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Drugs. 2018 Nov;78(17):1805-1816. doi: 10.1007/s40265-018-1007-2.
Tapentadol prolonged release (tapentadol PR) [Palexia SR in EU] is a long-acting tablet formulation of the strong central analgesic tapentadol, which acts as both a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor. Tapentadol PR is approved for chronic pain in various countries, with its EU indication (severe chronic pain manageable only with opioid analgesics) being the focus here. Well-designed trials and clinical practice data support tapentadol PR use in this setting. Short term, tapentadol PR was an effective and generally well tolerated analgesic for moderate to severe pain of varying aetiologies, including neuropathic pain. It provided analgesia at least as good as that of conventional strong opioids and appeared more favourable in terms of gastrointestinal tolerability, likely due to less potent MOR binding. Severe back pain with a neuropathic component responded well to moderate-dose tapentadol PR in some patients, while for others, an increase to the maximum recommended tapentadol PR dosage provided analgesia at least as good as that of moderate-dose tapentadol PR plus pregabalin and appeared to have some CNS tolerability benefits. Data also support the use of tapentadol PR in opioid rotation, including when conventional opioids are intolerable. Longer-term data in musculoskeletal pain conditions indicate continued benefit over up to 2 years' treatment with tapentadol PR with no evidence of tolerance. Thus, tapentadol PR is a useful option for the management of severe chronic pain.
盐酸曲马多控释片（盐酸曲马多控释片，在欧盟称为 Palexia SR）是一种长效的曲马多片剂，具有很强的中枢镇痛作用，既能作为μ阿片受体（MOR）激动剂，又能作为去甲肾上腺素再摄取抑制剂。盐酸曲马多控释片在多个国家批准用于慢性疼痛，其在欧盟的适应证（仅用阿片类镇痛药可控制的严重慢性疼痛）是这里的重点。精心设计的试验和临床实践数据支持在这种情况下使用盐酸曲马多控释片。短期来看，盐酸曲马多控释片对各种病因引起的中度至重度疼痛，包括神经痛，是一种有效且一般耐受性良好的镇痛药。它提供的镇痛效果至少与传统强效阿片类药物相当，在胃肠道耐受性方面似乎更有利，可能是由于 MOR 结合力较弱。一些患者中度剂量盐酸曲马多控释片治疗严重伴有神经病理性成分的背痛效果良好，而对另一些患者，增加到推荐的最大盐酸曲马多控释片剂量提供的镇痛效果至少与中度剂量盐酸曲马多控释片加普瑞巴林相当，并且似乎具有一些中枢神经系统耐受性方面的益处。数据还支持在阿片类药物转换中使用盐酸曲马多控释片，包括在不能耐受常规阿片类药物的情况下。在肌肉骨骼疼痛疾病的长期数据表明，在长达 2 年的盐酸曲马多控释片治疗期间持续获益，且无耐受性证据。因此，盐酸曲马多控释片是治疗严重慢性疼痛的有效选择。
