University of Tennessee, Knoxville, TN 37996, USA,
Louisiana State University School of Veterinary Medicine, Baton Rouge, LA 70803, USA.
J Avian Med Surg. 2021 Apr;35(1):45-50. doi: 10.1647/1082-6742-35.1.45.
Tapentadol is an analgesic agent that acts as both a µ-opioid receptor agonist and a norepinephrine reuptake inhibitor. It is a common therapeutic agent in human medicine for management of acute and chronic pain, and it is currently being investigated for use in veterinary medicine. Tapentadol was evaluated in Hispaniolan Amazon parrots () because there is only 1 other oral opioid-like analgesic agent, tramadol, which has been evaluated in an avian species. The effectiveness of tramadol after administration to a patient involves a complex physiologic metabolism and has been found to have variable pharmacokinetics between species. Because of the lack of active metabolites from tapentadol, less interspecific variation was expected. Seven Hispaniolan Amazon parrots were used to evaluate the pharmacokinetics of tapentadol after a single 30 mg/kg PO administration of a compounded 5 mg/mL tapentadol suspension. Blood samples were collected before (time 0) and 0.25, 0.5, 0.75, 1, 1.5, 3, and 6 hours after administration, following a balanced, incomplete-block design. Plasma tapentadol concentrations were measured by high-pressure liquid chromatography with mass spectrometry. Results revealed detectable plasma concentrations in only 2 of 7 birds (29%), and the bird with the highest plasma levels had a peak concentration () of 143 ng/mL and a half-life ( ) of 24.8 minutes. The variable plasma concentrations and short half-life of this drug in Hispaniolan Amazon parrots suggests that this drug would be of limited clinical use in this species; however, it is possible that this drug will be more bioavailable in other avian species.
酒石酸布托啡诺是一种镇痛药,同时作为μ-阿片受体激动剂和去甲肾上腺素再摄取抑制剂。它是人类医学中治疗急性和慢性疼痛的常用治疗药物,目前正在兽医医学中进行研究。在海地亚马逊鹦鹉中评估了酒石酸布托啡诺,因为只有 1 种其他口服类阿片样镇痛药曲马多已在禽类物种中进行了评估。曲马多在给患者给药后的有效性涉及复杂的生理代谢,并且已经发现其在物种之间的药代动力学存在差异。由于酒石酸布托啡诺没有活性代谢物,预计种间差异会更小。使用 7 只海地亚马逊鹦鹉评估了单次口服 30mg/kg 复合 5mg/ml 酒石酸布托啡诺混悬液后酒石酸布托啡诺的药代动力学。采用平衡不完全块设计,在给药前(时间 0)和给药后 0.25、0.5、0.75、1、1.5、3 和 6 小时采集血样。通过高压液相色谱-质谱法测量血浆酒石酸布托啡诺浓度。结果仅在 7 只鸟中的 2 只(29%)中检测到可检测的血浆浓度,血浆水平最高的鸟的峰值浓度()为 143ng/ml,半衰期()为 24.8 分钟。这种药物在海地亚马逊鹦鹉中的可变血浆浓度和短半衰期表明,这种药物在该物种中的临床应用将受到限制;然而,这种药物在其他禽类物种中可能具有更高的生物利用度。