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GLP-1 受体激动剂:心血管作用的临床观察。

GLP-1 receptor agonists: a clinical perspective on cardiovascular effects.

机构信息

Department of Physiology, University of Toronto, Canada.

出版信息

Diab Vasc Dis Res. 2012 Apr;9(2):95-108. doi: 10.1177/1479164112441526.

DOI:10.1177/1479164112441526
PMID:22496442
Abstract

The active incretin hormone glucagon-like peptide-1(7-36)amide (GLP-1) is a 30-amino acid peptide that exerts glucoregulatory and insulinotropic actions by functioning as an agonist for the GLP-1 receptor (GLP-1R). In addition to its anti-diabetic effects, GLP-1 has demonstrated cardioprotective actions. Here we review the cardiovascular effects of the GLP-1 analogues currently approved for the treatment of type 2 diabetes, namely exenatide and liraglutide. We discuss their anti-hyperglycaemic efficacy, and offer a clinical perspective of their effects on cardiovascular risk factors such as body weight, blood pressure, heart rate and lipid profiles, as well as their potential consequences on cardiovascular events, such as arrhythmias, heart failure, myocardial infarction and death. Lastly, we briefly review additional GLP-1R agonists in clinical development.

摘要

活性肠促胰岛素激素胰高血糖素样肽-1(7-36)酰胺 (GLP-1) 是一种 30 个氨基酸的肽,通过作为 GLP-1 受体 (GLP-1R) 的激动剂发挥其葡萄糖调节和胰岛素分泌作用。除了具有抗糖尿病作用外,GLP-1 还具有心脏保护作用。在这里,我们回顾了目前批准用于治疗 2 型糖尿病的 GLP-1 类似物的心血管作用,即 exenatide 和 liraglutide。我们讨论了它们的降血糖效果,并从临床角度探讨了它们对体重、血压、心率和血脂谱等心血管危险因素的影响,以及它们对心律失常、心力衰竭、心肌梗死和死亡等心血管事件的潜在影响。最后,我们简要回顾了临床开发中的其他 GLP-1R 激动剂。

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