Experiment 626230

Details

PropertyValue
Pharmacology
Administration routeORAL
OrganismCitrus paradisi (RUTACEAE)
CitationGARG,SK: KUMAR,N: BHARGAVA,VK: PRABHAKAR,SK:. (1998). EFFECT OF GRAPEFRUIT JUICE ON CARBAMAZEPINE BIOAVAILABILITY IN PATIENTS WITH EPILEPSY.. 64(3)
Amount utilized
Compound isolated
DiseaseA RANDOMIZED CROSSOVER STUDY CONSISTING OF 2 PHASES. TEN PATIENTS WITH EPILEPSY WHO HAD RECEIVED THERAPY WITH 200 MG CARBAMAZEPINE 3 TIMES A DAY FOR THE PREVIOUS 3 TO 4 WEEKS PARTICIPATED. THEY WERE GIVEN EITHER GRAPEFRUIT JUICE OF 300 ML WATER AT 8 AM ALONG WITH 200 MG CARBAMAZEPINE. EACH TREATMENT WAS SEPARATED BY 2 DAYS; SUBJECTS CONTINUED TO RECEIVE CARBAMAZEPINE THERAPY DURING THE 2-DAY PEROID. ON BOTH OCCASIONS, BLOOD SAMPLES WERE COLLECTED AT DIFFERENT TIME INTERVALS BETWEEN 0 TO 8 HOURS. CARBAMAZEPINE LEVELS WERE ESTIMATED BY REVERSED-PHASE HPLC TECHNIQUE. COMPARED WITH WATER, GRAPEFRUIT JUICE SIGNIFICANTLY INCREASED THE STEADT-STATE OEAJ CIBCEBTRATUIB (6.55 VERSUS 9.20 MLG/ML), TROUGH CONCENTRATION (4.51 VERSUS 6.28 MLG/ML), AND AREA UNDER THE PLASMA CONCENTRATION-TIME CURVE (43.99 VERSUS 61.95 ULG.H/ML) OF CARBAMAZEPINE. NO SIGNIFICANT EFFECT WAS FOUND IN THE TIME TO REACH PEAK PLASMA CONCENTRATION. GRAPEFRUIT JUICE INCREASES THE BIOAVALABILITY OF CARBAMAZEPINE BY INHIBITING CYP3A4 ENZYMES IN GUT WALL AND IN THE LIVER.
Dose amount300.0 MG
Number1
Qualitative result.
AnimalHUMAN ADULT
Per unitPERSON
Dose expressionDOSE
ExtractJUICE
GenderGIVEN TO BOTH SEXES