TABLE 4

Inhibition of CYP2D by GFA and quinidine

The inhibition constants (Ki values) were calculated from the appropriate nonlinear regression enzyme inhibition model. The mechanism of inhibition was determined graphically.

DrugKiMechanism of Inhibition
µM
GFA
 HLM1.20 ± 0.33Noncompetitive
 rCYP2D60.37 ± 0.16Noncompetitive
 MKLM0.38 ± 0.12Competitive
 DLM2.4 ± 1.3Competitive
Quinidine
 HLM0.19 ± 0.079Competitive
 rCYP2D60.027Competitive (Ching et al., 1995)
 MKLM3.64 ± 1.63Competitive
 DLM2.5 ± 1.29Noncompetitive