Pharmacokinetics of netobimin and microsomal metabolism of albendazole in infected gerbils with Echinococcus granulosus.
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.
García-Llamazares
J L
JL
Department of Physiology, Faculty of Veterinary, University of León, Spain.
Merino-Pelaez
G
G
Larrode-Pellicer
O
O
Redondo-Cardeña
P A
PA
Prieto-Fernández
J G
JG
Alvarez-de-Felipe
A I
AI
D015766:Albendazole / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000818:Animals; D000923:Anticestodal Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004195:Disease Models, Animal; D004443:Echinococcosis / Q000188:drug therapy* / Q000378:metabolism; D004446:Echinococcus; D005849:Gerbillinae; D006146:Guanidines / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008861:Microsomes / Q000378:metabolism
D000923:Anticestodal Agents; D006146:Guanidines; D015766:Albendazole; C049626:netobimin