Understanding the grapefruit-drug interaction.
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.
Flanagan
Dennis
D
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors; D001667:Binding, Competitive; D001682:Biological Availability; D032083:Citrus paradisi / Q000378:metabolism*; D051544:Cytochrome P-450 CYP3A; D065607:Cytochrome P-450 Enzyme Inhibitors; D005419:Flavonoids / Q000493:pharmacokinetics; D018565:Food-Drug Interactions; D011564:Furocoumarins / Q000493:pharmacokinetics; D041743:Herb-Drug Interactions; D006801:Humans; D020902:Hypericum / Q000009:adverse effects; D006993:Hypnotics and Sedatives / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D010084:Oxidation-Reduction
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D065607:Cytochrome P-450 Enzyme Inhibitors; D005419:Flavonoids; D011564:Furocoumarins; D006993:Hypnotics and Sedatives; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human