Oakland University, William Beaumont School of Medicine, 525 O'Dowd Hall, Rochester, MI 48309, USA.
Expert Opin Pharmacother. 2012 Feb;13(2):283-6. doi: 10.1517/14656566.2012.648616. Epub 2011 Dec 23.
Tapentadol is a newly approved novel analgesic drug with a dual mode of action: a mu-opioid agonist and an inhibitor of norepinephrine reuptake (MOR-NRI). Preclinical evidence supports a synergistic interaction between these two effects. It is the first opioid agonist to exhibit predominant norepinephrine reuptake inhibition with minimal serotonin effects. It is FDA approved for use in the US for moderate to severe pain in adults, available in the immediate release form for acute pain and as an extended-release formulation for chronic pain when continuous analgesia is required. Tapentadol has demonstrated reduced treatment-emergent opioid-related gastrointestinal adverse effects compared with pure opioid agonists. The synergistic mu-opioid and alpha(2)-adrenergic effects suggest the potential for particular utility in neuropathic pain states or other pain states associated with hyperalgesia.
μ-阿片受体激动剂和去甲肾上腺素再摄取抑制剂（MOR-NRI）。临床前证据支持这两种作用之间的协同相互作用。它是第一个表现出主要去甲肾上腺素再摄取抑制作用且对 5-羟色胺影响最小的阿片类激动剂。它已获得美国 FDA 批准，用于治疗成人中度至重度疼痛，有即时释放形式用于急性疼痛，也有缓释形式用于需要持续镇痛的慢性疼痛。与纯阿片类激动剂相比，曲马多显示出减少的治疗中出现的与阿片类相关的胃肠道不良反应。协同的 μ-阿片受体和 α2-肾上腺素能作用表明其在神经病理性疼痛状态或其他与痛觉过敏相关的疼痛状态中具有特殊用途的潜力。
