• Filippo Caraci, Flaminia Coluzzi, Franco Marinangeli, Sebastiano Mercadante, Giuseppe Rinonapoli, Patrizia Romualdi, Mariaflavia Nicora, and Anthony H Dickenson.
• Department of Drug Sciences, University of Catania, Catania, Italy.
• Curr Med Res Opin. 2020 May 1; 36 (5): I-XVII.

AbstractObjective: This paper presents and discusses recent evidence on the pathophysiological mechanisms of pain. The role of tapentadol - an analgesic molecule characterized by an innovative mechanism of action (i.e. µ-opioid receptor [MOR] agonism and inhibition of noradrenaline [NA] reuptake [NRI]) - in the modulation of pain, and the most recent pharmacological evidence on this molecule (e.g. the µ-load concept) are also presented and commented upon.Methods: Narrative review.Results: Solid evidence has highlighted the importance of central sensitization in the transition from acute to chronic pain. In particular, the noradrenergic system holds a major role in limiting central sensitization and the progression to chronic pain. Therefore, pharmacological modulation of the noradrenergic system appears to be a well-grounded strategy for the control of chronic pain. Tapentadol is characterized by a to-date-unique mechanism of action since it acts both as a MOR agonist and as an inhibitor of NA reuptake. The synergistic interaction of these two mechanisms allows a strong analgesic effect by acting on both ascending and descending pathways. Of note, the reduced µ-load of tapentadol has two important consequences: first, it limits the risk of opioid-related adverse events, as well as the risk of dependence; second, the NA component becomes predominant at least in some types of pain with consequent specific clinical efficacy in the treatment of neuropathic and chronic pain.Conclusions: According to these characteristics, tapentadol appears suitable in the treatment of chronic pain conditions characterized by both a nociceptive and a neuropathic component, such as osteoarthritis or back pain.

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