奈法唑酮:其神经化学机制、药代动力学和治疗重度抑郁症的应用综述

Handan He, J. Steven Richardson
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引用次数: 6

摘要

奈法唑酮是一种具有苯哌嗪结构的抗抑郁药物,其药理学特征与其他抗抑郁药物不同。像许多其他抗抑郁药一样,奈法唑酮抑制突触间隙对去甲肾上腺素和血清素的再吸收。与其他抗抑郁药不同,奈法唑酮也是5-HT2 - 5-羟色胺能受体的有效拮抗剂。此外,奈法唑酮是α1-肾上腺素能受体的弱拮抗剂,但对胆碱能、组胺能或多巴胺能受体的亲和力很小或没有亲和力。在安慰剂对照的临床试验中,奈法唑酮被发现是一种有效的抗抑郁药物,与丙咪嗪相比,它对心血管的作用最小,副作用也明显更少。由于奈法唑酮是一种有效的抗抑郁药,严重不良反应发生率低,它可能特别适用于对其他抗抑郁药的抗胆碱能或5 -羟色胺能副作用不能耐受的重性抑郁症患者,或对其他抗抑郁药治疗无效的患者。本文就奈法唑酮的作用机制、药代动力学及抗抑郁疗效进行综述。
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Nefazodone: A Review of Its Neurochemical Mechanisms, Pharmacokinetics, and Therapeutic Use in Major Depressive Disorder

Nefazodone, an antidepressant agent with a phenylpiperazine structure, has a pharmacological profile that is distinct from other antidepressant drugs. Like many other antidepressants, nefazodone inhibits the reuptake of norepinephrine and serotonin from the synaptic cleft. Unlike other antidepressants, nefazodone is also a potent antagonist of 5-HT2 serotonergic receptors. In addition, nefazodone is a weak antagonist of α1-adrenergic receptors, but has little or no affinity for cholinergic, histaminergic, or dopaminergic receptors. In placebo-controlled clinical trials, nefazodone has been found to be an effective antidepressant drug with minimal cardiovascular action and significantly fewer side effects than imipramine. Since nefazodone is an effective antidepressant with a low incidence of serious adverse effects, it may be particularly useful in major depressive disorder patients who are intolerant of the anticholinergic or serotonergic side effects of other antidepressants, or who do not respond to treatment with other antidepressant agents. In this paper, we review the mechanisms of action, the pharmacokinetics, and the antidepressant efficacy of nefazodone.

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