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异克舒令对马的心血管及药代动力学影响

Cardiovascular and pharmacokinetic effects of isoxsuprine in the horse.

作者信息

Matthews N S, Gleed R D, Short C E, Burrows K

出版信息

Am J Vet Res. 1986 Oct;47(10):2130-3.

PMID:3777634
Abstract

Isoxsuprine (0.6 mg/kg) administered IV to 6 standing horses produced substantial, transient decreases in systemic blood pressure, systemic vascular resistance, and stroke volume. It also produced substantial, transient increases in heart rate, cardiac output, and purposeful movement. Plasma concentrations of isoxsuprine peaked soon after the drug was administered IV and then decreased over a 12-hour period in a biexponential manner, with distribution and elimination half-lives of 14 minutes and 2.67 hours, respectively. Total body clearance and steady-state volume of distribution were calculated to be 53.8 ml/min/kg and 10.5 L/kg, respectively. When a recommended therapeutic dosage regimen (0.6 mg/kg 2 times a day, per os) was used in 4 of these horses, changes were not detected. Isoxsuprine was not detected in plasma after the drug was given orally. We conclude that 0.6 mg of isoxsuprine/kg given orally every 12 hours is not likely to produce cardiovascular changes in the resting horse and that this is probably because plasma concentrations are not high enough to do so.

摘要

对6匹站立的马静脉注射异克舒令(0.6毫克/千克)后,其全身血压、全身血管阻力和每搏输出量出现了显著的短暂下降。心率、心输出量和随意运动也出现了显著的短暂增加。静脉注射异克舒令后,血浆浓度在给药后不久达到峰值,然后在12小时内呈双指数下降,分布半衰期和消除半衰期分别为14分钟和2.67小时。计算得出总体清除率和稳态分布容积分别为53.8毫升/分钟/千克和10.5升/千克。当对其中4匹马使用推荐的治疗剂量方案(0.6毫克/千克,每日2次,口服)时,未检测到变化。口服给药后,血浆中未检测到异克舒令。我们得出结论,每12小时口服0.6毫克异克舒令/千克不太可能在静息马匹中产生心血管变化,这可能是因为血浆浓度不够高,不足以产生这种变化。

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