肖树华, 邵葆若, 颜克坚, 湛崇清, 刘瑞君, 杨惠中, 徐月琴, 郭惠芳, 吴珍, 俞子平. 硝唑咪衍生物S72014实验治疗动物血吸虫病的疗效与毒性的研究J. 药学学报, 1980, 15(8): 456-462.
引用本文: 肖树华, 邵葆若, 颜克坚, 湛崇清, 刘瑞君, 杨惠中, 徐月琴, 郭惠芳, 吴珍, 俞子平. 硝唑咪衍生物S72014实验治疗动物血吸虫病的疗效与毒性的研究J. 药学学报, 1980, 15(8): 456-462.
Xiao Shuhua, Shao Baoruo, Yan Kejian, Zhan Chongqing, Liu Ruijun, Yang Huizhong, xu Yueqin, Guo Huifang, Wu Zhen , Yu Ziping, . STUDIES ON THE EFFECTIVENESS AND TOXICITY OF A NIRIDAZOLE DERIVATIVE S 72014 IN EXPERIMENTAL CHEMOTHERAPY OF SCHISTOSOMIASIS JAPONICAJ. Acta Pharmaceutica Sinica, 1980, 15(8): 456-462.
Citation: Xiao Shuhua, Shao Baoruo, Yan Kejian, Zhan Chongqing, Liu Ruijun, Yang Huizhong, xu Yueqin, Guo Huifang, Wu Zhen , Yu Ziping, . STUDIES ON THE EFFECTIVENESS AND TOXICITY OF A NIRIDAZOLE DERIVATIVE S 72014 IN EXPERIMENTAL CHEMOTHERAPY OF SCHISTOSOMIASIS JAPONICAJ. Acta Pharmaceutica Sinica, 1980, 15(8): 456-462.

硝唑咪衍生物S72014实验治疗动物血吸虫病的疗效与毒性的研究

STUDIES ON THE EFFECTIVENESS AND TOXICITY OF A NIRIDAZOLE DERIVATIVE S 72014 IN EXPERIMENTAL CHEMOTHERAPY OF SCHISTOSOMIASIS JAPONICA

  • 摘要: 口服硝唑咪衍生物S 72014对小鼠血吸虫病的化疗指数为21.2,较硝唑咪的5.8为大。病兔用S 72014 50~200mg/kg/天的2~14天疗法治疗时,减虫率均在90%以上。感染犬与猴每天用S 72014,125~210 mg/kg治疗,3次分服,疗程为7~14天时,均获得治愈。S 72014对小鼠的毒性较硝唑咪的低9倍以上。S 72014对小鼠和犬的中枢神经系统的作用较硝唑咪的为轻。在所用的剂量下,S 72014对犬与猴的肝、肾功能无明显影响,对心电图则引起暂时性的S-T段压低和T波平坦。较大剂量的S 72014对犬与猴的中枢神经系统、肝及肾有暂时性的病理损害,且明显抑制雄性动物的生精过程。S 72014与硝唑咪对犬可引起严重的再生障碍性贫血,但对猴的造血功能则无影响。

     

    Abstract: S72014 is a derivative of niridazole. It has been found that the therapeutic index of S72014 to mice was 21.2, while that of niridazole was 5.8. When rabbits infected with schistostomes were treated orally with S72014 at the dosage of 200 mg/kg/day for 2~3 days, or 50~70 mg/kg/day, for 10~14 days, the worm reduction rates were higher than 90%, with part of the animals completely cured. After its administration to infected dogs at the dosage of 41.7 or 66.7 mg/kg thrice daily for 7 days, all the animals were found to be free of worms. The same promising effect was observed in infected monkeys treated with S72014 at the dosage of 70 mg/kg thrice daily for 14 days.The toxicity of S72014 to mice was at least nine fold lower than that of niridazole. In both mice and dogs, the toxic action of S72014 on the central nervous system was less than that of niridazole. After administration of S 72014 to dogs and monkeys, no apparent effect on hepatic and kidney function was observed, but the ECG showed a low voltage in S-T segement and flattened T wave. With bigger dosage of both drugs, reversible pathological lesions were observed in the liver, kidney and central nervous system of the dogs and monkeys, and the spermatogensis of male animals was suppressed significantly. In dogs treated with S 72014 or niridazole twice or thrice daily for 7~14 days, the most serious side effect was aplastic anemia, which, nevertheless, was not observed in monkeys.

     

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