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

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 1985Publisher:Elsevier BVJournal:Life Sciences, volume 36, pages 53-62 (issn: 0024-3205,

Authors: Ira K. Schwartz; Leslie C. Patchen; Carlos C. Campbell; Phuc Nguyen-Dinh; Frederick C. Churchill; Charlotte M. Dickinson;

doi: 10.1016/0024-3205(85)90285-1

pmid: 3965841

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

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Abstract

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.

Related Organizations

Austin Health & Human Services Department
United States

Keywords

Male, Magnetic Resonance Spectroscopy, Amodiaquine, Humans, Chromatography, Thin Layer, Biotransformation, Chromatography, High Pressure Liquid, Gas Chromatography-Mass Spectrometry, Mass Spectrometry

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	citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	111
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	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Top 1%
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 10%