Anesthesiology Research, William Beaumont Hospital, Department of Anesthesiology, 3601 W. 13 Mile Rd., Royal Oak, MI 48073, USA.
Expert Opin Pharmacother. 2009 Nov;10(16):2687-96. doi: 10.1517/14656560903313734.
Tapentadol is a novel, centrally acting analgesic with two mechanisms of action: micro-opioid receptor agonism and norepinephrine reuptake inhibition. It has demonstrated broad analgesic efficacy across multiple pain models. This article reviews the clinical development of tapentadol immediate release (IR), including results from Phase II and III clinical trials that evaluated the efficacy and safety of tapentadol IR in patients with moderate-to-severe acute pain. In clinical studies in patients with moderate-to-severe acute postoperative pain, osteoarthritis pain and/or low back pain, tapentadol IR 50, 75 or 100 mg every 4 - 6 h has demonstrated analgesic efficacy similar to that observed with the micro-opioid receptor agonist oxycodone HCl IR 10 or 15 mg every 4 - 6 h. However, at doses providing comparable analgesic efficacy, tapentadol IR has been associated with significantly lower incidences of nausea and/or vomiting and constipation, and a significantly lower rate of treatment discontinuation compared with oxycodone IR. The observed efficacy across different pain models and favorable gastrointestinal tolerability profile associated with tapentadol IR indicate that this novel analgesic is an attractive treatment option for the relief of moderate-to-severe acute pain.
曲马多是一种新型中枢作用镇痛药，具有两种作用机制：μ-阿片受体激动作用和去甲肾上腺素再摄取抑制作用。它在多种疼痛模型中表现出广泛的镇痛疗效。本文综述了曲马多速释制剂（IR）的临床开发情况，包括 II 期和 III 期临床试验的结果，这些试验评估了曲马多 IR 在中重度急性疼痛患者中的疗效和安全性。在中重度急性术后疼痛、骨关节炎疼痛和/或腰痛患者的临床研究中，曲马多 IR 50、75 或 100mg 每 4-6 小时一次的疗效与观察到的μ阿片受体激动剂盐酸羟考酮 IR 10 或 15mg 每 4-6 小时一次的疗效相似。然而，在提供相当的镇痛疗效的剂量下，与羟考酮 IR 相比，曲马多 IR 与恶心和/或呕吐、便秘的发生率显著降低，以及治疗中断的发生率显著降低。曲马多 IR 在不同疼痛模型中的观察到的疗效和良好的胃肠道耐受性特征表明，这种新型镇痛药是缓解中重度急性疼痛的一种有吸引力的治疗选择。
