Tapentadol in pain management: a μ-opioid receptor agonist and noradrenaline reuptake inhibitor.

Several mechanisms can be proposed to explain an apparent synergistic analgesic action between μ-opioid and α(2)-adrenergic receptor agonists. Combining both effects in a single molecule eliminates the potential for drug-drug interactions inherent in multiple drug therapy. Tapentadol is the first US FDA-approved centrally acting analgesic having both μ-opioid receptor agonist and noradrenaline (norepinephrine) reuptake inhibition activity with minimal serotonin reuptake inhibition.