Table 1

Enzyme kinetic parameters for fluvoxamine inhibition of (S)-mephenytoin metabolism and free fractions of fluvoxamine in microsomal incubations from six human livers

Human LiverKmVmaxKi,totalFree Fraction1-aKi,ub
μM nmol/min/mg protein nM f u,mic nM
HL105370.543230.2787
HL114210.162010.3468
HL134280.251850.3768
HL135330.0682410.3277
HL152430.0572560.3179
HL157390.0482010.3876
Mean340.192350.3376
S.D.7.90.19510.047.1

Protein concentration is 0.5 mg/ml.

  • 1-a Fluvoxamine spiked concentration was 0.3 μM.