Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule

Drugs Today (Barc). 2009 Jul;45(7):483-96. doi: 10.1358/dot.2009.45.7.1395291.


Tapentadol exerts its analgesic effects through micro opioid receptor agonism and noradrenaline reuptake inhibition in the central nervous system. Preclinical studies demonstrated that tapentadol is effective in a broad range of pain models, including nociceptive, inflammatory, visceral, mono- and polyneuropathic models. Moreover, clinical studies showed that tapentadol effectively relieves moderate to severe pain in various pain care settings. In addition, it was reported to be associated with significantly fewer treatment discontinuations due to a significantly lower incidence of gastrointestinal-related adverse events compared with equivalent doses of oxycodone. The combination of these reduced treatment discontinuation rates and tapentadol efficacy for the relief of moderate to severe nociceptive and neuropathic pain may offer an improvement in pain therapy by increasing patient compliance with their treatment regimen.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adrenergic Uptake Inhibitors / adverse effects
  • Adrenergic Uptake Inhibitors / pharmacology
  • Adrenergic Uptake Inhibitors / therapeutic use
  • Analgesics / adverse effects
  • Analgesics / pharmacology*
  • Analgesics / therapeutic use
  • Animals
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Humans
  • Pain / drug therapy*
  • Phenols / adverse effects
  • Phenols / pharmacology*
  • Phenols / therapeutic use
  • Receptors, Opioid, mu / agonists
  • Tapentadol


  • Adrenergic Uptake Inhibitors
  • Analgesics
  • Phenols
  • Receptors, Opioid, mu
  • Tapentadol