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Vildagliptin: a review of its use in the management of type 2 diabetes mellitus.

机译:维格列汀:其在2型糖尿病治疗中的应用综述。

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摘要

Vildagliptin (Galvus) is an antihyperglycaemic agent that selectively inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme. Such inhibition prevents the degradation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This results in improved glycaemic control as determined by glycated haemoglobin (HbA(1c)) and fasting plasma glucose (FPG) levels, and, in addition, an enhancement of pancreatic alpha- and beta-cell function. Vildagliptin is indicated in the EU and elsewhere in the world for the management of type 2 diabetes mellitus in combination with metformin, a sulfonylurea or a thiazolidinedione in patients with inadequate glycaemic control following monotherapy. Vildagliptin is also available as a fixed-dose formulation with metformin (Eucreas).Oral vildagliptin in combination with metformin, a sulfonylurea or a thiazolidinedione improved glycaemic control in adults with type 2 diabetes and appeared to slow the progression of beta-cell degeneration in trials of 24-52 weeks' duration. In trials in patients with diabetes inadequately controlled with metformin, vildagliptin provided an additional reduction of HbA(1c) levels of 1.1% and was shown to be as effective as pioglitazone as add-on therapy in a noninferiority trial. Vildagliptin had a low risk of hypoglycaemia, was weight-neutral overall and was generally well tolerated. Further investigation is required to accurately position vildagliptin relative to other, well established antidiabetic agents. However, the addition of vildagliptin expands the range of treatment options available, and as such, offers further potential for the management of patients with type 2 diabetes that is inadequately controlled with monotherapy.
机译:维格列汀(Galvus)是一种抗高血糖药,可选择性抑制二肽基肽酶4(DPP-4)酶。这种抑制作用可防止肠降血糖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)降解。通过糖化血红蛋白(HbA(1c))和空腹血浆葡萄糖(FPG)水平确定,这可以改善血糖控制,此外,还可以增强胰腺α和β细胞功能。在欧盟和世界其他地方,维尔格列汀在单药治疗后血糖控制不足的患者中与二甲双胍,磺酰脲或噻唑烷二酮联用治疗2型糖尿病。维达列汀也可以与二甲双胍(Eucreas)一起制成固定剂量制剂。口服维达列汀联合二甲双胍,磺酰脲或噻唑烷二酮可改善2型糖尿病成年人的血糖控制,并且在试验中似乎减慢了β细胞变性的进程持续时间为24-52周。在二甲双胍控制不充分的糖尿病患者试验中,维格列汀可进一步降低HbA(1c)水平1.1%,并且在非劣效性试验中显示出与吡格列酮一样有效。维格列汀低血糖的风险低,总体上是体重中性的,并且一般耐受性良好。需要进一步研究以使维格列汀相对于其他公认的抗糖尿病药准确定位。但是,维格列汀的添加扩大了可用的治疗选择范围,因此,为单药治疗无法充分控制的2型糖尿病患者的治疗提供了进一步的潜力。

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