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首页> 外文期刊>Drugs of today: Medicamentos de actualidad >Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes.
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Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes.

机译：西格列汀：新型DPP-4抑制剂用于治疗2型糖尿病的概况。

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Novel therapeutic strategies for type 2 diabetes are needed, since the current treatment options neither address all pathophysiological mechanisms nor achieve the glycemic target goals. A general islet-cell dysfunction including insulin- and glucagon-secretion defects contributes to the pathophysiology of type 2 diabetes. Improving islet function by incretin hormone action is a novel therapeutic approach. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are important incretin hormones contributing to 50-70% of the stimulation of insulin secretion after a meal. Dipeptidyl-peptidase IV (DPP-4) inhibitors inhibit the degradation of GLP-1 and GIP as well as that of other regulatory peptides. Sitagliptin, a DPP-4 inhibitor, is orally active and has been shown to be efficacious and safe in clinical studies. Sitagliptin has received approval in Mexico, the United States and other countries. Like other DPP-4 inhibitors, sitagliptin reduces hemoglobin A1c (HbA1c), fasting and postprandial glucose by glucose-dependent stimulation of insulin secretion and inhibition of glucagon secretion. Sitagliptin is weight neutral. Indirect measures show a possible improvement of beta-cell function. Sitagliptin does not cause a higher rate of hypoglycemia in comparison to metformin or placebo. This article gives an overview of the mechanisms of action, pharmacology and clinical trial results of sitagliptin.
机译：由于目前的治疗方案既无法解决所有病理生理机制，也无法实现血糖目标，因此需要用于2型糖尿病的新型治疗策略。包括胰岛和胰高血糖素分泌缺陷在内的一般胰岛细胞功能障碍均与2型糖尿病的病理生理有关。通过肠降血糖素激素作用改善胰岛功能是一种新颖的治疗方法。胰高血糖素样肽1（GLP-1）和葡萄糖依赖性促胰岛素肽（GIP）是重要的肠降血糖素激素，在餐后刺激胰岛素分泌的50-70％。二肽基肽酶IV（DPP-4）抑制剂抑制GLP-1和GIP以及其他调节肽的降解。西他列汀，一种DPP-4抑制剂，具有口服活性，在临床研究中已被证明是有效和安全的。西他列汀已在墨西哥，美国和其他国家/地区获得批准。像其他DPP-4抑制剂一样，西他列汀通过葡萄糖依赖性刺激胰岛素分泌和抑制胰高血糖素分泌来降低血红蛋白A1c（HbA1c），禁食和餐后葡萄糖。西他列汀对体重无影响。间接措施显示可能会改善β细胞功能。与二甲双胍或安慰剂相比，西他列汀不会引起更高的低血糖发生率。本文概述了西他列汀的作用机理，药理作用和临床试验结果。

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