CYP2C8 inhibitors are chemicals that block the action of the CYP2C8 enzyme, which is essential for the body's metabolism of endogenous substances and a variety of medications. These compounds have the ability to modify drug metabolism and clearance by inhibition of this enzyme, which may result in changes to the toxicity or efficacy of medications. Examples of CYP2C8 inhibitors include the following: Gemfibrozil is a well-known CYP2C8 inhibitor that is frequently prescribed to treat elevated triglyceride and cholesterol levels. It functions by inhibiting the enzyme's activity, which may lead to higher concentrations of medications like repaglinide that are processed by CYP2C8. Clopidogrel: Clopidogrel inhibits CYP2C8, while being mainly recognized as an antiplatelet drug used to prevent heart attacks and strokes. The metabolism of medications such as repaglinide and paclitaxel may be affected by this inhibition. Trimethoprim: Another CYP2C8 inhibitor, trimethoprim is frequently used as an antibiotic to treat a variety of bacterial illnesses. Pioglitazone and repaglinide levels may rise as a result of its inhibitory actions. It has been demonstrated that the drug montelukast, which treats allergic rhinitis and asthma, inhibits CYP2C8 function. It may therefore have an impact on how medications like pioglitazone and repaglinide are metabolized. Quercetin: A naturally occurring CYP2C8 inhibitor, quercetin is a flavonoid present in a wide range of fruits and vegetables. Its inclusion in the diet may affect how medications such as paclitaxel and repaglinide are metabolized. Fluconazole: This antifungal drug inhibits CYP2C8, which impacts how medications like repaglinide and paclitaxel are metabolized. Amiodarone: A CYP2C8 inhibitor, amiodarone is used to treat specific heart rhythm abnormalities. Its inhibitory actions may affect the way medications such as repaglinide and pioglitazone are metabolized. Ticlopidine: A CYP2C8 inhibitor and additional antiplatelet drug. Its use may have an impact on how medications like repaglinide and paclitaxel are metabolized. These are only a few examples of drugs that block the function of CYP2C8. Healthcare providers must be aware of possible drug interactions when co-administering these inhibitors with medications that are CYP2C8 metabolized in order to alter dosages appropriately.
