Population pharmacokinetics of butorphanol following intramuscular administration to exercised thoroughbred horses

IF 1.5 4区 农林科学 Q3 PHARMACOLOGY & PHARMACY Journal of veterinary pharmacology and therapeutics Pub Date : 2024-04-30 DOI:10.1111/jvp.13450
Heather K. Knych, Daniel Weiner, Daniel S. McKemie, Megan Traynham, Jeff Blea
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Abstract

Butorphanol is commonly administered, both by the intravenous and intramuscular routes, to racehorses to facilitate handling for diagnostic procedures. As the administration of butorphanol for therapeutic purposes is considered appropriate, in order to avoid inadvertent positive drug tests, a thorough understanding of the pharmacokinetics of this drug is necessary. In the current study, 12, exercised Thoroughbred horses were administered a single intramuscular dose of 0.1 mg/kg butorphanol, and serum and urine samples were collected at various times post drug administration for determination of butorphanol concentrations using a highly sensitive liquid chromatography tandem mass spectrometry method. Serum data were modeled using a nonlinear mixed effect population PK model. The maximum concentration (C max) and time to maximum concentration (T max) were 139.9 ± 72.8 ng/mL and 0.43 ± 0.44 h (mean ± SD), respectively. Although likely not clinically relevant, but important for drug testing purposes, a prolonged terminal phase was observed, yielding a terminal half-life of 7.67 ± 1.86 h. Using the blood screening limits proposed by the Horseracing Integrity and Welfare Unit, the detection time for intramuscular administration of butorphanol was estimated to be 96 h.

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运动纯血马肌肉注射丁吗啡诺后的群体药代动力学。
布托诺啡通常通过静脉注射和肌肉注射两种途径给赛马使用,以方便诊断程序的操作。由于布托诺啡用于治疗目的被认为是适当的,为了避免因疏忽而导致药物检测呈阳性,有必要全面了解这种药物的药代动力学。在当前的研究中,对 12 匹经过锻炼的纯血马肌肉注射了 0.1 毫克/千克的丁吗啡酚,并在用药后的不同时间收集血清和尿液样本,使用高灵敏度的液相色谱串联质谱法测定丁吗啡酚的浓度。使用非线性混合效应群体 PK 模型对血清数据进行建模。最大浓度(Cmax)和达到最大浓度的时间(Tmax)分别为 139.9 ± 72.8 ng/mL 和 0.43 ± 0.44 h(平均值 ± SD)。虽然可能与临床无关,但对药物检测目的很重要,观察到一个较长的终末期,得出终末半衰期为 7.67 ± 1.86 h。
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来源期刊
CiteScore
3.10
自引率
15.40%
发文量
69
审稿时长
8-16 weeks
期刊介绍: The Journal of Veterinary Pharmacology and Therapeutics (JVPT) is an international journal devoted to the publication of scientific papers in the basic and clinical aspects of veterinary pharmacology and toxicology, whether the study is in vitro, in vivo, ex vivo or in silico. The Journal is a forum for recent scientific information and developments in the discipline of veterinary pharmacology, including toxicology and therapeutics. Studies that are entirely in vitro will not be considered within the scope of JVPT unless the study has direct relevance to the use of the drug (including toxicants and feed additives) in veterinary species, or that it can be clearly demonstrated that a similar outcome would be expected in vivo. These studies should consider approved or widely used veterinary drugs and/or drugs with broad applicability to veterinary species.
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