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度洛西汀用于慢性疼痛管理:药理学与临床应用

[Duloxetine for chronic pain management: pharmacology and clinical use].

作者信息

Masuda Ritsuko, Itoh Miho, Suzuki Toshiyasu

机构信息

Department ofAnesthesiology, Tokai University School of Medicine, Isehara 259-1193.

出版信息

Masui. 2013 Jul;62(7):814-21.

Abstract

The purpose of this article is to provide an overview of some of the important information related to safety and tolerability of duloxetine. Duloxetine, a potent reuptake inhibitor of serotonin and noradrenaline, is effective for the treatment of major depressive disorder, anxiety disorder, and painful diabetic neuropathy (PDN). Duloxetine is safe and well-tolerated across indications, with few reported serious side effects. Common adverse events are consistent with the pharmacology of the molecule and are mainly referable to the gastrointestinal and the nervous systems. Duloxetine should not be used in combination with CYP 1A2 inhibitors or nonselective, irreversible monoamine oxidase inhibitors. Duloxetine has a generally favorable side effect profile and dosing is simple. Nausea is the most common side effect, but it occurs less frequently if treatment is initiated at 30 mg . day-1 and titrated after one week to 60 mg . day-1, an efficacious dosage at which pain relief can occur within one week. Clinical trials have demonstrated the analgesic efficacy of duloxetine for PDN and fibromyalgia in addition to improvements in quality-of-life measurements. Furthermore trials for osteoarthritis, headache, and the pain associated with Parkinson disease may provide insight into alternative uses for duloxetine.

摘要

本文旨在概述与度洛西汀安全性和耐受性相关的一些重要信息。度洛西汀是一种强效的5-羟色胺和去甲肾上腺素再摄取抑制剂,对治疗重度抑郁症、焦虑症及糖尿病性周围神经痛(PDN)有效。度洛西汀在各适应症中均安全且耐受性良好,鲜有严重副作用的报道。常见不良事件与该分子的药理作用相符,主要涉及胃肠道和神经系统。度洛西汀不应与CYP 1A2抑制剂或非选择性、不可逆单胺氧化酶抑制剂联合使用。度洛西汀总体副作用情况良好,给药方式简单。恶心是最常见的副作用,但如果起始治疗剂量为30mg·日-1,并在一周后滴定至60mg·日-1(此为有效剂量,一周内即可缓解疼痛),则恶心的发生频率会降低。临床试验已证明度洛西汀对PDN和纤维肌痛具有镇痛效果,此外还能改善生活质量指标。此外,针对骨关节炎、头痛及帕金森病相关疼痛的试验可能会为度洛西汀的其他用途提供线索。

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