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Drug interactions with grapefruit juice

B Ameer1, R A Weintraub

  • 1Princeton Junction, New Jersey, USA.

Clinical Pharmacokinetics
|August 1, 1997
PubMed
Summary
This summary is machine-generated.

Grapefruit juice can significantly increase oral drug bioavailability, sometimes altering drug effects. This interaction, likely due to grapefruit compounds inhibiting drug metabolism in the gut, necessitates individual drug evaluation.

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Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacology

Background:

  • Grapefruit juice consumption can increase oral drug bioavailability by up to threefold.
  • This interaction affects various drug classes, including calcium antagonists, benzodiazepines, and antihistamines, potentially altering their therapeutic effects.

Purpose of the Study:

  • To investigate the mechanisms behind grapefruit juice's effect on drug bioavailability.
  • To identify the specific components in grapefruit juice responsible for these interactions.
  • To assess the clinical significance of grapefruit juice-drug interactions.

Main Methods:

  • Review of clinical drug interaction studies involving grapefruit juice.
  • Analysis of pharmacokinetic data to determine changes in drug bioavailability.
  • Hypothesizing mechanisms based on enzyme inhibition, particularly cytochrome P450 3A (CYP3A).

Main Results:

  • Grapefruit juice components, potentially flavonoids like naringin and furanocoumarins, inhibit drug metabolism.
  • The primary mechanism appears to be the inhibition of CYP3A enzymes in the gastrointestinal tract.
  • Consistent findings across diverse CYP3A substrates support this inhibitory hypothesis.

Conclusions:

  • Grapefruit juice significantly impacts oral drug bioavailability, primarily by inhibiting intestinal drug metabolism.
  • The specific components responsible are still under investigation, with naringin and furanocoumarins as likely candidates.
  • Drug-grapefruit interactions should be evaluated individually, as seen with cyclosporin, rather than by drug class.