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Pharmacology: Pharmacodynamics: Sitagliptin is a dipeptidyl peptidase IV (DPP-IV) inhibitor.
Sitagliptin inhibit dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels.
lncretin hormones (eg. glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decrease glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-IV enzyme.
Pharmacokinetics: Absorption: Rapid.
Distribution: ~198 L.
Protein binding: 38%.
Metabolism: Not exclusively metabolized, minor metabolism via CYP3A4 and 2C8 to metabolites (inactive).
Bioavailability: ~87%.
Half-life elimination: 12.4 hours.
Time to peak, plasma: 1 to 4 hours.
Excretion: Urine 87% (~79% as unchanged drug, 16% as metabolites).
Feces 13%.
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