Understanding the grapefruit-drug interaction
Flanagan, D.
General Dentistry 53(4): 282-285; Quiz 286
2005
ISSN/ISBN: 0363-6771 PMID: 16158798 Document Number: 586977
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.