Table 1.
Chloroquine pharmacokinetic data from healthy mammalian species
Matrix and species | n | Wt (kg) | Half-life (h) | CLa (liters/h/kg) | Va (liters/kg) | Reference |
---|---|---|---|---|---|---|
Plasma | ||||||
Mice | 0.03 | 46.6 | 9.9 | 667 | —f | |
Ratsb | 0.25 | 10.8 | 10.4 | 163 | 55 | |
Rabbitsc | 5 | 1.25 | 26.7 | 5.9 | 226 | 50 |
Monkeysc | 6 | 4.5 | 18.8 | 2.34 | 63 | 57 |
Human, adults | 11 | 75 | 282 | 0.58 | 204 | 27 |
Human, adults | 5 | 72 | 1,392 | 0.88 | 710 | 22 |
Human, adults | 7 | 58 | 217 | 0.68 | 181 | 3 |
Human, adults | 6 | 54 | 250 | 0.74 | 261 | 69 |
Human, adults | 8 | 58 | 192 | 0.55 | 154 | 69 |
Human, adults | 10 | 54 | 268 | 0.66 | 132 | 19 |
Human, adults | 5 | 64 | 386 | 0.44 | 250 | 71 |
Human, adults | 4 | 76 | 374 | 0.58 | 302 | 71 |
Human, adults | 5 | 73 | 479 | 0.57 | 283 | 71 |
Human, adults | 6 | 45 | 67 | 0.83 | 82.6 | 17 |
Human, adults | 5 | 58 | 70.5 | 0.62 | 63.5 | 17 |
Human, adults | 30 | 52 | 291 | 0.46 | 129.5 | 32 |
Total no. of human adultsd | 102 | |||||
Mean ± SEM | 62 ± 3 | 304 ± 31 | 0.63 ± 0.04 | 211 ± 22 | ||
Whole blood | ||||||
Micee | 0.025 | 16.5 | 13.1 | 11 | ||
Rabbits | 8 | 2.0 | 223 | 0.31 | 86 | 2 |
Dogs, beagle | 7 | 11.8 | 302 | 0.13 | 53 | 1 |
Human, adults | 5 | 72 | 1,248 | 0.091 | 81 | 22 |
Human, adults | 7 | 59 | 150 | 0.21 | 45.3 | 47 |
Human, adults | 17 | 66.5 | 162 | 0.25 | 57.8 | 59 |
CL is apparent clearance (CL/F), and V is apparent volume of distribution (V/F).
Pharmacokinetic parameters determined from concentration-time profile of 48 h after dose.
Pharmacokinetic parameters determined from concentration-time profile of 24 h after dose.
Pharmacokinetic data from 12 human studies comprising 102 volunteers.
Pharmacokinetic parameters determined from concentration-time profile of 4 h after dose.
—, present study.