Experiment 610724
Worktypes
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Citrus paradisi (RUTACEAE) |
| Citation | LUNDAHL,J: REGARDH,CG: EDGAR,B: JOHNSSON,G:. (1997). EFFECTS OF GRAPEFRUIT JUICE INGESTION - PHARMACOKINETICS AND HAEMODYNAMICS OF INTRAVENOUSLY AND ORALLY ADMINISTERED FELODIPINE IN HEALTHY MEN.. 52(2) |
| Amount utilized | |
| Compound isolated | |
| Disease | A RANDOMIZED, FOUR-WAY, CROSSOVER STUDY OF 12 HEALTHY MALES WHO INGESTED GRAPEFRUIT JUICE PRIOR TO AN ORAL DOSE OF FELODIPINE. ORAL DRUG ADMINISTRATION IT DID LEAD TO AN INCREASE IN THE MEAN AUC AND CMAX BY 72% AND 173%, RESPECTIVELY, AND THE MEAN ABSOLUTE BIOAVAILABILITY WAS INCREASED BY 112%. THE FRACTION OF THE ORAL FELODIPINE DOSE REACHING THE PORTAL SYSTEM WAS INCREASED FROM 45% TO 80% WHEN INTAKE OF DRUG WAS PRECEASED BY GRAPEFRUIT JUICE INGESTION. THE PHARMACOKINETICS OF THE PRIMARY METABOLITE, DEHYDROFELODIPINE, WAS AFFECTED BY THE INTAKE OF JUICE, RESULTING IN A 46% INCEASE IN CMAX. JUICE INTAKE IMMEDIATELY BEFORE ORAL FELODIPINE RESULTED IN MORE PRONOUNCED HAEMODYNAMIC EFFECTS OF THE DRUG AS MEASURED BY DIASTOLIC BLOOD PRESSURE AND HEART RATE. VASCULAR-RELATED ADVERSE EVENTS WERE REPORTED MORE FREQUENTLY WHEN ORAL DRUG ADMINISTRATION WAS PRECEDED BY JUICE INTAKE COMPARED WITH CONTROL TREATMENT. THE MAIN ACUTE EFFECT OF THE GRAPEFRUITE JUICE ON THE PLASMA CONCENTRATIONS OF FELODIPINE IS MEDIATED BY INHIBITION OF GUT WALL METABOLISM. |
| Dose amount | 150.0 ML |
| Number | 1 |
| Qualitative result | . |
| Animal | HUMAN ADULT |
| Per unit | PERSON |
| Dose expression | DOSE |
| Extract | JUICE |
| Gender | GIVEN TO BOTH SEXES |