Table 5

Predicted lornoxicam/phenprocoumon interactions

Lornoxicam (inhibitor)(S)-Phenprocoumon (substrate)Lornoxicam (substrate)rac-Phenprocoumon (inhibitor)
Therapeutic concentration (μM)[I] = 35-a [S] = 0.0185-b [S] = 35-a [I] = 0.0535-c
K m (μM)0.65-d 12
K i (μM)121.2
f h 0.975-e 15-a
f m 0.605-e 0.95-a
[I]/K i 0.250.044
Percent inhibition19.53.4
R 0.81
R c 1.131
R observed 1.245-b ?5-f

Drug/drug interactions were predicted as described in the text. The therapeutic concentration describes the concentration expected in the cytosol of the hepatocyte under therapeutic conditions. These values were derived as described in the text. Percent inhibition,R, and Rc were calculated as described in the text. Robserved indicates the degree of change in AUCSS or CSS in a clinical interaction study.

  • 5-a Skjodt and Davies, 1998.

  • 5-b Masche et al., 1999b.

  • 5-c Kitteringham et al., 1984.

  • 5-d Jones et al., 1996.

  • 5-e Toon et al., 1985.

  • 5-f no clinical data available.