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甲氯芬那酸及其两种代谢产物在马匹中的研究——药代动力学及对运动耐力的影响

Studies of meclofenamic acid and two metabolites in horses--pharmacokinetics and effects on exercise tolerance.

作者信息

Johansson I M, Kallings P, Hammarlund-Udenaes M

机构信息

University of Uppsala, Equine Drug Research Laboratory, Sweden.

出版信息

J Vet Pharmacol Ther. 1991 Sep;14(3):235-42. doi: 10.1111/j.1365-2885.1991.tb00832.x.

Abstract

The pharmacokinetics and the effects on treadmill exercise of the anti-inflammatory drug meclofenamic acid were studied in seven Standardbred horses after single intravenous and/or oral doses. The decline in plasma concentration after a single intravenous dose of meclofenamic acid (2.2 mg/kg b.wt) was described by a two-compartment open model. The average elimination half-life was 1.4 h, the apparent volume of distribution 0.14 l/kg and the plasma clearance 0.12 l/h kg. Absorption was the rate-limiting step after oral administration. Non-compartmental analysis showed a mean absorption time of 4.3 h. The pharmacokinetics of two metabolites of meclofenamic acid were also studied in two of the horses. The elimination half-lives of the two metabolites were virtually the same in each horse (3.0 h and 3.4 h). The blood lactate response to exercise was significantly decreased after treatment with meclofenamic acid, indicating a lower utilization of the glycolytic ('anaerobic') energy contribution during exercise. Circulatory capacity was apparently unaffected with an unchanged heart rate response to exercise.

摘要

在7匹标准赛马单次静脉注射和/或口服抗炎药甲氯芬那酸后,研究了其药代动力学及对跑步机运动的影响。单次静脉注射甲氯芬那酸(2.2mg/kg体重)后,血浆浓度下降情况由二室开放模型描述。平均消除半衰期为1.4小时,表观分布容积为0.14L/kg,血浆清除率为0.12L/(h·kg)。口服给药后吸收是限速步骤。非房室分析显示平均吸收时间为4.3小时。还在2匹马中研究了甲氯芬那酸两种代谢物的药代动力学。两种代谢物在每匹马中的消除半衰期基本相同(3.0小时和3.4小时)。用甲氯芬那酸治疗后,运动时血乳酸反应显著降低,表明运动期间糖酵解(“无氧”)能量贡献的利用率较低。循环能力显然未受影响,运动时心率反应未变。

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