Single-Dose Pharmacokinetics of Amprenavir Coadministered with Grapefruit Juice

In this crossover study in 12 healthy volunteers, coadministration of amprenavir (1,200 mg; single dose) with grapefruit juice slightly reduced the maximum concentration of drug in serum (C(max)) compared to administration with water (7.11 versus 9.10 μg/ml), slightly increased the time to C(max) (1.13 versus 0.75 h), and did not affect the area under the concentration-time curve from 0 to 12 h (AUC(0-12)), the AUC(0-∞), or the concentration at 12 h. Therefore, grapefruit juice does not clinically significantly affect amprenavir pharmacokinetics.