Experiment 66815
Worktypes
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Citrus paradisi (RUTACEAE) |
| Citation | LIBERSA,CC: BRIQUE,SA: MOTTE,KB: CARON,JF: GUEDON-MOREAU,LM: HUMBERT,L: VINCENT,A: DEVOS,P: LHERMITTE,MA:. (2000). DRAMATIC INHIBITION OF AMIODARONE METABOLISM INDUCED BY GRAPEFRUIT JUICE.. 49(4) |
| Amount utilized | |
| Compound isolated | |
| Disease | ELEVEN HEALTHY ADULT VOLUNTEERS TOOK PART IN A SINGLE SEQUENCE, REPEATED-MEASURES DESIGN STUDY. EACH SUBJECT, WHO HAD BEEN EVALUATED 6 MONTHS PREVIOUSLY FOR AMIODARONE PHARMACOKINETICS, WAS GIVEN A SINGLE ORAL DOSE OF AMOIDARONE (17 MG KG-1) WITH THREE GLASSES OF 300 ML OF GRAPEFRUIT JUICE ON THE SAME DAY. GRAPEFRUIT JUICE COMPLETELY INHIBITED THE PRODUCTION OF N-DEA, THE MAJOR METABOLITE OF AMIODARONE, IN ALL SUBJECTS AND INCREASED THE AREA-UNDER-THE-CURVE (AUC) MAXIMUM CONCENTRATION OF AMIODARONE (CMAX) BY 50% AND 84%, RESPECTIVELY, AS COMPARED WITH THE CONTROL PERIOD DURING WHICH WATER HAD BEEN ADMINISTRATED INSTEAD OF GRAPEFRUIT JUICE. GRAPEFRUIT JUICE DRAMATICALLY ALTERS THE METABOLISM OF AMOIDARONE WITH COMPLETE INHIBITION OF N-DEA PRODUCTION. THESE RESULTS ARE IN AGREEMENT WITH IN VITRO DATA POINTING TO THE INVOLVEMENT OF CYP3 A IN THE METABOLISM OF AMIODARONE AND SUGGESTS THAT THIS INTERACTION SHOULD BE TAKEN INTO ACCOUNT WHEN PRESCRIBING THIS ANTIARRHYTHMIC DRUG. |
| Dose amount | 900.0 ML |
| Number | 2 |
| Qualitative result | ACTIVE |
| Animal | HUMAN ADULT |
| Per unit | DAY |
| Dose expression | DOSE |
| Extract | JUICE |
| Gender | MALE |