Pharmacokinetics of netobimin and microsomal metabolism of albendazole in infected gerbils with Echinococcus granulosus

Abstract

A comparison of the pharmacokinetic profiles of netobimin (NTB), albendazole sulfoxide (ABZSO) and albendazole sulfone (ABZSO2) was performed in gerbils (Meriones unguiculatus) with intra-abdominal hydatidosis and in healthy gerbils. The infection was developed after peritoneal inoculation of protoscolices of Echinooccus granulosus from sheep. Plasma concentrations of NTB, ABZSO and ABZSO2 were measured by HPLC after oral administration of 50 mg NTB kg(-1). The results showed an incomplete biotransformation of NTB over the experimental time; and this increased in infected animals. ABZSO and ABZSO2 pharmacokinetic profiles were unaffected and were similar in both non-infected and infected animals. Both hepatic and intestinal microsomal sulfoxidase activities were measured. Since infected gerbils induced hepatic activity and decreased intestinal activity, the total activity was not different in infected and non-infected animals. In summary, intra-abdominal hydatid disease affected the pharmacokinetic profile of NTB, but ABZSO and ABZSO2 plasma concentrations were not different in infected and non-infected gerbils.

Dicrocoeliosis of Old Mouflon Ewes - Effect on Biotransformation Enzymes and Metabolism of Anthelmintics In Vitro

“…From the pharmacological point of view, the study of the effect of parasitism directly on biotransformation of antiparasitic drugs is particularly important. In gerbils infected by Echinococcus granulosus, a higher plasma concentration of ABZSO 2 after ABZ administration and an increased ABZ sulfoxidation in hepatic microsomes were found (compared with the control animals) [40]. On the other hand, a significant decrease in ABZ sulfonation during experimental fascioliosis in sheep in vivo as well as in vitro was reported [41].…”

Dicrocoeliosis of Old Mouflon Ewes - Effect on Biotransformation Enzymes and Metabolism of Anthelmintics In Vitro

“…In gerbils infected by Echinococcus granulosus, a higher plasma concentration of ABZSO 2 after ABZ administration and an increased ABZ sulfoxidation in hepatic microsomes were found (compared with the control animals) [40]. On the other hand, a significant decrease in ABZ sulfonation during experimental fascioliosis in sheep in vivo as well as in vitro was reported [41].…”