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J Clin Pharmacol ; 43(2): 171-9, 2003 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-12616670

RESUMEN

To determine the impact of gastric hypoacidity and acidic beverages on delavirdine mesylate pharmacokinetics in HIV-infected subjects, matched subjects with (n = 11) and without (n = 10) gastric hypoacidity received delavirdine 400 mg tid with either water or an acidic beverage (usually orange juice). The pharmacokinetics of delavirdine and its N-desalkyl metabolite were determined over 8 hours after 14 days of each treatment. Gastric pH was measured at baseline and during each pharmacokinetic evaluation. Delavirdine exposure (Cmax, AUC0-->8 h, and Cmin) was approximately 50% lower and the extent of delavirdine metabolism was higher in subjects with gastric hypoacidity. Orange juice produced a lower mean gastric pH compared to water and increased delavirdine absorption by 50% to 70% in subjects with gastric hypoacidity. However, orange juice had a marginal impact on delavirdine exposure in subjects without gastric hypoacidity. HIV-infected subjects with gastric hypoacidity significantly malabsorb delavirdine. Delavirdine administration with acidic beverages improves, but dose not normalize, absorption in these subjects.


Asunto(s)
Delavirdina/farmacocinética , Mucosa Gástrica/metabolismo , Infecciones por VIH/metabolismo , Adulto , Área Bajo la Curva , Bebidas , Citrus , Estudios Cruzados , Delavirdina/metabolismo , Femenino , Mucosa Gástrica/efectos de los fármacos , Humanos , Concentración de Iones de Hidrógeno , Absorción Intestinal , Masculino
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