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

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

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 microsome...

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Veröffentlicht in:Drug Metabolism and Pharmacokinetics 1994, Vol.9(supplement), pp.144-147
Hauptverfasser: CHIBA, Kan, SAITOH, Atuko, CHIBA, Tomie, ISHIZAKI, Takashi, TANI, Masanao, HAYASHI, Masahiro, MATUI, Masayoshi, SHIBA, Kunio, KANEKO, Hideo, NAKATUKA, Iwao, YABUSAKI, Yoshiyasu, NAKAZAWA, Hiroshi
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Sprache:eng
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Zusammenfassung: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
ISSN:0916-1139
DOI:10.2133/dmpk.9.supplement_144