在猫的口服塔潘塔多尔的药理动力学
J Lakritz1, T K Aarnes1, B Alva1
1Department of Veterinary Clinical Sciences, The Ohio State University College of Veterinary Medicine, Columbus, Ohio, USA.
Journal of veterinary pharmacology and therapeutics
|June 23, 2023
概括
猫的口服塔达尔显示塔达尔-O-硫酸盐是主要的代谢物. 需要进行进一步的研究,以将塔达洛度与猫患者的止痛作用联系起来.
科学领域:
- 兽医药理学 兽医药理学
- 药物新陈代谢 药物新陈代谢
- 药理动力学 药理动力学
背景情况:
- 塔潘塔多尔是一种双重作用机制的止痛药.
- 它在猫中的药理动力学,特别是口服后的药理动力学,尚未得到充分证实.
- 了解猫类药物代谢对于安全有效的疼痛管理至关重要.
研究的目的:
- 在健康的猫中描述单次口服剂量塔潘塔多尔化的药理动力学.
- 在猫血中识别和量化塔潘塔多尔及其主要代谢物.
- 为了确定猫的塔潘塔多尔的主要代谢途径.
主要方法:
- 展望实验研究涉及五只健康的成年混合品种猫.
- 在18.8±1.0毫克/公斤口服的塔潘塔多尔化.
- 在24小时内连续取血样,并通过超高性能液体染色学-双重质谱法进行血分析.
主要成果:
- 塔潘塔多尔-O-硫酸盐是主要代谢物,占相对暴露的90.6%.
- 高峰血度 (Cmax) 不同,塔潘塔多尔-O-硫酸盐显示最高的平均Cmax (15,757 ng/mL).
- 平均半衰期从2.4小时的塔潘塔多尔到10.8小时的塔潘塔多尔-O-硫酸盐.
结论:
- 塔达尔在猫中经历了广泛的新陈代谢,主要形成塔达尔-O-硫酸盐.
- 药物动力学特征表明,口服后,tapendadol-O-sulfate是主要的循环部分.
- 需要进行进一步的研究,以将血度与猫的止痛功效相关联.
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