Metabolism of Praziquantel in Erythromycin, Acetylspi-ramycin and Dexamethasone Induced Rat Liver Micro-somes  

吡喹酮在大环内酯类抗生素和糖皮质激素诱导的大鼠肝微粒体中的代谢

作　　者：赵梁立[1] 黄婉芸[1] 全钰珠[1] 

机构地区：[1]重庆医科大学药理教研室

出　　处：《Journal of Chinese Pharmaceutical Sciences》1995年第2期75-81,共7页中国药学（英文版）

摘　　要：Our results show that in liver microsomes from erythromycin,acetylspiramycin and dexamethsone pretreated rats,the rate of praziquantel( PQT)disappearence was increased as compared with control rat When microsomes from erythromycin-treated rats were exposed to PQT in the presence of potassium ferricyanide which broke down the cytochrome P-450 Fe(Ⅱ)-metabolite complexes and restored the functional cytochrome P-450,PQT metabolism was further increased. Acetylspiramycin did not form the complexes, so potassium ferricyanide showed no effect on the PQT metabolism in microsomes from acetylspiramycin-treated rats. Triacetyloleandomycin,a specific inhibitor of cytochrome P-450ⅢAI, inhibited PQT metabolism by 53% in liver microsomes from dexamethasone-treated rats.These results indicate the cytochrome P-450ⅢA seems to be involved in metabolism of PQT in rat liver microsomes.我们的结果表明，只有经细胞色素Ｐ－４５０ⅢＡｌ同功酶特异的诱导剂（红霉素和地塞米松）处置过的大鼠肝微粒体能显著地代谢吡喹酮（ＰＱＴ），高铁氧化钾能破坏细胞色素Ｐ－４５０Ｆｅ（Ⅱ）一代谢物的复合物，使细胞色素Ｐ－４５０ⅢＡｌ同功酶的活性恢复。因此，当微粒体和ＰＱＴ的温孵体系中加入高铁氰化钾时，ＰＱＴ在经多剂红霉素处置后的微粒体中的代谢速率进一步增加，而乙酰螺旋霉素诱导的细胞色素Ｐ－４５０并不形成复合物，因此，高铁氰化钾不影响ＰＱＴ在经乙酰螺旋霉素处置后的微粒体中的代谢。三乙酰竹桃霉素作为细胞色素Ｐ一４５０ⅢＡｌ的特异抑制剂，能抑制ＰＱＴ在地塞米松处置过的肝微粒体内的代谢速率５３％。以上结果表明，大鼠肝细胞色素Ｐ－４５０ⅢＡｌ同功酶参与ＰＱＴ在大鼠肝微粒体内的代谢。

关 键 词：Praziquantel  Liver microsomes DEXAMETHASONE ERYTHROMYCIN Cytochrome P-450:Rat 

分 类 号：R978.19[医药卫生—药品]