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Amodiaquine might appear as an alternative in prophylaxis of chloroquine-resistant P. falciparum malaria. In an attempt to explain the discrepancy between its in vivo-in vitro activity, a pharmacokinetic study was conducted in healthy subjects with HPLC assays. The results showed that: amodiaquine was no more detected in the blood, a main metabolite (monodesethyl derivative) appeared as the active form of the drug in vivo, metabolite's half-life had a mean value of 15.6 +/- 5.4 days. This study shows that monodesethylamodiaquine (and not amodiaquine) must be monitored in vitro. Furthermore the high individual variations of blood levels and half-life's values suggest that the weekly prophylactic schedule must be eventually re-evaluated.
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