The Analgesic Effect of Two Different Extended-Release Meloxicam Formulations for Attenuation of Hypersensitivity in Rats (Rattus norvegicus).

Yufei Ge, Eden D Alamaw, Katechan Jampachaisri, Patrick Sharp, Cholawat Pacharinsak, Monika K Huss
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Abstract

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) frequently administered every 24 hours to control mild to moderate pain in rodents. Extended-release meloxicam offers a refinement of less frequent dosing and an extended therapeutic window compared with the standard daily-dosed meloxicam formulation. The aim of this study was to compare the analgesic efficacy of 2 different extended-release meloxicam formulations to a standard meloxicam formulation in a rat incisional pain model. Adult Long-Evans rats (n = 33) were randomly assigned into one of 4 treatment groups (n = 8-9 per group): (1) saline (0.9% NaCl, 5 mL/kg, SC, once); (2) meloxicam (Melox; 2 mg/kg, SC, every 24 hours); (3) meloxicam extended-release polymer (Melox-ER; 4 mg/kg, SC, once); or (4) meloxicam extended-release suspension (Melox-XR; 4 mg/kg, SC, once). Under isoflurane anesthesia, a 1-cm longitudinal skin incision was made on the plantar hind paw 5 minutes after drug administration. Mechanical and thermal hypersensitivity assessments were performed one day before surgery (-24 hour), 4 hours after surgery (4 hour), and 3 consecutive days following surgery (24, 48, and 72 hours). Mechanical (4-48 hours) and thermal (4-72 hours) hypersensitivity were observed in the saline group. Melox-ER did not attenuate mechanical or thermal hypersensitivity at any time point. Melox and Melox-XR attenuated mechanical hypersensitivity at the 48-hour time point. No abnormal clinical signs were noted, but injection site reactions were noted in the Melox, Melox-ER, and Melox-XR groups. Further research is needed to evaluate rat meloxicam analgesic dosages for incisional pain.

两种不同缓释美洛昔康制剂对褐家鼠超敏反应的镇痛作用。
美洛昔康是一种非甾体抗炎药(NSAID),通常每24小时服用一次,用于控制啮齿类动物的轻度至中度疼痛。与标准日给药美洛昔康制剂相比,缓释美洛昔康提供了较少频繁给药的改进和延长的治疗窗口。本研究的目的是比较两种不同的缓释美洛昔康制剂与标准美洛昔康制剂在大鼠切口疼痛模型中的镇痛效果。将33只成年Long-Evans大鼠随机分为4个治疗组(每组8-9只):(1)生理盐水(0.9% NaCl, 5 mL/kg, SC, 1次);(2)美洛昔康(Melox; 2mg /kg, SC,每24小时一次);(3)美洛昔康缓释聚合物(Melox-ER; 4mg /kg, SC, 1次);(4)美洛昔康缓释混悬液(Melox-XR; 4mg /kg, SC, 1次)。异氟醚麻醉下,给药后5分钟,在大鼠足底后爪处做1 cm纵向皮肤切口。术前1天(-24小时)、术后4小时(4小时)和术后连续3天(24、48、72小时)进行机械和热超敏反应评估。生理盐水组出现机械(4-48小时)和热(4-72小时)超敏反应。Melox-ER在任何时间点均未减弱机械或热超敏反应。Melox和Melox- xr在48小时时间点减弱机械超敏反应。Melox组、Melox- er组和Melox- xr组均未发现异常临床症状,但均有注射部位反应。对于大鼠切口疼痛,美洛昔康镇痛剂量的评价有待进一步研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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