Influence of different compounds on metabolism of meloxicam by human CYP 3A4
Activator | Activity As % of Control | |
---|---|---|
10 μM | 100 μM | |
Control | 100 | 100 |
Quinine | 90 | 260 |
Cinchonine | 60 | 140 |
Cinchonidine | 170 | 120 |
Quinuclidine | 25 | 12 |
Chloroquine | 5 | 5 |
Hydroquinidine | 360 | 1200 |
Hydroxyquinuclidine | 100 | 19 |
Primaquine | 5 | 7 |
Meloxicam (10 μM) was incubated in 0.1 M Tris buffer, pH 7.4, at 37°C with human CYP 3A4 (0.5 mg of protein/ml), an NADPH-generating system (consisting of 1.2 mM NADP, 0.7 U of glucose 6-phosphate dehydrogenase/ml, 8 mM glucose 6-phosphate), and in the presence of different compounds at two concentrations (10 and 100 μM) for 60 min (mean of duplicate experiments), control 1.7 pmol/min/mg protein. Values were corrected for basic activity (0.14 pmol/min/mg protein) of control microsomes not expressing CYP 3A4.