Mikhail Nasser
Endocrinology Division, Olive View-UCLA Medical Center, David Geffen School of Medicine, 14445 Olive View Drive, Sylmar, CA 91342, USA.
Vasc Health Risk Manag. 2008;4(6):1221-7. doi: 10.2147/vhrm.s3374.
Sitagliptin and vildagliptin represent a new class of anti-diabetic agents that enhance the action of incretin hormones through inhibition of dipeptidyl peptidase-4 (DPP-4), the enzyme that normally inactivates incretin hormones. Because of their distinct mechanism of action, DPP-4 inhibitors can be used as add-on therapy to other classes of drugs for treatment of type 2 diabetes. The objective of this review is to critically evaluate clinical trials of sitagliptin and vildagliptin in combination with pioglitazone. The addition of either sitagliptin or vildagliptin to ongoing pioglitazone therapy is associated with reduction in average hemoglobin A1c (HbA1c) levels of approximately 0.7% compared with placebo and 1% compared with baseline after 24 weeks. When started concomitantly in drug-naïve patients, the combination of pioglitazone 30 mg and vildagliptin 100 mg qd reduces HbA1c by 1.9% after 24 weeks, compared with 1.1% with pioglitazone monotherapy. In general, the addition of DPP-4 inhibitors to pioglitazone was well tolerated, did not increase the incidence of hypoglycemia, and did not substantially worsen the weight-gain induced by pioglitazone. The combination of sitagliptpin or vildagliptin with pioglitazone can be a useful therapeutic approach in patients with type 2 diabetes who cannot tolerate metformin or a sulfonylurea.
西他列汀和维格列汀代表了一类新型抗糖尿病药物，它们通过抑制二肽基肽酶-4（DPP-4）来增强肠促胰岛素激素的作用，DPP-4是一种通常使肠促胰岛素激素失活的酶。由于其独特的作用机制，DPP-4抑制剂可作为其他类药物的附加疗法用于治疗2型糖尿病。本综述的目的是严格评估西他列汀和维格列汀与吡格列酮联合应用的临床试验。与安慰剂相比，在正在进行的吡格列酮治疗中添加西他列汀或维格列汀，24周后平均糖化血红蛋白（HbA1c）水平降低约0.7%，与基线相比降低1%。在初治患者中同时开始使用时，吡格列酮30 mg与维格列汀100 mg每日一次联合应用24周后HbA1c降低1.9%，而吡格列酮单药治疗为1.1%。一般来说，在吡格列酮治疗中添加DPP-4抑制剂耐受性良好，不会增加低血糖的发生率，也不会使吡格列酮引起的体重增加显著恶化。对于不能耐受二甲双胍或磺脲类药物的2型糖尿病患者，西他列汀或维格列汀与吡格列酮联合应用可能是一种有效的治疗方法。
