Tapentadol: an Overview of the Safety Profile

Overview

Journal J Pain Res

Publisher Dove Medical Press

Date 2019 Jun 14

PMID 31190968

Citations 9

Authors

Enrico Polati

Pier Luigi Canonico

Vittorio Schweiger

Massimo Collino

Affiliations

Soon will be listed here.

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.

Citing Articles

Pharmacodynamic characteristics and influencing factors of tapentadol for chronic pain relief under dose titration.

Xin L, Zhu H, Niu S, Han X, Pang H, Li J Front Pain Res (Lausanne). 2025; 5:1474529.

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Analgesic efficacy of tapentadol in chronic joint disorders in horses: plasma serotonin concentration and adrenocortical response as biomarkers of pain-induced stress.

Costa G, Tabbi M, Bruschetta G, Spadola F, Leonardi F, Bruno F Front Vet Sci. 2025; 11:1505398.

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Tapentadol: A Comprehensive Review of Its Role in Pain Management.

Zavaleta-Monestel E, Anchia-Alfaro A, Villalobos-Madriz J, Munich A, Garcia-Montero J, Quesada-Villasenor R Cureus. 2024; 16(11):e74307.

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Pharmacological Treatments and Therapeutic Drug Monitoring in Patients with Chronic Pain.

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Fixed Dose Versus Loose Dose: Analgesic Combinations.

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References

Dunkley E, Isbister G, Sibbritt D, Dawson A, Whyte I . The Hunter Serotonin Toxicity Criteria: simple and accurate diagnostic decision rules for serotonin toxicity. QJM. 2003; 96(9):635-42. DOI: 10.1093/qjmed/hcg109. View

Byas-Smith M, Chapman S, Reed B, Cotsonis G . The effect of opioids on driving and psychomotor performance in patients with chronic pain. Clin J Pain. 2005; 21(4):345-52. DOI: 10.1097/01.ajp.0000125244.29279.c1. View

Buynak R, Shapiro D, Okamoto A, Van Hove I, Rauschkolb C, Steup A . 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. Expert Opin Pharmacother. 2010; 11(11):1787-804. DOI: 10.1517/14656566.2010.497720. View

Wild J, Grond S, Kuperwasser B, Gilbert J, McCann B, Lange B . Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Pain Pract. 2010; 10(5):416-27. DOI: 10.1111/j.1533-2500.2010.00397.x. View

Kress H . Tapentadol and its two mechanisms of action: is there a new pharmacological class of centrally-acting analgesics on the horizon?. Eur J Pain. 2010; 14(8):781-3. DOI: 10.1016/j.ejpain.2010.06.017. View

Mailis-Gagnon A, Lakha S, Furlan A, Nicholson K, Yegneswaran B, Sabatowski R . Systematic review of the quality and generalizability of studies on the effects of opioids on driving and cognitive/psychomotor performance. Clin J Pain. 2012; 28(6):542-55. DOI: 10.1097/AJP.0b013e3182385332. View

Dart R, Cicero T, Surratt H, Rosenblum A, Bucher Bartelson B, Adams E . Assessment of the abuse of tapentadol immediate release: the first 24 months. J Opioid Manag. 2012; 8(6):395-402. DOI: 10.5055/jom.2012.0139. View

Merchant S, Provenzano D, Mody S, Ho K, Etropolski M . Composite measure to assess efficacy/gastrointestinal tolerability of tapentadol ER versus oxycodone CR for chronic pain: pooled analysis of randomized studies. J Opioid Manag. 2013; 9(1):51-61. DOI: 10.5055/jom.2013.0147. View

Kwong W, Hammond G, Upmalis D, Okamoto A, Yang M, Kavanagh S . Bowel function after tapentadol and oxycodone immediate release (IR) treatment in patients with low back or osteoarthritis pain. Clin J Pain. 2013; 29(8):664-72. DOI: 10.1097/AJP.0b013e318274b695. View

10.

Cowan A, Raffa R, Tallarida C, Tallarida R, Christoph T, Schroder W . Lack of synergistic interaction between the two mechanisms of action of tapentadol in gastrointestinal transit. Eur J Pain. 2014; 18(8):1148-56. DOI: 10.1002/j.1532-2149.2014.00461.x. View

11.

Tzschentke T, Christoph T, Kogel B . The mu-opioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: the case of tapentadol. CNS Drugs. 2014; 28(4):319-29. DOI: 10.1007/s40263-014-0151-9. View

12.

Baron R, Kern U, Muller M, Dubois C, Falke D, Steigerwald I . Effectiveness and Tolerability of a Moderate Dose of Tapentadol Prolonged Release for Managing Severe, Chronic Low Back Pain with a Neuropathic Component: An Open-label Continuation Arm of a Randomized Phase 3b Study. Pain Pract. 2014; 15(5):471-86. DOI: 10.1111/papr.12199. View

13.

Biondi D, Xiang J, Etropolski M, Moskovitz B . Evaluation of blood pressure and heart rate in patients with hypertension who received tapentadol extended release for chronic pain: a post hoc, pooled data analysis. Clin Drug Investig. 2014; 34(8):565-76. PMC: 4102827. DOI: 10.1007/s40261-014-0209-y. View

14.

Etropolski M, Kuperwasser B, Flugel M, Haufel T, Lange B, Rauschkolb C . Safety and tolerability of tapentadol extended release in moderate to severe chronic osteoarthritis or low back pain management: pooled analysis of randomized controlled trials. Adv Ther. 2014; 31(6):604-20. DOI: 10.1007/s12325-014-0128-6. View

15.

Hegmann K, Weiss M, Bowden K, Branco F, DuBrueler K, Els C . ACOEM practice guidelines: opioids and safety-sensitive work. J Occup Environ Med. 2014; 56(7):e46-53. DOI: 10.1097/JOM.0000000000000237. View

16.

Sabatowski R, Scharnagel R, Gyllensvard A, Steigerwald I . Driving Ability in Patients with Severe Chronic Low Back or Osteoarthritis Knee Pain on Stable Treatment with Tapentadol Prolonged Release: A Multicenter, Open-label, Phase 3b Trial. Pain Ther. 2014; 3(1):17-29. PMC: 4108021. DOI: 10.1007/s40122-014-0025-3. View

17.

Butler S, McNaughton E, Black R . Tapentadol abuse potential: a postmarketing evaluation using a sample of individuals evaluated for substance abuse treatment. Pain Med. 2014; 16(1):119-30. DOI: 10.1111/pme.12524. View

18.

Lauche R, Klose P, Radbruch L, Welsch P, Hauser W . [Opioids in chronic noncancer pain-are opioids different? A systematic review and meta-analysis of efficacy, tolerability and safety in randomized head-to-head comparisons of opioids of at least four week's duration]. Schmerz. 2014; 29(1):73-84. DOI: 10.1007/s00482-014-1432-4. View

19.

Thakur D, Dickerson S, Bhutani M, Junor R . Impact of prolonged-release oxycodone/naloxone on outcomes affecting patients' daily functioning in comparison with extended-release tapentadol: a systematic review. Clin Ther. 2015; 37(1):212-24. DOI: 10.1016/j.clinthera.2014.12.001. View

20.

Borys D, Stanton M, Gummin D, Drott T . Tapentadol toxicity in children. Pediatrics. 2015; 135(2):e392-6. DOI: 10.1542/peds.2014-2096. View