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Effect of Seville Orange Juice (SOJ) and Grapefruit Juice (GFJ) on Indinavir (IDV) Pharmacokinetics (PK) in Healthy Volunteers.

PENZAK SR, ACOSTA EP, TURNER M, EDWARDS DJ, HON YY, DESAI HD, JANN MW; Interscience Conference on Antimicrobial Agents and Chemotherapy (41st : 2001 : Chicago, Ill.).

Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2001 Dec 16-19; 41: abstract no. A-488.

Mercer Univ., Southern School of Pharmacy, Atlanta, GA

BACKGROUND: Both SOJ and GFJ inhibit intestinal CYP3A4 while GFJ has also been shown to inhibit intestinal P-glycoprotein (P-gp). The purpose of this study was to determine the influence of intestinal CYP3A4 and P-gp modulation with these juices on IDV pharmacokinetics (PK). METHODS: 13 subjects were studied in a 3-way crossover design. All subjects received IDV 800 mg every 8 hours x 1 day, and a single 800 mg dose the next a.m. (Day 2). The last dose on Day 1 and the a.m. dose on Day 2 were taken with 8 oz of SOJ, single strength GFJ, and water (control). Blood was collected for IDV analysis pre-dose (0 hr), 0.5, 1, 2, 3, 4, and 5 hrs after the Day 2 IDV dose. PK parameters were determined by noncompartmental methods and repeated measures ANOVA was used to compare results accross groups. Geometric mean (95% confidence intervals) results are reported below: RESULTS: [table: see text] Neither SOJ nor GFJ produced statistically significant changes in IDV PK compared to control (water). CONCLUSION: Modulation of intestinal CYP3A4 +/- P-gp by SOJ and GFJ does not significantly alter the systemic availability of IDV, suggesting that these enterocyte proteins do not substantially contribute to interindividual variability in the systemic availability of IDV. Supported by: The American Foundation for Pharmaceutical Education; The Burroughs Wellcome Fund

Publication Types:
  • Meeting Abstracts
Keywords:
  • Beverages
  • CYP3A protein, human
  • Citrus
  • Cross-Over Studies
  • Cytochrome P-450 Enzyme System
  • Indinavir
  • Intestines
  • blood
  • pharmacokinetics
Other ID:
  • GWAIDS0029090
UI: 102268722

From Meeting Abstracts




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