Malaria is the most important endemic parasitic disease in the world. Conditions are favorable for transmission of the disease in 60% of Brazil's territory. Over 500,000 cases per year are recorded in the country. However, the geographic distribution is uneven, which may explain differences in the efficacy and effectiveness of antimalarial drugs. We conducted an extensive literature review of antimalarial treatment in Brazil from 1980 to 2005 in order to identify evidence that might have been available for the 2001 Edition of the Malaria Treatment Manual, the official Ministry of Health guidelines. Only a few studies, of low methodological quality, were identified by the search. None of the studies would have been capable of generating evidence-based guidelines according to the current classification of levels of pharmacological and clinical evidence. Studies published after 2001 drew on more evidence and are expected to provide the basis for the next edition of the manual, due in 2007. References in the 2001 Edition were outdated, possibly perceived as traditional references in the field, but lacking in specificity for region, population, and/or type of malaria.