Jain M K, Gupta S, Katiyar J C, Maitra S C, Singh J, Bhakuni D S
Indian J Exp Biol. 1989 May;27(5):454-9.
Methyl 5(6)-(alpha-hydroxyphenyl methyl) benzimidazole-2-carbamate, a major metabolite of mebendazole was evaluated against Cysticercus fasciolaria (larval form of Taenia taeniaeformis) in rats. The metabolite was assessed in various doses. A regimen of 50 mg/kg x 10 (ip), given one day apart, was found to be most effective and killed all the mature cysticerci. On developing cysts, the treatment was initiated in two schedules; 5 days prior to (d-5 to d-1) and 5 days after (d + 6 to d + 10) administration of T. taeniaeformis eggs to rats. The later protocol with 100 mg/kg x 5 dose (ip) resulted in 95% inhibition in the establishment of cysticerci. Activity of mebendazole against mature cysts was parallel to metabolite whereas against developing cysts, it was inferior. The time related topographical changes that occurred in mature C. fasciolaris after treatment with metabolite (50 mg/kg x 10, ip, one day apart) were observed by scanning electron microscopy. There was loss of contractivity, gradual disappearance of microtriches and progressive degeneration of tegument. Similar changes were noticed with mebendazole. The possession of better efficacy and higher safety range [Indian J Exp. Biol, 25 (1987) 871], suggests that the metabolite can be a potential anthelmintic for man and animals.
5(6)-(α-羟基苯甲基)苯并咪唑-2-氨基甲酸甲酯是甲苯达唑的主要代谢产物，对大鼠豆状囊尾蚴（带状绦虫幼虫形态）进行了评估。该代谢产物以不同剂量进行了评估。发现按50mg/kg×10次（腹腔注射）、间隔一天给药的方案最为有效，能杀死所有成熟囊尾蚴。在形成囊肿后，治疗分两个时间点开始；在给大鼠投喂带状绦虫卵前5天（第-5天至第-1天）和投喂后5天（第+6天至第+10天）。后一种方案采用100mg/kg×5次剂量（腹腔注射），可使囊尾蚴的形成受到95%的抑制。甲苯达唑对成熟囊肿的活性与该代谢产物相似，而对发育中的囊肿，其活性则较差。通过扫描电子显微镜观察了用该代谢产物（50mg/kg×10次，腹腔注射，间隔一天）处理后成熟豆状囊尾蚴随时间发生的形态学变化。观察到其收缩性丧失、微绒毛逐渐消失以及皮层进行性退化。甲苯达唑也观察到类似变化。该代谢产物具有更好的疗效和更高的安全范围[《印度实验生物学杂志》，25(1987)871]，表明它可能是人和动物潜在的驱虫药。
