Effects of phenobarbital and 3-methylcholanthrene pretreatment on the pharmacokinetics of praziquantel in rats.
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Date
1992-06-25
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Abstract
The effects of phenobarbital (PB) and 3-methylcholanthrene (MC) pretreatment on the phannac~kinetics of praziquantel (PZQ), a
schistosomicide were studied in Spnrgue-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 &fold decrtase in AUC, a 5-fold decrease in
Cmax and an 8-fold increase in Ch compared to the saline treated controls. The MC-pretreated rats and their oliveoil treated
controls did not show any statistically significant diffmnces 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.
Description
An article with illustrations.
Keywords
Praziquante, pharmacokinetics, phenobarbital, 3-methylcholanthrene, cytochrome P450 induction
Citation
Masimirembwa C.M, Naik Y.S and Hasler J.A. (1993) Effects of phenobarbital and 3-methylcholanthrene pretreatment on the pharmacokinetics of praziquantel in rats.