Table 2.
Drugs used for the various studies with references and total and free plasma concentrations in patients
| Reference(s) | Compound | Mol wt | % protein binding | Mean therapeutic Cmax |
|||
|---|---|---|---|---|---|---|---|
| ng/ml |
μMa |
||||||
| Total | Free | Total | Free | ||||
| Eurartesim SmPCb | Piperaquine 4H2PO4 | 927.50 | 99 | 448c | 4.5 | 0.836 | 0.008 |
| Dihydroartemisinin | 284.35 | 90 | 752 | 75 | 2.65 | 0.265 | |
| Coartem SmPC | Lumefantrine | 528.94 | 99 | 9,800 | 98 | 18.5 | 0.185 |
| Artemether | 298.37 | 95 | 84 | 3.9 | 0.281 | 0.013 | |
| 45, 49 | Chloroquine 2H2PO4 | 515.86 | 59 | 320 | 131 | 1 | 0.41 |
| 45, 49 | Halofantrine HCl | 536.88 | 83 | 1,799 | 305.8 | 3.35 | 0.57 |
| 45, 49 | Mefloquine HCl | 414.77 | 98 | 1,037 | 20.7 | 2.5 | 0.05 |
| 32 | Dofetilide | 441.56 | 70 | 2 | 0.6 | 1.36 | 0.41 |
a
Data are in nM for dofetilide.
b
SmPC, summary of product characteristics.
c
The datum was obtained from single-dose Cmax by applying an accumulation factor of 2.5.