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Pharmacology: Pharmacodynamics: Vildagliptin is a complete dipeptidyl peptidase (DPP)-4 inhibitor; which results in increased postprandial and fasting endogenous levels of the incretins glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) from gut and intestine. Increased levels of these hormones improves glucose-dependent insulin secretion (pancreas secretes insulin when blood sugar is too high after food consumption). However, these hormones are rapidly degraded by the proteolytic enzyme DPP-4. Inhibition of DPP-4 enzyme resulting in prolonged serum level and activity of GLP-1 and GIP; thereby facilitating insulin secretion and decreasing glucagon secretion in type 2 diabetes mellitus.
Pharmacokinetics: Time to peak concentration: 1.7 hours.
Bioavailability: 85%. Concomitant intake of food does not influence the oral bioavailability.
Protein binding: 9.3%.
Vd: 71 L.
Metabolism: Possible hydrolysis via kidneys and dipeptidyl peptidase-4. Not metabolized via CYP450 enzymes.
Excretion: Renal: 85% (major route of elimination), 23% unchanged, fecal: 15%.
Elimination half-life: 3 hours.
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