Toxicity and repository antimalarial activity of octanoyl primaquine

Octanoyl primaquine, a new compound synthesized in our College, was dissolved in castor oil and tea seed oil (3: 2). In mice, a single sc of 400 mg/kg almost completely prevented or suppressed patent infections of trophozoite-inducedup to 3—4 wks (Table 1). In antirelapse experiments against secondary tissue schizonts in rhesus monkeys, im 10 mg/kg showed an appreciable activity against tissue stage (Table 2). The acute sc LDin mice=798±28 mg/kg. In dogs, im 60 mg/kg, not 30 mg/kg, caused intestinal bleedings in one of the 5 dogs, and a slight hyperemia of injected muscle tissue was found at the im sites in 5 d. No discernible gross reactions were observed at 72, 120 and 168 h after im in rabbits. All of the 16 monkeys tolerated the dose of 5—20 mg/kg well.