Heath D D, Christie M J, Chevis R A
Parasitology. 1975 Apr;70(2):273-85. doi: 10.1017/s0031182000049738.
Oral administration of mebendazole at a rate of 1 g/kg feed (approximately 50 mg/kg body weight/day) for 14 days killed mature and immature cysticerci of Taenia pisiformis in rabbits, and multiplying tetrathyridia of Mesocestoides corti in mice. Progressive degrees of parasite damage caused by mebendazole treatment could be assessed by histological examination of calcereous corpuscles. A single subcutaneous injection of 10 percent mebendazole in carrier, at a rate of 100 mg/kg body weight, resulted in the death of all M. corti tetrathyridia in mice within 4 weeks, but the drug in saline was slowly mobilized and was relatively ineffective. Neither subcutaneous injections of mebendazole in saline or in carrier could kill cysticerci of T. pisiformis within 5 weeks, but the drug in carrier was effective after several months. Mebendazole in saline was effective when injected intraperitoneally, but adhesions often resulted from this route of administration. Echinococcus granulosus protoscoleces administered to mice by intraperitoneal injection were rapidly encapsulated by host lymphoid cells. The vesiculating protoscoleces were all contained within a fibrous capsule for more than 2 months after infection, but by 4 months almost all had grown free of the host reaction. Treatment of the encapsulated protoscoleces with mebendazole in feed for 14-21 days caused collapse of the outer cysts and death of the germinal membrane of all but the innermost protoscoleces. Six weeks later, however, cysts had regrown from surviving germinal tissue and a further treatment with mebendazole in feed for 14-21 days again did not destroy all germinal cells. Treatment of the 4-month-old scoleces with mebendazole in feed for 14 days caused all cysts to collapse and destroyed practically all E. granulosus germinal tissue. Three subcutaneous injections of mebendazole at fortnightly intervals, of drug in saline at 500 mg/kg body weight, or in carrier at 100 mg/dg body weight, were required in order apparently to kill all secondary cysts of E. granulosus. Host lymphoid cells were not able to traverse the laminated membrane of either untreated or collapsed cysts, and it has been shown that only a small amount of living germinative tissue is required to produce a new E. granulosus cyst. These factors could contribute to the relative ability of E. granulosus cysts to recover from mebendazole treatment, compared with cysticerci or tetrathyridia. The effectiveness of mebendazole thus seemed to depend on the formulation of the drug and its route of administration. Mebendazole is probably the first anthelmintic to have a lethal effect on larval cestodes. When applied orally there do not appear to be any adverse effects due to treatment.
以1克/千克饲料(约50毫克/千克体重/天)的剂量口服甲苯咪唑14天,可杀死兔体内豆状带绦虫的成熟和未成熟囊尾蚴,以及小鼠体内冠状膜壳绦虫的增殖四膜虫。甲苯咪唑治疗引起的寄生虫损伤程度可通过对石灰小体的组织学检查来评估。以100毫克/千克体重的剂量在载体中单次皮下注射10%的甲苯咪唑,可导致小鼠体内所有冠状膜壳绦虫四膜虫在4周内死亡,但盐水中的药物释放缓慢且相对无效。在盐水中或载体中皮下注射甲苯咪唑,在5周内均无法杀死豆状带绦虫的囊尾蚴,但载体中的药物在几个月后有效。盐水中的甲苯咪唑腹腔注射有效,但这种给药途径常导致粘连。通过腹腔注射给小鼠接种细粒棘球绦虫原头节,会迅速被宿主淋巴细胞包裹。感染后2个多月,形成囊泡的原头节都被包裹在纤维囊中,但到4个月时,几乎所有原头节都已脱离宿主反应生长。用饲料中的甲苯咪唑治疗包裹的原头节14 - 21天,会导致外层囊肿塌陷,除最内层原头节外,所有生发膜死亡。然而,6周后,囊肿从存活的生发组织中重新生长,再次用饲料中的甲苯咪唑治疗14 - 21天,仍不能破坏所有生发细胞。用饲料中的甲苯咪唑治疗4个月大的头节14天,会使所有囊肿塌陷,并几乎破坏所有细粒棘球绦虫的生发组织。显然需要每两周皮下注射三次甲苯咪唑,盐水中的药物剂量为500毫克/千克体重,或载体中的药物剂量为100毫克/分升体重,才能杀死细粒棘球绦虫的所有继发囊肿。宿主淋巴细胞无法穿过未处理或已塌陷囊肿的分层膜,并且已经表明,只需少量活的生发组织就能产生新的细粒棘球绦虫囊肿。与囊尾蚴或四膜虫相比,这些因素可能导致细粒棘球绦虫囊肿从甲苯咪唑治疗中恢复的相对能力。因此,甲苯咪唑的有效性似乎取决于药物的剂型及其给药途径。甲苯咪唑可能是第一种对幼虫绦虫有致死作用的驱虫药。口服给药时,治疗似乎没有任何不良反应。