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Enhancement of the antimalarial effect of chloroquine by chloropheniramine in vivo

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Summary The efficacy of chloroquine and chloroquine plus chloropheniramine, a histamine H1 receptor blocker which reverses chloroquine insensitivity in Plasmodium falciparum in vitro, was studied in 96 children with acute symptomatic uncomplicated falciparum malaria. The chloroquine/chloropheniramine combination produced a significantly higher cure rate than chloroquine alone and cured 77% of children with chloroquine treatment failures. Children with chloroquine treatment failure had mean plasma chloroquine concentrations above the minimum therapeutic concentration for the area. Chloroquine concentrations in plasma and red blood cells and ratio of red cell to plasma chloroquine concentrations on days 3 and 7 after initiation of therapy were not significantly different in the two groups. Chloroquine/chloropheniramine produces a higher cure rate than chloroquine alone and reverses chloroquine insensitivity in Plasmodium falciparum in vivo. It may be a useful way of optimising the antimalarial effect of chloroquine.

Keywords: Chloroquine resistance; children; chloroquine; chlorpheniramine; falciparum malaria; in vivo; reversal

Document Type: Original Article


Affiliations: Department of Pharmacology and Therapeutics and Postgraduate Institute for Medical Research and Training, University of Ibadan,Ibadan, Nigeria

Publication date: March 1, 1998


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