TABLE 3

Estimated pharmacokinetic and pharmacodynamic parameters


Parameter

Final Estimate

CV%
Pharmacokinetic parameters
   ka (min–1) 0.02 4.96
   Vmax (μg/min/kg) 5324 6.89
   Km (μg/ml) 579 12.5
   CLin (ml/min/kg) 0.01 20.1
   CLout (ml/min/kg) 0.06 19.7
   Vp (ml/kg) 458 2.47
   VECF (ml/kg) 1.16a c
   F 0.92a c
Pharmacodynamic parameters
   kin 3.28b c
   kout (min–1) 0.03 40.0
   Imax 0.51 22.4
   IC50, acute (μg/ml) 12.7 103
   IC50, chronic (μg/ml)
99.1
46.3
  • a Parameter was fixed, not estimated

  • b Secondary parameter calculated as: kin = Ro × kout

  • c Not applicable