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Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT.
He, Yan-Ling; Wang, Yibin; Bullock, Julie M; Deacon, Carolyn F; Holst, Jens Juul; Dunning, Beth E; Ligueros-Saylan, Monica; Foley, James E.
Afiliación
  • He YL; DMSc, Exploratory Development, Novartis Institutes of Biomedical Research Inc, 400 Technology Square, Building 605, Rm 811, Cambridge, MA 02139-3584, USA. yanling.he@novartis.com
J Clin Pharmacol ; 47(5): 633-41, 2007 May.
Article en En | MEDLINE | ID: mdl-17442688
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.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirrolidinas / Adamantano / Glicoproteínas / Diabetes Mellitus Tipo 2 / Inhibidores de la Dipeptidil-Peptidasa IV / Inhibidores de la Adenosina Desaminasa / Hipoglucemiantes / Nitrilos Tipo de estudio: Clinical_trials Límite: Female / Humans / Male / Middle aged Idioma: En Revista: J Clin Pharmacol Año: 2007 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Buscar en Google
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Imprimir
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirrolidinas / Adamantano / Glicoproteínas / Diabetes Mellitus Tipo 2 / Inhibidores de la Dipeptidil-Peptidasa IV / Inhibidores de la Adenosina Desaminasa / Hipoglucemiantes / Nitrilos Tipo de estudio: Clinical_trials Límite: Female / Humans / Male / Middle aged Idioma: En Revista: J Clin Pharmacol Año: 2007 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido