Modulation of sensitization processes in the management of pain and the importance of descending pathways: a role for tapentadol?. (3rd May 2020)

• Record Type: Journal Article
• Authors: Caraci, Filippo; Coluzzi, Flaminia; Marinangeli, Franco; Mercadante, Sebastiano; Rinonapoli, Giuseppe; Romualdi, Patrizia; Nicora, Mariaflavia; Dickenson, Anthony H.
• Is Part Of: Current medical research and opinion. Volume 36:Number 5(2020)
• Page Start: (I)
• Page End: (XVII)
• Publication Date: 2020-05-03
• Subjects: Tapentadol -- neuropathic pain -- pharmacology -- µ-load; Clinical medicine -- Periodicals; Therapeutics -- Periodicals; 615.5
• DOI: 10.1080/03007995.2019.1703664
• Languages: English
• ISSNs: 0300-7995

Abstract

Abstract: Objective: 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.