Department of General Surgery, Chi-Mei Medical Center, Tainan and Liouying, Taiwan; Department of Electrical Engineering, Southern Taiwan University of Science and Technology, Tainan, Taiwan.
Department of Anesthesiology, Chi-Mei Medical Center, Tainan, Taiwan; Department of the Senior Citizen Service Management, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
Eur J Pharmacol. 2019 Oct 5;860:172544. doi: 10.1016/j.ejphar.2019.172544. Epub 2019 Jul 15.
Brompheniramine as an antihistamine blocked sodium channels, and local anesthetics by blocking sodium channels produced the local anesthetic effects. The authors aimed to assess local anesthetic quality and duration of brompheniramine when compared to the local anesthetic mepivacaine. After rats were shaved and injected subcutaneously on the dorsal skin, the panniculus reflex, induced via applying a noxious pinprick to the skin (injected area), was scored. The dose-response curve and nociceptive block duration of brompheniramine were constructed and compared with mepivacaine. The cutaneous analgesic effects in both brompheniramine and mepivacaine groups were concentration-dependent. On the basis of the amount required to produce a 50% block effect (ED, 50% effective dose), the drug's potency was brompheniramine (0.89 [0.82-0.96] μmol) better than mepivacaine (2.45 [2.17-2.76] μmol) (P < 0.01). Full recovery time of brompheniramine was more prolonged than mepivacaine's (P < 0.01) on infiltrative cutaneous analgesia when comparing EDs, EDs and EDs. Our preclinical data demonstrated that subcutaneous brompheniramine induces dose-relatedly analgesic effects, and brompheniramine induces prolonged analgesic duration when compared with mepivacaine. Brompheniramine also provokes better cutaneous analgesia than mepivacaine.
溴苯那敏作为一种抗组胺药，通过阻断钠通道产生局部麻醉作用，局部麻醉剂也是通过阻断钠通道产生局部麻醉作用。作者旨在评估溴苯那敏的局部麻醉质量和持续时间与局部麻醉剂甲哌卡因的比较。给大鼠剃毛后，在背部皮肤皮下注射，通过对皮肤（注射区域）施加刺痛针来评分潘尼克反射。构建了溴苯那敏的剂量反应曲线和痛觉阻断持续时间，并与甲哌卡因进行了比较。溴苯那敏和甲哌卡因组的皮肤镇痛作用均呈浓度依赖性。基于产生 50%阻断效应所需的剂量（ED，50%有效剂量），药物的效价溴苯那敏（0.89 [0.82-0.96] μmol）优于甲哌卡因（2.45 [2.17-2.76] μmol）（P < 0.01）。比较 EDs、EDs 和 EDs 时，溴苯那敏的完全恢复时间比甲哌卡因的恢复时间更长浸润性皮肤镇痛。我们的临床前数据表明，皮下注射溴苯那敏可引起剂量相关的镇痛作用，与甲哌卡因相比，溴苯那敏可引起更长的镇痛持续时间。溴苯那敏还能引起比甲哌卡因更好的皮肤镇痛作用。
