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卡洛芬在犊牛体内的药效学和手性药代动力学

Pharmacodynamics and chiral pharmacokinetics of carprofen in calves.

作者信息

Delatour P, Foot R, Foster A P, Baggot D, Lees P

机构信息

Ecole Nationale Veterinaire de Lyon, Marcy l'Etoile, France.

出版信息

Br Vet J. 1996 Mar;152(2):183-98. doi: 10.1016/s0007-1935(96)80073-x.

Abstract

The non-steroidal anti-inflammatory drug, carprofen, was administered intravenously as the racemate at a dose rate of 0.7 mg kg-1 to six Friesian bull calves aged 8-10 weeks. Anti-inflammatory properties were indicated by attenuation of temperature rise at sites of intradermal injection of the irritants, carrageenin and dextran, but responses were not statistically significant at most recording times. Carrageenin- and dextran-induced swelling were not significantly reduced by carprofen. Carprofen reduced ex vivo serum thromboxane B2 synthesis but this effect was also not significant at most sampling times. Enantioselective pharmacokinetics of carprofen was demonstrated, plasma concentrations of the R(-) enantiomer predominating at all sampling times. It is concluded that inhibition of cyclo-oxygenase is unlikely to be the sole mechanism of action of carprofen in calves.

摘要

非甾体抗炎药卡洛芬以消旋体形式静脉注射给药,剂量为0.7毫克/千克,用于6头8至10周龄的弗里斯兰公牛犊。皮内注射刺激物角叉菜胶和右旋糖酐后,体温上升的减弱表明了其抗炎特性,但在大多数记录时间,反应无统计学意义。卡洛芬对角叉菜胶和右旋糖酐诱导的肿胀没有显著降低作用。卡洛芬降低了体外血清血栓素B2的合成,但在大多数采样时间,这种作用也不显著。已证明卡洛芬具有对映体选择性药代动力学,在所有采样时间,R(-)对映体的血浆浓度占主导。结论是,环氧化酶抑制不太可能是卡洛芬在犊牛体内的唯一作用机制。

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