Department of General Surgery, Chi-Mei Medical Center, Liouying, Tainan, Taiwan.
Department of Electrical Engineering, Southern Taiwan University of Science and Technology, Tainan, Taiwan.
Pharmacol Rep. 2020 Aug;72(4):827-832. doi: 10.1007/s43440-019-00028-7. Epub 2019 Dec 20.
This study sought to assess the cutaneous (peripheral) analgesic effects of antihistamine chlorpheniramine, compared with the long-lasting local anesthetic bupivacaine.
After chlorpheniramine and bupivacaine were subcutaneously injected under the dorsal skin of the rats, the cutaneous analgesia effect was quantitatively evaluated by scoring the number to which the animal failed to react (cutaneous trunci muscle reflex). The quality and duration of chlorpheniramine and bupivacaine on infiltrative cutaneous analgesia were compared.
We revealed that subcutaneous chlorpheniramine, as well as the local anesthetic bupivacaine elicited cutaneous analgesia in a dosage-dependent manner. Based on their EDs (50% effective doses), the relative potency was found to be chlorpheniramine [1.13 (1.05-1.22) μmol] < bupivacaine [0.52 (0.46-0.58) μmol] (p < 0.01). When comparing the EDs, EDs and EDs, full recovery time induced by chlorpheniramine was longer (p < 0.01) than that induced by bupivacaine.
Our preclinical data demonstrated that both chlorpheniramine and bupivacaine dose-dependently provoked the cutaneous analgesic effects. Chlorpheniramine with a more prolonged duration was less potent than bupivacaine in inducing cutaneous analgesia.
本研究旨在评估抗组胺药氯苯那敏的皮肤（周围）镇痛作用，并与长效局部麻醉剂布比卡因进行比较。
在大鼠背部皮肤下皮下注射氯苯那敏和布比卡因后，通过评分动物未反应的次数（竖毛肌反射）定量评估皮肤镇痛效果。比较了氯苯那敏和布比卡因对浸润性皮肤镇痛的质量和持续时间。
我们发现，皮下氯苯那敏和局部麻醉剂布比卡因均以剂量依赖性方式引起皮肤镇痛。根据它们的 ED50（50%有效剂量），相对效力为氯苯那敏[1.13（1.05-1.22）μmol]<布比卡因[0.52（0.46-0.58）μmol]（p<0.01）。比较 ED50、ED95 和 ED99 时，氯苯那敏诱导的完全恢复时间比布比卡因更长（p<0.01）。
我们的临床前数据表明，氯苯那敏和布比卡因均剂量依赖性地引起皮肤镇痛作用。氯苯那敏的持续时间更长，但其诱导皮肤镇痛的效力低于布比卡因。
