Differences in sensory nerve block between levobupivacaine and bupivacaine at low concentrations in humans and animals

Akiyuki Sakamoto, Satoshi Tanaka, Takashi Ishida, Mikito Kawamata
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Abstract

Physiochemical properties of levobupivacaine and bupivacaine are identical, but pharmacokinetic and pharmacodynamics properties differ due to stereoselective interactions at the molecular sites of action. An evaluation of nerve block characteristicsis essential for optimal clinical application. This study compared the sensory blocking characteristics of levobupivacaine to bupivacaine in humans and model animals. Levobupivacaine and bupivacaine were compared for sensory block efficacy using a randomized, double-blinded, crossover study design. Eighteen healthy volunteers were randomized to receive levobupivacaine or bupivacaine by subcutaneous injection into the forearm, followed by the other drug 1 week later with injection order counterbalanced across subjects. Tactile detection and mechanical pain thresholds were determined using von Frey hairs and thermal pain threshold using a thermal stimulator. Effects of levobupivacaine and bupivacaine, on the spiking activity of spinal dorsal horn (SDH) neurons evoked by innocuous or noxious stimuli were also compared in anesthetized Sprague–Dawley rats by in vivo extracellular recordings. There were no significant differences in mechanical and thermal pain thresholds following levobupivacaine or bupivacaine injection at 0.025%, 0.0625%, and 0.125%. There was also no significant difference in tactile detection threshold following levobupivacaine or bupivacaine injection at 0.125%. However, tactile detection threshold was significantly higher after administration of bupivacaine at 0.025% and 0.0625% compared to equivalent doses of levobupivacaine. Subcutaneous injection of bupivacaine at 0.05% also induced significantly greater inhibition of SDH neuron spiking activity evoked by innocuous stimuli compared to an equivalent dose of levobupivacaine, while there was no significant difference in suppression of spiking activity evoked by noxious stimuli. Low-dose bupivacaine induces greater suppression tactile sensation than low-dose levobupivacaine. Thus, low-dose levobupivacaine demonstrates relatively greater blocking selectivity for noxious over innocuous stimuli compared to low-dose bupivacaine. Levobupivacaine may be advantageous for applications where pain must be suppressed but non-nociceptive sensations maintained.
低浓度左布比卡因和布比卡因对人类和动物感觉神经阻滞作用的差异
左布比卡因和布比卡因的理化性质相同,但由于分子作用位点的立体选择性相互作用,其药代动力学和药效学性质有所不同。评估神经阻滞特性对于优化临床应用至关重要。本研究比较了左布比卡因和布比卡因在人体和模型动物中的感觉阻滞特性。研究采用随机、双盲、交叉研究设计,比较了左布比卡因和布比卡因的感觉阻滞效果。18 名健康志愿者被随机分配到前臂皮下注射左布比卡因或布比卡因,1 周后再注射另一种药物,不同受试者的注射顺序保持一致。使用 von Frey 绒毛测定触觉检测和机械痛阈值,使用热刺激器测定热痛阈值。通过体内细胞外记录,还比较了左旋布比卡因和布比卡因对麻醉 Sprague-Dawley 大鼠脊髓背角(SDH)神经元在无害或有害刺激下诱发的尖峰活动的影响。在注射 0.025%、0.0625% 和 0.125% 的左旋布比卡因或布比卡因后,机械痛阈和热痛阈没有明显差异。注射 0.125% 的左旋布比卡因或布比卡因后,触觉阈值也没有明显差异。不过,与同等剂量的左布比卡因相比,注射 0.025% 和 0.0625% 的布比卡因后触觉检测阈值明显更高。与同等剂量的左旋布比卡因相比,皮下注射0.05%的布比卡因对无害刺激诱发的SDH神经元尖峰活动的抑制作用也明显更强,而对有害刺激诱发的尖峰活动的抑制作用则无明显差异。与低剂量左旋布比卡因相比,低剂量布比卡因对触觉的抑制更大。因此,与低剂量布比卡因相比,低剂量左旋布比卡因对有害刺激的阻断选择性相对高于无害刺激。左布比卡因在必须抑制疼痛但保持非痛觉的应用中可能更具优势。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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