Three DPP-4 Inhibitors Compared - Similarities and Differences

被引:0
作者
Beil, W. [1 ]
机构
[1] Hannover Med Sch, Inst Klin Pharmakol, D-30625 Hannover, Germany
来源
DIABETES STOFFWECHSEL UND HERZ | 2011年 / 20卷 / 02期
关键词
DPP-4; inhibitors; pharmacodynamics; pharmacokinetics; DIPEPTIDYL PEPTIDASE-4 INHIBITOR; BETA-CELL FUNCTION; DRUG-INTERACTIONS; DIABETES-MELLITUS; P-GLYCOPROTEIN; SITAGLIPTIN; PHARMACOKINETICS; PHARMACODYNAMICS; VILDAGLIPTIN; SAXAGLIPTIN;
D O I
暂无
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
DPP-4 inhibitors glucose-dependently stimulate insulin secretion and inhibit glucagon release; in theory, DDP-4 inhibitors can be combined with any other therapy approach available. Administering metformin together with DPP-4 inhibitors combines a variety of synergetic principles, with metformin increasing GLP-1 formation and DDP-4 inhibitors inhibiting GLP-1 breakdown. DPP-4 inhibitors reduce HbA(1c) values by an additional 0.7 to 1.1 percentage points in combination with metformin, and do not pose any inherent risk of inducing hypoglycaemia. DPP-4 inhibitors vary in certain pharmacodynamic and pharmacokinetic properties. According to the data available, vildagliptin is the fastest acting DDP-4 inhibitor, raising GLP-1 levels to a significantly higher degree in direct comparison with sitagliptin. Sitagliptin is primarily excreted unchanged via the kidneys by P-glycoprotein transport. Vildagliptin is hydrolysed outside the liver, and eliminated as an inactive metabolite via the kidneys. Saxagliptin is mainly metabolised by cytochrome P450 3A4. Of the three DDP-4 inhibitors, vildagliptin has the lowest potential for interaction with other drugs.
引用
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页码:79 / 84
页数:6
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