Experiment 67424

Details

PropertyValue
Pharmacology
OrganismEmpty organism
CitationEDWARDS,DJ: FITZSIMMONS,ME: SCHUETZ,EG: YASUDA,K: DUCHARME,MP: WARBASSE,LH: WOSTER,PM: SCHUETZ,JD: WATKINS,P:. (1999). 6',7'-DIHYDROXYBERGAMOTTIN IN GRAPEFRUIT JUICE AND SEVILLE ORANGE JUICE: EFFECTS ON CYCLOSPORINE DISPOSITION, ENTEROCYTE CYP3A4, AND P-GLYCOPROTEIN.. 65(3)
Amount utilized
Compound isolated
DiseaseA RANDOMIZED CROSSOVER STUDY DESIGN WAS USED IN WHICH SUBJECTS RECEIVED A SINGLE ORAL DOSE OF 7.5 MG/KG CYCLOSPORINE WITH WATER, GRAPEFRUIT JUICE, AND SEVILLE ORANGE JUICE. AFTER AN OVERNIGHT FAST, SUBJECTS INGESTED 8 OUNCES OF WATER OR JUICE 30 MINUTES BEFORE ADMINISTRATION OF CYCLOSPORINE AND 3 1/2, 7 1/2, AND 11 1/2 HOURS AFTER THE CYCLOSPORINE DOSE. BLOOD SAMPLES WERE COLLECTED. AREA UNDER THE WHOLE BLOOD CONCENTRATION-TIME CURVE AND PEAK CONCENTRATION OF CYCLOSPORINE WERE INCREASE BY 55% AND 35%, RESPECTIVELY, WITH GRAPEFRUIT JUICE (P<.05). SEVILLE ORANGE JUICE HAD NO INFLUENCE ON CYCLOSPORINE DISPOSITION BUT REDUCED ENTEROCYTE CONCENTRATIONS OF CYP3A4 BY AN AVERAGE OF 40%. 6',7'-DIHYDROXYBERGAMOTTIN DID NOT INHIBIT P-GLYCOPROTEIN AT CONCENTRATIONS UP TO 50 MICROMOL/L.
Dose amountVAR
Number1
Qualitative resultINACTIVE
AnimalCELL CULTURE
Dose expressionCONC USED