A STATISTICAL-ANALYSIS OF THE ANTIMALARIAL ACTIVITY OF PROGUANIL AND CYCLOGUANIL IN HUMAN VOLUNTEERS

Proguanil, an orally administered antimalarial drug, was given to 36 i ndividuals (200 mg daily for 3 days). The antimalarial activity in pla sma samples collected after the drug administration was then determine d by bioassay. Concentrations of proguanil and cycloguanil (the princi pal active metabolite) in these samples were also measured by high per formance liquid chromatography. A regression analysis was then perform ed on these variables to determine if the antimalarial activity of the samples was due to proguanil alone or to proguanil and cycloguanil to gether. The analysis indicated that cycloguanil is the main determinan t of antimalarial activity after proguanil administration and that the activity of cycloguanil is not influenced by the presence of proguani l.