Summary
Plasma and urine concentrations of amodiaquine (AQ) and desethylamodiaquine (AQm) have been measured after oral administration of AQ 200, 400 and 600 mg in randomised order to 6 healthy subjects.
The relationships between AQ dose size and the areas under the plasma concentration vs time curves for AQ and AQm were linear. Likewise there were linear relationships between AQ dose size and the mass of both AQ and AQm excreted in the urine.
These data indicate that after oral administration within this dose range AQ displays first-order pharmacokinetics.
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References
Bruce Chwatt LJ (1980) Essential malariology. W. Heinemann, London
Churchill F, Patchen L, Campbell C, Schwartz I, Nguyen-Dinh P, Dickinson C (1985) Amodiaquine as a pro-drug: The importance of metabolite(s) in the antimalarial effect of amodiaquine in humans. Life Sci 36: 53–62
Churchill F, Mount D, Patchen L, Björkman A (1986) Isolation, characterization and standardization of a major metabolite of amodiaquine by chromatographic and spectroscopic methods. J Chromatogr 377: 307–318
Frisk-Holmberg M, Bergkvist Y, Domeij-Nyberg B, Hellström L, Jansson F (1979) Chloroquine serum concentration and side effects: Evidence for dose-dependent kinetics. Clin Pharmacol Ther 25: 345–350
Hatton C, Peto T, Bunch C, Pasvol G, Russell S, Singer C, Edwards G, Winstanley P (1986) Frequency of severe neutropaenia associated with amodiaquine prophylaxis against malaria. Lancet 1: 411–414
Lind D, Levi J, Vincent P (1973) Amodiaquine-induced agranulocytosis: Toxic effect of amodiaquine in bone marrow cultures in vitro. Br Med J 1: 458–460
Neftel K, Woodtly W, Schmidt M, Frick P, Fehr J (1986) Amodiaquine-induced agranulocytosis and liver damage. Br Med J 292: 721–723
Rhodes E, Ball J, Frankin I (1986) Amodiaquine-induced agranulocytosis: Inhibition of colony growth in bone marrow by antimalarial agents. Br Med J 292: 717–718
Watkins W, Sixsmith D, Spencer H, Boriga D, Kavinki D, Kipinger T, Koech D (1984) Effectiveness of amodiaquine as treatment for chloroquine-resistant plasmodium falciparum infections in Kenya. Lancet 1: 357–359
Winstanley PA, Edwards G, Orme M, Breckenridge A (1987) The disposition of amodiaquine in man after oral administration. Br J Clin Pharmacol 23: 1–7
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Winstanley, P.A., Edwards, G., Orme, M.L. et al. Effect of dose size on amodiaquine pharmacokinetics after oral administration. Eur J Clin Pharmacol 33, 331–333 (1987). https://doi.org/10.1007/BF00637573
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DOI: https://doi.org/10.1007/BF00637573