Department of Anesthesiology, China Medical University Hospital, Taichung, Taiwan.
School of Medicine, College of Medicine, China Medical University, Taichung, Taiwan.
J Pharm Pharmacol. 2018 Apr;70(4):543-549. doi: 10.1111/jphp.12894. Epub 2018 Feb 13.
The objective of this experiment was to investigate spinal anaesthetic effects of pramoxine and its comparison with bupivacaine, a long-lasting local anaesthetic.
After intrathecal injection, three neurobehavioural assessments, which consisted of nociceptive, proprioceptive and motor block, were constructed in rats. The effects of bupivacaine and pramoxine (four doses of each drug) in a dose-related manner were conducted to obtain the ED (50% effective dose). Pramoxine potency and duration at provoking spinal nociceptive, proprioceptive and motor block were compared with those of bupivacaine.
We manifested that pramoxine provoked dose-relatedly spinal blockades of nociception, proprioception and motor function. Based on the ED , the rank potency at producing spinal nociceptive, proprioceptive and motor block was bupivacaine (0.90 (0.82-1.02), 1.00 (0.92-1.08) and 1.16 (1.02-1.34) μmol/kg) greater (P < 0.01 for the differences) than pramoxine (15.47 (14.04-17.05), 16.46 (15.06-17.99), and 17.77 (16.48-19.15) μmol/kg). The spinal block duration created by bupivacaine was not predominantly different (P > 0.05 for the differences) from that created by pramoxine at the equipotent doses (ED , ED and ED ).
Our preclinical experiment indicated that pramoxine elicited a dose-related spinal block, was less potent than bupivacaine and had a similar duration of spinal block compared with bupivacaine.
本实验旨在研究普鲁卡因胺的脊髓麻醉效果,并将其与长效局部麻醉剂布比卡因进行比较。
鞘内注射后,在大鼠中构建了三种神经行为评估,包括伤害感受、本体感受和运动阻滞。以剂量相关的方式进行布比卡因和普鲁卡因胺(每种药物四个剂量)的作用,以获得 ED(50%有效剂量)。普鲁卡因胺引起脊髓伤害感受、本体感受和运动阻滞的效价和持续时间与布比卡因进行了比较。
我们表明普鲁卡因胺引起了与剂量相关的脊髓阻滞,包括伤害感受、本体感受和运动功能。基于 ED,产生脊髓伤害感受、本体感受和运动阻滞的效价强度顺序为布比卡因(0.90(0.82-1.02)、1.00(0.92-1.08)和 1.16(1.02-1.34)μmol/kg)大于(差异 P<0.01)普鲁卡因胺(15.47(14.04-17.05)、16.46(15.06-17.99)和 17.77(16.48-19.15)μmol/kg)。布比卡因和普鲁卡因胺在等效剂量(ED、ED 和 ED)产生的脊髓阻滞持续时间没有显著差异(差异 P>0.05)。
我们的临床前实验表明,普鲁卡因胺引起了与剂量相关的脊髓阻滞,效价低于布比卡因,与布比卡因相比,脊髓阻滞持续时间相似。