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纳布啡在甲苯噻嗪镇静马体内的药效学和药代动力学。

Pharmacodynamics and pharmacokinetics of nalbuphine in xylazine‑sedated horses.

机构信息

University of Sadat City.

出版信息

Vet Ital. 2022 Dec 31;58(3). doi: 10.12834/VetIt.2408.16506.1.

DOI:10.12834/VetIt.2408.16506.1
PMID:37219832
Abstract

This study describes the selected pharmacodynamics and pharmacokinetics of nalbuphine (NAL) in xylazine (XYL)‑sedated horses. Five adult healthy horses were randomly received 2 treatments at a 1‑week interval; XYL treatment (0.55 mg/kg IV) and XYL/NAL treatment (XYL, 0.55 mg/kg IV; NAL, 0.3 mg/kg IV). The measured pharmacodynamic variables were sedative and analgesic effects and the effect on ataxia and some physiological parameters. for the pharmacokinetics of NAL, its plasma concentrations were measured using HPLC and a 2‑compartment analysis was performed. Greater and prolonged sedation was evident after XYL/NAL treatment compared with XYL treatment. Slightly improved and prolonged analgesia was demonstrated after XYL/NAL treatment. Significant changes in blood pressure and respiratory rate lasted for a shorter duration with XYL/NAL treatment than with XYL treatment. After XYL treatment, rectal temperature was significantly different from baseline and XYL/NAL treatment. Elimination half‑life of NAL was 3.47 ± 1.39 hours and total body clearance was 2.88 ± 0.73 L/kg/hour. In conclusion, addition of NAL to XYL resulted in remarkable advantages on the measured parameters. The obtained pharmacokinetics of NAL could be useful in determining the effective NAL infusion rate, which could be further evaluated as an adjunctive agent to XYL for prolonged sedation in horses.

摘要

本研究描述了纳布啡(NAL)在水合氯醛(XYL)镇静马中的药效学和药代动力学特征。5 匹成年健康马在 1 周间隔内随机接受 2 种治疗;XYL 治疗(0.55mg/kg IV)和 XYL/NAL 治疗(XYL,0.55mg/kg IV;NAL,0.3mg/kg IV)。测量的药效学变量为镇静和镇痛效果以及共济失调和一些生理参数的影响。对于 NAL 的药代动力学,使用 HPLC 测量其血浆浓度,并进行了 2 室分析。与 XYL 治疗相比,XYL/NAL 治疗后镇静作用更大且持续时间更长。与 XYL 治疗相比,XYL/NAL 治疗后镇痛作用略有改善且持续时间更长。与 XYL 治疗相比,XYL/NAL 治疗后血压和呼吸频率的显著变化持续时间更短。在 XYL 治疗后,直肠温度与基线和 XYL/NAL 治疗均有显著差异。NAL 的消除半衰期为 3.47±1.39 小时,总体清除率为 2.88±0.73 L/kg/hour。总之,NAL 与 XYL 联合使用在测量参数上具有显著优势。获得的 NAL 药代动力学可用于确定有效 NAL 输注率,这可进一步作为 XYL 的辅助剂用于马的长时间镇静。

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