Metabolism and Distribution of Primaquine in Monkeys

Abstract

Rhesus monkeys were administered primaquine diphosphate (6.0 to 10.5 mg/kg, I.V.), and plasma samples were analyzed by high performance liquid chromatography for the presence of the unchanged drug and the major metabolite , 8-(3-carboxy-l-methylpropylamino)-6-methoxyquinoline (II). Primaquine had an unusually high affinity for tissue compartments which produced a rapid initial drop in plasma concentration. Within 15 minutes, the plasma concentration of II far exceeded that of primaquine. 35 to 83 % of the primaquine dose was converted to II; moreover, metabolite II possessed much lower affinity for the tissue compartments than primaquine itself.