Single-dose pharmacokinetics of indinavir and the effect of food.

Antimicrobial Agents and Chemotherapy
K C YehS Waldman

Abstract

Indinavir sulfate is a human immunodeficiency virus type 1 (HIV-1) protease inhibitor indicated for treatment of HIV infection and AIDS in adults. The purpose of this report is to summarize single-dose studies which characterized the pharmacokinetics of the drug and the effect of food in healthy volunteers. Indinavir concentrations in plasma and urine were obtained by high-pressure liquid chromatography and UV detection assay methods. The results indicate that indinavir was rapidly absorbed in the fasting state, with the time to the maximum concentration in plasma occurring at approximately 0.8 h for all doses studied. Over the 40- to 1,000-mg dose range studied, concentrations in plasma and urinary excretion of unchanged drug increased greater than dose proportionally. The nonlinear pharmacokinetics were attributed to the dose-dependent oxidative metabolism of first-pass metabolism as well as to metabolism in the systemic circulation. Renal clearance slightly exceeded the glomerular filtration rate, suggesting a net tubular secretion component. At high concentrations in plasma, tubular secretion appeared to be lowered because there was a trend for a decreased renal clearance. Administration of 400 mg of indinavir sulfate follo...Continue Reading

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Citations

Jan 31, 2002·The Annals of Pharmacotherapy·Brian M Sadler, Daniel S Stein
May 22, 2001·AIDS Patient Care and STDs·M Sarcletti, R Zangerle
Feb 19, 2021·Experimental Biology and Medicine·Nneka Pu KorieOsbourne Quaye
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Jul 3, 2002·Drugs·Lars E Schmidt, Kim Dalhoff
Dec 9, 2020·Drug Development and Industrial Pharmacy·Mariana Domingues BianchinIrene Clemes Külkamp-Guerreiro
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Sep 21, 2013·Drug Development and Industrial Pharmacy·Julieta C ImperialeAlejandro Sosnik
Sep 12, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Sara AlgeelaniDavid J Greenblatt
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May 20, 1999·The Annals of Pharmacotherapy·A L Tseng, M M Foisy
Aug 11, 2011·BMC Bioinformatics·Carola SöhngenDietmar Schomburg

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