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沙格列汀用于2型糖尿病管理的临床概述。

Clinical overview of saxagliptin for Type 2 diabetes management.

作者信息

Rosenstock Julio

机构信息

a Dallas Diabetes and Endocrine Center, Medical City, 7777 Forest Lane C-685, Dallas, TX 75230, USA.

出版信息

Expert Rev Endocrinol Metab. 2010 Nov;5(6):809-823. doi: 10.1586/eem.10.60.

Abstract

Saxagliptin (Onglyza™, Bristol-Myers Squibb, NJ, USA and AstraZeneca, DE, USA) is a potent, orally active, once-daily dipeptidyl peptidase-4 inhibitor that is indicated as an adjunct to diet and exercise alone, or in combination with metformin, a thiazolidinedione or a sulfonylurea to improve glycemic control in adults with Type 2 diabetes mellitus. By inhibiting dipeptidyl peptidase-4, saxagliptin increases concentrations of the intact forms of the incretin hormones, glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide, prolonging their effects. Saxagliptin also improves β-cell function, increases postprandial insulin secretion and reduces postprandial glucagon secretion. Saxagliptin is generally well tolerated with weight-neutral effects and a low incidence of hypoglycemia. Multicenter randomized trials have shown that saxagliptin as monotherapy, as initial therapy with metformin or as add-on therapy with metformin, a sulfonylurea or a thiazolidinedione leads to significant decreases in glycated hemoglobin levels, fasting and postprandial plasma glucose levels and higher percentages of patients attaining target glycated hemoglobin of less than 7% compared with controls.

摘要

沙格列汀(欧唐宁™,美国新泽西州百时美施贵宝公司和美国德国阿斯利康公司)是一种强效的、口服有效的、每日一次的二肽基肽酶-4抑制剂,适用于单独作为饮食和运动的辅助治疗,或与二甲双胍、噻唑烷二酮类药物或磺脲类药物联合使用,以改善2型糖尿病成人患者的血糖控制。通过抑制二肽基肽酶-4,沙格列汀可提高肠促胰岛素激素胰高血糖素样肽-1和葡萄糖依赖性促胰岛素多肽完整形式的浓度,延长它们的作用时间。沙格列汀还可改善β细胞功能,增加餐后胰岛素分泌并减少餐后胰高血糖素分泌。沙格列汀一般耐受性良好,对体重无影响,低血糖发生率低。多中心随机试验表明,沙格列汀作为单药治疗、与二甲双胍联合作为初始治疗或与二甲双胍、磺脲类药物或噻唑烷二酮类药物联合作为附加治疗,与对照组相比,可显著降低糖化血红蛋白水平、空腹和餐后血糖水平,且达到糖化血红蛋白目标值低于7%的患者百分比更高。

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