title: Pharmacokinetics and pharmacodynamics of enalapril and its active metabolite, enalaprilat, at four different doses in healthy horses.
abstract: Pharmacokinetic and pharmacodynamic of IV enalapril at 0.50 mg/kg, PO placebo and PO enalapril at three different doses (0.50, 1.00 and 2.00 mg/kg) were analyzed in 7 healthy horses. Serum concentrations of enalapril and enalaprilat were determined for pharmacokinetic analysis. Angiotensin-converting enzyme (ACE) activity, serum ureic nitrogen (SUN), creatinine and electrolytes were measured, and blood pressure was monitored for pharmacodynamic analysis. The elimination half-lives of enalapril and enalaprilat were 0.67 and 2.76 h respectively after IV enalapril. Enalapril concentrations after PO administrations were below the limit of quantification (10 ng/ml) in all horses and enalaprilat concentrations were below the limit of quantification in 4 of the 7 horses. Maximum mean ACE inhibitions from baseline were 88.38, 3.24, 21.69, 26.11 and 30.19% for IV enalapril at 0.50 mg/kg, placebo and PO enalapril at 0.50, 1.00 and 2.00 mg/kg, respectively. Blood pressures, SUN, creatinine and electrolytes remained unchanged during the experiments.
authors: Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain.
authors: Manuel
authors: M
authors: Gómez-Díez
authors: Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain; Department of Animal Medicine and Surgery, School of Veterinary Medicine, University of Córdoba, Spain. Electronic address: pv1mujua@uco.es.
authors: Ana
authors: A
authors: Muñoz
authors: Department of Pharmacology, Toxicology and Legal and Forensic Medicine, School of Veterinary Medicine, University of Córdoba, Spain.
authors: Juan Manuel Serrano
authors: JM
authors: Caballero
authors: Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain; Department of Animal Medicine and Surgery, School of Veterinary Medicine, University of Córdoba, Spain.
authors: Cristina
authors: C
authors: Riber
authors: Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain.
authors: Francisco
authors: F
authors: Castejón
authors: Department of Pharmacology, Toxicology and Legal and Forensic Medicine, School of Veterinary Medicine, University of Córdoba, Spain.
authors: Juan Manuel
authors: JM
authors: Serrano-Rodríguez
mesh_terms: D061605:Administration, Intravenous; D000284:Administration, Oral; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001806:Blood Urea Nitrogen; D003404:Creatinine / Q000097:blood; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004656:Enalapril / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D015773:Enalaprilat / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006207:Half-Life; D006736:Horses / Q000378:metabolism*; D018709:Statistics, Nonparametric
chemical_list: D000806:Angiotensin-Converting Enzyme Inhibitors; D004656:Enalapril; D003404:Creatinine; D015773:Enalaprilat
keywords: Angiotensin-converting enzyme inhibitor; Blood pressure; Enalapril; Enalaprilat; Horses