Sitagliptin: a novel agent for the management of type 2 diabetes mellitus.
Author(s): Pham DQ, Nogid A, Plakogiannis R.
Affiliation(s): College of Pharmacy and Health Sciences, Western University, Pomona, CA
91766-1854, USA. dqpham@westernu.edu
Publication date & source: 2008, Am J Health Syst Pharm. , 65(6):521-31
PURPOSE: The pharmacologic, pharmacokinetic, safety, clinical efficacy, and role
of sitagliptin in the management of type 2 diabetes mellitus are reviewed.
SUMMARY: Sitagliptin is a dipeptidyl-peptidase IV (DPP4) inhibitor that increases
insulin release and decreases glucagon levels by preventing the activation of
incretin hormones--glucagon-like peptide-1 and glucose-dependent insulinotropic
polypeptide. The clinical trials reviewed provide evidence that sitagliptin,
either alone or in combination with metformin or thiazolidinediones, is effective
in reducing glycosylated hemoglobin (HbA(1c)), fasting plasma glucose, and
two-hour postprandial glucose levels in patients with type 2 diabetes.
Specifically, sitagliptin has a role in patients who have been compliant with
their oral hypoglycemic agents but unable to attain target HbA(1c) values with
monotherapy and lifestyle modifications. Sitagliptin is generally well tolerated,
with the frequency of adverse events being similar to placebo and a low frequency
of hypoglycemia. Sitagliptin does not appear to alter the pharmacokinetics of
metformin, rosiglitazone, glyburide, simvastatin, warfarin, or oral
contraceptives. The addition of sitagliptin to a patient's oral antidiabetic
regimen would necessitate close monitoring for adverse events and possible drug
interactions. The sitagliptin dosage recommended by the manufacturer is 100 mg
once daily as monotherapy or in combination with metformin or a
thiazolidinedione. No formal pharmacoeconomic evaluations of sitagliptin therapy
have been conducted.
CONCLUSION: Sitagliptin, a DPP4 inhibitor, offers a novel treatment option for
patients with type 2 diabetes mellitus.
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