Tawatsin A, Sirisinha S, Vajrasthira S, Bunnag D, Harinasuta T
Tropenmed Parasitol. 1984 Jun;35(2):85-90.
In vitro and in vivo experiments were employed in the screening of potential anthelmintic agents against Opisthorchis viverrini infection in hamsters. A few selected groups of compounds tested included those that are commercially available as well as those that are still being tested by various pharmaceutical firms. The compounds tested in the present study were praziquantel, amoscanate, albendazole, flubendazole, metrifonate, metronidazole and benzodiazepine derivatives. Results from both in vitro and in vivo experiments showed that at the dosages employed, praziquantel was the only one that gave complete cure, as judged from faecal egg examination and worm recovery at the time of sacrifice. It was therapeutically effective against different developmental stages of O. viverrini including the metacercariae. Moreover, the drug was also effective as a chemoprophylactic agent when given 6 to 12 hr prior to being exposed to infective metacercariae. Other compounds tested were considerably less active although some might have permanently damaged the fluke reproductive capacity, while others were able to suppress egg-laying capacity only temporarily. Together, results suggests that the ineffectiveness of most agents tested in this study is not related to their inability to attain concentrations high enough to kill or damage the flukes in the biliary system but is most likely due the inherent lack of capacity to kill the flukes.
采用体外和体内实验筛选针对仓鼠华支睾吸虫感染的潜在驱虫剂。测试的几组选定化合物包括市售化合物以及各制药公司仍在测试的化合物。本研究中测试的化合物有吡喹酮、硝硫氰胺、阿苯达唑、氟苯达唑、敌百虫、甲硝唑和苯二氮䓬衍生物。体外和体内实验结果均表明，在所使用的剂量下，从粪便虫卵检查和处死时的虫体回收情况判断，吡喹酮是唯一能实现完全治愈的药物。它对华支睾吸虫的不同发育阶段包括后尾蚴具有治疗效果。此外，在接触感染性后尾蚴前6至12小时给药时，该药物作为化学预防剂也有效。测试的其他化合物活性明显较低，尽管有些可能会永久性损害吸虫的生殖能力，而其他一些仅能暂时抑制产卵能力。总体而言，结果表明本研究中测试的大多数药物无效并非与其无法达到足以杀死或损害胆道系统中吸虫的浓度有关，而很可能是由于其内在缺乏杀死吸虫的能力。
