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氟伏沙明:其药理学及在抑郁症治疗中的应用的最新综述

Fluvoxamine. An updated review of its pharmacology, and therapeutic use in depressive illness.

作者信息

Wilde M I, Plosker G L, Benfield P

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1993 Nov;46(5):895-924. doi: 10.2165/00003495-199346050-00008.

Abstract

Fluvoxamine facilitates serotoninergic neurotransmission via potent and selective inhibition of serotonin (5-hydroxytryptamine; 5-HT) reuptake into presynaptic neurones. The overall antidepressant efficacy of fluvoxamine 100 to 300 mg/day for 4 to 6 weeks in once daily or divided dosage regimens appears to be at least comparable to that of imipramine and similar to that of clomipramine, dothiepin, desipramine, amitriptyline, lofepramine, maprotiline, mianserin and moclobemide. The efficacy of fluvoxamine has been maintained for up to 1 year, but long term data are limited, and there are no comparative studies of fluvoxamine with other selective serotonin reuptake inhibitors. In some studies, fluvoxamine appeared to have an earlier beneficial effect on suicidal ideation and/or anxiety or somatic complaints compared with imipramine, dothiepin and maprotiline. Gastrointestinal adverse effects, especially nausea, are commonly reported with fluvoxamine but are generally mild to moderate in severity. The tolerability profile of fluvoxamine appears to be more favourable than that of tricyclic antidepressants in terms of cardiotoxic and anticholinergic adverse effects, sedation, weight gain and death from overdosage. Thus, fluvoxamine is an effective and well tolerated antidepressant agent that is becoming established as an alternative to older agents in patients with mild, moderate or severe depression. Fluvoxamine may be particularly beneficial in potentially suicidal patients with severe depression, in those with an underlying compulsive personality or cardiovascular disorder, in patients with coexistent anxiety or agitation, and in the elderly.

摘要

氟伏沙明通过有效且选择性地抑制5-羟色胺(5-羟色胺;5-HT)再摄取到突触前神经元中,促进5-羟色胺能神经传递。氟伏沙明100至300mg/天,持续4至6周,每日一次或分剂量给药方案的总体抗抑郁疗效似乎至少与丙咪嗪相当,与氯米帕明、多塞平、地昔帕明、阿米替林、洛非帕明、马普替林、米安色林和吗氯贝胺相似。氟伏沙明的疗效已维持长达1年,但长期数据有限,且尚无氟伏沙明与其他选择性5-羟色胺再摄取抑制剂的比较研究。在一些研究中,与丙咪嗪、多塞平和马普替林相比,氟伏沙明似乎对自杀观念和/或焦虑或躯体不适有更早的有益作用。胃肠道不良反应,尤其是恶心,是氟伏沙明常见的报告不良反应,但严重程度一般为轻至中度。就心脏毒性和抗胆碱能不良反应、镇静、体重增加和过量用药致死而言,氟伏沙明的耐受性似乎比三环类抗抑郁药更有利。因此,氟伏沙明是一种有效且耐受性良好的抗抑郁药,在轻度、中度或重度抑郁症患者中已逐渐成为替代传统药物的选择。氟伏沙明对患有严重抑郁症的潜在自杀患者、具有潜在强迫性人格或心血管疾病的患者、伴有焦虑或激动的患者以及老年人可能特别有益。

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