Discovery Research Laboratories, Nippon Shinyaku Co., Ltd., 14, Nishinosho-monguchi-cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan.
Eur J Pharmacol. 2012 Feb 15;676(1-3):75-80. doi: 10.1016/j.ejphar.2011.12.002. Epub 2011 Dec 14.
Tramadol is a widely used analgesic that stimulates the μ opioid receptor and inhibits serotonin and noradrenalin reuptake. There have been studies on the analgesic effects of tramadol based on the tail-flick test, the formalin test, and the induction of allodynia by sciatic-nerve ligation. However, the effects of tramadol on behaviors related to bladder pain and bladder overactivity induced by cystitis have not been reported. To investigate the usefulness of tramadol for patients with cystitis, we investigated these effects of tramadol in rodent cystitis models. Intraperitoneal injection of cyclophosphamide caused bladder-specific inflammation and increases in pain-related behaviors, the number of voids and bladder weight in mice. Tramadol suppressed the cyclophosphamide-induced pain-related behaviors but did not affect the number of voids or the bladder weight. During continuous-infusion cystometrograms in anesthetized rats, cyclophosphamide shortened the intercontraction interval, indicating bladder overactivity. Tramadol significantly prolonged the intercontraction interval, and the effect was partially blocked by the opioid antagonist naloxone. This finding indicates that μ opioid receptors may be involved in the action of tramadol. In conclusion, tramadol ameliorated cyclophosphamide-induced bladder-pain-related behaviors and bladder overactivity in rodents. These findings suggest that tramadol might be a treatment option for cystitis-induced bladder pain and bladder overactivity.
曲马多是一种广泛使用的镇痛药,它刺激μ阿片受体并抑制 5-羟色胺和去甲肾上腺素的再摄取。已有研究基于甩尾试验、福尔马林试验以及坐骨神经结扎诱导的痛觉过敏,对曲马多的镇痛效果进行了研究。然而,曲马多对膀胱炎引起的与膀胱疼痛和膀胱过度活动相关的行为的影响尚未报道。为了研究曲马多对膀胱炎患者的有用性,我们在鼠膀胱炎模型中研究了曲马多的这些作用。环磷酰胺腹腔注射引起膀胱特异性炎症,并增加小鼠与疼痛相关的行为、排尿次数和膀胱重量。曲马多抑制环磷酰胺引起的与疼痛相关的行为,但不影响排尿次数或膀胱重量。在麻醉大鼠的持续膀胱测压图中,环磷酰胺缩短了收缩间期,表明膀胱过度活动。曲马多显著延长了收缩间期,该作用部分被阿片受体拮抗剂纳洛酮阻断。这一发现表明μ阿片受体可能参与了曲马多的作用。总之,曲马多改善了环磷酰胺诱导的鼠膀胱疼痛相关行为和膀胱过度活动。这些发现表明,曲马多可能是治疗膀胱炎引起的膀胱疼痛和膀胱过度活动的一种选择。