羊群中不同剂量的静脉注射后的梅洛西卡姆的药理动力学
Huseyin Gungor1, Orhan Corum2, Duygu Durna Corum2
1Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Sivas Cumhuriyet University, Sivas, Turkiye.
Journal of veterinary pharmacology and therapeutics
|November 30, 2023
概括
这项研究表明,在绵羊中静脉注射的梅洛西卡姆显示出非线性药理动力学. 较高剂量 (≥1 mg/kg) 会导致不可预测的血度,影响治疗疗效.
科学领域:
- 兽医药理学 兽医药理学
- 药理动力学 药理动力学
- 动物健康 动物健康
背景情况:
- 梅洛西卡姆是一种用于兽医的非类固醇抗炎药物 (NSAID).
- 了解其在绵羊中的药理动力学特征对于有效的治疗用途至关重要.
- 之前的研究表明,梅洛西卡姆的潜在剂量依赖性影响.
研究的目的:
- 为了确定梅洛西卡姆在不同剂量 (0.5,1和2毫克/公斤) 静脉注射给绵羊后的药理学变化.
- 评估剂量升级对关键药理动力学参数的影响.
- 评估是否达到治疗度并保持相关的持续时间.
主要方法:
- 六只阿卡拉斯曼羊接受了0.5,1和2毫克/公斤的静脉注射梅洛西卡姆,采用交叉设计,有15天的洗期.
- 使用高性能液态染色法-紫外线 (HPLC-UV) 量化了血梅洛西卡姆度.
- 用非分组分析分析了药理动力学参数.
主要成果:
- 梅洛西卡姆在0.5mg/kg剂量下可检测长达48小时,在1和2mg/kg剂量下可检测长达96小时.
- 增加剂量导致终端清除半衰期延长和增加度-时间曲线 (AUC) 下的剂量正常化面积.
- 总清除率下降,而稳定状态分布体积 (Vdss) 和初始血度 (C0.083h) 显示了剂量依赖的变化,表明非线性动力学.
结论:
- 梅洛西卡姆在静脉注射后在绵羊中表现出非线性药理动力学.
- 1mg/kg及以上的剂量会导致不可预测的血度,可能会影响治疗结果.
- 建议对羊的静脉注射梅洛西卡姆进行仔细的剂量选择,以确保可预测的疗效和安全.
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