Division of Neurological Pain Research and Therapy, Department of Neurology, University Hospital of Schleswig-Holstein, Kiel, Germany.
Department of Anesthesiology and Critical Care Medicine, Philipps-University, Marburg, Germany.
Pain Pract. 2017 Jun;17(5):678-700. doi: 10.1111/papr.12515. Epub 2016 Oct 25.
Tapentadol prolonged release (PR) for the treatment of moderate to severe chronic pain combines 2 modes of action. These are μ-opioid receptor agonism and noradrenaline reuptake inhibition in a single molecule that allow higher analgesic potency through modulation of different pharmacological targets within the pain transmitting systems. At the same time, this can also serve as a clue for modulation of different pain-generating mechanisms according to nociceptive, neuropathic, or mixed pain conditions. Tapentadol PR has now been on the market for 5 years, with over 4.6 million people treated worldwide. A panel of pain specialists convened in Germany to review the clinical program and to discuss the role of tapentadol PR in the management of chronic pain. The clinical study program demonstrated effective and generally well-tolerated treatment for up to 2 years in a broad range of chronic pain conditions, including those with neuropathic pain components. This was confirmed in routine clinical practice observations. Head-to-head studies with World Health Organization (WHO) III opioids such as oxycodone controlled release and oxycodone/naloxone PR showed at least comparable pain relief in the treatment of moderate-to-severe musculoskeletal pain. Rotation from poorly tolerated WHO III opioids to tapentadol PR provided effective pain relief and better symptom control for musculoskeletal pain compared to previous medication. Functionality, health status and quality of life also improved under tapentadol PR treatment. The gastrointestinal tolerability profile was more favorable compared to other tested WHO III opioids. Tapentadol PR has a good safety profile and no evidence of acquired tolerance from the long-term data so far collected. Overall, tapentadol PR represents an effective and generally well-tolerated alternative to "classical" opioidergic drugs.
盐酸他喷他多控释片（PR）用于治疗中重度慢性疼痛，结合了两种作用模式。这两种作用模式是 μ-阿片受体激动作用和去甲肾上腺素再摄取抑制作用，通过调节疼痛传递系统中的不同药理学靶点，使药物具有更高的镇痛效力。同时，这也可以作为根据伤害感受性、神经性或混合性疼痛状况调节不同疼痛产生机制的线索。盐酸他喷他多控释片已经上市 5 年，全球有超过 460 万人接受了治疗。一组德国疼痛专家聚在一起，审查了该药物的临床研究计划，并讨论了盐酸他喷他多控释片在慢性疼痛管理中的作用。临床研究计划表明，在广泛的慢性疼痛状况下，包括伴有神经性疼痛成分的疼痛状况，该药物的治疗有效且通常具有良好的耐受性，最长可达 2 年。这一结果在常规临床实践观察中得到了证实。与世界卫生组织（WHO）三级阿片类药物（如盐酸羟考酮控释片和盐酸羟考酮/纳洛酮控释片）的头对头研究表明，在治疗中重度肌肉骨骼疼痛方面，至少有相当的疼痛缓解作用。与先前的药物相比，从耐受性差的 WHO 三级阿片类药物转换为盐酸他喷他多控释片治疗肌肉骨骼疼痛，可以提供有效的疼痛缓解和更好的症状控制。在接受盐酸他喷他多控释片治疗后，功能、健康状况和生活质量也得到了改善。与其他经过测试的 WHO 三级阿片类药物相比，该药物的胃肠道耐受性更好。盐酸他喷他多控释片具有良好的安全性，从目前收集的长期数据来看，没有出现获得性耐受的证据。总的来说，盐酸他喷他多控释片是一种有效的、通常具有良好耐受性的替代“经典”阿片类药物。
