The magnitude of the potential interaction between boosted protease inhibitors and grapefruit juice is difficult to predict as the effect of grapefruit juice is concentration, dose and preparation dependent and varies widely across brands.
Single-dose pharmacokinetics of amprenavir coadministered with grapefruit juice.
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Study Design
Crossover study in 12 healthy volunteers
Study Results
Coadministration of amprenavir (1,200 mg; single dose) with grapefruit juice slightly reduced the maximum concentration of drug in serum (Cmax) compared to administration with water (7.11 versus 9.10 μg/ml), slightly increased the time to Cmax (1.13 versus 0.75 h), and did not affect the area under the concentration-time curve from 0 to 12 h (AUC0-12), the AUC0-∞, or the concentration at 12 h. Therefore, grapefruit juice does not clinically significantly affect amprenavir pharmacokinetics.
Study Conclusions
Changes in pharmacokinetic parameters with the concomitant use of amprenavir with grapefruit juice were not found to be clinically significant. While, co-administration of grapefruit juice with indinavir in a clinical study caused a decrease in the pharmacokinetic parameters of indinavir; earlier studies have found no significant changes in the pharmacokinetic parameters with the co-administration of both agents as compared to a control. The magnitude of the potential interaction between boosted protease inhibitors and grapefruit juice is difficult to predict as the effect of grapefruit juice is concentration, dose and preparation dependent and varies widely across brands.
References
Demarles D, Gillotin C, Bonaventure-Paci S, Vincent I, Fosse S, Taburet AM. Single-dose pharmacokinetics of amprenavir coadministered with grapefruit juice. Antimicrobial Agents And Chemotherapy. 2002; 5: 1589-1590.
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