Sitagliptin is a potent, competitive, first selective and reversible inhibitor of the DPP-IV enzyme in the management of type 2 diabetes mellitus. Article includes the pharmacology, pharmacokinetics, safety, and efficacy of sitagliptin. Results of a small trial comparing sitagliptin with glipizide indicate that both treatments are comparable. The efficacy of sitagliptin has also been demonstrated when used as adjunctive therapy with metformin. Weight gain and hypoglycemia have not been seen with sitagliptin therapy. Sitagliptin increases post-meal insulin secretion ("incretin effect”) by enhancing the postprandial GLP-1 response ("incretin enhancer"), in a glucose-dependent manner. It improves glycaemic control (HbA1c) in type 2 diabetic patients treated by diet alone, by metformin, by sulfonylurea, by glitazone or by a metformin-sufonylurea combined therapy. The glucose-lowering effect is similar to that of glipizide, but with the advantage of no weight gain and no hypoglycaemic episodes. The tolerance to sitagliptin is excellent. Treatment is simple, with 100 mg once daily, without need of titration or home blood glucose monitoring. Review of the literature to date implies sitagliptin may be effective as monotherapy in type 2 diabetes. In addition, existing evidence supports the use of sitagliptin as adjunct therapy to sulfonylureas and metformin.
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