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单次静脉注射或持续静脉输注布托啡诺在马体内的药代动力学及不良反应

Pharmacokinetics and adverse effects of butorphanol administered by single intravenous injection or continuous intravenous infusion in horses.

作者信息

Sellon D C, Monroe V L, Roberts M C, Papich M G

机构信息

Department of Food Animal and Equine Medicine, College of Veterinary Medicine, North Carolina State University, Raleigh 27606, USA.

出版信息

Am J Vet Res. 2001 Feb;62(2):183-9. doi: 10.2460/ajvr.2001.62.183.

Abstract

OBJECTIVE

To determine an infusion rate of butorphanol tartrate in horses that would maintain therapeutic plasma drug concentrations while minimizing development of adverse behavioral and gastrointestinal tract effects.

ANIMALS

10 healthy adult horses.

PROCEDURE

Plasma butorphanol concentrations were determined by use of high-performance liquid chromatography following administration of butorphanol by single IV injection (0.1 to 0.13 mg/kg of body weight) or continuous IV infusion (loading dose, 17.8 microg/kg; infusion dosage, 23.7 microg/kg/h for 24 hours). Pharmacokinetic variables were calculated, and changes in physical examination data, gastrointestinal tract transit time, and behavior were determined over time.

RESULTS

A single IV injection of butorphanol was associated with adverse behavioral and gastrointestinal tract effects including ataxia, decreased borborygmi, and decreased defecation. Elimination half-life of butorphanol was brief (44.37 minutes). Adverse gastrointestinal tract effects were less apparent during continuous 24-hour infusion of butorphanol at a dosage that resulted in a mean plasma concentration of 29 ng/ml, compared with effects after a single IV injection. No adverse behavioral effects were observed during or after continuous infusion.

CONCLUSIONS AND CLINICAL RELEVANCE

Continuous IV infusion of butorphanol for 24 hours maintained plasma butorphanol concentrations within a range associated with analgesia. Adverse behavioral and gastrointestinal tract effects were minimized during infusion, compared with a single injection of butorphanol. Continuous infusion of butorphanol may be a useful treatment to induce analgesia in horses.

摘要

目的

确定酒石酸布托啡诺在马匹中的输注速率,以维持治疗性血浆药物浓度,同时尽量减少不良行为和胃肠道效应的发生。

动物

10匹健康成年马。

程序

单次静脉注射(0.1至0.13毫克/千克体重)或持续静脉输注(负荷剂量,17.8微克/千克;输注剂量,23.7微克/千克/小时,持续24小时)酒石酸布托啡诺后,采用高效液相色谱法测定血浆布托啡诺浓度。计算药代动力学变量,并随时间确定体格检查数据、胃肠道转运时间和行为的变化。

结果

单次静脉注射酒石酸布托啡诺与不良行为和胃肠道效应相关,包括共济失调、肠鸣音减弱和排便减少。布托啡诺的消除半衰期较短(44.37分钟)。与单次静脉注射后的效应相比,以导致平均血浆浓度为29纳克/毫升的剂量持续24小时输注酒石酸布托啡诺期间,不良胃肠道效应不太明显。持续输注期间或之后未观察到不良行为效应。

结论及临床意义

持续静脉输注酒石酸布托啡诺24小时可使血浆布托啡诺浓度维持在与镇痛相关的范围内。与单次注射酒石酸布托啡诺相比,输注期间不良行为和胃肠道效应降至最低。持续输注酒石酸布托啡诺可能是诱导马匹镇痛的一种有用治疗方法。

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