Tapentadol differs from tramadol in its mechanism. Which statement correctly distinguishes tapentadol from tramadol?

• A Tapentadol is a prodrug requiring CYP2D6 activation; tramadol is active as dispensed
• B Tapentadol is a mu-opioid agonist and norepinephrine reuptake inhibitor with no significant serotonin reuptake inhibition; tramadol inhibits both serotonin and norepinephrine reuptake ✓
• C Tapentadol activates kappa receptors; tramadol activates mu receptors
• D Tapentadol causes more serotonin syndrome risk than tramadol

Explanation

Tapentadol is a centrally acting analgesic with direct mu-opioid agonism and selective norepinephrine reuptake inhibition (NRI), with negligible serotonin reuptake inhibition. Tramadol is also a dual-mechanism drug but inhibits both serotonin and norepinephrine reuptake and requires CYP2D6 conversion of O-desmethyltramadol for its opioid activity. The lack of significant serotonin activity in tapentadol reduces its risk of serotonin syndrome when combined with serotonergic drugs. Tapentadol also has lower constipation and nausea rates.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

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