TABLE 3

Time-dependent CYP2D6 inhibition kinetic parameters at pH 7.0 and pH 7.4

Results for the ratio between pH 7.0 and pH 7.4 are given.

Substrate/Inhibitor	fu_{mic pH 7}	K_{I,u pH 7}	k_{inact pH 7}	fu_{mic pH 7.4}	K_{I,u pH 7.4}	k_{inact pH 7.4}	K_I,u	K_inact
		nM	min⁻¹		nM	min⁻¹	Ratio	Ratio
Bufuralol
Paroxetine	0.196	106.43	0.163	0.148	62.60	0.189	1.70	0.86
Desethylamiodarone	0.0011^{^a}	1.47	0.021	0.0011^{^a}	1.41	0.015	1.05	1.40
Dextromethorphan
Paroxetine	0.196	167.38	0.190	0.148	70.30	0.196	2.38	0.97
Desethylamiodarone	0.0011^{^a}	2.19	0.019	0.0011^{^a}	2.38	0.011	0.92	1.73

↵^a fu_mic for inhibitor under in vitro assay conditions prior to dilution (0.5 mg/mL) was calculated from Austin et al. (2002).