(1992-06-25) Masimirembwa, Collen M.; Naik, Yogeshkumar S.; Hasler, Julia A.
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.