TABLE 1

Estimated human clinical concentrations and Ki values for CYP2D6 inhibition by bupropion and metabolites


Inhibitor

Total Clinical Plasma Cmaxa

fu

Unbound Clinical Plasma Cmax

Estimated Human Liver Concentrationb

Ki
μM μM μM μM
Bupropion 0.67 0.16c 0.11 0.605–1.03 21
Hydroxybupropion 4.01 0.23a 0.92 5.06–8.65 13.3
Threohydrobupropion 2.34 0.58a 1.35 7.43–12.7 5.4
Erythrohydrobupropion
0.43
0.58a
0.25
1.38–2.35
1.7
  • a Findlay et al., 1981

  • b Based on a liver/plasma ratio of 5.5:1–9.4:1 (determined from qWBA studies in rats dosed with 14C-hydroxybupropion)

  • c Internal data; not published