SAFETY PROFILE OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS

M. Ganeva
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Abstract

Dipeptidyl peptidase-4 inhibitors (DPP-4 inhibitors) are oral antidiabetic agents commonly used for the treatment of type 2 diabetes mellitus. More than ten years of clinical experience with this group of drugs provides evidence of their efficacy and good tolerability especially in patients at risk of hypoglycemia. DPP-4 inhibitors act by increasing the levels of the incretins glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) and thus augmenting glucose-induced insulin secretion. The enzyme DPP-4 degrades plenty of substrates including chemokines, cytokines, and neuropeptides. Thus the inhibition of DPP-4 may affect many biological and pathological processes. Although rarely DPP-4 inhibitors have been reported to induce the development of infections, heart failure, liver injury and pancreatitis. The long-term effects of DPP-4 inhibition on the immune function are still not clarified. The close monitoring of polymorbid patients using DPP-4 inhibitors, and the reporting of possible adverse reactions associated with these drugs is warranted.
二肽基肽酶-4抑制剂的安全性分析
二肽基肽酶-4抑制剂(DPP-4抑制剂)是一种常用的口服降糖药,用于治疗2型糖尿病。这组药物超过十年的临床经验证明了它们的疗效和良好的耐受性,特别是对有低血糖风险的患者。DPP-4抑制剂的作用是增加胰高血糖素样肽-1 (GLP-1)和葡萄糖依赖性胰岛素促胰岛素肽(GIP)的水平,从而增加葡萄糖诱导的胰岛素分泌。DPP-4酶可降解大量底物,包括趋化因子、细胞因子和神经肽。因此,抑制DPP-4可能影响许多生物学和病理过程。虽然很少有DPP-4抑制剂引起感染、心力衰竭、肝损伤和胰腺炎的报道。抑制DPP-4对免疫功能的长期影响尚不清楚。密切监测使用DPP-4抑制剂的多病患者,并报告与这些药物相关的可能的不良反应是必要的。
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