Zegpi C, Gonzalez C, Pinardi G, Miranda H F
Pharmacology Program, ICBM, Faculty of Medicine, Universidad de Chile, Clasificador 70.000, Independencia 1027, Santiago 7, Chile.
Pharmacol Res. 2009 Oct;60(4):291-5. doi: 10.1016/j.phrs.2009.04.005. Epub 2009 Apr 15.
The antinociceptive activity of dexketoprofen was studied in mice using the formalin assay for orofacial pain. The interaction between dexketoprofen and co-administered tramadol was studied using isobolographic analysis. The intraperitoneal administration of dexketoprofen or tramadol, showed dose-dependent antinociceptive activity in both phases of the assay. When administered together, the interaction was mildly synergistic during the first phase, and antagonistic in the second phase. Selective opioid receptor antagonists where used in order to measure the analgesic activity of tramadol in other regions of the CNS. The co-administration of dexketoprofen and tramadol, with previous administration of naltrexone, showed high synergistic activity during the first phase, and less but still synergistic during the second. When using naltrindole, the interaction was mildly more synergistic than the mixture dexketoprofen+tramadol during both phases. Using norbinaltorphimine, the interaction was synergistic in both phases, more marked in the second. These results suggest that the opioid activity of tramadol has an inhibiting effect in antinociceptive activity of the interaction between dexketoprofen and tramadol during the inflammatory (late) stages of pain.
使用福尔马林口腔面部疼痛试验在小鼠中研究了右酮洛芬的抗伤害感受活性。使用等效应线图分析研究了右酮洛芬与共同给药的曲马多之间的相互作用。腹腔注射右酮洛芬或曲马多在试验的两个阶段均显示出剂量依赖性抗伤害感受活性。一起给药时,在第一阶段相互作用为轻度协同,在第二阶段为拮抗。使用选择性阿片受体拮抗剂以测量曲马多在中枢神经系统其他区域的镇痛活性。右酮洛芬和曲马多与先前给予纳曲酮共同给药时,在第一阶段显示出高协同活性,在第二阶段协同作用较小但仍存在。使用纳曲吲哚时,在两个阶段相互作用均比右酮洛芬+曲马多混合物稍具协同性。使用诺宾阿片受体拮抗剂时,在两个阶段相互作用均为协同,在第二阶段更明显。这些结果表明,在疼痛的炎症(晚期)阶段,曲马多的阿片样活性对右酮洛芬和曲马多之间相互作用的抗伤害感受活性具有抑制作用。