Effect of grapefruit juice on pharmacokinetics of itraconazole in healthy subjects.
OBJECTIVE
To examine the effect of grapefruit juice on the disposition of oral administered itraconazole in healthy subjects.


METHODS
Twenty-two healthy male subjects received a single 100 mg dose of itraconazole with either 350 ml grapefruit juice, orange juice or mineral water. Plasma concentrations of itraconazole were measured by HPLC, and pharmacokinetic parameters; Cmax, Tmax, T1/2, AUC, and AUC corrected by human body surface area: AUC/S, were calculated.


RESULTS
Grapefruit juice had no effect on any pharmacokinetic parameter of itraconazole. However, T1/2, AUC, or AUC/S were significantly decreased in orange juice treatment group compared to those in mineral water group (average decrease 56%, p < 0.01, 41%, p < 0.05, and 43%, p < 0.05, respectively).


CONCLUSIONS
Coadministration of grapefruit juice did not affect any pharmacokinetic parameter of itraconazole while that of orange juice decreased the parameters of T1/2, AUC, and AUC/S of the drug.
Kawakami
M
M
Internal Medicine I, National Defense Medical College, Tokorozawa, Saitama, Japan.
Suzuki
K
K
Ishizuka
T
T
Hidaka
T
T
Matsuki
Y
Y
Nakamura
H
H
D000328:Adult; D000935:Antifungal Agents / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001628:Beverages; D002957:Citrus; D006207:Half-Life; D006801:Humans; D017964:Itraconazole / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male
D000935:Antifungal Agents; D017964:Itraconazole