Human P450 metabolism of warfarin.

Article Details

Citation

Kaminsky LS, Zhang ZY

Human P450 metabolism of warfarin.

Pharmacol Ther. 1997;73(1):67-74. doi: 10.1016/s0163-7258(96)00140-4.

PubMed ID
9014207 [ View in PubMed
]
Abstract

The anticoagulant drug warfarin occurs as a pair of enantiomers that are differentially metabolized by human cytochromes P450 (CYP). R-warfarin is metabolized primarily by CYP1A2 to 6- and 8-hydroxywarfarin, by CYP3A4 to 10-hydroxywarfarin, and by carbonyl reductases to diastereoisomeric alcohols. S-warfarin is metabolized primarily by CYP2C9 to 7-hydroxywarfarin. Potential warfarin-drug interactions could occur with any of a very wide range of drugs that are metabolized by these P450s, and a number of such interactions have been reported. The efficacy of warfarin is affected primarily when metabolism of S-warfarin is altered.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
(R)-warfarinCytochrome P450 1A1ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 1A2ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 2C18ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 2C19ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 2C8ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 2C9ProteinHumans
Unknown
Substrate
Details
(R)-warfarinCytochrome P450 3A4ProteinHumans
Unknown
Substrate
Details
(S)-WarfarinCytochrome P450 2C18ProteinHumans
Unknown
Substrate
Details
(S)-WarfarinCytochrome P450 2C8ProteinHumans
Unknown
Substrate
Details
(S)-WarfarinCytochrome P450 2C9ProteinHumans
Unknown
Substrate
Details
Drug Interactions
DrugsInteraction
Acenocoumarol
Imatinib
Imatinib may increase the anticoagulant activities of Acenocoumarol.
Acenocoumarol
Methylene blue
The serum concentration of Acenocoumarol can be increased when it is combined with Methylene blue.
Acenocoumarol
Etoricoxib
The serum concentration of Acenocoumarol can be increased when it is combined with Etoricoxib.
Acenocoumarol
Dronabinol
The serum concentration of Acenocoumarol can be increased when it is combined with Dronabinol.
Acenocoumarol
Aldesleukin
The serum concentration of Acenocoumarol can be increased when it is combined with Aldesleukin.
Food Interactions
DrugInteraction
(R)-warfarinExercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum levels of R-warfarin.
(R)-warfarinExercise caution with St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum levels of R-warfarin.