TABLE 5

Ki values for the inhibition of human liver microsomal codeine glucuronidation determined in the absence and presence of 2% (w/v) bovine serum albumin

Ki ± S.E. of parameter fit is shown. Data were best fitted with the expression for competitive inhibition, except for inhibition by dextropropoxyphene (noncompetitive inhibition).

InhibitorKi
Without BSAWith 2%BSA
μM
Dextropropoxyphene29.1 ± 1.2a3.55 ± 0.3a
Fluconazole1341 ± 0.04202 ± 0.001a
Ketoconazole11.3 ± 1.5a0.66 ± 0.01a
Methadone2.95 ± 0.05a0.32 ± 0.03a
  • a Ki value based on the unbound concentration in the incubation medium (i.e. corrected for binding to HLM and BSA.