Jewsbury J M
Acta Pharmacol Toxicol (Copenh). 1981;49 Suppl 5:123-30. doi: 10.1111/j.1600-0773.1981.tb03263.x.
The introduction and development of the organophosphorous drug metrifonate, first as an insecticide and then for the treatment of urinary schistosomiasis, has followed an unusual course. In its most widely accepted treatment regimen it is safe, effective and apparently without significant side effects. These facts, together with its low cost and ease of dosing, lead to a field trial of its efficacy in the treatment and prevention of infection in children in an area of high S. haematobium and S. mansoni endemicity in Rhodesia (Zimbabwe). Three doses of 7.5 mg/kg b.wt. given at fortnightly intervals reduced significantly the infection rates and the egg counts in S. haematobium patients. Subsequent treatment at the same dose level but at intervals of four weeks maintained a low level of infection and of egg output. On the other hand infection rates and egg output rose in unprotected children. There was however no comparable effect on S. mansoni. Apart from the expected and previously reported drop in cholinesterase values there were no untoward side effects: the exact significance of the drop in cholinesterase values remains unclear. The implications of these results for the wide-scale use of metrifonate as a therapeutic and as a prophylactic for Schistosoma haematobium infection is discussed.
有机磷药物敌百虫，最初作为杀虫剂，后来用于治疗尿路血吸虫病，其引入和发展历程不同寻常。在其最广泛接受的治疗方案中，它安全、有效，且显然没有明显的副作用。这些事实，连同其低成本和易于给药的特点，促使在罗德西亚（津巴布韦）一个埃及血吸虫和曼氏血吸虫高度流行地区对其治疗和预防儿童感染的疗效进行了现场试验。每两周给予三次7.5毫克/千克体重的剂量，显著降低了埃及血吸虫病患者的感染率和虫卵计数。随后以相同剂量水平但间隔四周进行治疗，维持了低感染水平和低虫卵排出量。另一方面，未受保护的儿童的感染率和虫卵排出量上升。然而，对曼氏血吸虫病没有类似的效果。除了预期的且先前报道的胆碱酯酶值下降外，没有出现不良副作用：胆碱酯酶值下降的确切意义仍不清楚。讨论了这些结果对广泛使用敌百虫作为埃及血吸虫感染的治疗药物和预防药物的意义。
