Experiment 68693
Worktypes
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Citrus paradisi (RUTACEAE) |
| Citation | TANAKAGA,H: OHNISHI,A: MATSUO,H: MURAKAMI,H: SATA,H: KURODA,K: URAE,A: HIGUCHI,S: SAWADA,Y:. (2000). PHARMACOKINETIC ANALYSIS OF FELODIPINE-GRAPEFRUIT JUICE INTERACTION BASED ON AN IRREVERSIBLE ENZYME INHIBITION MODEL.. 49(1) |
| Amount utilized | |
| Compound isolated | |
| Disease | INGESTION OF GRAPEFRUIT JUICE (GF) ALTERS THE PHARMACOKINETICS OF VARIOUS ORALLY ADMINISTERED DRUGS. QUANTITATIVE EVALUATION OF THIS GFJ-DRUG INTERACTION IS REQUIRED FOR THE PROPER CLINICAL MANAGEMENT OF PATIENTS. USING FELODIPINE AS A MODEL DRUGS, PHARMACOKINETIC MODLE WAS CONSTRUCTED BASED ON IRREVERSIBLE INHIBITON OF INTESTINAL CYTOCHROME P450 3A4 (CYP3A4) BY GFJ. THE MODEL GAVE A TURNOVER RATE OF CYP3A4 OF 0.0849 H-1, CORRESPONDING TO A HALF-TIME OF 8.16 H, IN AGREEEMENT WITH REPORTED VALUES. THE AUC-TIME PROFILES OF FELODIPINE ER IN THE CASE OF DIFFERENT AMOUNTS AND SCHEDULES OF GFJ INGESTION WERE SIMULATED USING THE PARAMETER VALUES ESTIMATED FROM THE MODEL. THE MODELLING LEADS TO THE IMPORTANT CONCLUSION THAT GFJ- FELODIPINE INTERACTION INCREASES WITH INCREASING FREQUENTLY AND AMOUNT OF GFJ INGESTION, AND THAT AN INTERVAL OF 2-3 DAYS BETWEEN GFJ INTAKE AND FELODIPINE ADMINSITRATION IS NECESSARY IF GJF-FELODIPINE INTERACTIONS IS TO BE AVOIDED. |
| Dose amount | 200.0 ML |
| Number | 1 |
| Qualitative result | ACTIVE |
| Animal | HUMAN ADULT |
| Per unit | DAY |
| Dose expression | DOSE |
| Extract | JUICE |
| Gender | MALE |