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 (Cmax) compared to administration with water (7.11 versus 9.10 microg/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 (AUC(0-12)), the AUC(0-infinity), or the concentration at 12 h. Therefore, grapefruit juice does not clinically significantly affect amprenavir pharmacokinetics.
Demarles
D
D
Laboratoire Glaxo SmithKline, Marly-le-Roi, France. dd79951@gsk.com
Gillotin
C
C
Bonaventure-Paci
S
S
Vincent
I
I
Fosse
S
S
Taburet
A M
AM
D000284:Administration, Oral; D000328:Adult; D001628:Beverages; D002219:Carbamates; D002957:Citrus; D018592:Cross-Over Studies; D005260:Female; D018565:Food-Drug Interactions; D005663:Furans; D017320:HIV Protease Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D013449:Sulfonamides / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D002219:Carbamates; D005663:Furans; D017320:HIV Protease Inhibitors; D013449:Sulfonamides; C095108:amprenavir