Drug-grapefruit juice interactions

Garvan C. Kane, James J. Lipsky

Research output: Contribution to journalReview article

262 Scopus citations

Abstract

Grapefruit juice, a beverage consumed in large quantities by the general population, is an inhibitor of the intestinal cytochrome P-450 3A4 system, which is responsible for the first-pass metabolism of many medications. Through the inhibition of this enzyme system, grapefruit juice interacts with a variety of medications, leading to elevation of their serum concentrations. Most notable are its effects on cyclosporine, some 1,4-dihydropyridine calcium antagonists, and some 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. In the case of some drugs, these increased drug concentrations have been associated with an increased frequency of dose-dependent adverse effects. The P-glycoprotein pump, located in the brush border of the intestinal wall, also transports many cytochrome P-450 3A4, substrates, and this transporter also may be affected by grapefruit juice. 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.

Original languageEnglish (US)
Pages (from-to)933-942
Number of pages10
JournalMayo Clinic proceedings
Volume75
Issue number9
DOIs
StatePublished - Jan 1 2000

ASJC Scopus subject areas

  • Medicine(all)

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