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April 1, 2000British Journal of Clinical PharmacologyOpen Access

Dramatic inhibition of amiodarone metabolism induced by grapefruit juice

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Why the study?

Does grapefruit juice alter the pharmacokinetics of amiodarone in healthy adult volunteers?

Population

11 healthy adult volunteers

Comparison

Single oral dose of amiodarone with three… vs Control period with a single oral dose of…

Design

Other

Authors

CLChristian LibersaUniversité de LilleSBSerge A. BriqueInsermKMKokou B. Motte

Discussion

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Implication

May warrant caution with grapefruit juice in amiodarone users; leaves open clinical outcome impact in patients.

Structured PICO

Does grapefruit juice alter the pharmacokinetics of amiodarone in healthy adult volunteers?

P
Population
11 healthy adult volunteers
I
Intervention
Single oral dose of amiodarone (17 mg kg-1) with three glasses of 300 ml of grapefruit juice on the same day
C
Comparator
Control period (evaluated 6 months previously) with a single oral dose of amiodarone and water instead of grapefruit juice
O
Outcome
Amiodarone kinetics (AUC and Cmax) and N-desethylamiodarone (N-DEA) productionsurrogate

Grapefruit juice significantly increases amiodarone exposure by inhibiting its CYP3A-mediated metabolism, highlighting a clinically relevant food-drug interaction.

Cite This Study

Libersa et al. (2000) studied this question.

synapsesocial.com/papers/6a7fa4fb044998269cd7706dhttps://doi.org/10.1046/j.1365-2125.2000.00163.x
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Grapefruit Juice Alters the Systemic Bioavailability and Cardiac Repolarization of Terfenadine in Poor Metabolizers of Terfenadine1996 · 62 citations
  2. 2Pharmacodynamics of Intravenous Amiodarone in the Dog1984 · 32 citations
  3. 3Inactivation of Cytochrome P450 3A4 by Bergamottin, a Component of Grapefruit Juice1998 · 312 citations
  4. 4Effect of phenobarbitone on the pharmacokinetics and tissue levels of amiodarone in the rat1985 · 9 citations
  5. 5Grapefruit Component Interacting with Rat and Human P450 CYP3A: Possible Involvement of Non-Flavonoid Components in Drug Interaction.1997 · 71 citations