Via practica 4/2010

Sitagliptine – representative of the new group of drugs indicated in the treatment of type 2 diabetes mellitus

Inhibition of the enzyme dipeptidyl peptidase-4 (DDP-4) prevents degradation of in cretin hormones (glucagone–like peptide-1 [GLP-1] and glucose-dependent insulinotropic polypeptide [GIP-1]), that leads to the increase of plasma level of these hormones and prolongation of half-life with following increase of postprandial glucose-dependent insulin secretion and decrease of postprandial glucagon level. At present, there are in Slovak Republic approved two DPP-4 inhibitors: sitagliptine and vildagliptine. The first DPP-4 inhibitor that was introduced to the market in the Slovak Republic in October 2007 was sitagliptin. DPP-4 inhibitors are administered orally. Sitagliptin is indicated in the treatment of type 2 diabetes mellitus as dual therapy in combination with: 1. metformin, in patients with insufficient glycemic control despite maximal tolerated dose of monotherapy with metformin, 2. a sulphonylurea, in patients with insufficient glycemic control despite maximal tolerated dose of a suphonylurea and for whom metformin is inappropriate due to contraindications or intolerance, 3. a thiazolidindione, in patients with insufficient glycemic control and for whom the use of a thiazolidindione is appropriate. Possible is also tripple combination – combination of sitagliptine with metformin and a sulphonylurea, in patients with insufficient glycemic control of dual therapy with metformin and a sulphonylurea. Side effects of sitagliptine are rare, only slight increase of the nasopharyngitis and upper respiratory tract infections was reported. Gastrointestinal side effects in patients receiving sitagliptine are uncommon and regarding glucose–dependent stimulation of insulin secretion sitagliptine does not cause hypoglycemias and weight gain.

Keywords: type 2 diabetes mellitus, sitagliptine, efficacy, tolerability