(R)-Primaquine

(R)-Primaquine ((−)-Primaquine) (11.1-100 mg/kg; p.o.; once daily; for 3 consecutive days) exhibits dose-dependent blood schizonticidal activity against Plasmodium berghei in Swiss Webster mice. At a dose of 100 mg/kg/day administered for 3 days, it achieves 100% suppression of parasitemia, 100% survival rate, and a 40% cure rate^[3].
(R)-Primaquine (10-160 mg/kg; p.o.; daily administration; for 3 consecutive days) exhibits causal prophylactic activity against liver-stage Plasmodium berghei infection induced by sporozoites in ICR mice, with an ED₈₀ of 63.7 mg/kg/day, and achieves 100% protection at 80 mg/kg/day.^[3]
(R)-Primaquine (2-10 mg/kg; p.o.; daily administration; for 21 consecutive days) shows no efficacy against Pneumocystis carinii infection in immunosuppressed BALB/c mice when administered at the highest dose of 10 mg/kg/day for 21 days^[3].
(R)-Primaquine (6.25-12.5 mg/kg; intraperitoneal injection; twice daily for 7 consecutive days) causes only mild hemolysis in G6PD-deficient human erythrocytes transplanted into NOD-SCID mice. At doses up to 12.5 mg/kg/day administered for 7 days, its hemolytic activity is significantly lower than that of (S)-primaquine^[3].
(R)-Primaquine (4.86 mg/kg; p.o.; once daily; for 3 consecutive days) is well tolerated in female Beagle dogs after administration at a dose of 4.86 mg/kg/day for 3 days, with no significant systemic toxicity, methemoglobinemia, or organ damage observed^[3].
(R)-Primaquine (1.3-4.5 mg/kg/day; oral administration; once daily; for 7 consecutive days) induces dose-dependent increases in methemoglobin, reticulocytes, and alanine transaminase (ALT) in healthy G6PD-normal rhesus monkeys, and no severe reversible hepatotoxicity is observed at doses up to 4.5 mg/kg/day^[4].