Tapentadol
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Tapentadol is an opioid used to manage severe pain that has not responded to non-opioid medications, and for which opioid analgesic therapy is appropriate.
Tapentadol is an opioid used to manage severe pain that has not responded to non-opioid medications, and for which opioid analgesic therapy is appropriate.
Tapentadol is a centrally-acting synthetic analgesic. Although their clinical relevance is unclear, tapentadol is believed to have two main mechanisms of action. Tapentadol is a selective mu-opioid receptor (MOR) agonist: it binds to MOR with an affinity greater than or equal to ten-fold affinity compared to delta- and kappa-opioid receptors. Tapentadol also inhibits noradrenaline reuptake, thereby increasing noradrenaline levels and activating alpha-2 receptors to promote analgesia. Tapentadol is a weak serotonin reuptake inhibitor; however, this action does not contribute to its analgesic effect.
用于治疗严重到需要阿片类镇痛剂且替代治疗不充分的急性疼痛。
