Grapefruit–medication interactions: Forbidden fruit or avoidable consequences?¶
Bailey, Dresser, & Arnold. (2013). Grapefruit–medication interactions: Forbidden fruit or avoidable consequences?: Forbidden fruit or avoidable consequences?. Canadian Medical Association Journal.
Cited by¶
1 citation across 1 artifact.
Each citation links to the sentence it supports in the citing article.
Domain-specific¶
- Elimination Pathway
- A drug predominantly metabolized by CYP3A4 is vulnerable to induction by rifampicin (which accelerates metabolism and lowers plasma exposure) and to inhibition by ketoconazole or grapefruit furanocoumarins (which saturate the enzyme and raise exposure)
This sourceCMAJ review establishing that grapefruit furanocoumarins inactivate intestinal CYP3A4 irreversibly and thereby raise the oral bioavailability of CYP3A4 substrate drugs.
Supported in partVerified against a saved copy of the source
“Furanocoumarins are metabolized by CYP3A4 to reactive intermediates that bond covalently to the active site of the enzyme, causing irreversible inactivation (mechanism-based inhibition).”
- A drug predominantly metabolized by CYP3A4 is vulnerable to induction by rifampicin (which accelerates metabolism and lowers plasma exposure) and to inhibition by ketoconazole or grapefruit furanocoumarins (which saturate the enzyme and raise exposure)
Verification¶
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