【摘要】 提要对樯酰苯胺（603马来酸盐）的毒性研究,分为小鼠急性毒性、狗的亚急性毒性和小鼠致畸试验三个方面进行。给小鼠口服即灌胃（po）、腹腔注射（ip）和静脉注射（iv）的LD₅₀分别为1145±257、236.84±30.1和65.8±5.9mg/kg,连续给药7～10d,蓄积毒性不明显。狗的亚急性毒性试验,用本药肌肉注射（im）每天15 mg/kg,连续给药6周,主要反应产生癫痫样的惊厥、流涎、恶心、呕吐、体重减轻。其中一条狗因惊厥反复发作而死亡,病理切片见到肝细胞坏死和肾小球明显充血。血象、心电图、肝肾功能和尿常规未见异常。致畸试验未见胎仔畸变,但却发现约2％的胎仔有胸骨骨化迟缓现象。更多还原

【Abstract】 Gallanilide has significant antiarrhythmic effects on experimental arrhythmias in mice, rats, guinea pigs and dogs. Toxicity observations included acute toxioity in mice, subacute toxioity in dogs and teratogenic effects on mice. In mice the median lethal dose (LD50) of gallanilide was 1145±257mg/kg by oral administration, 236.8 ±30.1mg/kg by intraperitoneal injection and 65.8±5.9mg/kg by intravenous injection. With intraperitoneal injections of one-half of the median lethal dose onoe a day for 7 or 10 days consecutively, no significant cumulative effect of the agent was seen in mice.In the 6 weeks subaoute toxicity experiments on dogs, doses of 15 mg/kg/day intramuscularly caused transient tonic-clonio grand mal like seizures lasting 3-6 minutes; salivation, nausea, vomiting and loss of body weight were also observed. One of the three dogs died of repeated seizures on the 40th day. Pathological examination revealed cell necrosis in the liver and congestion in the glomeruli of the kidney, at doses of 10 mg/kg/day intramuscularly, no significant changes in the liver or kidney functions, ECG, or routine blood or urine tests were seen.When mice were given gallanilide 50 63 or 80 mg/kg/day by subcutaneous administration, commencing from 6-14 days after gestation, about 2 percent of the fetuses showed delayed ossification of the sternum. Fetal death rate was not increased and no other internal or skeletal malformations of the surviving fetuses were found.更多还原