Rezende M L, Grimsrud K N, Stanley S D, Steffey E P, Mama K R
Department of Clinical Sciences, College of Veterinary Medicine and Biomedical Sciences, Colorado State University, Fort Collins, CO, USA.
J Vet Pharmacol Ther. 2015 Feb;38(1):15-23. doi: 10.1111/jvp.12138. Epub 2014 Jul 28.
The aim of the study was to describe the pharmacokinetics and selected pharmacodynamics of intravenous dexmedetomidine in horses. Eight adult horses received 5 μg/kg dexmedetomidine IV. Blood samples were collected before and for 10 h after drug administration to determine dexmedetomidine plasma concentrations. Pharmacokinetic parameters were calculated using noncompartmental analysis. Data from one outlier were excluded from the statistical summary. Behavioral and physiological responses were recorded before and for 6 h after dexmedetomidine administration. Dexmedetomidine concentrations decreased rapidly (elimination half-life of 8.03 ± 0.84 min). Time of last detection varied from 30 to 60 min. Bradycardia was noted at 4 and 10 min after drug administration (26 ± 8 and 29 ± 8 beats/min respectively). Head height decreased by 70% at 4 and 10 min and gradually returned to baseline. Ability to ambulate was decreased for 60 min following drug administration, and mechanical nociceptive threshold was increased during 30 min. Blood glucose peaked at 30 min (134 ± 24 mg/dL) and borborygmi were decreased for the first hour after dexmedetomidine administration. Dexmedetomidine was quickly eliminated as indicated by the rapid decrease in plasma concentrations. Physiological, behavioral, and analgesic effects observed after dexmedetomidine administration were of short duration.
本研究的目的是描述静脉注射右美托咪定在马匹体内的药代动力学及选定的药效学。八匹成年马静脉注射5μg/kg右美托咪定。给药前及给药后10小时采集血样,以测定右美托咪定的血浆浓度。使用非房室分析计算药代动力学参数。统计汇总中排除了一个异常值的数据。记录右美托咪定给药前及给药后6小时的行为和生理反应。右美托咪定浓度迅速下降(消除半衰期为8.03±0.84分钟)。最后一次检测时间为30至60分钟。给药后4分钟和10分钟出现心动过缓(分别为26±8次/分钟和29±8次/分钟)。给药后4分钟和10分钟头部高度下降70%,并逐渐恢复至基线。给药后60分钟内行走能力下降,给药后30分钟内机械性伤害性感受阈值升高。血糖在30分钟时达到峰值(134±24mg/dL),右美托咪定给药后第一小时肠鸣音减弱。如血浆浓度迅速下降所示,右美托咪定很快被清除。右美托咪定给药后观察到的生理、行为和镇痛作用持续时间较短。