Department of Pharmacology, Theodor Bilharz Research Institute, Warak El-Hadar, Imbaba PO Box 30, Giza 12411, Egypt.
Mem Inst Oswaldo Cruz. 2011 Nov;106(7):814-22. doi: 10.1590/s0074-02762011000700006.
Praziquantel (PZQ) is currently the only drug widely used for the treatment of schistosomiasis, but the antimalarial drug mefloquine (Mef) possesses interesting antischistosomal properties. Combination therapy with these two drugs has been suggested as a strategy for transmission control, as PZQ is active against adult worms and Mef is active against schistosomula. To examine the efficacy of combination therapy, Schistosoma mansoni-reinfected mice were separated into seven groups: untreated (I), treated with PZQ in doses of 200 mg/kg (II) or 1,000 mg/kg (III), treated with Mef in doses of 200 mg/kg (IV) or 400 mg/kg (V); each dose was divided equally and given on two consecutive days. Group VI was treated with doses of PZQ + Mef as in groups II and IV, respectively, while group VII was treated with PZQ + Mef as in groups III and V, respectively. PZQ + Mef at the reduced doses of 200 mg/kg each enhanced the therapeutic efficacy over the reduced PZQ dose alone as shown by a very high reduction in the total numbers of mature worms (95% vs. 49%), immature worms (96% vs. 29%) and the complete eradication of immature females, mature females and immature eggs. The reduction in worm burden was associated with the healing of hepatic granulomatous lesions and the normalisation of all liver enzymes. Therefore, the use of Mef with PZQ is more effective than PZQ alone and should be considered for clinical trials in humans as a potential treatment regimen to prevent treatment failures in areas with high rates of schistosomiasis.
吡喹酮(PZQ)是目前广泛用于治疗血吸虫病的唯一药物,但抗疟药甲氟喹(Mef)具有有趣的抗血吸虫特性。联合使用这两种药物已被提议作为一种传播控制策略,因为 PZQ 对成虫有效,而 Mef 对尾蚴有效。为了研究联合治疗的疗效,感染曼氏血吸虫的小鼠被分为七组:未治疗组(I)、用 200 mg/kg(II)或 1000 mg/kg(III)剂量的 PZQ 治疗组、用 200 mg/kg(IV)或 400 mg/kg(V)剂量的 Mef 治疗组;每个剂量分为两天连续给药。第六组用与第二组和第四组相同剂量的 PZQ + Mef 治疗,而第七组用与第三组和第五组相同剂量的 PZQ + Mef 治疗。与单独使用低剂量 PZQ 相比,低剂量(各 200 mg/kg)的 PZQ + Mef 增强了治疗效果,表现为成熟虫体(95%对 49%)、未成熟虫体(96%对 29%)的总数和未成熟雌性虫体的完全消除、成熟雌性虫体和未成熟虫卵。减少虫荷与肝肉芽肿病变的愈合以及所有肝酶的正常化有关。因此,与单独使用 PZQ 相比,Mef 联合使用 PZQ 更有效,应考虑在人类中进行临床试验,作为预防高血吸虫病地区治疗失败的潜在治疗方案。