a Dipartimento di Scienze Veterinarie per la Salute, la Produzione Animale e la Sicurezza Alimentare , Università degli Studi di Milano , via Celoria 10, 20133 Milano , Italy.
Vet Q. 2014;34(3):143-51. doi: 10.1080/01652176.2014.963208. Epub 2014 Oct 9.
Tramadol is a synthetic codeine analogue used as an analgesic in human and veterinary medicine. It is not approved for use in horses, but could represent a valid tool for pain treatment in this species.
The serum pharmacokinetic profile and urinary excretion of tramadol and its metabolites (O-desmethyltramadol [M1], N-desmethyltramadol [M2] and N,O-desmethyltramadol [M5]) was investigated in a multidrug anaesthetic and analgesic approach for orchiectomy in horses. The evaluation of the degree of cardiovascular stability, the intraoperative effect and postoperative analgesia obtained by the visual analogue scale are also reported. Animal and methods: Tramadol (4 mg/kg BW) was administered intravenously to eight male yearlings as a bolus over 60 seconds, 5 min after intubation and 15 min prior to surgery. Drug quantification was performed in serum and urine for tramadol, M1, M2 and M5 by high-performance liquid chromatography with fluorimetric detection.
Mean tramadol concentration was 14.87 ± 11.14 μg/mL at 0.08 h, and 0.05 ± 0.06 μg/mL at 10 h. Serum concentrations of M1 and M2 metabolites were quite limited. For M1 and M2, median maximum concentration (Cmax) and time to achieve maximum concentration (Tmax) were 0.05 μg/mL and 0.75 h, and 0.08 μg/mL and 2 h, respectively; M5 was never detected. In urine, tramadol was the most recovered compound, followed by M1, M2 and M5.
Showing no adverse events and based on the kinetic behaviour, pre-operative tramadol IV at a dose of 4 mg/kg BW might be useful and safe as analgesic in horses undergoing surgery.
曲马多是一种合成可待因类似物，在人类和兽医医学中用作镇痛药。它未被批准用于马，但在该物种的疼痛治疗中可能是一种有效的工具。
在马的去势手术多药物麻醉和镇痛方法中，研究曲马多及其代谢物（O-去甲基曲马多[M1]、N-去甲基曲马多[M2]和 N,O-去甲基曲马多[M5]）的血清药代动力学特征和尿排泄。还报告了心血管稳定性评估、术中效果和术后镇痛的视觉模拟评分。
8 匹雄性幼驹静脉注射曲马多（4mg/kg BW），60 秒内推注，插管后 5 分钟和手术前 15 分钟。通过高效液相色谱法和荧光检测法在血清和尿液中定量测定曲马多、M1、M2 和 M5。
曲马多的平均浓度在 0.08 小时为 14.87±11.14μg/mL，在 10 小时为 0.05±0.06μg/mL。M1 和 M2 代谢物的血清浓度相当有限。对于 M1 和 M2，Cmax 和 Tmax 的中位数最大值分别为 0.05μg/mL 和 0.75 小时，0.08μg/mL 和 2 小时；M5 从未检测到。在尿液中，曲马多是回收最多的化合物，其次是 M1、M2 和 M5。
基于无不良反应和药代动力学行为，术前静脉注射曲马多 4mg/kg BW 可能对接受手术的马具有有用和安全的镇痛作用。
