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Pharmacodynamics of Vildagliptin in Patients With Type 2 Diabetes During OGTT
Author(s) -
He YanLing,
Wang Yibin,
Bullock Julie M.,
Deacon Carolyn F.,
Holst Jens Juul,
Dunning Beth E.,
LiguerosSaylan Monica,
Foley James E.
Publication year - 2007
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006299137
Subject(s) - vildagliptin , medicine , pharmacodynamics , glucagon , crossover study , diabetes mellitus , insulin , endocrinology , type 2 diabetes , type 2 diabetes mellitus , dipeptidyl peptidase 4 , oral administration , dipeptidyl peptidase 4 inhibitor , incretin , meal , placebo , pharmacokinetics , alternative medicine , pathology
This randomized, open‐label, placebo‐controlled, 7‐period crossover study assessed dose‐response relationships following single oral doses (10–400 mg) of vildagliptin in 16 patients with type 2 diabetes mellitus. Plasma levels of parent drug, dipeptidyl peptidase‐4 activity, glucose, insulin, and glucagon were measured during 75‐g oral glucose tolerance tests performed after an overnight fast, 30 minutes after drug administration. The t max for parent drug was observed between 0.5 and 1.5 hours postdose. Both C max and AUC 0–8 h increased dose proportionately. Both onset and duration of dipeptidyl peptidase‐4 inhibition were dose dependent, but >90% inhibition occurred within 45 minutes and was maintained for ≥4 hours after each dose. Glucose excursions and glucagon levels during oral glucose tolerance tests were significantly and similarly decreased after each dose of vildagliptin, and insulin levels were significantly and similarly increased after each dose level. Unlike findings during mixed‐meal challenges, vildagliptin increases plasma insulin levels during oral glucose tolerance tests in patients with type 2 diabetes mellitus.