Department of Physical Therapy, College of Medicine, National Cheng Kung University, Tainan, Taiwan; Institute of Allied Health Sciences, College of Medicine, National Cheng Kung University, Tainan, Taiwan.
Department of Anesthesiology, Chi Mei Medical Center, Tainan, Taiwan; Center for General Education, Southern Taiwan University of Science and Technology, Tainan, Taiwan.
Pharmacol Rep. 2018 Jun;70(3):565-569. doi: 10.1016/j.pharep.2017.12.006. Epub 2017 Dec 20.
We aimed to evaluate the effect of doxylamine, a first generation antihistamine, as a local analgesic agent by comparing its effect to bupivacaine.
After blocking the cutaneous trunci muscle reflex (CTMR) by subcutaneous injection of doxylamine, we assessed doxylamine's cutaneous analgesic effect in rats. The dose-related effect and duration of doxylamine on infiltrative cutaneous analgesia were compared with that of bupivacaine.
We demonstrated that doxylamine, as well as the local anesthetic bupivacaine produced the cutaneous analgesic effects in a dose-related fashion. At the equipotent dose (50% effective doses (ED)), the relative potency was bupivacaine (0.41 (0.36-0.48) mmol)> doxylamine (7.39 (6.91-7.91)mmol) (p<0.01). On an equipotent basis (ED, ED and ED), subcutaneous doxylamine resulted in greater duration of action (p<0.01) than bupivacaine at producing cutaneous analgesia.
The result of this experiment indicated that doxylamine has the local anesthetic property less potent than bupivacaine, but its nociceptive block duration is longer than that of bupivacaine at an equianalgesic dose.
我们旨在通过比较 doxylamine（第一代抗组胺药）与布比卡因的效果来评估其作为局部镇痛剂的效果。
通过皮下注射 doxylamine 阻断竖脊肌反射（CTMR）后，我们评估了 doxylamine 在大鼠中的皮肤镇痛效果。比较 doxylamine 与布比卡因对浸润性皮肤镇痛的剂量相关作用和持续时间。
我们证明 doxylamine 与局部麻醉剂布比卡因一样具有剂量相关的皮肤镇痛作用。在等效剂量（50%有效剂量（ED））下，相对效力为布比卡因（0.41（0.36-0.48）mmol）> doxylamine（7.39（6.91-7.91）mmol）（p<0.01）。在等效基础上（ED、ED 和 ED），皮下 doxylamine 产生皮肤镇痛的作用持续时间比布比卡因更长（p<0.01）。
该实验结果表明，doxylamine 的局部麻醉性能弱于布比卡因，但在等镇痛剂量下，其痛觉阻断持续时间长于布比卡因。
