Kadota T, Kawano S, Chikazawa H, Kondoh H, Kuroyanagi K, Ohta S, Ishikawa K, Kai S, Kohmura H, Takahashi N
Drug Safety Research Department, Bristol-Myers Research Institute, Ltd., Aichi, Japan.
J Toxicol Sci. 1990 Apr;15 Suppl 1:1-14. doi: 10.2131/jts.15.supplementi_1.
Buspirone hydrochloride (abbr. to BH), an anxiolytic drug, was examined for its intravenous, subcutaneous or oral acute toxicity using Crj: CD-1 (ICR) mice, Crj: CD (Sprague-Dawley) rats and beagle dogs of both sexes. The results obtained were summarized as follows: 1. Drug-related toxic signs included decreased activity and convulsions accompanied with salivation and opisthotonus in mice and rats treated with BH regardless of administration routes, and tremors and clonic convulsions accompanied with salivation in dogs treated with BH orally. 2. Pathological examinations revealed distention of the stomach in dead rats treated with BH orally, and hypersecretion of gastric juice and alterations (viz. edema, necrosis and petechia) on the superficial mucous membrane in the gastropyloric region in dead dogs treated with BH orally. 3. The cause of death was considered to be due to respiratory insufficiency in every species of animals examined. 4. LD50 values (mg/kg) were as follows: [table: see text] 5. No sex differences were observed in every species of animals regardless of administration routes on the basis of toxicological parameters examined.
对盐酸丁螺环酮(简称BH),一种抗焦虑药物,使用Crj:CD-1(ICR)小鼠、Crj:CD(Sprague-Dawley)大鼠和雌雄比格犬,分别进行静脉注射、皮下注射或口服急性毒性试验。所得结果总结如下:1. 与药物相关的毒性体征包括,无论给药途径如何,接受BH治疗的小鼠和大鼠出现活动减少、惊厥,并伴有流涎和角弓反张,口服BH治疗的犬出现震颤和阵挛性惊厥,并伴有流涎。2. 病理检查显示,口服BH治疗的死亡大鼠胃扩张,口服BH治疗的死亡犬胃幽门区浅表黏膜胃液分泌过多以及出现改变(即水肿、坏死和瘀点)。3. 在所检查的每种动物中,死亡原因均被认为是呼吸功能不全。4. LD50值(mg/kg)如下:[表格:见原文]5. 基于所检查的毒理学参数,无论给药途径如何,在所检查的每种动物中均未观察到性别差异。