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1型大麻素受体阻断在降低心脏代谢风险中的作用:安全性、耐受性及治疗潜力

Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: safety, tolerability, and therapeutic potential.

作者信息

Steinberg Benjamin A, Cannon Christopher P

机构信息

Department of Medicine, Johns Hopkins Hospital, Baltimore, Maryland, USA.

出版信息

Am J Cardiol. 2007 Dec 17;100(12A):27P-32P. doi: 10.1016/j.amjcard.2007.10.011.

DOI:10.1016/j.amjcard.2007.10.011
PMID:18154743
Abstract

Rimonabant is the first selective blocker of the cannabinoid-1 receptor in development for the treatment of obesity, diabetes mellitus, and cardiometabolic risk factors. (Recently, an FDA Advisory Committee recommended a delay in the approval of rimonabant because of safety issues that need to be addressed in further studies.) Although it is associated with favorable effects on weight, waist circumference, serum lipids, C-reactive protein, and an improvement in glycemic control in type 2 diabetes, there are concerns about side effects. Generally, rimonabant has been well tolerated, with a primary side effect of nausea. Other side effects seen in trials have been anxiety and depressive symptoms, as well as neurologic events, albeit at low rates. When rimonabant becomes clinically available, physicians should be vigilant regarding the expected side effects and use alternative therapies if needed.

摘要

利莫那班是首个处于研发阶段用于治疗肥胖症、糖尿病和心血管代谢风险因素的大麻素-1受体选择性阻滞剂。(最近,美国食品药品监督管理局咨询委员会建议推迟利莫那班的批准,因为安全性问题需要在进一步研究中解决。)尽管它对体重、腰围、血脂、C反应蛋白有有益影响,并能改善2型糖尿病的血糖控制,但仍存在副作用方面的担忧。总体而言,利莫那班耐受性良好,主要副作用为恶心。试验中观察到的其他副作用包括焦虑和抑郁症状以及神经学事件,尽管发生率较低。当利莫那班上市后,医生应警惕预期的副作用,并在需要时使用替代疗法。

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