Maki J, Yanagisawa T
Department of Parasitology, Kitasato University School of Medicine, Sagamihara, Japan.
J Helminthol. 1988 Mar;62(1):35-9. doi: 10.1017/s0022149x00011172.
Comparative efficacy of mebendazole and flubendazole, a p-fluor analogue of mebendazole against the encysted larvae of Trichinella spiralis (USA strain) in the diaphragm of mice and rats were studied in order to provide a better understanding of the structure-activity relationship within the benzimidazole series. Drugs given 10-100 mg/kg/day for 3 consecutive days (35-37 days post-infection) or at 300 mg/kg, 35 days post infection were significantly effective in decreasing early encysted larvae in mice. No significant differences in effectiveness against the early encysted larvae could be observed between the drugs under the present experimental conditions. Mebendazole was found to be more effective that flubendazole in decreasing old encysted larvae in mice treated 70-72 days post-infection based on a comparative study of their ED50 values. When rats were given the drugs at the dose of 10 mg/kg/day for 3 consecutive days, mebendazole was significantly effective against both early and old encysted larvae while flubendazole was not.
为了更好地理解苯并咪唑类药物的构效关系,研究了甲苯咪唑与氟苯达唑(甲苯咪唑的对氟类似物)对小鼠和大鼠膈肌中旋毛虫(美国株)包囊幼虫的相对疗效。在感染后35 - 37天连续3天给予10 - 100mg/kg/天的药物,或在感染后35天给予300mg/kg的药物,对减少小鼠早期包囊幼虫有显著效果。在本实验条件下,观察到这两种药物对早期包囊幼虫的疗效无显著差异。根据对它们半数有效剂量(ED50)值的比较研究,发现在感染后70 - 72天治疗的小鼠中,甲苯咪唑在减少陈旧包囊幼虫方面比氟苯达唑更有效。当以10mg/kg/天的剂量连续3天给大鼠用药时,甲苯咪唑对早期和陈旧包囊幼虫均有显著疗效,而氟苯达唑则无此效果。