Department of Anesthesiology, Chi-Mei Medical Center, Yong Kang, Tainan, Taiwan.
Department of General Surgery, Chi-Mei Medical Center, Tainan and Liouying, Taiwan.
J Pharm Pharmacol. 2018 Dec;70(12):1654-1661. doi: 10.1111/jphp.13017. Epub 2018 Sep 25.
The aim of this experiment was mainly to examine the effects of intrathecally injected doxylamine and triprolidine, two antihistamine drugs spinal motor and sensory functions.
After intrathecally injecting the rats with five different doses, the dose-response curves of spinal sensory and motor block with doxylamine and triprolidine were constructed. In comparison with the local anaesthetic mepivacaine, the quality and duration of spinal anaesthesia with doxylamine or triprolidine were conducted.
Doxylamine, mepivacaine and triprolidine elicited spinal motor and sensory (nociception and proprioception) blockades in a dose-dependent fashion. On the ED (50% effective dose) basis, the rank order of drug potency was triprolidine > mepivacaine > doxylamine (P < 0.05) at provoking spinal motor, proprioceptive and nociceptive blockades. On the equianaesthetic doses (ED , ED and ED ), the duration of spinal anaesthesia with doxylamine was longer (P < 0.01) than that with mepivacaine or triprolidine. Moreover, doxylamine or triprolidine displayed greater potency (ED ) (P < 0.05) and duration (P < 0.05) of sensory block over motor block.
Doxylamine or triprolidine produces a dose-dependent effect of spinal motor and sensory block. Triprolidine with a better nociception-selective action over motor block has a better potency than mepivacaine or doxylamine. Doxylamine and triprolidine produce longer durations than mepivacaine.
本实验主要目的是考察鞘内注射两种抗组胺药 doxylamine 和 triprolidine 对脊髓运动和感觉功能的影响。
鞘内注射 5 种不同剂量的 doxylamine 和 triprolidine 后，构建 doxylamine 和 triprolidine 对脊髓感觉和运动阻滞的量效曲线。与局部麻醉药甲哌卡因相比，研究 doxylamine 或 triprolidine 产生的脊髓麻醉的质量和持续时间。
doxylamine、mepivacaine 和 triprolidine 以剂量依赖性方式引起脊髓运动和感觉（痛觉和本体感觉）阻滞。在引起脊髓运动、本体感觉和痛觉阻滞的 ED （50%有效剂量）基础上，药物效力的顺序为 triprolidine>mepivacaine>doxylamine（P<0.05）。在等麻醉剂量（ED 、ED 和 ED ）下，doxylamine 产生的脊髓麻醉持续时间比甲哌卡因或 triprolidine 长（P<0.01）。此外，doxylamine 或 triprolidine 对感觉阻滞的效力（ED ）（P<0.05）和持续时间（P<0.05）均大于运动阻滞。
doxylamine 或 triprolidine 产生剂量依赖性脊髓运动和感觉阻滞作用。与甲哌卡因或 doxylamine 相比，triprolidine 对运动阻滞具有更好的痛觉选择性作用，具有更好的效力。doxylamine 和 triprolidine 产生的持续时间比甲哌卡因长。
