Table 2

Plasma and CSF pharmacokinetics in rhesus monkey 3 F-ddA versus F-ddI 20 mg/kg i.v. push

ParameterF-ddA DoseF-ddI Dose
F-ddA
 AUC (μg/ml)h plasma2.13
  CSF0.43
  CSF/plasma ratio0.20
 MRT (h) plasma0.21
  CSF2-b 0.71
 ClTB (ml/min/kg)156
 C pmax (μg/ml) plasma8.67
 CSF0.46
F-ddI
 AUC (μg/ml)h plasma18.430.9
  CSF0.790.52
  ratio0.0430.017
 MRT (h) plasma1.261.59
  CSF1.330.99
 T 1/2 elim (h) plasma1.061.67
  CSF2-a 1.241.38
 ClTB (ml/min/kg)10.8
 C pmax (μg/ml) plasma17.8048.5
  CSF0.330.21
Ratios of AUC
 F-ddA/F-ddI plasma0.12
 F-ddA/F-ddI CSF0.54
 total CSF/total plasma2-b 0.0600.017

  • ↵2-a Apparent elimination constant (intercompartmental transfer rate unknown).

  • ↵2-b Total AUC from compound and metabolite in F-ddA equivalents.