Table 1

Benzydamine metabolism by liver preparations

SpeciesSystemReferenceKmVmax1-aV/K1-b In vitro t1/2CLint′Well-stirred CLb
μM ml/min/mg min ml/min/kg
HumanFMO3 Lang and Rettie, 2000 80  ± 836  ± 20.0434.012.6
HLM Stormer et al., 2000 64  ± 176.9  ± 3.60.11101.916.7
RatRLM Kawaji et al., 1993 15  ± 137  ± 32.474446.068.9
Humanhepatocytes14551.714.4
HLM+NADPH1-c 8.938.413.2
HLM-NADPH15.122.610.6
Rathepatocytes2.33254.168.5

Benzydamine in vivo CL = 2.4 ml/min/kg (Chasseud and Catanese, 1985; Schoenwald et al., 1987) assuming a 70 kg human.

  • RLM, rat liver microsomes; HLM, human liver microsomes.

  • 1-a  Vmax in nmol/min/mg, except FMO3 in nmol/min/nmol.

  • 1-b  FMO3 V/K, in ml/min/nmol, was converted to ml/min/mg assuming 80 pmol/mg human liver microsomes (Haining et al., 1997).

  • 1-c  HLM were prewarmed with or without NADPH present, and reaction was initiated with either NADPH or substrate.