Davis R P, Bailey D R
Bull World Health Organ. 1972;46(6):747-59.
In a controlled clinical trial, Tanzanian schoolchildren with urinary schistosomiasis, many of whom had coexisting hookworm infection, were randomly allocated to one of three groups that were treated with doses of 7.5, 10.0, and 12.5 mg per kg of body weight, respectively, of metrifonate, orally, up to 3 times at 14-day intervals. No serious side effects were observed during or after the administration of single or repeated doses. A few hours after medication, plasma cholinesterase was almost completely inhibited, regardless of the dose given, while erythrocyte cholinesterase was almost completely inhibited, regardless of the dose given, while erythrocyte cholinesterase was inhibited down to 40-60% of the pretreatment level, depending on the dose. Plasma cholinesterase was inhibited to a greater extent than erythrocyte cholinesterase but showed a more rapid recovery of activity. A moderate accumulation of unreactivated erythrocyte cholinesterase occurred at all dose levels with this regime. Four weeks after the last dose of drug, plasma cholinesterase activity was nearly normal in all the treated children. Erythrocyte cholinesterase activity returned to normal 8-15 weeks after the last dose. The therapeutic results confirmed the efficacy of metrifonate against Schistosoma haematobium. There was an additional though less striking effect against hookworm.
在一项对照临床试验中，患有泌尿血吸虫病的坦桑尼亚学童（其中许多人同时感染钩虫）被随机分为三组，分别口服按每公斤体重7.5、10.0和12.5毫克剂量的敌百虫，每隔14天给药，最多3次。在单次或重复给药期间及之后均未观察到严重副作用。给药后数小时，无论给予何种剂量，血浆胆碱酯酶几乎完全被抑制，而红细胞胆碱酯酶则被抑制至预处理水平的40% - 60%，具体取决于剂量。血浆胆碱酯酶的抑制程度大于红细胞胆碱酯酶，但活性恢复更快。在该治疗方案的所有剂量水平下，未再激活的红细胞胆碱酯酶均出现中度蓄积。在最后一剂药物给药四周后，所有接受治疗的儿童血浆胆碱酯酶活性几乎恢复正常。红细胞胆碱酯酶活性在最后一剂给药8 - 15周后恢复正常。治疗结果证实了敌百虫对埃及血吸虫的疗效。对钩虫也有额外的、虽不太显著的作用。
