The systemic availability of itraconazole capsules may be reduced secondary to elevated gastric pH and possibly by presystemic intestinal metabolism via CYP3A4. Grapefruit juice is acidic and an inhibitor of intestinal CYP3A4. To determine the effect of grapefruit juice on the systemic availability of itraconazole capsules, serum itraconazole and hydroxy-itraconazole concentrations were determined in eleven healthy volunteers studied in a randomized, two-way crossover design. Concurrent grapefruit juice resulted in a 43% decrease in the mean itraconazole AUG(0-48) (2507 ng.hr/ml versus 1434 ng.hr/ml, p = 0.046) and a 47% decrease in the mean hydroxy-itraconazole AUC(0-72) (7264 ng.hr/ml versus 3880 ng.hr/mL, p = 0.025. Grapefruit juice also significantly increased the mean itraconazole T-max (5.5 versus 4 hours). We conclude that concomitant grapefruit juice does not enhance the systemic availability of itraconazole capsules, but rather appears to impair itraconazole absorption. Therefore, concomitant grapefruit juice will not likely be useful in improving the oral availability of itraconazole capsules.
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Univ Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Univ Arkansas Med Sci Hosp, Coll Pharm, Little Rock, AR 72205 USAUniv Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Gubbins, Paul O.
Gurley, Bill J.
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Univ Arkansas Med Sci Hosp, Coll Pharm, Little Rock, AR 72205 USA
Dept Pharmaceut Sci, Little Rock, AR USAUniv Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Gurley, Bill J.
Williams, David K.
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Univ Arkansas Med Sci, Coll Publ Hlth, Little Rock, AR 72205 USA
Univ Arkansas Med Sci, Coll Med, Little Rock, AR 72205 USAUniv Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Williams, David K.
Penzak, Scott R.
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机构:Univ Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Penzak, Scott R.
McConnell, Scott A.
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机构:Univ Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
McConnell, Scott A.
Franks, Amy M.
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Univ Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Univ Arkansas Med Sci Hosp, Coll Pharm, Little Rock, AR 72205 USAUniv Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA
Franks, Amy M.
Saccente, Michael
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Univ Arkansas Med Sci, Coll Med, Little Rock, AR 72205 USAUniv Arkansas Med Sci, Coll Pharm, Dept Pharm Practice, Little Rock, AR 72205 USA