Ebeid F A, Metwally A A, Botros S S, Bennet J L
Pharmacology Department, Theodor Bilharz Research Institute, Imbaba-Giza, Egypt.
Arzneimittelforschung. 1994 Nov;44(11):1268-70.
In this work, praziquantel (EMBAY 8440, CAS 55268-74-1), an oral antihelminthic drug effective against the three species of schistosomes pathogenic to man, was tested alone and in combination with cimetidine (CAS 51481-61-9), aH2-receptor antagonist having a known potentiative power when combined with other drugs. Both drugs were tested in different doses and regimen either alone or in combination by giving them to S. mansoni infected Swiss albino mice (100 cercariae/mouse) 7 weeks post infection. Cimetidine was tested in doses of 50, 100 and 200 mg/kg for 2 consecutive days; praziquantel was given in doses of 100 and 500 mg/kg for 2 consecutive days. It was found that the best regimen was that of cimetidine and praziquantel when given simultaneously. Both drugs when given in a dose of 100 mg/kg for 2 consecutive days reduced the total worm load by 84.61%, while a percent reduction of 75.1% and 88.9% was recorded in hepatic and intestinal tissue egg load, respectively. Maximum efficacy was recorded when both drugs were given simultaneously at 200 mg/kg for 2 consecutive days. This regimen completely eradicated all schistosome worms and resulted in the maximum reduction in total tissue egg load (92%). The efficacy of this regimen was nearly the same as that of the full dose of praziquantel (500 mg/kg for 2 consecutive days), gave 100% worm eradication and 95% reduction in total tissue egg load.
在本研究中,吡喹酮(EMBAY 8440,化学物质登记号55268-74-1)是一种口服抗蠕虫药物,对三种寄生于人体的血吸虫均有效,单独以及与西咪替丁(化学物质登记号51481-61-9)联合进行了测试。西咪替丁是一种H2受体拮抗剂,与其他药物联合使用时具有已知的增效作用。两种药物均以不同剂量和给药方案单独或联合给药,于感染曼氏血吸虫7周后的瑞士白化小鼠(每只小鼠感染100条尾蚴)身上进行测试。西咪替丁以50、100和200 mg/kg的剂量连续给药2天;吡喹酮以100和500 mg/kg的剂量连续给药2天。结果发现,最佳给药方案是西咪替丁和吡喹酮同时给药。两种药物均以100 mg/kg的剂量连续给药2天,可使虫体总数减少84.61%,而肝组织和肠组织虫卵负荷分别减少75.1%和88.9%。当两种药物均以200 mg/kg的剂量连续给药2天同时使用时,疗效最佳。该给药方案完全清除了所有血吸虫虫体,并使组织虫卵总数负荷最大程度降低(92%)。该给药方案的疗效与全剂量吡喹酮(500 mg/kg连续给药2天)的疗效几乎相同,可实现100%的虫体清除率以及组织虫卵总数负荷降低95%。