Enhancement of the antimalarial efficacy of amodiaquine by chlorpheniramine in vivo
Enhancement of the antimalarial efficacy of amodiaquine by chlorpheniramine in vivo
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DOI：
10.1590/s0074-02762007005000038
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发表时间：
2007-06-01
期刊：
影响因子：
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通讯作者：
Oduola, Ayoade MJ
中科院分区：
文献类型：
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作者：
Sowunmi, Akintunde;Gbotosho, Grace O;Oduola, Ayoade MJ
恶性疟原虫对阿莫地喹（AQ）的耐药性在体外可以用抗组胺药和三环类抗抑郁药逆转，但其在体内的意义尚不清楚。本报告介绍了氯苯那敏（一种H-1受体拮抗剂，可在体外逆转氯喹（CQ）耐药性并增强其体内疗效）对AQ抗疟疗效的增强作用，在5名CQ和/或AQ治疗失败的儿童中，这些儿童随后接受AQ + CP联合治疗并治愈，尽管感染儿童的寄生虫携带与AQ抗性相关的突变pfcrtT 76和pfmdr 1 Y86等位基因。这提示了逆转现象的潜在临床应用。
Resistance in Plasmodium falciparum to amodiaquine (AQ) can be reversed in vitro with with antihistaminic and tricyclic antidepressant compounds, but its significance in vivo is unclear. The present report presents the enhancement of the antimalarial efficacy of AQ by chlorpheniramine, an H-1 receptor antagonist that reverses chloroquine (CQ) resistance in vitro and enhances its efficacy in vivo, in five children who failed CQ and/or AQ treatment, and who were subsequently retreated and cured with a combination of AQ plus CP, despite the fact that parasites infecting the children harboured mutant pfcrtT76 and pfmdr1Y86 alleles associated with AQ resistance. This suggests a potential clinical appliation of the reversal phenomenon.