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Tapentadol immediate release for the relief of moderate-to-severe acute pain.

机译：他喷他多立即释放可缓解中度至重度急性疼痛。

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摘要

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.
机译：他喷他多是一种新型的中枢镇痛药，具有两种作用机理：微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均显示出广泛的镇痛效果。本文回顾了他喷他多立即释放（IR）的临床发展，包括II和III期临床试验的结果，该试验评估了他喷他多IR在中度至重度急性疼痛患者中的疗效和安全性。在针对中度至重度急性术后疼痛，骨关节炎疼痛和/或腰痛的患者的临床研究中，他喷他多IR 50、75或100 mg每4-6小时一次，其镇痛效果与微阿片类药物相似受体激动剂羟考酮HCl IR每4-6小时10或15 mg。但是，与羟考酮IR相比，他喷他多IR在提供可比镇痛效果的剂量下与恶心和/或呕吐和便秘的发生率显着降低，并且中止治疗的比率也显着降低。在不同的疼痛模型中观察到的疗效以及与他喷他多IR相关的胃肠道耐受性特征表明，这种新型镇痛药是缓解中度至重度急性疼痛的有吸引力的治疗选择。

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