Comparative ventricular electrophysiologic effect of racemic bupivacaine, levobupivacaine, and ropivacaine on the isolated rabbit heart.
Comparative ventricular electrophysiologic effect of racemic bupivacaine, levobupivacaine, and ropivacaine on the isolated rabbit heart.
复制标题
外消旋布比卡因、左布比卡因和罗哌卡因对离体兔心脏心室电生理效应的比较。
DOI：
10.1097/00000542-200009000-00028
复制
发表时间：
2000
期刊：
影响因子：
8.8
通讯作者：
Alain Edouard
中科院分区：
文献类型：
--
作者：
J. Mazoit;Anne Decaux;Hervé Bouaziz;Alain Edouard
背景
许多局部麻醉剂具有不对称四面体碳，这赋予异构体之间的立体选择性差异。作者试图量化外消旋布比卡因、左布比卡因和罗哌卡因对心肌心室传导和心肌收缩力的抑制作用。
方法
作者研究了在离体兔心脏制剂中输注的三种药物的药代动力学（流出浓度）和药效学（QRS增宽）。所有数据均采用混合效应模型同时拟合，因此可以在三种药物参数之间进行精确的统计学比较。对QRS增宽的频率依赖性分别进行拟合。
结果
外消旋布比卡因、左布比卡因和罗哌卡因以1：0.4：0.3的比例诱导QRS时限的计算最大增加。Css 50，在稳态时引起QRS持续时间最大增加的一半的剂量，对于所有三种药物是相似的（22 μ m游离浓度）。观察到QRS增宽的频率依赖性，外消旋布比卡因、左布比卡因和罗哌卡因的比例分别为1：0.5：0.25。
结论
在离体兔心脏中，外消旋布比卡因、左布比卡因和罗哌卡因以1：0.4：0.3的比例诱导QRS持续时间增加，其以大致相同的比例具有速率依赖性。
BACKGROUND
Numerous local anesthetics have an asymmetric tetrahedron carbon, which confers stereoselective differences between the isomers. The authors attempted to quantify the depressant effect of racemic bupivacaine, levobupivacaine, and ropivacaine on myocardial ventricular conduction and on myocardial contractility.
METHODS
The authors studied the pharmacokinetics (outflow concentration) and pharmacodynamics (QRS widening) of the three drugs infused in an isolated rabbit heart preparation. All data were fitted simultaneously with use of mixed-effect modeling, thus allowing precise statistical comparison between the three drug parameters. The rate dependence of QRS widening was fitted separately.
RESULTS
Racemic bupivacaine, levobupivacaine, and ropivacaine induced a calculated maximum increase in QRS duration in the ratio 1:0.4:0.3. Css50, the dose which caused half the maximum increase in QRS duration at steady state, was similar for all three drugs (22 micrometer free concentration). A rate dependence of QRS widening was observed, which was in the ratio 1:0.5:0.25 for racemic bupivacaine, levobupivacaine, and ropivacaine, respectively.
CONCLUSIONS
In the isolated rabbit heart, racemic bupivacaine, levobupivacaine, and ropivacaine induce an increase in QRS duration in the respective ratio of 1:0.4:0.3, which was rate dependent in approximately the same ratio.