K.L. Maddy Equine Analytical Pharmacology Laboratory, School of Veterinary Medicine, University of California, Davis, California, USA.
Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, California, USA.
J Vet Pharmacol Ther. 2021 Sep;44(5):745-753. doi: 10.1111/jvp.12993. Epub 2021 Jun 25.
Flunixin meglumine is a highly efficacious nonsteroidal anti-inflammatory drug commonly used in equine medicine and especially in performance horses. Recently, a new transdermal flunixin meglumine product has been approved for use in cattle. Although not currently approved for use in the horse, the convenience of this product may prove appealing for use in horses, warranting study. Six horses were administered a single transdermal dose of 500 mg and blood and urine samples collected for up to 96 h post-administration. Serum for determination of thromboxane concentrations and whole blood samples was collected at various time and challenged with lipopolysaccharide, calcium ionophore, or methanol to induce ex vivo synthesis of eicosanoids. Concentrations of flunixin, 5-OH flunixin, and eicosanoids were measured using LC-MS/MS and non-compartmental pharmacokinetic analysis performed on concentration data. Serum concentrations of flunixin and 5-OH flunixin were above the limit of quantitation at 96 h post-administration in both serum and urine. The mean (range) for C , T and the terminal half-life were 515.6 (369.7-714.0) ng/ml, 8.67 (8.0 12.0) h, and 22.4 (18.3-42.5) h, respectively. Following transdermal administration, based on effects on eicosanoid synthesis, flunixin meglumine inhibited cyclooxygenase 1 and 2 and 15-lipooxygenase activity, with anti-inflammatory effects lasting for 24-72 h.
氟尼辛葡甲胺是一种高效的非甾体抗炎药，常用于马医学，特别是运动马。最近，一种新的透皮氟尼辛葡甲胺产品已被批准用于牛。虽然目前尚未批准用于马，但该产品的便利性可能对马有吸引力，因此有必要进行研究。六匹马单次给予 500mg 透皮剂量，在给药后 96 小时内采集血液和尿液样本。在不同时间采集用于测定血栓素浓度的血清和全血样本，并使用脂多糖、钙离子载体或甲醇进行挑战，以诱导花生四烯酸的体外合成。使用 LC-MS/MS 测量氟尼辛、5-OH 氟尼辛和花生四烯酸的浓度，并对浓度数据进行非房室药代动力学分析。在血清和尿液中，给药后 96 小时内血清和尿液中均检测到氟尼辛和 5-OH 氟尼辛的浓度超过定量限。C 、 T 和终末半衰期的平均值（范围）分别为 515.6（369.7-714.0）ng/ml、8.67（8.0-12.0）h 和 22.4（18.3-42.5）h。透皮给药后，基于对花生四烯酸合成的影响，氟尼辛葡甲胺抑制环加氧酶 1 和 2 以及 15-脂氧合酶活性，抗炎作用持续 24-72 小时。
