Ebeid F A, Seif el-Din S H, Ezzat A R
Department of Pharmacology, Theodor Bilharz Research Institute, Imbaba, Guiza, Egypt.
Arzneimittelforschung. 2000 Sep;50(9):867-74. doi: 10.1055/s-0031-1300304.
The effect of Schistosoma mansoni infection on drug-metabolizing enzymes was investigated before and after treatment of S. mansoni-infected male albino mice with the antibilharzial drug praziquantel (CAS 55268-74-1). The drug was given in a total dose of 1000 mg/kg, and was administered at 500 mg/kg of body weight for two consecutive days each of 500 mg/kg of body weight. The drug was given 49 days after infection with 80 Egyptian strains of S. mansoni cercariae/mouse. The hepatic content of cytochrome P-450, cytochrome b-5 and NADPH cytochrome P-450 reductase were determined at 4, 8, 24, 72 h, one and two weeks after the second dose of treatment. The enzymes were determined in the microsomal fraction after homogenization and ultracentrifugation at 105,000 x g. The results indicate a marked decrease of most enzymes in the infected groups compared to normal controls. Two weeks after treatment there was an improvement of the level of most enzymes towards the normal values. The levels of liver function tests were also improved. Concerning the oogram pattern, there was a rapid change even after 8 h after the second dose of treatment. It was concluded that the antibilharzial drug could be considered as a safe drug with a rapid onset of action.
在用抗血吸虫药吡喹酮(CAS 55268-74-1)治疗曼氏血吸虫感染的雄性白化小鼠前后,研究了曼氏血吸虫感染对药物代谢酶的影响。药物总剂量为1000mg/kg,以500mg/kg体重连续给药两天,每次500mg/kg体重。在感染80条埃及品系曼氏血吸虫尾蚴/小鼠后49天给药。在第二次给药后的4、8、24、72小时、1周和2周时,测定细胞色素P-450、细胞色素b-5和NADPH细胞色素P-450还原酶的肝脏含量。在匀浆并以105,000×g超速离心后,在微粒体部分测定这些酶。结果表明,与正常对照组相比,感染组中大多数酶明显减少。治疗两周后,大多数酶的水平向正常值有所改善。肝功能测试水平也有所改善。关于脑电图模式,即使在第二次给药后8小时也有快速变化。得出的结论是,抗血吸虫药可被视为一种起效迅速的安全药物。