Title : Induction of cytochrome P450 3A4 and P-glycoprotein by the isoxazolyl-penicillin antibiotic flucloxacillin.

Pub. Date : 2006 Feb

PMID : 16472102






4 Functional Relationships(s)
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1 Induction of cytochrome P450 3A4 and P-glycoprotein by the isoxazolyl-penicillin antibiotic flucloxacillin. Floxacillin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 However, incubation of human LS 180 colorectal adenocarcinoma cells with flucloxacillin led to a dose-dependent induction of MDR1 as well as of CYP3A4 mRNA, which was also confirmed in primary human hepatocytes. Floxacillin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 At high concentrations, flucloxacillin activated the human Pregnane-X-Receptor, PXR, a ligand-dependent transcription factor that is the target of many drugs that induce CYP3A4, with consequences for the metabolism of other drugs. Floxacillin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 These findings indicate that flucloxacillin has the potential to induce expression of both CYP3A4 as well as P-glycoprotein, most likely through activation of the nuclear hormone receptor PXR. Floxacillin cytochrome P450 family 3 subfamily A member 4 Homo sapiens