Effect of nilvadipine, a dihydropyridine calcium antagonist, on cytochrome P450 activities in human hepatic microsomes.
Article Details
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Niwa T, Shiraga T, Hashimoto T, Kagayama A
Effect of nilvadipine, a dihydropyridine calcium antagonist, on cytochrome P450 activities in human hepatic microsomes.
Biol Pharm Bull. 2004 Mar;27(3):415-7.
- PubMed ID
- 14993813 [ View in PubMed]
- Abstract
The effects of nilvadipine, a dihydropyridine calcium antagonist, on cytochrome P450 (CYP) activities in human hepatic microsomes were investigated. Nilvadipine competitively inhibited CYP1A2-mediated 7-ethoxyresorufin O-deethylase, CYP2A6-mediated coumarin 7-hydroxylase, CYP2C8/9-mediated tolbutamide methylhydroxylase, CYP2C19-mediated S-mephenytoin 4'-hydroxylase, and CYP3A4-mediated nifedipine oxidase activities, and the inhibition constant (Ki) values were 13.0, 35.8, 5.02, 24.5 and 44.3 microM, respectively. On the other hand, no inhibition of CYP2B6-mediated 7-benzyloxyresorufin O-debenzylation, CYP2D6-mediated bufuralol 1'-hydroxylation, or CYP2E1-mediated chlorzoxazone 6-hydroxylation by nilvadipine at 40 microM concentration was observed. The free fractions of nilvadipine in the incubation mixture estimated by ultracentrifugation were 18.9-27.4%. These results suggest that nilvadipine would not cause clinically significant interactions with other drugs, which are metabolized by CYPs, via the inhibition of metabolism.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Nilvadipine Cytochrome P450 2A6 Protein Humans UnknownInhibitorDetails Nilvadipine Cytochrome P450 2C19 Protein Humans UnknownInhibitorDetails Nilvadipine Cytochrome P450 2C8 Protein Humans UnknownInhibitorDetails Nilvadipine Cytochrome P450 2E1 Protein Humans UnknownSubstrateDetails Nilvadipine Cytochrome P450 3A4 Protein Humans UnknownSubstrateInhibitorDetails