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Tapentadol: an overview of the safety profile

Authors Polati E, Canonico PL, Schweiger V, Collino M

Received 8 October 2018

Accepted for publication 27 February 2019

Published 16 May 2019 Volume 2019:12 Pages 1569—1576

DOI https://doi.org/10.2147/JPR.S190154

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Amy Norman

Peer reviewer comments 3

Editor who approved publication: Dr Katherine Hanlon


Enrico Polati,1 Pier Luigi Canonico,2 Vittorio Schweiger,1 Massimo Collino3

1Anesthesia and Intensive Care, Pain Relief Center, Ospedale Policlinico GB Rossi, Verona, Italy; 2Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Novara, Italy; 3Department of Drug Science and Technology, University of Turin, Turin, Italy

Abstract: Long-term opioid therapy may be associated with analgesic efficacy and also predictable adverse events, including cardiovascular and pulmonary events, gastrointestinal disorders, endocrinological harms, psychological problems, impairment of driving ability, and risk of abuse. These effects of opioids are mostly due to the wide expression of the mu receptor. Tapentadol, a centrally acting analgesic, is the first agent of a new class of drugs (MOR-NRI), since it combines two mechanisms of action, namely μ-opioid receptor (MOR) agonism and noradrenaline reuptake inhibition. Noteworthy, MOR activation with tapentadol is markedly lower compared with that exerted by classical opioids, thus likely resulting in fewer opioid-related adverse effects. In this review, we discuss current safety data on tapentadol, with a focus on some specific events, risk of abuse, and driving ability, a well-accepted proxy of the ability of taking critical decisions.

Keywords: tapentadol, safety, pain

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