TABLE 2

Reversible CYP2D6 inhibition kinetic parameters at pH 7.0 and pH 7.4.

Ratio between pH 7.0 and pH 7.4 results are given.

Substrate/Inhibitorfumic pH 7Ki,u pH 7fumic pH 7.4Ki,u pH 7.4Ki,u
μMμMRatio
Bufuralol
 Quinidine0.9340.0900.9390.0412.21
 Amiodarone0.00200.0960.00160.1120.86
 Desethylamiodarone0.00460.0780.00430.0870.89
 Clozapine0.84328.60.83028.41.01
 Paroxetine0.493a0.460.410a0.331.39
Dextromethorphan
 Quinidine0.946a0.0510.951a0.0261.95
 Amiodarone0.0026a0.0830.0020a0.1340.62
 Desethylamiodarone0.0057a0.0430.0054a0.0341.27
 Clozapine0.870a14.90.859a15.60.96
 Paroxetine0.549a0.320.465a0.281.14
  • a fumic for inhibitor under in vitro assay conditions calculated from Austin et al. (2002).