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高剂量美索巴莫在马匹中的药理学与药代动力学

The pharmacology and pharmacokinetics of high-dose methocarbamol in horses.

作者信息

Muir W W, Sams R A, Ashcraft S

机构信息

Department of Veterinary Clinical Sciences, Ohio State University, Columbus 43210-1089, USA.

出版信息

Equine Vet J Suppl. 1992 Feb(11):41-4. doi: 10.1111/j.2042-3306.1992.tb04771.x.

DOI:10.1111/j.2042-3306.1992.tb04771.x
PMID:9109959
Abstract

The haemodynamic, respiratory and behavioural effects and pharmacokinetics of methocarbamol were studied in eight healthy, adult horses after intravenous (i.v.) and oral administration of large dosages. Heart rate, cardiac output, mean pulmonary arterial blood pressure, systolic, diastolic and mean aortic blood pressure, respiratory rate and arterial blood gases did not change after either i.v. (30 mg/kg bodyweight [bwt]) or oral (50 and 100 mg/kg bwt) dosages of methocarbamol. Mild to moderate depression was observed in five of eight horses administered i.v. methocarbamol, and in all horses administered oral methocarbamol. Plasma methocarbamol concentration declined very rapidly during the initial or rapid disposition phase after i.v. administration; the terminal elimination half-life ranged from 59 to 90 mins. Peak plasma methocarbamol concentrations following oral administration occurred within 15 to 45 mins and oral bioavailability ranged from 50.7 to 124 percent.

摘要

在八匹健康成年马静脉注射和口服大剂量美索巴莫后,研究了其血液动力学、呼吸和行为影响以及药代动力学。静脉注射(30mg/kg体重[bwt])或口服(50和100mg/kg bwt)美索巴莫后,心率、心输出量、平均肺动脉血压、收缩压、舒张压和平均主动脉血压、呼吸频率及动脉血气均无变化。在静脉注射美索巴莫的八匹马中有五匹以及所有口服美索巴莫的马中观察到轻度至中度的抑郁。静脉注射后,在初始或快速处置阶段,血浆美索巴莫浓度迅速下降;终末消除半衰期为59至90分钟。口服后血浆美索巴莫浓度在15至45分钟内达到峰值,口服生物利用度为50.7%至124%。

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