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

Langford, Richard M. and Knaggs, Roger and Farquhar-Smith, Paul and Dickenson, Anthony H. (2016) Is tapentadol different from classical opioids?: a review of the evidence. British Journal of Pain, 10 (4). pp. 217-221. ISSN 2049-4645

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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.

Item Type: Article
Keywords: Tapentadol, opioids, pain pharmacology, analgesics, analgesic mechanisms of action
Schools/Departments: University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number: https://doi.org/10.1177/2049463716657363
Depositing User: Knaggs, Roger
Date Deposited: 22 Jan 2018 12:18
Last Modified: 27 Jun 2018 10:02
URI: http://eprints.nottingham.ac.uk/id/eprint/49225

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