Table 1.
Comparison of pharmacokinetic and pharmacodynamic properties of CQ and HCQ.
| Parameters | Chloroquine | Hydroxychloroquine |
|---|---|---|
| Formulation | Chloroquine phosphate | Hydroxychloroquine sulfate |
| Absorption | Upper gastrointestinal tract | Upper gastrointestinal tract |
| Bioavailability | 70-80% | 70-80% |
| Plasma protein binding | 40-50% | 40-50% |
| Volume of distribution in plasma | 65,000L | 42,257L |
| Volume of distribution in blood | 15,000L | 5,500L |
| Metabolism by liver | Desethylchloroquine | Desethylchloroquine Desethylhydroxychloroquine |
| Total blood clearance | 129 ± 35 mL/min | 96 ± 5 mL/min |
| Total plasma clearance | 1099 ± 155 mL/min | 667 ± 235 mL/min |
| Elimination half life | 288 hours | 1200 hours |
| Terminal half life | 45 ± 15 days | 41 ± 11 days |
| Renal clearance | 51% | 21% |
| Unmetabolized excretion | 58% | 62% |