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Proguanil and chlorproguanil
General information
Proguanil is one of the antimalarial drugs most widely used for prophylactic purposes, usually in combination with chloroquine or atovaquone in malaria prophylaxis, and with atovaquone in malaria treatment [ ]. A biguanide, it is rapidly absorbed in standard doses and mainly excreted by the kidneys. Its antimalarial effect is due to its metabolite cycloguanil. However, its metabolism varies individually, and this is reflected in a variable degree of efficacy [ ].
A derivative, chlorproguanil, is similarly effective in chemoprophylaxis of malaria tropica [ ].
No serious adverse reactions to proguanil have been reported in otherwise healthy patients [ ]. Rashes and hair loss can occur. Mouth ulcers have been mentioned, as have abdominal discomfort and vomiting. The incidence of mouth ulcers in a group of soldiers was 24% in those taking proguanil only and 37% in those taking proguanil 200 mg + chloroquine either 300 or 150 mg weekly [ ]. With the use of large doses hematuria has been seen.
Organs and systems
Hematologic
Since chlorproguanil + dapsone exerts lower resistance pressure on Plasmodium falciparum than pyrimethamine + sulfadoxine does, a randomized trial in out-patients with uncomplicated falciparum malaria was conducted in Africa in 910 children [ ]. Treatment failure was more common with pyrimethamine + sulfadoxine. Despite the rapid elimination of chlorproguanil + dapsone, children treated with this combination did not have more episodes of malaria than those who were treated with pyrimethamine + sulfadoxine. However, there was a higher incidence of anemia.
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