Jennings F W
Department of Veterinary Parasitology, University of Glasgow, U.K.
Trop Med Parasitol. 1991 Sep;42(3):157-60.
A detailed study of the combined effect of suramin, MK 436 (5-nitroimidazole) and Cymelarsan (melaminylthioarsenate) was investigated in the murine CNS-trypanosomiasis model. Using a combination of Cymelarsan and MK 436 without preliminary suramin, complete cures were obtained with a 2 day treatment of 15.0 mg/kg MK 436 and 5.0 mg/kg Cymelarsan. If the MK 436 was reduced to 10 mg/kg then 4 consecutive daily treatments were required. If the Cymelarsan was reduced to 2.5 mg/kg either a 3 day treatment in combination with 15.0 mg/kg or a 4 day treatment with 10 mg/kg MK 436 was necessary. Utilizing the single suramin (20 mg/kg) dose followed by combined MK 436/Cymelarsan a 2 day treatment with 10 mg/kg (or twice daily 5.0 mg/kg) MK 436 and 2.5 mg/kg Cymelarsan gave complete cures. Maximum cure rate for suramin followed by a one day treatment with 15 mg/kg MK 436 and 5.0 mg/kg Cymelarsan was 4/6 mice, indicating that a one day treatment regimen might be possible with slightly increases dose rates of the two trypanocides. A two day treatment period for CNS-trypanosomiasis is therefore feasible with the dose levels used in these experiments provided a combination chemotherapeutic regimen of suramin, MK 436, Cymelarsan are employed.
在小鼠中枢神经系统锥虫病模型中，对苏拉明、MK 436（5-硝基咪唑）和赛美拉胂（蜜胺基硫代砷酸盐）的联合作用进行了详细研究。在未预先使用苏拉明的情况下，使用赛美拉胂和MK 436联合治疗，以15.0 mg/kg的MK 436和5.0 mg/kg的赛美拉胂进行2天治疗可实现完全治愈。如果将MK 436降至10 mg/kg，则需要连续4天每日治疗。如果将赛美拉胂降至2.5 mg/kg，则要么与15.0 mg/kg联合进行3天治疗，要么与10 mg/kg的MK 436进行4天治疗。先使用单剂量苏拉明（20 mg/kg），然后联合使用MK 436/赛美拉胂，以10 mg/kg（或每日两次5.0 mg/kg）的MK 436和2.5 mg/kg的赛美拉胂进行2天治疗可实现完全治愈。先使用苏拉明，随后用15 mg/kg的MK 436和5.0 mg/kg的赛美拉胂进行一天治疗，最大治愈率为4/6只小鼠，这表明如果略微提高两种杀锥虫剂的剂量率，一天治疗方案可能可行。因此，对于中枢神经系统锥虫病，使用这些实验中所采用的剂量水平，只要采用苏拉明、MK 436、赛美拉胂的联合化疗方案，为期两天的治疗期是可行的。
