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用于治疗2型糖尿病的肠促胰岛素类似物和肠促胰岛素增强剂

[Incretin mimetics and incretin enhancers for the treatment of type 2 diabetes].

作者信息

Scheen A J, Radermecker R P, Philips J C, Paquot N

机构信息

Service de diabétologie, nutrition et maladies métaboliques et Unité de pharmacologie clinique, CHU Sart Tilman, B-4000 Liège.

出版信息

Rev Med Suisse. 2007 Aug 29;3(122):1884, 1886-8.

Abstract

Glucagon-like peptide-1 (GLP-1) is a gut hormone secreted in response to a meal ingestion, which is rapidly degraded by a specific enzyme, dipeptidylpeptidase-4 (DPP-4). It enhances insulin secretion in a glucose-dependent manner, inhibits glucagon secretion, retards gastric emptying,... Two pharmacological approaches have been developed to increase the abnormally low GLP-1 levels in type 2 diabetic patients: either to subcutaneously inject an agent closed to GLP-1 (exenatide), which is partially resistant to the action of DPP-4, either to orally administer a selective DPP-4 inhibitor (sitagliptin,...). These new drugs offer improved blood glucose control of type 2 diabetic patients, without inducing hypoglycaemia and with favourable effects on body weight.

摘要

胰高血糖素样肽-1(GLP-1)是一种在进食后分泌的肠促胰岛素激素,它会被特异性酶二肽基肽酶-4(DPP-4)迅速降解。它以葡萄糖依赖的方式增强胰岛素分泌,抑制胰高血糖素分泌,延缓胃排空……目前已开发出两种药理学方法来提高2型糖尿病患者异常低的GLP-1水平:一种是皮下注射一种与GLP-1类似的药物(艾塞那肽),它对DPP-4的作用有部分抗性;另一种是口服选择性DPP-4抑制剂(西格列汀……)。这些新药能改善2型糖尿病患者的血糖控制,不会引起低血糖,并且对体重有有利影响。

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