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Pathway Description
Fluconazole Metabolism
Homo sapiens
Category:
Metabolite Pathway
Sub-Category:
Metabolic
Created: 2022-02-03
Last Updated: 2023-10-25
Fluconazole, known commonly as the brand name Driflucan, is an antifungal drug taken mainly orally in the form of a pill, but can also be applied topically. When taken orally it is transported from the intestine into the intestinal epithelial cell possibly via solute carrier family 15 member 1, one of 3 drug transporters into epithelial cells. It is then transported into blood vessels via ATP-binding cassette sub-family C member 3. It is then transported into the liver via transporter P-glycoprotein 1. Once in the liver, 2% is metabolized into Fluconazole N-oxide by Cytochrome P450 3A4 and 6.5% is metabolized into Glucuronidated metabolite, Fluconazole by UDP-glucuronosyltransferase 2B7. Fluconazole N-Oxide has an unknown structure due to the unknown location of the oxygen. Fluconazole also inhibits the enzymes Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C19, and Cytochrome P450 3A5, which are enzymes in the liver that are similar to the enzyme Fluconazole inhibits in fungal yeast cells. Fluconazole has shown to be selective to fungal cytochrome enzymes, but in patients who take Fluconazole over a long period of time or already have liver dysfunction, this can cause hepatotoxicity. Fluconazole N-oxide and Glucuronidated metabolite, Fluconazole are transported via P-glycoprotein 1 back into the blood to travel to the kidney where it will be excreted through the urine. 93.3% of the dose is excreted in the urine, 80% of which is the unchanged Fluconazole.
References
Fluconazole Metabolism References
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