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      Tapentadol: an overview of the safety profile

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          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.

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          Most cited references 44

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          The Hunter Serotonin Toxicity Criteria: simple and accurate diagnostic decision rules for serotonin toxicity

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            Efficacy and safety of tapentadol extended release for the management of chronic low back pain: results of a prospective, randomized, double-blind, placebo- and active-controlled Phase III study.

            To evaluate the efficacy and safety of tapentadol extended release (ER) for the management of moderate to severe chronic low back pain. Patients (N = 981) were randomized 1:1:1 to receive tapentadol ER 100 - 250 mg b.i.d., oxycodone HCl controlled release (CR) 20 - 50 mg b.i.d., or placebo over 15 weeks (3-week titration period, 12-week maintenance period). Efficacy was assessed as change from baseline in average pain intensity (11-point NRS) at week 12 of the maintenance period and throughout the maintenance period; last observation carried forward was used to impute missing pain scores. Adverse events (AEs) were monitored throughout the study. Tapentadol ER significantly reduced average pain intensity versus placebo at week 12 (least squares mean difference vs placebo [95% confidence interval], -0.8 [-1.22, -0.47]; p < 0.001) and throughout the maintenance period (-0.7 [-1.06,-0.35]; p < 0.001). Oxycodone CR significantly reduced average pain intensity versus placebo at week 12 (-0.9 [-1.24,-0.49]; p < 0.001) and throughout the maintenance period (-0.8 [-1.16,-0.46]; p < 0.001). Tapentadol ER was associated with a lower incidence of treatment-emergent AEs (TEAEs) than oxycodone CR. Gastrointestinal TEAEs, including constipation, nausea, and vomiting, were among the most commonly reported TEAEs (placebo, 26.3%; tapentadol ER, 43.7%; oxycodone CR, 61.9%). The odds of experiencing constipation or the composite of nausea and/or vomiting were significantly lower with tapentadol ER than with oxycodone CR (both p < 0.001). Tapentadol ER (100 - 250 mg b.i.d.) effectively relieved moderate to severe chronic low back pain over 15 weeks and had better gastrointestinal tolerability than oxycodone HCl CR (20 - 50 mg b.i.d.).
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              Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain.

              Tapentadol is a novel, centrally acting analgesic with 2 mechanisms of action: µ-opioid receptor agonism and norepinephrine reuptake inhibition. This randomized, open-label phase 3 study (ClinicalTrials.gov Identifier: NCT00361504) assessed the long-term safety and tolerability of tapentadol extended release (ER) in patients with chronic knee or hip osteoarthritis pain or low back pain. Patients were randomized 4:1 to receive controlled, adjustable, oral, twice-daily doses of tapentadol ER (100 to 250 mg) or oxycodone HCl controlled release (CR; 20 to 50 mg) for up to 1 year. Efficacy evaluations included assessments at each study visit of average pain intensity (11-point numerical rating scale) over the preceding 24 hours. Treatment-emergent adverse events (TEAEs) and discontinuations were monitored throughout the study. A total of 1,117 patients received at least 1 dose of study drug. Mean (standard error) pain intensity scores in the tapentadol ER and oxycodone CR groups, respectively, were 7.6 (0.05) and 7.6 (0.11) at baseline and decreased to 4.4 (0.09) and 4.5 (0.17) at endpoint. The overall incidence of TEAEs was 85.7% in the tapentadol ER group and 90.6% in the oxycodone CR group. In the tapentadol ER and oxycodone CR groups, respectively, TEAEs led to discontinuation in 22.1% and 36.8% of patients; gastrointestinal TEAEs led to discontinuation in 8.6% and 21.5% of patients. Tapentadol ER (100 to 250 mg bid) was associated with better gastrointestinal tolerability than oxycodone HCl CR (20 to 50 mg bid) and provided sustainable relief of moderate to severe chronic knee or hip osteoarthritis or low back pain for up to 1 year. © 2010 World Institute of Pain.
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                Author and article information

                Journal
                J Pain Res
                J Pain Res
                JPR
                jpainres
                Journal of Pain Research
                Dove
                1178-7090
                16 May 2019
                2019
                : 12
                : 1569-1576
                Affiliations
                [1 ]Anesthesia and Intensive Care, Pain Relief Center, Ospedale Policlinico GB Rossi , Verona, Italy
                [2 ]Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale , Novara, Italy
                [3 ]Department of Drug Science and Technology, University of Turin , Turin, Italy
                Author notes
                Correspondence: Enrico PolatiAnestesia e Rianimazione, Ospedale Policlinico GB Rossi , Piazzale Scuro 10, 37134Verona, ItalyTel +39 045 812 4311Fax +39 045 812 4435Email Enrico.polati@ 123456univr.it
                Article
                190154
                10.2147/JPR.S190154
                6529613
                31190968
                © 2019 Polati et al.

                This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                Page count
                Figures: 1, Tables: 1, References: 52, Pages: 8
                Categories
                Review

                Anesthesiology & Pain management

                pain, safety, tapentadol

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