EFFECT OF GRAPEFRUIT JUICE ON CYCLOSPORINE PHARMACOKINETICS IN RENAL TRANSPLANT PATIENTS1
1996; Wolters Kluwer; Volume: 62; Issue: 1 Linguagem: Inglês
10.1097/00007890-199607150-00023
ISSN1534-6080
AutoresDavid I. Min, Yi‐Min Ku, Paul J. Perry, Ferdinand O. Ukah, Kay Ashton, Maureen Martin, Lawrence G. Hunsicker,
Tópico(s)Drug Transport and Resistance Mechanisms
ResumoThis study investigated the effect of grapefruit juice on cyclosporine A (CsA) bioavailability in 10 renal transplant patients. Under CsA steady state conditions, patients were randomly administered their usual dose of CsA with either 8 ounces of grapefruit juice or 8 ounces of water. Using a crossover design, a 12-hr pharmacokinetic study was then conducted. Grapefruit juice increased the area under the concentration versus time curve(4281±1497 ng·hr/ml [grapefruit juice] vs. 3415±1288 ng·hr/ml [water], P=0.029) and 12-hr trough(244±214 ng/ml [grapefruit juice] vs. 132±56 ng/ml [water],P=0.09), but it did not change peak concentration(734±290 ng/ml [grapefruit juice] vs. 708±305 ng/ml [water],P=0.76). In addition, grapefruit juice delayed the time to peak concentration compared with water (5.4±3.0 hr [grapefruit juice] vs. 2.8±0.8 hr [water], P=0.025). These data suggest that concurrent administration of grapefruit juice with CsA will delay the absorption of CsA and increase the drug exposure of CsA without changing peak concentration.
Referência(s)