CYP2C8 Inhibitors

    CYP2C8 inhibitors include, but are not limited to, amiodarone, clopidogrel, fluoxetine, gemfibrozil, isoniazid, montelukast, nortriptyline, quercetin, trimethoprim, and verapamil. See glossary page for more information.

    Summary

    CYP2C8 inhibitors are compounds that reduce the activity of the CYP2C8 enzyme, which can reduce drug metabolism, potentially impacting the effects of drug therapy.

    CYP2C8 is a cytochrome P450 (CYP) enzyme found primarily in the liver that is involved in the metabolism of any medications that are CYP2C8 substrates.[1] CYP2C8 inhibitors can reduce the body’s metabolism of these medications.

    The table below outlines some of the most common or clinically relevant CYP2C8 inhibitors.[2][1][3] Importantly, this list is not exhaustive.

    CYP2C8 Inhibitors
    Amiodarone
    Clopidogrel
    Fluoxetine
    Gemfibrozil
    Isoniazid
    Montelukast
    Nortriptyline
    Quercetin
    Trimethoprim
    Verapamil

    References

    1. ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
    2. ^Song Y, Li C, Liu G, Liu R, Chen Y, Li W, Cao Z, Zhao B, Lu C, Liu YDrug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes.Clin Pharmacokinet.(2021-May)
    3. ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)