TABLE 4

Predicted and observed pharmacokinetic parameters of CYP3A4 inducers after multiple oral doses

InducerDose RegimenCmax, ssAUCssReference
PredictedObservedPredictedObserved
μg/mlμg · h/ml
Rifampin300 mg b.i.d. for 14 days4.044.5 ± 1.4433.213.5 ± 4.2Drusano et al., 1986
Carbamazepine200 mg b.i.d. for 32 days6.78–12.2a6.97 ± 0.6498.7–182a70.3 ± 8.92Rapeport et al., 1996
Phenobarbital100 mg q.d. for 38 days13.416.8354342Reidenberg et al., 1995
  • a The predicted Cmax, ss and AUCss values for CBZ are the range of Simcyp predictions using the in vitro CYP3A4 induction data from the respective three hepatocyte donors (donor 1, 2, or 3 in Table 2).