Ochoa-Aguilar A, Sotomayor-Sobrino M A, Jaimez R, Rodríguez R, Plancarte-Sánchez R, Ventura-Martinez R
Departmento de Farmacología, Facultad de Medicina, Universidad Nacional Autónoma de México, C.P. 04510, Delegación Coyoacán, Ciudad de México, México.
Clínica del Dolor, Instituto Nacional de Cancerología.
Drug Dev Res. 2017 Mar;78(2):105-115. doi: 10.1002/ddr.21381. Epub 2017 Mar 26.
Preclinical Research The aim of this study was to determine the antiallodynic effect of acute administration of the β-lactam antimicrobials, ceftriaxone (CFX) and clavulanic acid (CLAV), for the control of established pain on a model of neuropathic pain (NP). We also investigated the involvement of dopaminergic and opioidergic pathways as well as alterations in serum concentrations of TNF-α in the antiallodynic actions of these drugs. CFX, CLAV, or gabapentin (GAP), a reference drug, were administered i.p. twelve days after constriction of the sciatic nerve in rats. Mechanic and cold allodynia were evaluated for 3 h and alterations in serum concentration of TNF-α determined. Both CFX and CLAV had antiallodynic effects in response to mechanical and cold stimulation, similar to GAP. The antiallodynic effects of CFX and CLAV were blocked by haloperidol (HAL), a D2 receptor antagonist, and by naloxone (NLX), an opioid receptor antagonist. Additionally, serum TNF-α levels were attenuated following CFX and CLAV administration. These results suggest that acute administration of CFX and CLAV may represent a promising approach for treating the acute allodynia of NP, and that the mechanisms involved in these effects involve activation of dopaminergic and opioidergic pathways as well as modulation of TNF-α production. Drug Dev Res 78 : 105-115, 2017. © 2017 Wiley Periodicals, Inc.
临床前研究 本研究的目的是确定β-内酰胺类抗菌药物头孢曲松(CFX)和克拉维酸(CLAV)急性给药对神经病理性疼痛(NP)模型中已确立疼痛的抗痛觉过敏作用。我们还研究了多巴胺能和阿片样物质能途径的参与情况以及这些药物抗痛觉过敏作用中血清肿瘤坏死因子-α(TNF-α)浓度的变化。在大鼠坐骨神经结扎12天后,腹腔注射CFX、CLAV或作为对照药物的加巴喷丁(GAP)。评估3小时内的机械性和冷痛觉过敏情况,并测定血清TNF-α浓度的变化。CFX和CLAV对机械性和冷刺激均有抗痛觉过敏作用,与GAP相似。CFX和CLAV的抗痛觉过敏作用被D2受体拮抗剂氟哌啶醇(HAL)和阿片受体拮抗剂纳洛酮(NLX)阻断。此外,给予CFX和CLAV后血清TNF-α水平降低。这些结果表明,CFX和CLAV急性给药可能是治疗NP急性痛觉过敏的一种有前景的方法,且这些作用涉及的机制包括多巴胺能和阿片样物质能途径的激活以及TNF-α产生的调节。《药物研发研究》78: 105 - 115, 2017。© 2017威利期刊公司。