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作 者:麦智广[1] 丁振海[1] 项育英 张进 吕浩[1] 余爱国 叶美珍 蔡惠莉
机构地区:[1]第二军医大学放射医学研究室
出 处:《第二军医大学学报》1989年第6期549-552,共4页Academic Journal of Second Military Medical University
摘 要:辐射增敏剂CMCa为甲硝基咪唑类衍生物,它对肿瘤乏氧细胞有明显的辐射致敏作用,且能浓集癌组织内,是一种有辐射增敏及肿瘤定位特性的化合物。急性毒性试验,犬的近似致死量(ALD)为3.43g/kg,最低致死量(MLD)为4.0 g/kg。小剂量1 g/kg,临床及血相、肝肾功能等无明显变化,属安全剂量。中等剂量(2g/kg),则有呕吐、恶心等胃肠道症状,实验室变化不显著。大剂量(4.0g/kg)表现胃肠道及中枢神经等明显症状。致死原因主要由于DIC,招致脑部血管内凝血,形成血栓性斑块阻塞,各主要实质脏器及肺部出血,是以在此药物剂量范围不能用于临床。由于药物易于沉淀,极不稳定,要考虑改进剂型,临用时新鲜配制,以冀减少药物毒性。Metronidazole derivative CMCa is a kind of radiosensitizers to tumor hypoxic cells. It can highly concentrated in cancer tissues. Acute toxicity assay revealed that ALD was 3.43 g/kg and MLD was 4.0g/kg. No significant changes in clinical symptoms, blood pictures and hepatorenal function were found at small dose (1g/kg), but at middle dose (2 g/kg) nausea and vomiting might occur but not significant in laboratory findings. However at larger dose (4.0 g/kg) the G-I and CNS symptoms were marked, and the cause of death was DIC. So, it can not be used in clinically at this dosage. Owing to the unstability of CMCa it should be prepared freshly before usage.
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