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二肽基肽酶-IV(DPP-4)抑制剂维格列汀在2型糖尿病管理中的新作用

Emerging role of dipeptidyl peptidase-IV (DPP-4) inhibitor vildagliptin in the management of type 2 diabetes.

作者信息

Kalra Sanjay

机构信息

Bharti Hospital, Wazir Chand Colony, Kunjpura Road, Kamal, Haryana - 132 001.

出版信息

J Assoc Physicians India. 2011 Apr;59:237-45.

Abstract

Diabetes mellitus (DM) is one of the most common chronic disorders, with increasing prevalence worldwide. Type 2 diabetes (T2DM), a multifaceted disease involving multiple pathophysiological defects, accounts for nearly 85-95% of total reported cases of DM. Chances of developing T2DM are increased by obesity and physical inactivity and are augmented further with age. Two most important unmet needs associated with the management of T2DM are the lack of lasting efficacy in reducing hyperglycemia and failure to target primary causes. Different classes of Oral Hypoglycemic Agents (OHA's) with nearly equipotent efficacy are now available targeting the different pathophysiologic factors contributing to T2DM; however, almost all of them are associated with one or the other kind of adverse effect. Several studies have found that certain diabetes drugs may carry increased cardiovascular (CV) risks compared to others. The new approach in management of T2DM based upon the effects of incretin hormones; Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Vildagliptin is a drug from a new class of medications called dipeptidyl peptidase IV (DPP4) inhibitors. By inhibiting DPP-4, vildagliptin causes an increase in GLP-1, an intestinal hormone that aids in glucose homeostasis and insulin secretion. Vildagliptin has a half-life of about 90 minutes; however, > or = 50% of DPP4 inhibition continues for more than 10 hours, allowing for once- or twice-daily dosing. Clinical trials have shown that vildagliptin is effective in significantly lowering glycosylated hemoglobin (HbA1c), fasting plasma glucose, and prandial glucose levels. beta-cell function may also be improved. The drug has placebo like tolerability and rate of hypoglycemia events. Vildagliptin expands non-injectable treatment options available for management of T2DM patients, who are poorly controlled with monotherapy.

摘要

糖尿病(DM)是最常见的慢性疾病之一,在全球范围内的患病率不断上升。2型糖尿病(T2DM)是一种涉及多种病理生理缺陷的多方面疾病,占报告的DM病例总数的近85 - 95%。肥胖和缺乏身体活动会增加患T2DM的几率,且随着年龄增长这一几率会进一步增加。与T2DM管理相关的两个最重要的未满足需求是降低高血糖缺乏持久疗效以及未能针对主要病因。现在有针对导致T2DM的不同病理生理因素的几类疗效几乎相当的口服降糖药(OHA);然而,几乎所有这些药物都与一种或另一种不良反应相关。多项研究发现,与其他药物相比,某些糖尿病药物可能会增加心血管(CV)风险。基于肠促胰岛素激素;胰高血糖素样肽 - 1(GLP - 1)和葡萄糖依赖性促胰岛素多肽(GIP)的作用,出现了T2DM管理的新方法。维格列汀是一种来自名为二肽基肽酶IV(DPP4)抑制剂的新型药物。通过抑制DPP - 4,维格列汀会使GLP - 1增加,GLP - 1是一种有助于葡萄糖稳态和胰岛素分泌的肠道激素。维格列汀的半衰期约为90分钟;然而,≥50%的DPP4抑制作用会持续超过10小时,允许每日给药一次或两次。临床试验表明,维格列汀可有效显著降低糖化血红蛋白(HbA1c)、空腹血糖和餐后血糖水平。β细胞功能也可能得到改善。该药物具有类似安慰剂的耐受性和低血糖事件发生率。维格列汀扩展了可用于治疗单药治疗控制不佳的T2DM患者的非注射治疗选择。

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