Understanding the grapefruit-drug interaction.

Dennis Flanagan

PubMed · 16158798

Understanding the grapefruit-drug interaction.

Abstract

The inhibitory interaction of grapefruit juice and CYP3A4 medication metabolism was discovered in 1989. CYP3A4 enzymes are responsible for the metabolism of more than 60% of orally-administered drugs. Grapefruit components inhibit CYP3A4 drug oxidation and P-glycoprotein transportation, allowing more systemic drug bioavailability. This inhibitory interaction should be kept in mind when prescribing drugs that are metabolized by CYP3A4, such as orally administered midazolam, triazolam, and diazepam.

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ATP Binding Cassette Transporter, Subfamily B, Member 1 Binding, Competitive Biological Availability Citrus paradisi Cytochrome P-450 CYP3A Cytochrome P-450 Enzyme Inhibitors Flavonoids Food-Drug Interactions Furocoumarins Herb-Drug Interactions Humans Hypericum Hypnotics and Sedatives Liver Oxidation-Reduction Journal Article

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Dennis Flanagan. Understanding the grapefruit-drug interaction.. https://pubmed.ncbi.nlm.nih.gov/16158798/

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