AMODIAQUINE AS A PRODRUG - IMPORTANCE OF METABOLITE(S) IN THE ANTIMALARIAL EFFECT OF AMODIAQUINE IN HUMANS
AMODIAQUINE AS A PRODRUG - IMPORTANCE OF METABOLITE(S) IN THE ANTIMALARIAL EFFECT OF AMODIAQUINE IN HUMANS
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DOI：
10.1016/0024-3205(85)90285-1
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发表时间：
1985-01-01
期刊：
影响因子：
6.1
通讯作者：
DICKINSON, CM
中科院分区：
文献类型：
--
作者：
CHURCHILL, FC;PATCHEN, LC;DICKINSON, CM
现有的检测体液中4-氨基喹啉抗疟药阿莫地喹的分析方法是非特异性的，并且掩盖了服用药物的人的血液中几乎不存在阿莫地喹的事实。我们分离了阿莫地喹的四种代谢物。其中一个主要代谢物为脱乙基阿莫地喹，另一个经质子核磁共振波谱初步鉴定为2-羟基脱乙基阿莫地喹。我们开发了一种反相高效液相色谱(HPLC)方法，将这两种主要代谢物彼此分离，并从阿莫地喹中分离出来，从而可以单独进行定量。讨论了这些发现对服用阿莫地喹的人的体外敏感性测试和血液分析的影响。
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 desethyl-amodiaquine, 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.