<p>Tapentadol: an overview of the safety profile</p>

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.

Modulation of sensitization processes in the management of pain and the importance of descending pathways: a role for tapentadol?

“…A Cochrane review reports minimal adverse effects after 13 years of therapy [71]. Another paper confirms the reduced risk of side effects in comparison with opioids [48].…”

“…No differences in the tolerability profile were disclosed between elderly and younger patients [49]. In addition, tapentadol appears to be better tolerated compared with opioids in studies evaluating specific adverse events, such as gastrointestinal events, hypertension, serotonin syndrome, endocrine toxicity, respiratory depression and, most importantly for young and adult patients, convulsions [48]. The large amount of data collected in clinical trials and in 'field-practice' studies strongly supports the premise of a very good tolerability profile of tapentadol.…”

“…The estimate was remarkably consistent and led to the conclusion that the μ-load of tapentadol is ≤40% (relative to pure MOR agonists, such as morphine, oxycodone and fentanyl, which have by definition a µ-load of 100%). This reduced µ-load in clinical settings likely underlies the more favorable tolerability profile of tapentadol compared with strong classical opioids [48].…”

Novel Insights on the Management of Pain: Highlights From the ‘Science of Relief’ Meeting

“…Overall, these effects of opioids are mostly due to the widespread expression of the μ-receptor in neuronal and other tissues in the human body. Noteworthy, as described above, the μ-load of tapentadol is markedly lower compared with that of classical opioids, therefore resulting in fewer opioid-related adverse effects [33]. The safety of tapentadol has been discussed recently in a comprehensive review, which provides further details and the incidence of specific adverse events [33].…”

The use of tapentadol in the treatment of pain in a patient with tonsil cancer with poor tolerance of previously used opioids – case report

“…Nasilenie objawu niekiedy utrudnia codzienne funkcjonowanie, uniemożliwiając sprawne posługiwanie się sztućcami podczas spożywania posiłków lub samodzielne przyjmowanie płynów doustnych. W dotychczas przeprowadzonych badaniach z zastosowaniem tapentadolu nie obserwowano przypadków istotnych klinicznie drgawek ani napadów padaczkowych [32]. Również u prezentowanego chorego nie stwierdzono drżenia kończyn podczas stosowania tapentadolu, pomimo że objaw ten był istotnie wyrażony podczas przyjmowania oksykodonu.…”