Dyhre H, Lång M, Wallin R, Renck H
Department of Anaesthesia and the Hospital Pharmacy, University Hospital MAS, Malmö, Sweden.
Acta Anaesthesiol Scand. 1997 Nov;41(10):1346-52. doi: 10.1111/j.1399-6576.1997.tb04656.x.
There is a current interest in local anaesthetic drugs/formulations exhibiting long durations of sensory block and minor motor-blocking effects.
To compare the duration of sensory and motor blockade in peripheral nerve blocks induced by the new agents ropivacaine and levobupivacaine, with that of racemic bupivacaine and pethidine.
Groups of 8 male Sprague-Dawley rats were subjected to infraorbital (IONB) or sciatic nerve block (SNB) employing 0.2 ml of differently concentrated solutions of bupivacaine, levobupivacaine, ropivacaine or pethidine. The sensory blocking effect in IONB is expressed as (i) the time to elicitation of an abdominal jerk by electrical stimulation at arbitrarily chosen (threshold) intensities (IONB degree 3, 5, 8 and 10), and as (ii) the area under the curve (AUC, threshold intensities vs time). The duration of motor block in SNB is given as the time from injection to regained ability to walk and grip normally with the toes. Comparisons of the dose-effect relationships for the investigated agents were made by analysis of covariance.
In IONB the log (dose)-log (effect) lines for bupivacaine, levobupivacaine and ropivacaine did not deviate from parallelism. The duration of sensory block induced by equimolar doses of these agents was similar, although bupivacaine exerted more pronounced effects than levobupivacaine (AUC by 25%, P=0.001; IONB degree 3 by 14%, P=0.03). In SNB only the log (dose)-log (duration) lines for bupivacaine vs levobupivacaine were found not to deviate from parallelism, both agents exerting similar durations of action. The motor-blocking effects of ropivacaine showed an inverse dose-duration relationship (P=0.019).
Equimolar doses of the investigated local anaesthetics exerted similar durations of sensory blockade in a peripheral nerve block model in the rat.
目前人们对具有长时间感觉阻滞和轻微运动阻滞作用的局部麻醉药物/制剂很感兴趣。
比较新型药物罗哌卡因和左旋布比卡因与消旋布比卡因和哌替啶在外周神经阻滞中引起的感觉和运动阻滞持续时间。
将8只雄性Sprague-Dawley大鼠分为几组,分别采用0.2 ml不同浓度的布比卡因、左旋布比卡因、罗哌卡因或哌替啶进行眶下神经阻滞(IONB)或坐骨神经阻滞(SNB)。IONB中的感觉阻滞效果表示为:(i)在任意选定(阈值)强度下通过电刺激引发腹部抽搐的时间(IONB程度3、5、8和10),以及(ii)曲线下面积(AUC,阈值强度与时间)。SNB中的运动阻滞持续时间表示为从注射到恢复正常行走和用脚趾抓握能力的时间。通过协方差分析对所研究药物的剂量-效应关系进行比较。
在IONB中,布比卡因、左旋布比卡因和罗哌卡因的对数(剂量)-对数(效应)线不偏离平行性。这些药物等摩尔剂量引起的感觉阻滞持续时间相似,尽管布比卡因的作用比左旋布比卡因更明显(AUC高25%,P = 0.001;IONB程度3高14%,P = 0.03)。在SNB中,仅发现布比卡因与左旋布比卡因的对数(剂量)-对数(持续时间)线不偏离平行性,两种药物的作用持续时间相似。罗哌卡因的运动阻滞作用呈现剂量-持续时间反比关系(P = 0.019)。
在所研究的局部麻醉药等摩尔剂量下,在大鼠外周神经阻滞模型中引起的感觉阻滞持续时间相似。