McKellar Q A, Bogan J A, von Fellenberg R L, Ludwig B, Cawley G D
Department of Veterinary Pharmacology, University of Glasgow, Scotland, UK.
Equine Vet J. 1991 Jul;23(4):280-4. doi: 10.1111/j.2042-3306.1991.tb03718.x.
Carprofen, a non-steroidal anti-inflammatory drug (NSAID) was administered to three Thoroughbred geldings and three Shetland ponies to determine its plasma disposition and tolerance. The main pharmacokinetic characteristics of carprofen in horses and ponies were a volume of distribution of 0.08 to 0.32 litres/kg (mean +/- se = 0.23 +/- 0.04) a systemic clearance of 26.4 to 78.5 ml/min (mean +/- se = 44.9 +/- 8.0) and a plasma elimination half-life of 14.5 to 31.4 h (mean +/- se = 21.9 +/- 2.3). There was no evidence of any accumulation of carprofen in plasma when the drug was given orally at a dose rate of 0.7 mg/kg for 14 consecutive days. Carprofen was well tolerated following intravenous (iv) and oral administration. Intramuscular (im) administration resulted in elevated levels of plasma creatine kinase suggesting muscle cell damage. According to the results of this study carprofen can be regarded as a long-acting NSAID in horses from a pharmacokinetic point of view. Either iv, im or the oral route of administration could be used to achieve high carprofen plasma concentrations.
将卡洛芬(一种非甾体抗炎药)给予3匹纯种马和3匹设得兰矮种马,以确定其血浆处置情况和耐受性。卡洛芬在马和矮种马体内的主要药代动力学特征为:分布容积为0.08至0.32升/千克(均值±标准误=0.23±0.04),全身清除率为26.4至78.5毫升/分钟(均值±标准误=44.9±8.0),血浆消除半衰期为14.5至31.4小时(均值±标准误=21.9±2.3)。当以0.7毫克/千克的剂量率连续口服给药14天时,没有证据表明卡洛芬在血浆中会蓄积。静脉注射(iv)和口服卡洛芬后耐受性良好。肌肉注射(im)导致血浆肌酸激酶水平升高,提示肌肉细胞受损。根据本研究结果,从药代动力学角度来看,卡洛芬可被视为马的长效非甾体抗炎药。静脉注射、肌肉注射或口服给药途径均可用于达到较高的卡洛芬血浆浓度。