NCIt definition : An orally available, synthetic benzenoid that acts as an agonist for the mu-opioid
receptor (MOR) and inhibits the reuptake of noradrenaline, with potential anti-nociceptive
activity. Upon oral administration, tapentadol binds to the MOR which enhances MOR-mediated
signaling, interferes with the sensation of pain and results in an analgesic effect.
Tapentadol also inhibits the reuptake of noradrenaline, which increases the levels
of noradrenaline (NA), activates the inhibitory alpha-2 receptors and results in an
analgesic effect.;