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Metabolism of mefenamic acid and diclofenac was studied using human liver microsomes and recombinant human P450 (CYP2C8, 9, 18 and 19) and compared with that of tolbutamide and S-mephenytoin. Anti-human CYP2C antibodies inhibited all the reactions mentioned above by upto 90% in human liver microsomes. However, the mean Vmax/Km values of diclofenac 4'-hydroxylation and mefenamic acid 3'-hydroxylation in the microsomes obtained from putative poor metabolizers of S-mephenytoin did not differ from those from extensive metabolizers. In addition, there were high correlations (r=0.91-96, P<0.01) among the activities of diclofenac 4'-hydroxylation, mefenamic acid 3'-hydroxylation and tolbutamide hydroxylation, whereas the correlation of these activities with S-mephenytoin 4'-hydroxylation capacity was insignificant or low. Among the CYP2C isoforms studied, CYP2C9 exhibited the highest activities in diclofenac 4'-hydroxylation and mefenamic acid 3'-hydroxylation, whereas CYP2C19 showed a comparable activity with CYP2C9 (70% of CYP2C9) for mefenamic acid. In conclusion, P450 isoform responsible for the metabolism of diclofenac, mefenamic acid and tolbutamide appears to be identical, whereas it seems to be different from that of S-mephenytoin. The study with recombinant P450 suggested that CYP2C9 is an isoform of P450 responsible for the 4'-hydroxylation of diclofenac and mefenamic acid, while CYP2C19 may also be involved in the metabolism of mefenamic acid in addition to CYP2C9.

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ISOFORM(S) OF CYTOCHROME P450 RESPONSIBLE FOR THE METABOLISM OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS: OXIDATIVE METABOLISM OF MEFENAMIC ACID AND DICLOFENAC BY CYP2C SUBFAMILY