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[当月药物。利莫那班(Acomplia):内源性大麻素系统的首个CB1受体拮抗剂]

[Medication of the month. Rimonabant (Acomplia): first CB1 receptor antagonist of the endocannabinoid system].

作者信息

Scheen A J, Van Gaal L F

机构信息

Université de Liège, Belgique.

出版信息

Rev Med Liege. 2008 Jan;63(1):50-5.

Abstract

Rimonabant (Acomplia) is the first selective CB1 receptor blocker of the endocannabinoid system. Clinical trials showed that, compared to placebo, rimonabant 20 mg/ day consistently increases weight loss, reduces waist circumference, improves atherogenic dyslipidaemia (low HDL cholesterol, high triglycerides, high small dense LDL), diminishes insulin resistance, reduces HbA1c levels, and contributes to lower blood pressure and C-reactive protein levels. Almost half of the most important metabolic effects occur beyond weight loss, suggesting direct peripheral effects of rimonabant, especially in visceral adipose tissue as suggested by the increase in adiponectin levels. Rimonabant at a daily dose of 20 mg is indicated as an adjunct to diet and exercise for the treatment of obese patients, or overweight patients with associated risk factor(s) such as type 2 diabetes or dyslipidaemia. Adverse effects concern digestive tract (nausea, mostly transient) and psychological disorders (depressed mood, anxiety), in relation to the mechanism of action of the drug. Therefore, rimonabant is contra-indicated in case of depression and/or in patients receiving antidepressants.

摘要

利莫那班(Acomplia)是首个内源性大麻素系统的选择性CB1受体阻滞剂。临床试验表明,与安慰剂相比,利莫那班每日20毫克持续增加体重减轻、减小腰围、改善致动脉粥样硬化性血脂异常(低高密度脂蛋白胆固醇、高甘油三酯、高小而密低密度脂蛋白)、减轻胰岛素抵抗、降低糖化血红蛋白水平,并有助于降低血压和C反应蛋白水平。几乎一半最重要的代谢作用发生在体重减轻之外,这表明利莫那班有直接的外周作用,尤其是在内脏脂肪组织中,脂联素水平升高就表明了这一点。每日剂量20毫克的利莫那班被指定为饮食和运动的辅助药物,用于治疗肥胖患者或伴有2型糖尿病或血脂异常等相关危险因素的超重患者。不良反应涉及消化道(恶心,大多为短暂性)和心理障碍(情绪低落、焦虑),这与药物的作用机制有关。因此,抑郁症患者和/或正在服用抗抑郁药的患者禁用利莫那班。

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