Amodiaquine as a prodrug: Importance of metabolite(s) in the antimalarial effect of amodiaquine in humans
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 ide...
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| Veröffentlicht in: | Life sciences (1973) 1985-01, Vol.36 (1), p.53-62 |
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| container_title | Life sciences (1973) |
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| creator | Churchill, Frederick C. Patchen, Leslie C. C. Campbell, Carlos Schwartz, Ira K. Nguyen-Dinh, Phuc Dickinson, Charlotte M. |
| description | 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. |
| doi_str_mv | 10.1016/0024-3205(85)90285-1 |
| format | Article |
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Campbell, Carlos ; Schwartz, Ira K. ; Nguyen-Dinh, Phuc ; Dickinson, Charlotte M.</creator><creatorcontrib>Churchill, Frederick C. ; Patchen, Leslie C. ; C. Campbell, Carlos ; Schwartz, Ira K. ; Nguyen-Dinh, Phuc ; Dickinson, Charlotte M.</creatorcontrib><description>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.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(85)90285-1</identifier><identifier>PMID: 3965841</identifier><identifier>CODEN: LIFSAK</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>Amodiaquine - metabolism ; Amodiaquine - therapeutic use ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiparasitic agents ; Biological and medical sciences ; Biotransformation ; Chromatography, High Pressure Liquid ; Chromatography, Thin Layer ; Gas Chromatography-Mass Spectrometry ; Humans ; Magnetic Resonance Spectroscopy ; Male ; Mass Spectrometry ; Medical sciences ; Pharmacology. 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Campbell, Carlos</creatorcontrib><creatorcontrib>Schwartz, Ira K.</creatorcontrib><creatorcontrib>Nguyen-Dinh, Phuc</creatorcontrib><creatorcontrib>Dickinson, Charlotte M.</creatorcontrib><title>Amodiaquine as a prodrug: Importance of metabolite(s) in the antimalarial effect of amodiaquine in humans</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>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.</description><subject>Amodiaquine - metabolism</subject><subject>Amodiaquine - therapeutic use</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Biotransformation</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Chromatography, Thin Layer</subject><subject>Gas Chromatography-Mass Spectrometry</subject><subject>Humans</subject><subject>Magnetic Resonance Spectroscopy</subject><subject>Male</subject><subject>Mass Spectrometry</subject><subject>Medical sciences</subject><subject>Pharmacology. 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Campbell, Carlos ; Schwartz, Ira K. ; Nguyen-Dinh, Phuc ; Dickinson, Charlotte M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-dee07518b96cbd57b574028062a72cacc8fe8cbe462f4b6d20800b95f5370a0c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Amodiaquine - metabolism</topic><topic>Amodiaquine - therapeutic use</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiparasitic agents</topic><topic>Biological and medical sciences</topic><topic>Biotransformation</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Chromatography, Thin Layer</topic><topic>Gas Chromatography-Mass Spectrometry</topic><topic>Humans</topic><topic>Magnetic Resonance Spectroscopy</topic><topic>Male</topic><topic>Mass Spectrometry</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Churchill, Frederick C.</creatorcontrib><creatorcontrib>Patchen, Leslie C.</creatorcontrib><creatorcontrib>C. Campbell, Carlos</creatorcontrib><creatorcontrib>Schwartz, Ira K.</creatorcontrib><creatorcontrib>Nguyen-Dinh, Phuc</creatorcontrib><creatorcontrib>Dickinson, Charlotte M.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Churchill, Frederick C.</au><au>Patchen, Leslie C.</au><au>C. 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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.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>3965841</pmid><doi>10.1016/0024-3205(85)90285-1</doi><tpages>10</tpages></addata></record> |
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| ispartof | Life sciences (1973), 1985-01, Vol.36 (1), p.53-62 |
| issn | 0024-3205 1879-0631 |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Amodiaquine - metabolism Amodiaquine - therapeutic use Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Biotransformation Chromatography, High Pressure Liquid Chromatography, Thin Layer Gas Chromatography-Mass Spectrometry Humans Magnetic Resonance Spectroscopy Male Mass Spectrometry Medical sciences Pharmacology. Drug treatments |
| title | Amodiaquine as a prodrug: Importance of metabolite(s) in the antimalarial effect of amodiaquine in humans |
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