EFFECTS OF PHENOBARBITAL AND 3-METHYLCHOLANTHRENE PRETREATMENT ON THE PHARMACOKINETICS OF PRAZIQUANTEL IN RATS

被引：7

作者：

MASIMIREMBWA, CM ^{[1
]}

NAIK, YS ^{[1
]}

HASLER, JA ^{[1
]}

机构：

[1] UNIV ZIMBABWE,DEPT BIOCHEM,HARARE,ZIMBABWE

来源：

EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS | 1993年 / 18卷 / 03期

关键词：

PRAZIQUANTEL; PHARMACOKINETICS; PHENOBARBITAL; 3-METHYLCHOLANTHRENE; CYTOCHROME P450 INDUCTION;

D O I：

10.1007/BF03188806

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of phenobarbital (PB) and 3-methylcholanthrene (MC) pretreatment on the pharmacokinetics of praziquantel (PZQ), a schistosomicide were studied in Sprague-Dawley rats. Blood samples at different time intervals were obtained by severing the tail vein and were analyzed for unchanged PZQ by HPLC. The PB-pretreated rats showed a 6-fold decrease in AUC, a 5-fold decrease in C-max and an 8-fold increase in CL(tot) compared to the saline treated controls. The MC-pretreated rats and their olive-oil treated controls did not show any statistically significant differences in the above parameters. These results suggest that PZQ is extensively metabolised by PB-inducible cytochrome P-450 isoforms and not by MC-inducible isoforms. These findings also suggest that the bioavailability of praziquantel could be altered to a significant extent in humans taking drugs that are phenobarbital type inducers.

引用

页码：261 / 264

页数：4

共 13 条

[1] PRAZIQUANTEL [J].