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绿头鸭(Anas platyrhynchos)单次肌肉注射或血管内注射阿法沙龙后的药代动力学和药效学

Pharmacokinetics and pharmacodynamics of alfaxalone after a single intramuscular or intravascular injection in mallard ducks (Anas platyrhynchos).

作者信息

Kruse Tamara N, Messenger Kristen M, Bowman Andrew S, Aarnes Turi K, Wittum Thomas E, Flint Mark

机构信息

Department of Veterinary Preventive Medicine, College of Veterinary Medicine, The Ohio State University, Columbus, Ohio.

Department of Molecular Biomedical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina.

出版信息

J Vet Pharmacol Ther. 2019 Nov;42(6):713-721. doi: 10.1111/jvp.12804. Epub 2019 Aug 21.

Abstract

Pharmacokinetics and pharmacodynamics of alfaxalone was performed in mallard ducks (Anas platyrhynchos) after single bolus injections of 10 mg/kg administered intramuscularly (IM; n = 10) or intravenously (IV; n = 10), in a randomized cross-over design with a washout period between doses. Mean (±SD) C following IM injection was 1.6 (±0.8) µg/ml with T at 15.0 (±10.5) min. Area under the curve (AUC) was 84.66 and 104.58 min*mg/ml following IV and IM administration, respectively. Volume of distribution (V ) after IV dose was 3.0 L/kg. The mean plasma clearance after 10 mg/kg IV was 139.5 (±67.9) ml min  kg . Elimination half-lives (mean [±SD]) were 15.0 and 16.1 (±3.0) min following IV and IM administration, respectively. Mean bioavailability at 10 mg/kg IM was 108.6%. None of the ducks achieved a sufficient anesthetic depth for invasive procedures, such as surgery, to be performed. Heart and respiratory rates measured after administration remained stable, but many ducks were hyperexcitable during recovery. Based on sedation levels and duration, alfaxalone administered at dosages of 10 mg/kg IV or IM in mallard ducks does not induce clinically acceptable anesthesia.

摘要

在野鸭(绿头鸭)中进行了阿法沙龙的药代动力学和药效学研究。采用随机交叉设计,在给药剂量之间设置洗脱期,分别对10只野鸭肌肉注射(IM;n = 10)和静脉注射(IV;n = 10)10mg/kg的单次推注剂量。肌肉注射后的平均(±标准差)血药浓度C为1.6(±0.8)μg/ml,达峰时间T为15.0(±10.5)分钟。静脉注射和肌肉注射后的曲线下面积(AUC)分别为84.66和104.58分钟*mg/ml。静脉给药后的分布容积(V)为3.0L/kg。静脉注射10mg/kg后的平均血浆清除率为139.5(±67.9)ml·min⁻¹·kg⁻¹。静脉注射和肌肉注射后的消除半衰期(平均[±标准差])分别为15.0和16.1(±3.0)分钟。10mg/kg肌肉注射时的平均生物利用度为108.6%。没有一只鸭子达到足以进行侵入性手术(如外科手术)的麻醉深度。给药后测量的心率和呼吸频率保持稳定,但许多鸭子在恢复过程中过度兴奋。基于镇静水平和持续时间,在野鸭中静脉注射或肌肉注射10mg/kg剂量的阿法沙龙不能诱导出临床可接受的麻醉效果。

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