TABLE 2

Inhibition of BUP metabolism by ketoconazole and trimethoprim

Results are expressed as percentage inhibition of either BUP consumption or Nor-BUP production by pooled human liver microsomes in vitro (mean of duplicates).




Inhibition of Nor-BUP Production

Inhibition of BUP Consumption
%
Ketoconazole (μM)
    0.25 27.0 52.7
    0.5 42.7 75.2
    1 62.4 85.4
    1.5 64.9 88.5
Trimethoprim (μM)
    10 15.0 0
    25 22.0 0.5
    50 24.6 2.4
    100
30.8
5.1