Duration of effect of grapefruit juice on the pharmacokinetics of the CYP3A4 substrate simvastatin

@article{Lilja2000DurationOE,
  title={Duration of effect of grapefruit juice on the pharmacokinetics of the CYP3A4 substrate simvastatin},
  author={Jari J. Lilja and Kari T. Kivistö and Pertti J. Neuvonen},
  journal={Clinical Pharmacology \& Therapeutics},
  year={2000},
  volume={68}
}
Grapefruit juice is a potent inhibitor of CYP3A4‐mediated drug metabolism. We wanted to investigate how long the inhibitory effect of grapefruit juice lasts, with the CYP3A4 substrate simvastatin used as a model drug. 
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178 Citations

Effects of grapefruit juice on the pharmacokinetics of sildenafil

The influence of grapefruit juice, containing inhibitors of intestinal CYP3A4, on the pharmacokinetics of sildenafil and N‐desmethylsildenAFil is investigated.

Effect of extended exposure to grapefruit juice on cytochrome P450 3A activity in humans: Comparison with ritonavir

Time course of recovery of cytochrome p450 3A function after single doses of grapefruit juice

Effect of Grapefruit Juice Volume on the Reduction of Fexofenadine Bioavailability: Possible Role of Organic Anion Transporting Polypeptides

Fruit Juices as Perpetrators of Drug Interactions: The Role of Organic Anion–Transporting Polypeptides

This article reviews the current literature on interactions between clinically used OATP substrates and fruit juice consumption and significantly reduces the oral bioavailability of numerous important medicines relying on this anion transporter pathway for absorption.

Interaction of grapefruit juice and calcium channel blockers.

  • D. Sica
  • Medicine
    American journal of hypertension
  • 2006

Review Article: Cytochrome P450 enzyme, and transport protein mediated herb–drug interactions in renal transplant patients: Grapefruit juice, St John's Wort – and beyond! (Review Article)

Aim:  To survey the evidence for plant‐products to modify cytochrome P450 enzyme, and transport protein mediated drug metabolism in renal transplant patients.

A more balanced approach to drug-grapefruit juice interactions

We question Pirmohamed’s focus on “severe, sometimes fatal, interactions” between grapefruit juice and drugs,1 which may bias BMJ readers and add to the excessive fear around grapefruit juice for…

Grapefruit juice-drug interaction issues.

Concomitant drug and food intake create the opportunity for an interaction that may change (increase or decrease) drug benefit or toxicity.

Interactions Between Grapefruit Juice and Cardiovascular Drugs

  • D. BaileyG. Dresser
  • Medicine, Biology
    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.
...

References

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Grapefruit juice—simvastatin interaction: Effect on serum concentrations of simvastatin, simvastatin acid, and HMG‐CoA reductase inhibitors

Grapefruit juice has minimal effects on plasma concentrations of lovastatin‐derived 3‐hydroxy‐3‐methylglutaryl coenzyme A reductase inhibitors

To evaluate the effect of regular‐strength grapefruit juice, a cytochrome P4503A 4 (CYP3A4) inhibitor, on the pharmacokinetics of a commonly prescribed regimen of oral lovastatin, a large number of patients were prescribed the drug.

Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole

Disposition of intravenous and oral cyclosporine after administration with grapefruit juice

Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model.

UNLABELLED Aims Ingestion of grapefruit juice (GFJ) alters the pharmacokinetics of various orally administered drugs. Quantitative evaluation of this GFJ-drug interaction is required for the proper…

Grapefruit juice—terfenadine single‐dose interaction: Magnitude, mechanism, and relevance

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.

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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.

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Intersubject changes in felodipine and dehydrofelodipines AUC supported inhibition of both primary and secondary metabolic steps as a mechanism, and the interaction could not be predicted from baseline pharmacokinetics with water and did not result in more consistent bioavailability among individuals.