Gallwitz Baptist
Dept. Medicine IV, Eberhard Karls University, Tuebingen, Germany.
Vasc Health Risk Manag. 2007;3(2):203-10. doi: 10.2147/vhrm.2007.3.2.203.
Sitagliptin (Januvia, Merck Pharmaceuticals) is a dipeptidyl-peptidase inhibitor (DPP-4 inhibitor) that has recently been approved for the therapy of type 2 diabetes. Like other DPP-4 inhibitors its action is mediated by increasing levels of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). Sitagliptin is effective in lowering HbA1c, and fasting as well as postprandial glucose in monotherapy and in combination with other oral antidiabetic agents. It stimulates insulin secretion when hyperglycemia is present and inhibits glucagon secretion. In clinical studies it is weight neutral. This article gives an overview of the mechanism of action, the pharmacology, and the clinical efficacy and safety of sitagliptin in type 2 diabetes therapy.
西他列汀（佳维乐，默克制药公司）是一种二肽基肽酶抑制剂（DPP - 4抑制剂），最近已被批准用于2型糖尿病的治疗。与其他DPP - 4抑制剂一样，其作用是通过提高肠促胰岛素激素胰高血糖素样肽 - 1（GLP - 1）和胃抑制多肽（GIP）的水平来介导的。西他列汀在单药治疗以及与其他口服抗糖尿病药物联合使用时，能有效降低糖化血红蛋白（HbA1c）、空腹血糖和餐后血糖。当血糖过高时，它刺激胰岛素分泌并抑制胰高血糖素分泌。在临床研究中，它对体重没有影响。本文概述了西他列汀在2型糖尿病治疗中的作用机制、药理学、临床疗效及安全性。
