Effects of Grapefruit Juice on Pharmacokinetic Exposure to Indinavir in HIV-Positive Subjects

The objective of this study was to determine the effects of double‐strength grapefruit juice on gastric pH and systemic bioavailability of indinavir in HIV‐infected subjects receiving indinavir. Fourteen HIV‐infected subjects took 800 mg of indinavir with 6 ounces (180 ml) of water or double‐strengt...

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Bibliographic Details
Published in:Journal of clinical pharmacology 2001-04, Vol.41 (4), p.435-442
Main Authors: Shelton, Mark J., Wynn, Heather E., Hewitt, Ross G., DiFrancesco, Robin
Format: Article
Language:English
Subjects:
Adult
Anti-HIV Agents - therapeutic use
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Beverages
Biological and medical sciences
Biological Availability
Chromatography, High Pressure Liquid
Citrus
Cross-Over Studies
Female
Food-Drug Interactions
Gastric Juice - metabolism
Half-Life
HIV Infections - drug therapy
HIV Infections - metabolism
Humans
Hydrogen-Ion Concentration
Indinavir - pharmacokinetics
Indinavir - pharmacology
Male
Medical sciences
Middle Aged
Models, Biological
Pharmacology. Drug treatments
Time Factors
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Summary:The objective of this study was to determine the effects of double‐strength grapefruit juice on gastric pH and systemic bioavailability of indinavir in HIV‐infected subjects receiving indinavir. Fourteen HIV‐infected subjects took 800 mg of indinavir with 6 ounces (180 ml) of water or double‐strength grapefruit juice. Gastric pH was measured and blood samples were collected for 5 hours after indinavir dosing. Grapefruit juice increased the mean gastric pH (from 1.39 ± 0.4 to 3.20 ± 0.3; p < 0.05) and slightly delayed the absorption of indinavir (tmax increased from 1.12 ± 0.8hto 1.56± 0.6 h; p < 0.05). However, there were no significant differences in indinavir exposure. Cmax was 16.7 ± 7.3 μ with water versus 13.9 ± 4.2 μ with grapefruit juice (p = NS), and AUC0–8 was 37.5 ± 19 with water versus 36.9 ± 15 with grapefruit juice (p = NS). The authors concluded that concomitant administration of grapefruit juice increases gastric pH and delays indinavir absorption but does not uniformly affect the systemic bioavailability of indinavir in HIV‐infected subjects.
ISSN:0091-2700
1552-4604
DOI:10.1177/00912700122010140