Xiao S H, Yang Y Q, You J Q, Shen B G, Jiao W, Chai J J
Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine.
Chin Med J (Engl). 1994 Jul;107(7):521-32.
The effects of mebendazole (Meb), albendazole (Alb) and albendazole sulfoxide (AlbSO) on metacestodes of Echinococcus granulosus have been studied. The results show that Meb and Alb exhibit less effect on protoscoleces in vitro, but in vivo the protoscolicidal effect of Meb is higher than that of Alb. Both Meb and Alb are efficacious in the treatment of mice infected with secondary cysts of E. granulosus. In terms of the minimal effective dose required, the occurrence of collapsed and shrunk cysts after treatment, the drug-induced damage on the germinal layer and the relationship between the drug content in the cyst wall and the damage of germinal layer, the effect of Meb on metacestodes of E. granulosus is higher than that of Alb. The results also indicated that lower drug absorption rate and thickening of the adventitia during longer disease course are the two major factors affecting the efficacy of Meb and Alb, hence suggesting that increase of Meb absorption may be expected to raise the therapeutic effect of the drug. Finally, Alb is not only metabolized to AlbSo and AlbSP in vivo, but also metabolized by the cysts exposed to Alb in vitro. Experimental chemotherapy showed that AlbSO is the major effective metabolite of Alb, and its curative dose is only one half of the parent compound.
已对甲苯咪唑(Meb)、阿苯达唑(Alb)和阿苯达唑亚砜(AlbSO)对细粒棘球绦虫成虫的作用进行了研究。结果表明,Meb和Alb在体外对原头蚴的作用较小,但在体内Meb的杀原头蚴作用高于Alb。Meb和Alb对感染细粒棘球绦虫继发性囊肿的小鼠均有治疗效果。就所需最小有效剂量、治疗后囊肿塌陷和缩小的发生率、药物对生发层的损伤以及囊壁药物含量与生发层损伤之间的关系而言,Meb对细粒棘球绦虫成虫的作用高于Alb。结果还表明,药物吸收率较低以及病程较长时外膜增厚是影响Meb和Alb疗效的两个主要因素,因此提示提高Meb的吸收率有望提高该药的治疗效果。最后,Alb在体内不仅代谢为AlbSo和AlbSP,在体外接触Alb的囊肿也会对其进行代谢。实验化疗表明,AlbSO是Alb的主要有效代谢产物,其治疗剂量仅为母体化合物的一半。