title: An angiotensin converting enzyme inhibitor, benazepril can be transformed to an active metabolite, benazeprilat, by the liver of dogs with ascitic pulmonary heartworm disease.
abstract: To examine whether an angiotensin converting enzyme (ACE) inhibitor, benazepril, can be transformed to the active metabolite, benazeprilat, by severely injured liver of dogs with ascitic heartworm disease, benazepril hydrochloride was administered orally to dogs once daily for 7 consecutive days at a dose rate of 0.29 mg/kg to 0.63 mg/kg of body weight, and plasma benazepril and benazeprilat concentrations were determined on the 1st and 7th administration days. In 7 dogs with ascitic pulmonary heartworm disease, plasma benazeprilat concentrations tended to be higher than in 7 control dogs both on the 1st and 7th administration days. The peak concentration and area under the concentration-time curve tended to be greater in dogs of the ascites group than in control dogs, but the statistics could not detect significant differences in the time to peak concentration and t(1/2) between the control and ascites groups. Plasma ACE activities decreased after administration of benazepril. In dogs with ascitic heartworm disease, benazepril was readily transformed to benazeprilat by the liver, and was effective for suppression of plasma ACE activity.
authors.affiliation: Laboratory of Internal Medicine, Division of Veterinary Medicine, Faculty of Agriculture, Gifu University, Gifu, Japan.
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Kitagawa
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Ohba
authors.forename: Yasuhito
authors.initials: Y
authors.lastname: Kuwahara
authors.forename: Rieko
authors.initials: R
authors.lastname: Ohne
authors.forename: Masahiro
authors.initials: M
authors.lastname: Kondo
authors.forename: Masakazu
authors.initials: M
authors.lastname: Nakano
authors.forename: Yoshihide
authors.initials: Y
authors.lastname: Sasaki
authors.forename: Katsuya
authors.initials: K
authors.lastname: Kitoh
mesh_terms: D000806:Angiotensin-Converting Enzyme Inhibitors / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D000818:Animals; D001201:Ascites / Q000097:blood / Q000378:metabolism / Q000662:veterinary; D001552:Benzazepines / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D001711:Biotransformation; D004184:Dirofilariasis / Q000097:blood / Q000378:metabolism*; D004283:Dog Diseases / Q000097:blood / Q000378:metabolism*; D004285:Dogs; D005260:Female; D008099:Liver / Q000378:metabolism*; D008109:Liver Diseases, Parasitic / Q000097:blood / Q000378:metabolism* / Q000662:veterinary; D008297:Male
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D001552:Benzazepines; C052133:benazeprilat; C044946:benazepril