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度洛西汀,一种用于治疗重度抑郁症、神经性疼痛以及与更年期相关的血管舒缩症状的5-羟色胺-去甲肾上腺素再摄取抑制剂。

Desvenlafaxine, a serotonin-norepinephrine uptake inhibitor for major depressive disorder, neuropathic pain and the vasomotor symptoms associated with menopause.

作者信息

Pae Chi-Un, Park Min-Hyeon, Marks David M, Han Changsu, Patkar Ashwin A, Masand Prakash S

机构信息

Department of Psychiatry, Holy Family Hospital, The Catholic University of Korea College of Medicine, Sosa-Dong, Wonmi-Gu, Pucheon, Kyounggi-Do, Republic of Korea.

出版信息

Curr Opin Investig Drugs. 2009 Jan;10(1):75-90.

PMID:19127490
Abstract

Desvenlafaxine, a serotonin-norepinephrine reuptake inhibitor (SNRI) developed by Wyeth, is a novel salt form of the isolated major active metabolite of the antidepressant venlafaxine. Desvenlafaxine was developed as a slow-release tablet formulation and rapidly penetrates the brain upon administration supporting its direct effects on neuronal systems of the brain. Unlike various other antidepressants including venlafaxine, desvenlafaxine is not metabolized by cytochrome p450 (CYP) enzyme pathways and is associated with minimal inhibition of CYP enzymes. This feature results in a comparatively low risk of drug-drug interaction and consistent intra-individual and inter-individual pharmacokinetic profiles. Desvenlafaxine has been recently approved by the US FDA for the treatment of major depressive disorder (MDD) based on a series of randomized, double-blind, placebo-controlled clinical trials indicating efficacy and safety for patients with MDD. Studies have also supported the potential utility of desvenlafaxine in the treatment of vasomotor symptoms of menopause, anxiety symptoms and painful physical symptoms. However, concerns including mixed efficacy and adverse events need to be further explored in future studies.

摘要

度洛西汀是惠氏公司研发的一种5-羟色胺-去甲肾上腺素再摄取抑制剂(SNRI),是抗抑郁药文拉法辛分离出的主要活性代谢物的一种新型盐类形式。度洛西汀被开发成缓释片剂剂型,给药后能迅速穿透大脑,这支持了其对大脑神经元系统的直接作用。与包括文拉法辛在内的其他各种抗抑郁药不同,度洛西汀不会通过细胞色素P450(CYP)酶途径代谢,并且对CYP酶的抑制作用极小。这一特性导致药物相互作用的风险相对较低,个体内和个体间的药代动力学特征较为一致。基于一系列随机、双盲、安慰剂对照的临床试验表明度洛西汀对重度抑郁症(MDD)患者有效且安全,该药最近已获得美国食品药品监督管理局(FDA)批准用于治疗重度抑郁症。研究还支持度洛西汀在治疗更年期血管舒缩症状、焦虑症状和疼痛性躯体症状方面的潜在效用。然而,包括疗效和不良事件混杂等问题需要在未来的研究中进一步探讨。 (注:原文中药物名称应为度洛西汀,前面翻译有误,已修正)

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[Non-hormonal treatment for vasomotor symptoms during menopause: role of desvenlafaxine].
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