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洛美沙星的临床前药理学研究表明,小鼠一次口服给药的半数致死量为1782,0mg/kg,静脉为340.2m/kg,皮下为995.3mg/kg。大鼠口服的LD50>5000mg/kg。大鼠口服洛美沙星50或200mg.kg90天,一般状况良好,食物水分消耗,血液、尿液、血清生化学以及主要脏器的组织病理学检查等未见明显异常,但800mg/kg组动物体重增长明显受抑制;部分动物出现尿药结晶;各给药组动物盲肠重量增加,且与给药剂量呈线性关系。小鼠口服本品对神经系统无明显影响,麻醉犬口服本品对呼吸系统和心血管系统也无明显影响,但静脉注射较大剂量本品时(10mg/kg)可使血压剧烈下降,呼吸频率和心率明显加快等。小鼠器官分化期给药的致畸胎试验表明洛美沙星无致畸胎作用。致突变试验中小鼠微核试验为阴性,但洛美沙星对鼠伤寒沙门氏菌TA102菌株具有诱变作用,Ames′试验结果为阳性。
Preclinical pharmacological studies of lomefloxacin showed that the mice were once orally administered with a lethal dose of 1782,0 mg / kg, a venous 340.2 m / kg, and a subcutaneous dose of 995.3 mg / kg. Oral LD50 rat> 5000mg / kg. Rats were orally given either lomefloxacin 50 or 200 mg. kg 90 days, the general condition is good, no obvious abnormalities were found in blood, urine, serum biochemistry and histopathological examination of major organs, but the body weight gain of 800 mg / kg group was significantly inhibited; some animals showed urine The crystal of drug was increased. The weight of cecum in each group was increased, and the dose was linear. Mice oral administration of this product has no significant effect on the nervous system, anesthetized dogs oral administration of this product on the respiratory system and cardiovascular system also had no significant effect, but intravenous injection of larger doses of this product (10mg / kg) can cause severe drop in blood pressure, Significantly faster frequency and heart rate. Teratogenicity tests administered to mice during organ differentiation indicate that lomefloxacin has no teratogenic effect. Mice micronucleus test was negative in mutagenicity test, but Lomefloxacin had mutagenic effect on Salmonella typhimurium TA102 strain, Ames’ test result was positive.