Volume 21, Issue 4
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645


Resistance of human plasmodia to folic acid antagonists, such as chlorguanide or pyrimethamine, became apparent soon after introduction of these agents for the prophylaxis and treatment of malaria about two decades ago. Malariologists were generally not too concerned with this development because these drugs, although valuable in the chemoprophylaxis of malaria and the prevention of its transmission, exert a slow effect against asexual blood forms and are not recommended for treatment of acute attacks of malaria. The 4-aminoquinolines, on the other hand, are rapidly effective against asexual erythrocytic parasites of any one of the four species that infect man. Their toxicity is low at doses ordinarily employed for therapy of malaria and they have been generally regarded as the drugs of choice for treatment of an acute attack of malaria. Consequently, with the emergence of chloroquine-resistant strains of in South America and Southeast Asia the potential gravity of the situation quickly became apparent because of the known limitations of other available antimalarial drugs.


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