TABLE 2

Relative P450 contribution to the hepatic metabolism, fluconazole dose, and estimated Cmax


Compound

fm

Fluconazole Dosea

Cmax b
CYP1A2
CYP2C9
CYP2C19
CYP2D6
CYP3A4/5
μM
Theophylline 1 NA NA NA NA 200 mg b.i.d. 34.6
Tolbutamide NA 0.72 0.28 NA NA 200 mg q.d. 34.6
Omeprazole NA NA 0.60 NA 0.40 100 mg q.d. 17.3
S-Warfarin NA 1 NA NA NA 300 mg q.d. 51.9
Phenytoin NA 0.90 0.10 NA NA 200 mg q.d. 34.6
Midazolam NA NA NA NA 0.94 200 mg q.d. 34.6
Sirolimus 0 0.15 0 0 0.85 200 mg q.d. 34.6
Cyclosporine NA NA NA NA 0.71 200 mg q.d. 34.6
Tacrolimus
0
0.08
0
0.01
0.47
200 mg q.d.
34.6
  • NA, no information available

  • a For reference, see Table 3

  • b Assume linear pharmacokinetics, i.e., double the dose, double the Cmax