Expert review of neurotherapeutics
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Tapentadol is a novel opioid agent with a dual mode of analgesic action. The inhibition of norepinephrine combined with moderate opioid agonist activity results in fewer gastrointestinal adverse effects compared with equianalgesic doses of oxycodone. Having no active metabolites and minimal protein binding, tapentadol provides improved tolerability with a lower potential for pharmacokinetic drug-drug interactions or accumulation with impaired renal or hepatic function when compared with oxycodone. Tapentadol immediate-release is currently US FDA approved for moderate-to-severe acute pain in adults.