能性更小,但目前尚不清楚过量用药的影响。老年人似乎对曲唑酮耐受性良好,很少加重精神症状,也不会产生神经副作用。

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