Clinically Significant Grapefruit Juice-Drug Interactions

  title={Clinically Significant Grapefruit Juice-Drug Interactions},
  author={W. Mccloskey and Kathy Zaiken and R. Couris},
  journal={Nutrition Today},
T he ability of grapefruit juice to increase drug levels in blood was accidentally discovered during a pharmacokinetic study designed to evaluate an interaction between felodipine (Plendil), a drug prescribed for treatment of hypertension, and ethanol. Double-strength grapefruit juice was used to mask the taste of the ethanol in this randomized, crossover, double-blind study. A nonintoxicating dose of ethanol or placebo was administered to subjects, followed by a 5-mg dose of felodipine. For… Expand
2 Citations
Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: influence of time between substrate and inducer administration.
A physiologically based pharmacokinetic (PBPK) model was developed to project the dynamics and magnitude of CYP3A4 induction in vivo from in vitro data generated with primary human hepatocytes and suggested that a concomitant administration of RIF and midazolam resulted in significant competitive inhibition limited to intestinal enzyme. Expand
External ear problems


Grapefruit juice-drug interactions.
In vitro findings support the flavonoid, naringin, or the furanocoumarin, 6',7'-dihydroxybergamottin, as being active ingredients, but a recent investigation indicated that neither of these substances made a major contribution to grapefruit juice-drug interactions in humans. Expand
Drug Interactions with Grapefruit Juice
The consistent findings across studies of diverse cytochrome P450 (CYP3A) 3A substrates support the mechanistic hypothesis that 1 or more grapefruit juice components inhibit CYP3A enzymes in the gastrointestinal tract. Expand
Grapefruit juice and prescription drug interactions Exploring mechanisms of this interaction and potential toxicity for certain drugs
Concomitant administration of grapefruit juice can increase the plasma concentration of numerous drugs in humans and decrease the concentration of a few others. Such elevations of drug piasmaExpand
Grapefruit juice and drug interactions. Exploring mechanisms of this interaction and potential toxicity for certain drugs.
The use of grapefruit juice with a few specific drugs may lower plasma drug concentrations by inhibiting drug absorption catalyzed by the organic anion transporting polypeptide (OATP). Expand
Grapefruit juice increases oral nimodipine bioavailability.
There was evidence for a more pronounced hemodynamic response in the grapefruit juice period and the null hypothesis "relevant interaction" thus could not be rejected for the primary pharmacokinetic parameters AUC and Cmax. Expand
Undesirable Effects of Citrus Juice on the Pharmacokinetics of Drugs
It is recommended that patients avoid citrus juice intake while taking medications and that healthcare providers advise against citrus Juice intake in this setting until any interactions with subject drugs can be clarified in clinical studies. Expand
Drug-grapefruit juice interactions.
This review discusses the proposed mechanisms of action and the medications involved in drug-grapefruit juice interactions and addresses the clinical implications of these interactions. Expand
Interactions Between Grapefruit Juice and Cardiovascular Drugs
  • D. Bailey, G. Dresser
  • Medicine
  • American journal of cardiovascular drugs : drugs, devices, and other interventions
  • 2004
Grapefruit juice may enhance drug toxicity for antiarrhythmic agents such as amiodarone, quinidine, disopyramide, or propafenone, and for the congestive heart failure drug, carvediol. Expand
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The effects of grapefruit juice on plasma concentrations of diazepam were investigated and the mean AUC(0−24) and Cmax was increased 3.2-fold and 1.5-fold, respectively, by the grapefruit Juice in this study. Expand
Effects of grapefruit juice ingestion – pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy men
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