Amodiaquine as a prodrug: importance of metabolite(s) in the antimalarial effect of amodiaquine in humans

Life Sci. 1985 Jan 7;36(1):53-62. doi: 10.1016/0024-3205(85)90285-1.


Existing analytical methods for assaying the 4-aminoquinoline antimalarial amodiaquine in body fluids are nonspecific and obscure the fact that little or no amodiaquine is present in the blood of dosed persons. We have isolated four metabolites of amodiaquine. The two major metabolites have been identified; one is desethylamodiaquine, and the other has been tentatively identified on the basis of proton nuclear magnetic resonance spectroscopy as 2-hydroxydesethylamodiaquine. We developed a reverse-phase high-performance liquid chromatographic (HPLC) method that separates the two major metabolites from each other and from amodiaquine, allowing separate quantification. The impact of these findings on in vitro sensitivity testing and blood analysis of persons dosed with amodiaquine is discussed.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amodiaquine / metabolism*
  • Amodiaquine / therapeutic use
  • Biotransformation
  • Chromatography, High Pressure Liquid
  • Chromatography, Thin Layer
  • Gas Chromatography-Mass Spectrometry
  • Humans
  • Magnetic Resonance Spectroscopy
  • Male
  • Mass Spectrometry


  • Amodiaquine