Is tapentadol different from classical opioids?: a review of the evidence

Langford, Richard M.; Knaggs, Roger; Farquhar-Smith, Paul; Dickenson, Anthony H.

Abstract

Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain. The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action. The reduced incidence of some of the typical opioid-induced side effects, compared to equianalgesic doses of classical opioids, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms. Both the pre-clinical and clinical profiles appear to be differentiated from those of classical opioids.

Citation

Langford, R. M., Knaggs, R., Farquhar-Smith, P., & Dickenson, A. H. (2016). Is tapentadol different from classical opioids?: a review of the evidence. British Journal of Pain, 10(4), https://doi.org/10.1177/2049463716657363

• Journal Article Type: Article
• Acceptance Date: Apr 30, 2016
• Online Publication Date: Jul 25, 2016
• Publication Date: Nov 1, 2016
• Deposit Date: Jan 22, 2018
• Publicly Available Date: Jan 22, 2018
• Journal: British Journal of Pain
• Print ISSN: 2049-4637
• Electronic ISSN: 2049-4645
• Publisher: SAGE Publications
• Peer Reviewed: Peer Reviewed
• Volume: 10
• Issue: 4
• DOI: https://doi.org/10.1177/2049463716657363
• Keywords: Tapentadol, opioids, pain pharmacology, analgesics, analgesic mechanisms of action
• Public URL: https://nottingham-repository.worktribe.com/output/819894
• Publisher URL: http://journals.sagepub.com/doi/10.1177/2049463716657363