Influence of quinidine on metabolism of meloxicam, testosterone, and nifedipine by human liver microsomes and recombinant human CYPs
Substrate | Substrate Concentration | Activator | Activator Concentration | Control | |
---|---|---|---|---|---|
μM | μM | % | |||
Microsomes | Meloxicam | 10 | 100 | ||
Microsomes | Meloxicam | 10 | Quinidine | 10 | 140 |
Microsomes | Meloxicam | 10 | Quinidine | 100 | 280 |
CYP 2C9 | Meloxicam | 10 | 100 | ||
CYP 2C9 | Meloxicam | 10 | Quinidine | 10 | 110 |
CYP 2C9 | Meloxicam | 10 | Quinidine | 100 | 60 |
CYP 3A4 | Meloxicam | 10 | 100 | ||
CYP 3A4 | Meloxicam | 10 | Quinidine | 10 | 160 |
CYP 3A4 | Meloxicam | 10 | Quinidine | 100 | 510 |
CYP 3A4 | Testosterone | 50 | 100 | ||
CYP 3A4 | Testosterone | 50 | Quinidine | 10 | 120 |
CYP 3A4 | Testosterone | 50 | Quinidine | 100 | 60 |
CYP 3A4 | Nifedipine | 200 | 100 | ||
CYP 3A4 | Nifedipine | 200 | Quinidine | 10 | 30 |
CYP 3A4 | Nifedipine | 200 | Quinidine | 100 | 10 |
Values were corrected for basic activity (0.14 pmol/min/mg protein) of control microsomes not expressing CYP 3A4 or CYP 2C9 (mean of duplicate to triplicate experiments).