Pharmacokinetics and preliminary safety of single-dose oral fluralaner at 10 and 25 mg/kg in healthy horses revealed no adverse reactions.

IF 1.4 3区农林科学 Q2 VETERINARY SCIENCES

American journal of veterinary research Pub Date : 2025-10-03 DOI:10.2460/ajvr.25.06.0200

Jessica M Morgan, Samantha R Gentille, Francesca D Goyette, Mallory L Lehman, Amber L Boss, Jennifer M Cassano, Heather K Knych, Stephen D White

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引用次数: 0

Abstract

Objective: To determine the safety and pharmacokinetics of a single dose of the oral ectoparasiticide fluralaner at 10 and 25 mg/kg in healthy horses.

Methods: 12 clinically healthy university-owned horses, 9 to 17 years of age, were administered a single oral dose of fluralaner at 10 or 25 mg/kg. Physical examinations, neurological examinations, plasma samples, hematology and biochemistry panels, and skin biopsies were collected throughout the 84-day trial period. Fluralaner concentrations were measured in plasma and skin by liquid chromatography-tandem mass spectrometry, and pharmacokinetics were evaluated in plasma using a noncompartmental analysis.

Results: After oral administration at 10 or 25 mg/kg, fluralaner was detected in all horses. Fluralaner was detectable in plasma for a mean of 42 ± 16.6 or 30.3 ± 3.61 days at the 10- and 25-mg/kg doses, respectively. Pharmacokinetic results for 10- and 25-mg/kg doses, respectively, were a terminal half-life of 6.03 ± 3.87 or 3.02 ± 0.25 days, maximum concentration of 162.1 ± 21.6 or 403.3 ± 129.5 ng/mL, and time to maximal concentration of 0.42 ± 0.14 or 0.64 ± 0.29 days. Skin concentrations in horses administered 25 mg/kg peaked 1 day postadministration at a median of 2.30 μg/g (IQR, 1.31 to 8.23 μg/g) and remained detectable to day 84. No adverse effects of fluralaner were detected.

Conclusions: Fluralaner is absorbed orally at 10 and 25 mg/kg in healthy horses and appears to be safe and well tolerated.

Clinical relevance: Fluralaner's persistence in skin and plasma after oral administration has potential as a treatment for select ectoparasites in the horse, although further study is needed to determine the appropriate dose and dose interval.

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单剂量口服氟拉烷（10和25 mg/kg）在健康马体内的药代动力学和初步安全性显示无不良反应。

目的：测定10和25 mg/kg单剂量口服外寄生虫药氟拉烷在健康马体内的安全性和药代动力学。方法：12匹9 ~ 17岁的临床健康大学养马，口服氟拉烷10或25 mg/kg单剂量。在84天的试验期间，收集体格检查、神经学检查、血浆样本、血液学和生化检查以及皮肤活检。采用液相色谱-串联质谱法测定血浆和皮肤中的氟拉烷浓度，并采用非区室分析评估血浆中的药代动力学。结果：口服氟拉烷10或25 mg/kg后，所有马均检测到氟拉烷。氟拉烷在10 mg/kg和25 mg/kg剂量组的血浆中检测到的平均时间分别为42±16.6天和30.3±3.61天。10 mg/kg和25 mg/kg剂量的药代动力学结果分别为：终半衰期为6.03±3.87或3.02±0.25 d，最大浓度为162.1±21.6或403.3±129.5 ng/mL，最大浓度为0.42±0.14或0.64±0.29 d。给药25 mg/kg的马的皮肤浓度在给药后1天达到峰值，中位数为2.30 μg/g (IQR， 1.31至8.23 μg/g)，并保持到第84天。氟拉烷未发现不良反应。结论：健康马口服氟拉烷10和25 mg/kg，似乎是安全且耐受性良好的。临床相关性：氟拉兰纳口服后在皮肤和血浆中的持久性有可能作为马体外寄生虫的治疗方法，尽管需要进一步的研究来确定合适的剂量和剂量间隔。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

American journal of veterinary research 农林科学-兽医学

CiteScore

1.70

自引率

10.00%

发文量

186

审稿时长

3 months

期刊介绍： The American Journal of Veterinary Research supports the collaborative exchange of information between researchers and clinicians by publishing novel research findings that bridge the gulf between basic research and clinical practice or that help to translate laboratory research and preclinical studies to the development of clinical trials and clinical practice. The journal welcomes submission of high-quality original studies and review articles in a wide range of scientific fields, including anatomy, anesthesiology, animal welfare, behavior, epidemiology, genetics, heredity, infectious disease, molecular biology, oncology, pharmacology, pathogenic mechanisms, physiology, surgery, theriogenology, toxicology, and vaccinology. Species of interest include production animals, companion animals, equids, exotic animals, birds, reptiles, and wild and marine animals. Reports of laboratory animal studies and studies involving the use of animals as experimental models of human diseases are considered only when the study results are of demonstrable benefit to the species used in the research or to another species of veterinary interest. Other fields of interest or animals species are not necessarily excluded from consideration, but such reports must focus on novel research findings. Submitted papers must make an original and substantial contribution to the veterinary medicine knowledge base; preliminary studies are not appropriate.