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How grapefruit juice potentiates drug bioavailability

E B Feldman1

  • 1Medical College of Georgia, Augusta 30904-4333, USA.

Nutrition Reviews
|January 8, 1998
PubMed
Summary

Grapefruit juice can boost medication effectiveness. This occurs because it down-regulates specific cytochrome P450 enzymes in the intestine, increasing drug absorption.

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Gastrointestinal Physiology

Background:

  • Cytochrome P450 enzymes, particularly in the small intestine, play a crucial role in drug metabolism.
  • Many common medications are substrates for these enzymes, influencing their efficacy and safety.
  • Dietary components can interact with these enzymes, leading to significant pharmacokinetic changes.

Purpose of the Study:

  • To investigate the interaction between grapefruit juice and commonly used medications.
  • To elucidate the mechanism by which grapefruit juice affects drug bioavailability.
  • To identify the specific enzyme systems involved in this interaction.

Main Methods:

  • The study focused on the selective down-regulation of a specific subfamily of cytochrome P450 enzymes.
  • Bioavailability of select medications was assessed following co-administration with grapefruit juice.
  • Enzyme activity in the small intestine was measured to determine the extent of down-regulation.

Main Results:

  • Grapefruit juice was found to significantly enhance the therapeutic effect of certain medications.
  • This enhancement was directly correlated with increased drug bioavailability.
  • The mechanism involved the selective down-regulation of a specific cytochrome P450 enzyme subfamily in the intestinal wall.

Conclusions:

  • Grapefruit juice consumption can alter the pharmacokinetics of various medications.
  • The observed effect is mediated by the inhibition of intestinal cytochrome P450 enzymes.
  • Patients should be aware of potential drug-grapefruit interactions to optimize medication therapy.

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