Table 2

In vitro inhibition of CYP2D6-catalyzed dextromethorphan O-demethylation by antipsychotic drugs

Antipsychotic DrugType of InhibitionKi
μM
Perphenazine2-b Partial Competitive0.8  ± 0.42-a
Thioridazine2-b Partial Competitive1.4  ± 0.8
ChlorpromazineCompetitive6.3  ± 3.8
Haloperidol2-b Partial Competitive7.2  ± 4.9
FluphenazineCompetitive9.4  ± 1.5
RisperidoneCompetitive21.9  ± 1.7
ClozapineCompetitive39.0  ± 14.4
cis-ThiothixeneCompetitive65.0  ± 42.7
  • 2-a Each value indicates mean ± S.D. obtained from three different livers.

  • 2-b Mean (S.D.) of α, a factor by which Kmchanges when inhibitor occupies the enzyme: perphenazine, 22.2 ± 1.6; thioridazine, 72.5 ± 28.9; haloperidol, 5.7 ± 1.9.