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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。
Radiation sensitizer CMCa is a p-nitroimidazole derivative which has obvious radiation-sensitizing effect on tumor hypoxia cells and can concentrate in cancer tissues. It is a compound with radiation sensitization and tumor localization. The acute toxicity test showed an approximate lethal dose (ALD) of 3.43 g / kg in dogs and a minimum lethal dose (MLD) of 4.0 g / kg. Small doses of 1 g / kg, clinical and blood, liver and kidney function, no significant change, is a safe dose. Moderate dose (2g / kg), then there vomiting, nausea and other gastrointestinal symptoms, laboratory changes were not significant. High-dose (4.0g / kg) showed obvious symptoms such as gastrointestinal tract and central nervous system. The main cause of death due to DIC, leading to intracranial coagulation of blood vessels, the formation of thrombotic plaque obstruction, the main real organs and pulmonary bleeding, so the drug dose range can not be used in clinical. As the drug is easy to precipitate, very unstable, to consider improving the dosage form, when used fresh preparation, in order to reduce drug toxicity.