TABLE 1

Pharmacokinetic parameters of primaquine tested in micea

Primaquine parameterValue(s)
WT mice (n = 3)CYP 2D KO/2D6 KI mice (n = 3)P value (WT vs KO/KI)CYP 2D KO mice (n = 3)P value (WT vs KO)
Plasma
    T1/2 (h)1.5 ± 0.43.9 ± 1.90.23.5 ± 0.90.04
    Tmax (h)1.0 ± 0.92.2 ± 1.80.41.6 ± 2.00.6
    Cmax (ng/ml)249.0 ± 37.01,001.3 ± 204.60.011,017.0 ± 139.90.006
    AUC0-last (h · ng/ml)596.8 ± 119.24,302.5 ± 319.90.000310,874.3 ± 1,470.70.007
    AUC0-inf (h · ng/ml)615.8 ± 112.96,453.5 ± 2,248.20.0510,999.8 ± 1,342.60.006
    VZ/F (ml/kg)73,395.1 ± 24,949.117,237.8 ± 2,950.50.69,601.8 ± 3,673.30.05
    CL/F (ml/h/kg)33,259.2 ± 6,439.13,324.5 ± 972.10.021,836.7 ± 227.80.01
    MRT0-last (h)1.81 ± 0.33.4 ± 0.50.026.1 ± 0.30.00004
Liver
    T1/2 (h)3.6 ± 1.22.9 ± 0.20.55.0 ± 1.50.3
    Tmax (h)0.5 ± 00.5 ± 0NA0.5 ± 0NA
    Cmax (ng/ml)4,915.5 ± 3,068.914,064.7 ± 3,078.40.0232,184.7 ± 9,347.10.041
    AUC0-last (h · ng/ml)8,683.8 ± 3,749.887,629.9 ± 7,742.60.0005286,582.4 ± 19,777.20.002
    AUC0-inf (h · ng/ml)10,355.6 ± 4,284.587,873.1 ± 7,693.90.0006297,827.5 ± 10,050.10.00002
    VZ/F (ml/kg)11,346.7 ± 6,543.3957.2 ± 145.60.1488.2 ± 156.70.1
    CL/F (ml/h/kg)2,219.8 ± 1,068.9228.8 ± 20.00.0867.2 ± 2.20.08
    MRT0-last (h)1.8 ± 0.55.0 ± 0.60.0026.2 ± 0.70.003
  • a Pharmacokinetic parameters from plasma and liver determinations are shown for the various mouse strains. Units for each parameter are indicated, and the errors shown are the standard deviations of the results from triplicate analyses. P values from comparisons of the KO and KO/KI strains to the WT C57BL/6 mice are also indicated. NA, not applicable; calculated values were identical and statistical analysis could not be performed.