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Data on tolerance of laboratory animals to the antimalarial preparation cycloquine

, : Data on tolerance of laboratory animals to the antimalarial preparation cycloquine. Med Parazitol I Parazitar Bolezni 28(4): 443-448

Cycloquine, which differs from amodiaquin only in having one additional 5-diethylaminomethyl group, is readily soluble in benzene, acetone, alcohol, ether, slightly soluble in petroleum ether and insoluble in water. In mice, the LD50'S of cycloquine, chloroquine and quinacrine were 380, 460 and 600 mg/kg orally and 215, 125 and 345 mg/kg subcutaneously. The tolerance of rats and rabbits to cycloquine after a single oral dose was somewhat lower than to chloroquine. After injection at 200 mgAg/day for 10 days, cycloquine was better tolerated by rats than chloroquine and particularly quinacrine. At the same doses, (he weight increase was the greatest in the group of animals given cycloquine and the lowest in the group of animals given quinacrine. In rats, given 100 mgAg of cycloquine by mouth daily for 10 days there were no pathological changes in blood or in the liver, kidney, heart muscle or spleen. Increasing the doses to 200 mgAg caused granular dystrophy of cells in the liver parenchyma and epithelium of the convoluted tubules of the kidneys, but had no effect on the general condition of the rats.


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