Cytochrome P450 2C8
Also known as: CYP2C8
Cytochrome P450 enzyme that metabolises repaglinide, pioglitazone, paclitaxel and amodiaquine.
CYP2C8 inhibition (e.g. gemfibrozil + repaglinide) raises substrate concentrations and the risk of hypoglycaemia; induction reduces the effect.
Substrates: repaglinide, pioglitazone, paclitaxel, amodiaquine, rosiglitazone.
Inhibitors: gemfibrozil, montelukast, trimethoprim, ketoconazole.
Inducers: rifampicin, carbamazepine, phenytoin.
The gemfibrozil + repaglinide interaction is clinically significant (severe hypoglycaemia) and documented in the repaglinide label.
DailyMed/FDA (NIH/NLM) — approved Repaglinide label; EMC-UK (MHRA) — SmPC
