Tapentadol for pain: a treatment evaluation
Tapentadol for pain: a treatment evaluation
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DOI：
10.1517/14656566.2012.648616
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发表时间：
2012-01
影响因子：
3.2
通讯作者：
C. Hartrick;Jose Rafael Rodríguez Hernandez
中科院分区：
文献类型：
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作者：
C. Hartrick;Jose Rafael Rodríguez Hernandez
他喷他多是一种新批准的新型镇痛药物，具有双重作用模式：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效应之间的协同作用。它是第一种表现出主要的去甲肾上腺素再摄取抑制作用的阿片类激动剂，具有最小的5-羟色胺作用。FDA批准其在美国用于成人中度至重度疼痛，可用于急性疼痛的速释形式，以及需要持续镇痛时用于慢性疼痛的缓释制剂。与纯阿片类激动剂相比，他喷他多已证明治疗后出现的阿片类相关胃肠道不良反应减少。协同μ-阿片样物质和α（2）-肾上腺素能效应表明在神经性疼痛状态或与痛觉过敏相关的其他疼痛状态中特别有用的潜力。
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.