TABLE 2

Mean inhibitor concentrations evaluated for metabolic drug-drug interaction prediction

InhibitorVictimVictim RouteInhibitor Plasma or Blood Concentration
Cavg,uCmax,obs,u[I]in,u (Cavg)a[I]in,u (Cmax)a
μM
FluvoxamineCaffeinep.o.0.2310.3756.716.85
KetoconazoleMidazolamp.o.0.3621.411.242.29
KetoconazoleMidazolami.v.0.8831.981.772.86
KetoconazoleTemazepamp.o.0.5051.391.392.28
FluoxetineBufuralolp.o.0.5890.8851.521.81
ClomipramineBufuralolp.o.0.0160.0330.1670.184
  • a Estimates of hepatic vein inlet concentration ([I]in) were corrected with published human B:P partitioning values when possible (see Table 3).