Phenytoin and cyp3a4

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  • Cytochrome P-450 CYP2D6
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  • Table of Substrates, Inhibitors and Inducers (including: CYP Enzymes, Clinical index drugs, transporters, and examples of clinical substrates, inhibitors, and inducers)

    Phenytoin is metabolized by several CYP enzymes (mainly 2C19, and 2C9, but a little of 3A4 too), and so there are multiple medications that can affect its metabolism

    The Flockhart Table displays drugs that inhibit or induce specific CYP enzymes, for example CYP3A (Flockhart, 2007)

    The orphan nuclear receptor, pregnane X receptor (PXR), have been found to play a critical role in the induction of CYP3A4

    It is classified by the U

    1 Divalproex is an enzyme inhibitor sometimes implicated in psychotropic drug-drug interactions

    The present clinical case illustrates the

    Bleeding events more often resulted from a combined mechanism (P-glycoprotein AND CYP3A4 inhibition), whereas thrombotic events resulted from either combined OR single

    The results of clinical studies suggest that piperine (usually in doses of 20 mg/day) can inhibit CYP3A4, CYP2C9, and PGP, resulting in moderate increases in plasma concentrations of CYP3A4 substrates (carbamazepine, midazolam, and possibly others), CYP2C9 substrates (diclofenac, phenytoin, and possibly warfarin and others), and PGP Phenytoin and carbamazepine are strong cytochrome P450 (CYP450) enzyme inducers, including the 3A4 enzyme system (CYP3A4)

    The synthetic 17α-ethynyl estradiol is a cytochrome P450 (CYP)3A4 inhibitor

    Oral Contraceptives containing ethinyl estradiol and norethindrone (CYP3A4 Inhibition)† Increased: Monitoring for adverse reactions related to oral contraceptives is recommended during coadministration

    Phenytoin is a well‐characterized CAR activator and known to elicit induction effect on metabolic enzymes and P‐gp primarily through activation CAR with minor contribution from PXR

    The inhibition and induction of CYPs are major mechanisms causing pharmacokinetic drug–drug interactions

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  • Phenytoin and cyp3a4
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