It is similar to tramadol in its dual mechanism of action. Namely, its ability to activate the mu opioid receptor and inhibit the reuptake of norepinephrine. It is not a pro drug and therefore does not rely on metabolism to produce its therapeutic effects. This makes it a useful moderate potency analgesic option for patients who do not respond adequately to more commonly used opioids due to genetic disposition (poor metabolizers of CYP3A4 and CYP2D6), as well as providing a more consistent dosage response range among the patient population.

The potency of tapentadol is somewhere between that of tramadol and morphine, with an analgesic efficacy comparable to that of oxycodone despite a lower incidence of side effects.

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