Scheen A J, Van Gaal L F
Université de Liège, Service de Diabétologie, Nutrition et Maladies métaboliques, CHU de Liège, Belgique.
Rev Med Liege. 2012 Feb;67(2):91-7.
Linagliptin (Trajenta) is a selective inhibitor of dipeptidyl peptidase-4, an enzyme that degrades two incretin hormones, GLP-1 ("Glucagon-Like Peptide-1") and GIP ("Glucose-dependent Insulinotropic Polypeptide"). As other molecules belonging to this pharmacological class, linagliptin improves blood glucose control of type 2 diabetic patients, without increasing hypoglycaemic risk, without promoting weight gain and with a good clinical and biological tolerance profile. Both efficacy and safety have been demonstrated in randomized controlled trials as monotherapy or in combination with other glucose-lowering agents, independent of demographic or clinical patient's characteristics. The pharmacokinetics specificity of linagliptin comprises its biliary excretion, with low hepatic metabolism (no drug-drug interactions) and, in contrast to other gliptins, its negligible renal elimination. Because of these favourable properties, linagliptin may be used without dose adjustment (5 mg once a day) in patients with renal impairment, as well as in elderly people.
利那格列汀（欧唐宁）是二肽基肽酶-4的选择性抑制剂，该酶可降解两种肠促胰岛素激素，即胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）。与该药理学类别中的其他分子一样，利那格列汀可改善2型糖尿病患者的血糖控制，不会增加低血糖风险，不会促进体重增加，且具有良好的临床和生物学耐受性。在随机对照试验中，无论是作为单一疗法还是与其他降糖药物联合使用，利那格列汀的疗效和安全性均已得到证实，且不受患者人口统计学或临床特征的影响。利那格列汀的药代动力学特性包括经胆汁排泄、肝脏代谢低（无药物相互作用），与其他格列汀类药物不同的是，其经肾脏清除可忽略不计。由于这些有利特性，利那格列汀在肾功能损害患者以及老年人中使用时无需调整剂量（每日一次，每次5mg）。
