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利多卡因在术后马匹12小时静脉输注期间的处置情况。

The disposition of lidocaine during a 12-hour intravenous infusion to postoperative horses.

作者信息

Milligan M, Kukanich B, Beard W, Waxman S

机构信息

Department of Clinical Sciences, Analytical Pharmacology Laboratory, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA.

出版信息

J Vet Pharmacol Ther. 2006 Dec;29(6):495-9. doi: 10.1111/j.1365-2885.2006.00797.x.

Abstract

Lidocaine is administered as an intravenous infusion to horses for a variety of reasons, but no study has assessed plasma lidocaine concentrations during a 12-h infusion to horses. The purpose of this study was to evaluate the plasma concentrations and pharmacokinetics of lidocaine during a 12-h infusion to postoperative horses. A second purpose of the study was to evaluate the in vitro plasma protein binding of lidocaine in equine plasma. Lidocaine hydrochloride was administered as a loading dose, 1.3 mg/kg over 15 min, then by a constant rate IV infusion, 50 microg/kg/min to six postoperative horses. Lidocaine plasma concentrations were measured by a validated high-pressure liquid chromatography method. One horse experienced tremors and collapsed 5.5 h into the study. The range of plasma concentrations during the infusion was 1.21-3.13 microg/mL. Lidocaine plasma concentrations were significantly increased at 0.5, 4, 6, 8, 10 and 12 h compared with 1, 2 and 3 h. The in vitro protein binding of lidocaine in equine plasma at 2 microg/mL was 53.06+/-10.28% and decreased to 27.33+/-9.72% and 29.52+/-6.44% when in combination with ceftiofur or the combination of ceftiofur and flunixin, respectively. In conclusion, a lower lidocaine infusion rate may need to be administered to horses on long-term lidocaine infusions. The in vitro protein binding of lidocaine is moderate in equine plasma, but highly protein bound drugs may displace lidocaine increasing unbound concentrations and the risk of lidocaine toxicity.

摘要

出于多种原因,利多卡因以静脉输注的方式给予马匹,但尚无研究评估对马匹进行12小时输注期间的血浆利多卡因浓度。本研究的目的是评估对术后马匹进行12小时输注期间利多卡因的血浆浓度和药代动力学。该研究的第二个目的是评估利多卡因在马血浆中的体外血浆蛋白结合情况。将盐酸利多卡因作为负荷剂量,在15分钟内给予1.3mg/kg,然后以50μg/kg/min的恒定速率静脉输注,给予6匹术后马匹。通过经过验证的高压液相色谱法测量利多卡因血浆浓度。在研究进行到5.5小时时,有一匹马出现震颤并倒下。输注期间血浆浓度范围为1.21 - 3.13μg/mL。与1、2和3小时相比,利多卡因血浆浓度在0.5、4、6、8、10和12小时时显著升高。利多卡因在马血浆中浓度为2μg/mL时的体外蛋白结合率为53.06±10.28%,当与头孢噻呋或头孢噻呋与氟尼辛的组合合用时,分别降至27.33±9.72%和29.52±6.44%。总之,对于长期接受利多卡因输注的马匹,可能需要给予较低的输注速率。利多卡因在马血浆中的体外蛋白结合率适中,但高蛋白结合药物可能会置换利多卡因,增加游离浓度以及利多卡因毒性风险。

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