Experiment 68187

Details

PropertyValue
Pharmacology
Administration routeORAL
OrganismCitrus paradisi (RUTACEAE)
CitationHO,PC: GHOSE,K: SAVILLE,D: WANWIMOLRUK,S:. (2000). EFFECT OF GRAPEFRUIT JUICE ON PHARMACOKINETICS AND PHARMACODYNAMICS OF VERAPAMIL ENANTIOMERS IN HEALTHY VOLUNTEERS.. 56(9/10)
Amount utilized
Compound isolated
DiseaseNINE HEALTHY MALE VOLUNTEERS FOLLOWED A RANDOMISED CROSS-OVER STUDY COMPRISING TWO TREATMENT PERIODS. PRETREATMENTS OF 200 ML ORANGE JUICE (CONTROL) OR GRAPEFRUIT JUCIE TWICE DAILY FOR 5 DAYS AND 120 MG VERAPAMIL (ORALLY) TWICE DAILY FOR 3 DAYS WERE GIVEN. ON THE STUDY DAY, THE SUBJECTS RECEIVED THE MORNING DOSE OF VERAPAMIL WITH EITHER ORANGE JUICE (CONTROL) OR GRAPEFRUIT JUICE. PLASMA AND URINE SAMPLES WERE COLLECTED FOR MEASUREMENT OF S- AND R-VERAPAMIL AND THE METABOLITES S- AND R-NORVERAPAMIL. BLOOD PRESSURE (BP), HEART RATE(HR) AND PR-INTERVAL WERE MONITORED. DURING THE GRAPEFRUIT JUICE PERIOD, THE STEADY-STATE PEAK AND TROUGH CONCENTATIONS OF S-VERAPAMIL WERE MODERATELY INCREASED. GRAPEFRUIT JUICE SIGNIFICANTLY INCREASED THE AREA UNDER THE PLASMA CONCENTRATION-TIME CURVE DURING THE 12-H DOSE INTERVAL S-VERAPAMIL BY 36%. SIMILAR RESULTS WERE OBTAINED FOR PEAK AND TROUGH CONCENTRATION OF R-VERAPAMIL. THE AUC0-12 H OF R-VERAPAMIL WAS INCREASED BY 28%. ELIMINATION HALF-TIME AND RENAL CLEARANCE OF BOTH S- AND R-VERAPAMIL WERE NOT AFFECTED. CONSIDERABLE INTER-SUBJECT VARIABILITY IN INTERACTION WAS SHOWN.
Dose amount400.0 ML
Number1
Qualitative resultACTIVE
AnimalHUMAN ADULT
Per unitDAY
Dose expressionDOSE
ExtractJUICE
GenderMALE