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Understanding the grapefruit-drug interaction.

Dennis Flanagan

Open publisher page 16 citations

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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What this paper is about

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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Available 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.

Key concepts: Grapefruit juice, CYP3A4, Triazolam, Pharmacology, Drug, Bioavailability, Drug interaction, Drug metabolism

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