1 Chloroquine, primaquine and ethidium inhibited thymidine incorporation into deoxyribonucleic acid of rat tissues when administered concurrently with the labelled precursor. 2 Chloroquine and primaquine inhibited the incorporation of uridine and adenine, but not orotate, into various ribonucleic acid fractions of liver of rats and mice. These drugs had no effect on leucine incorporation into hepatic protein in rats or mice. 3 Although chloroquine and primaquine are active against different stages in the life cycle of the malarial parasites, the two aminoquinolines exert similar effects in rodent tissues.
The distribution of primaquine was measured in seven rat tissues at 15–180 min after the intraperitoneal injection of the antimalarial 8-aminoquinoline. The half-life of unmetabolized primaquine was 4.0 h in lung, 1.7–1.9 h in blood, spleen, kidney and heart, and 1.2 h in liver. At each interval, the concentrations of unmetabolized primaquine were (in order): lung > liver, kidney, spleen > heart > brain ≧ blood. At 3 h after the injection of [6-O-methyl-3H]primaquine, unmetabolized primaquine constituted 10% of the total 3H in blood and 40–60% of the total 3H in liver, brain, heart and kidney.
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