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美金刚可引起大鼠脊髓对运动功能、本体感觉和痛觉的阻断。

Memantine elicits spinal blockades of motor function, proprioception, and nociception in rats.

作者信息

Chen Yu-Wen, Chiu Chong-Chi, Liu Kuo-Sheng, Hung Ching-Hsia, Wang Jhi-Joung

机构信息

Department of Physical Therapy & Graduate Institute of Rehabilitation Science, College of Health Care, China Medical University, Taichung, Taiwan.

Department of Medical Research, Chi-Mei Medical Center, Tainan, Taiwan.

出版信息

Fundam Clin Pharmacol. 2015 Dec;29(6):567-74. doi: 10.1111/fcp.12142. Epub 2015 Sep 10.

Abstract

Although memantine blocks sodium currents and produces local skin anesthesia, spinal anesthesia with memantine is unknown. The purpose of the study was to evaluate the local anesthetic effect of memantine in spinal anesthesia and its comparison with a widely used local anesthetic lidocaine. After intrathecally injecting the rats with five doses of each drug, the dose-response curves of memantine and lidocaine were constructed. The potencies of the drugs and durations of spinal anesthetic effects on motor function, proprioception, and nociception were compared with those of lidocaine. We showed that memantine produced dose-dependent spinal blockades in motor function, proprioception, and nociception. On a 50% effective dose (ED50 ) basis, the rank of potency was lidocaine greater than memantine (P < 0.05 for the differences). At the equipotent doses (ED25 , ED50 , ED75 ), the block duration produced by memantine was longer than that produced by lidocaine (P < 0.05 for the differences). Memantine, but not lidocaine, displayed more sensory/nociceptive block than motor block. The preclinical data demonstrated that memantine is less potent than lidocaine, whereas memantine produces longer duration of spinal anesthesia than lidocaine. Memantine shows a more sensory-selective action over motor blockade.

摘要

尽管美金刚可阻断钠电流并产生局部皮肤麻醉作用,但美金刚用于脊髓麻醉的情况尚不清楚。本研究的目的是评估美金刚在脊髓麻醉中的局部麻醉效果,并将其与广泛使用的局部麻醉药利多卡因进行比较。在给大鼠鞘内注射每种药物的五个剂量后,构建了美金刚和利多卡因的剂量-反应曲线。将这些药物的效能以及对运动功能、本体感觉和痛觉的脊髓麻醉作用持续时间与利多卡因进行了比较。我们发现美金刚对运动功能、本体感觉和痛觉产生剂量依赖性的脊髓阻滞。以50%有效剂量(ED50)为基础,效能排序为利多卡因大于美金刚(差异P<0.05)。在等效剂量(ED25、ED50、ED75)下,美金刚产生的阻滞持续时间比利多卡因长(差异P<0.05)。美金刚而非利多卡因表现出更多的感觉/痛觉阻滞而非运动阻滞。临床前数据表明,美金刚的效能比利多卡因低,而美金刚产生的脊髓麻醉持续时间比利多卡因长。美金刚在运动阻滞方面表现出更强的感觉选择性作用。

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