Gómez-Díez Manuel, Muñoz Ana, Caballero Juan Manuel Serrano, Riber Cristina, Castejón Francisco, Serrano-Rodríguez Juan Manuel
Equine Sport Medicine Centre, CEMEDE, School of Veterinary Medicine, University of Córdoba, Spain.
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.
Res Vet Sci. 2014 Aug;97(1):105-10. doi: 10.1016/j.rvsc.2014.06.006. Epub 2014 Jun 12.
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.
对7匹健康马匹分析了静脉注射0.50毫克/千克依那普利、口服安慰剂以及口服三种不同剂量（0.50、1.00和2.00毫克/千克）依那普利的药代动力学和药效学。测定依那普利和依那普利拉的血清浓度用于药代动力学分析。测量血管紧张素转换酶（ACE）活性、血清尿素氮（SUN）、肌酐和电解质，并监测血压用于药效学分析。静脉注射依那普利后，依那普利和依那普利拉的消除半衰期分别为0.67小时和2.76小时。口服给药后，所有马匹的依那普利浓度均低于定量限（10纳克/毫升），7匹马中有4匹马的依那普利拉浓度低于定量限。静脉注射0.50毫克/千克依那普利、安慰剂以及口服0.50、1.00和2.00毫克/千克依那普利后，与基线相比，ACE的最大平均抑制率分别为88.38%、3.24%、21.69%、26.11%和30.19%。实验期间，血压、SUN、肌酐和电解质保持不变。
