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首页> 外文OA文献 >SYNERGISTIC INTERACTION BETWEEN TAPENTADOL AND FLUPIRTINE IN THE RAT ORAFACIAL FORMALIN TEST
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SYNERGISTIC INTERACTION BETWEEN TAPENTADOL AND FLUPIRTINE IN THE RAT ORAFACIAL FORMALIN TEST

机译：坦帕多尔和氟吡丁在大鼠口腔福尔马林试验中的协同相互作用

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INTRODUCTION\udCombination therapy with two or more analgesics is widely\udused for conditions associated with moderate to severe pain.\udCombinations of diverse analgesics with different modes of\udaction can improve the risk-benefit ratio of analgesic treatments.\udTapentadol (TAP) is an atypical opioid with dual mechanisms\udof action; it is a l-opioid receptor (MOR) agonist and acts to\udinhibit norepinephrine (NE) reuptake1.\udFlupirtine (FLP) is a centrally acting non-opioid analgesic,\udwithout antipyretic or anti-inflammatory effects2. It inhibits the\udN-methyl-D-aspartate (NMDA) receptor indirectly.\udMolecules that inhibit the NMDA receptor are likely to have\udsynergistic or additive effects with other analgesics, particularly\udopioids. The aim of this study is to evaluate the antinociceptive\udeffect of tapentadol (TAP) and flupirtine (FLP), when administered\udseparately or in combination, as well as their synergistic\udinteraction in the orofacial formalin test in rats.\udMATERIALS AND METHODS\udThe orofacial formalin test in rats was used in this study. Fifty\udmicroliter of 2.5% formalin solution was injected subcutaneously\udinto the right upper lip. Thereafter the behavior (face\udrubbing) of the rats was recorded for 45 min. The degree of\udnociception was assessed as the area under the time course of\udresponse (face rubbing) curve (AUC). The isobologram was\udconstructed by connecting the ED30 of the FLP plotted on the\udabscissa with the ED30 of TAP plotted on the ordinate to obtain\udthe additive line.\udRESULTS AND CONCLUSIONS\udAfter IP injection of TAP at different doses (2, 5, 10 and\ud15 mg kg\ud1), the biphasic nociceptive behavior was reduced in\uda dose-dependent manner in both phase I and II. Conversely, IP\udinjection of FLP at different doses (0.6, 1.6, 3.3, 6.6, 16.6 and\ud22.2 mg kg\ud1) induced a dose-dependent antinociceptive effect\udin phase II only. TAP was found to be more potent and effective\udthan FLP. The interaction between TAP and FLP was synergistic\udin phase II with an interaction index (c) of 0.50 0.24.\udThe data reported in this study indicate that FLP enhances the\udanti-nociceptive effect of TAP and this drug combination might\udbe useful in the treatment of chronic pain.
机译：引言\ ud两种或多种镇痛药的联合疗法广泛用于\中度至重度疼痛相关的疾病。\ ud多种镇痛药的不同镇痛剂的联合使用可以提高镇痛药的风险收益率。\ udTapentadol（TAP）是具有双重作用\ udof作用的非典型阿片类药物；它是L型阿片受体（MOR）激动剂，起\ udin抑制去甲肾上腺素（NE）再摄取的作用。\ ud氟吡汀（FLP）是一种中枢作用的非阿片类镇痛药，没有解热或抗炎作用2。它可以间接抑制udN-甲基-D-天冬氨酸（NMDA）受体。抑制NMDA受体的udm分子可能与其他镇痛药，特别是拟类鸦片药物具有协同作用或累加作用。这项研究的目的是评估他喷他多（TAP）和氟吡汀（FLP）分开或组合使用时的镇痛效果/作用，以及它们在大鼠口福尔马林试验中的协同/相互作用。\ udMaterials and Methods \ ud在大鼠中进行了口面福尔马林测试。将五十微克2.5％福尔马林溶液皮下注射至右上唇。此后，记录大鼠的行为（面部\摩擦）45分钟。 \受痛程度评估为\\反应（面部摩擦）曲线（AUC）的时间过程下的面积。通过将\ udabscissa上绘制的FLP的ED30与纵坐标上绘制的TAP的ED30连接起来，得到等效线。\ ud结果与结论\ ud以不同剂量进行TAP的IP注射后（2、5 ，10和\ ud15 mg kg \ ud1）时，I和II期的双相伤害行为均以剂量依赖性方式降低。相反，IP \不同剂量（0.6、1.6、3.3、6.6、16.6和\ ud22.2 mg kg \ ud1）的FLP注射仅诱导剂量依赖性的镇痛作用\ udin II期。发现TAP比FLP更有效和有效。 TAP与FLP的相互作用为协同\ udin II期，相互作用指数（c）为0.50 0.24。\ ud本研究报告的数据表明FLP增强TAP的\ udanti-nociceptive效果，这种药物联合可能\有用在治疗慢性疼痛。

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