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作 者:黄建权[1] 傅得兴[2] 胡欣[2] 张君仁[1]
机构地区:[1]山东大学药学院药物分析研究所,济南250012 [2]卫生部北京医院药学部,北京100730
出 处:《中国新药杂志》2007年第6期486-488,共3页Chinese Journal of New Drugs
摘 要:维达列汀是一种口服有效的特异性二肽基肽酶Ⅳ(DPP-Ⅳ)抑制剂,能增强胰高血糖样肽I(GLP-1)活性和降低2型糖尿病患者的高血糖症状。研究表明,维达列汀无论是单用还是与其他抗糖尿病药物合用,均能明显降低具有临床意义的糖基化血红蛋白(HbA1c)水平,具有良好的耐受性,且无体重增加和浮肿等不良反应,低血糖和胃肠道等不良反应发生率也较低。现对其药理作用、药动学、临床研究和不良反应等进行综述。Vildagliptin is the first in a new class of oral antidiabetic agents known as dipeptidyl peptidase Ⅳ inhibitors (DPP-Ⅳ) or "incretin enhancers". Vildagliptin works by inhibiting DPP-Ⅳ, an enzyme that breaks down GLP-1. By delaying the degradation of GLP-1, vildagliptin extends the action of insulin while also suppressing the release of glucagon. This leads to a reduction in elevated blood glucose levels (hyperglycaemia) that is a characteristic feature of type 2 diabetes. Clinical results indicated that vildagliptin produces clinically significant reductions in HbA1c when used as monotherapy and in combination with other anti-diabetes agents. In general, the drug has proved to be well tolerated with low rates of hypoglycaemia and gastrointestinal side effects and no weight gain or oedema. This review presents the mechanism of action, pharmacokinetics, clinical studies and drug adverse reactions of vildagliptin.
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