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[曲马多的局部镇痛作用并非由阿片受体介导用于大鼠术后早期疼痛]

[Local analgesic effect of tramadol is not mediated by opioid receptors in early postoperative pain in rats].

作者信息

Sousa Angela Maria, Ashmawi Hazem Adel

机构信息

Laboratório de Investigação Médica (LIM-08), Faculdade de Medicina da Universidade de São Paulo (USP), São Paulo, SP, Brasil.

Laboratório de Investigação Médica (LIM-08), Faculdade de Medicina da Universidade de São Paulo (USP), São Paulo, SP, Brasil.

出版信息

Rev Bras Anestesiol. 2015 May-Jun;65(3):186-90. doi: 10.1016/j.bjan.2014.06.008. Epub 2015 Apr 2.

Abstract

BACKGROUND AND OBJECTIVES

Tramadol is known as a central acting analgesic drug, used for the treatment of moderate to severe pain. Local analgesic effect has been demonstrated, in part due to local anesthetic-like effect, but other mechanisms remain unclear. The role of peripheral opioid receptors in the local analgesic effect is not known. In this study, we examined role of peripheral opioid receptors in the local analgesic effect of tramadol in the plantar incision model.

METHODS

Young male Wistar rats were divided into seven groups: control, intraplantar tramadol, intravenous tramadol, intravenous naloxone-intraplantar tramadol, intraplantar naloxone-intraplantar tramadol, intravenous naloxone-intravenous tramadol, and intravenous naloxone. After receiving the assigned drugs (tramadol 5mg, naloxone 200μg or 0.9% NaCl), rats were submitted to plantar incision, and withdrawal thresholds after mechanical stimuli with von Frey filaments were assessed at baseline, 10, 15, 30, 45 and 60min after incision.

RESULTS

Plantar incision led to marked mechanical hyperalgesia during the whole period of observation in the control group, no mechanical hyperalgesia were observed in intraplantar tramadol group, intraplantar naloxone-intraplantar tramadol group and intravenous naloxone-intraplantar tramadol. In the intravenous tramadol group a late increase in withdrawal thresholds (after 45min) was observed, the intravenous naloxone-intravenous tramadol group and intravenous naloxone remained hyperalgesic during the whole period.

CONCLUSIONS

Tramadol presented an early local analgesic effect decreasing mechanical hyperalgesia induced by plantar incision. This analgesic effect was not mediated by peripheral opioid receptors.

摘要

背景与目的

曲马多是一种中枢性镇痛药,用于治疗中重度疼痛。其局部镇痛作用已得到证实,部分原因是具有类似局部麻醉药的作用,但其他机制尚不清楚。外周阿片受体在局部镇痛作用中的作用尚不清楚。在本研究中,我们研究了外周阿片受体在曲马多对足底切口模型的局部镇痛作用中的作用。

方法

将年轻雄性Wistar大鼠分为七组:对照组、足底注射曲马多组、静脉注射曲马多组、静脉注射纳洛酮-足底注射曲马多组、足底注射纳洛酮-足底注射曲马多组、静脉注射纳洛酮-静脉注射曲马多组和静脉注射纳洛酮组。给予指定药物(曲马多5mg、纳洛酮200μg或0.9%氯化钠)后,对大鼠进行足底切口,并在切口后基线、10、15、30、45和60分钟时用von Frey细丝评估机械刺激后的撤针阈值。

结果

在对照组中,足底切口在整个观察期内导致明显的机械性痛觉过敏,在足底注射曲马多组、足底注射纳洛酮-足底注射曲马多组和静脉注射纳洛酮-足底注射曲马多组中未观察到机械性痛觉过敏。在静脉注射曲马多组中,观察到撤针阈值后期升高(45分钟后),静脉注射纳洛酮-静脉注射曲马多组和静脉注射纳洛酮组在整个期间仍存在痛觉过敏。

结论

曲马多呈现出早期局部镇痛作用,可减轻足底切口诱导的机械性痛觉过敏。这种镇痛作用不是由外周阿片受体介导的。

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