Advertisement

Drugs

, Volume 78, Issue 17, pp 1805–1816 | Cite as

Tapentadol Prolonged Release: A Review in Pain Management

  • Emma D. DeeksEmail author
Adis Drug Evaluation

Abstract

Tapentadol prolonged release (tapentadol PR) [Palexia® SR in EU] is a long-acting tablet formulation of the strong central analgesic tapentadol, which acts as both a μ-opioid receptor (MOR) agonist and a noradrenaline reuptake inhibitor. Tapentadol PR is approved for chronic pain in various countries, with its EU indication (severe chronic pain manageable only with opioid analgesics) being the focus here. Well-designed trials and clinical practice data support tapentadol PR use in this setting. Short term, tapentadol PR was an effective and generally well tolerated analgesic for moderate to severe pain of varying aetiologies, including neuropathic pain. It provided analgesia at least as good as that of conventional strong opioids and appeared more favourable in terms of gastrointestinal tolerability, likely due to less potent MOR binding. Severe back pain with a neuropathic component responded well to moderate-dose tapentadol PR in some patients, while for others, an increase to the maximum recommended tapentadol PR dosage provided analgesia at least as good as that of moderate-dose tapentadol PR plus pregabalin and appeared to have some CNS tolerability benefits. Data also support the use of tapentadol PR in opioid rotation, including when conventional opioids are intolerable. Longer-term data in musculoskeletal pain conditions indicate continued benefit over up to 2 years’ treatment with tapentadol PR with no evidence of tolerance. Thus, tapentadol PR is a useful option for the management of severe chronic pain.

Notes

Acknowledgements

During the peer review process, the manufacturer of tapentadol PR was also offered the opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Compliance with Ethical Standards

Funding

The preparation of this review was not supported by any external funding.

Conflicts of interest

Emma Deeks is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.

References

  1. 1.
    Raffaeli W, Arnaudo E. Pain as a disease: an overview. J Pain Res. 2017;10:2003–8.CrossRefGoogle Scholar
  2. 2.
    Renn CL, Dorsey SG. The physiology and processing of pain: a review. AACN Clin Issues. 2005;16(3):277–90.CrossRefGoogle Scholar
  3. 3.
    Ossipov MH, Morimura K, Porreca F. Descending pain modulation and chronification of pain. Curr Opin Support Palliat Care. 2014;8(2):143–51.PubMedPubMedCentralGoogle Scholar
  4. 4.
    British Medical Association. Chronic pain: supporting safer prescribing of analgesics. 2017. http://www.bma.org.uk. Accessed 30 Oct 2018.
  5. 5.
    Tennant F. Types of chronic pain. 2015. https://www.practicalpainmanagement.com. Accessed 30 Oct 2018.
  6. 6.
    Ballantyne JC, Kalso E, Stannard C. WHO analgesic ladder: a good concept gone astray. BMJ. 2016;352:i20.CrossRefGoogle Scholar
  7. 7.
    Scottish Intercollegiate Guidelines Network. Management of chronic pain. A national clinical guideline. 2013. http://www.sign.ac.uk. Accessed 30 Oct 2018.
  8. 8.
    World Health Organization. WHO’s cancer pain ladder for adults. 2015. http://www.who.int. Accessed 30 Oct 2018.
  9. 9.
    Smith HS. Opioids and neuropathic pain. Pain Physician. 2012;15(3 Suppl):ES93–ES110.Google Scholar
  10. 10.
    Tzschentke TM, Christoph T, Kogel BY. The mu-opioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: the case of tapentadol. CNS Drugs. 2014;28(4):319–29.CrossRefGoogle Scholar
  11. 11.
    Raffa RB, Elling C, Tzschentke TM. Does ‘strong analgesic’ equal ‘strong opioid’? Tapentadol and the concept of ‘μ -load’. Adv Ther. 2018.  https://doi.org/10.1007/s12325-018-0778-x.CrossRefGoogle Scholar
  12. 12.
    Vadivelu N, Huang Y, Mirante B, et al. Patient considerations in the use of tapentadol for moderate to severe pain. Drug Healthc Patient Saf. 2013;5:151–9.CrossRefGoogle Scholar
  13. 13.
    Tzschentke TM, Christoph T, Kögel B, et al. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (Tapentadol HCl): a novel μ-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007;323(1):265–76.CrossRefGoogle Scholar
  14. 14.
    Schröder W, Tzschentke TM, Terlinden R, et al. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia. J Pharmacol Exp Ther. 2011;337(1):312–20.CrossRefGoogle Scholar
  15. 15.
    Schröder W, Vry JD, Tzschentke TM, et al. Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Eur J Pain. 2010;14(8):814–21.CrossRefGoogle Scholar
  16. 16.
    Oh C, Rengelshausen J, Mangold B, et al. A thorough QT/QTc study of multiple doses of tapentadol immediate release in healthy subjects. Int J Clin Pharmacol Ther. 2010;48(10):678–87.CrossRefGoogle Scholar
  17. 17.
    Biondi DM, Xiang J, Etropolski M, et al. 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.CrossRefGoogle Scholar
  18. 18.
    Serrie A, Lange B, Steup A. Tapentadol prolonged-release for moderate-to-severe chronic osteoarthritis knee pain: a double-blind, randomized, placebo- and oxycodone controlled release-controlled study. Curr Med Res Opin. 2017;33(8):1423–32.CrossRefGoogle Scholar
  19. 19.
    Buynak R, Shapiro DY, Okamoto A, et al. 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.CrossRefGoogle Scholar
  20. 20.
    Afilalo M, Etropolski MS, Kuperwasser B, et al. Efficacy and safety of tapentadol extended release compared with oxycodone controlled release for the management of moderate to severe chronic pain related to osteoarthritis of the knee: a randomized, double-blind, placebo-and active-controlled phase III study. Clin Drug Investig. 2010;30(8):489–505.CrossRefGoogle Scholar
  21. 21.
    Etropolski M, Kuperwasser B, Flugel M, et al. 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.CrossRefGoogle Scholar
  22. 22.
    Wild JE, Grond S, Kuperwasser B, et al. 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.CrossRefGoogle Scholar
  23. 23.
    Grunenthal Ltd. Palexia SR prolonged release tablets: summary of product characteristics. 2017. https://www.medicines.org.uk/. Accessed 30 Oct 2018.
  24. 24.
    Gohler K, Brett M, Smit JW, et al. Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Int J Clin Pharmacol Ther. 2013;51(4):338–48.CrossRefGoogle Scholar
  25. 25.
    Huntjens DR, Liefaard LC, Nandy P, et al. Population pharmacokinetic modeling of tapentadol extended release (ER) in healthy subjects and patients with moderate or severe chronic pain. Clin Drug Investig. 2016;36(3):213–23.CrossRefGoogle Scholar
  26. 26.
    Lange B, Kuperwasser B, Okamoto A, et al. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain. Adv Ther. 2010;27(6):381–99.CrossRefGoogle Scholar
  27. 27.
    Biondi DM, Xiang J, Etropolski M, et al. Tolerability and efficacy of tapentadol extended release in elderly patients ≥ 75 years of age with chronic osteoarthritis knee or low back pain. J Opioid Manag. 2015;11(5):393–403.CrossRefGoogle Scholar
  28. 28.
    Lange B, Sohns M, Tempero J, et al. Efficacy and safety of tapentadol prolonged release formulation in the treatment of elderly patients with moderate-to-severe chronic osteoarthritis knee pain: a pooled analysis of two double-blind, randomized, placebo-, and active-controlled trials. Curr Med Res Opin. 2018.  https://doi.org/10.1080/03007995.2018.1520085.CrossRefGoogle Scholar
  29. 29.
    Baron R, Likar R, Martin-Mola E, et al. Effectiveness of tapentadol prolonged release (PR) compared with oxycodone/naloxone PR for the management of severe chronic low back pain with a neuropathic component: a randomized, controlled, open-label, phase 3b/4 study. Pain Pract. 2016;16(5):580–99.CrossRefGoogle Scholar
  30. 30.
    Baron R, Martin-Mola E, Muller M, et al. Effectiveness and safety of tapentadol prolonged release (PR) versus a combination of tapentadol PR and pregabalin for the management of severe, chronic low back pain with a neuropathic component: a randomized, double-blind, phase 3b study. Pain Pract. 2015;15(5):455–70.CrossRefGoogle Scholar
  31. 31.
    Lange B, von Zabern D, Elling C, et al. Efficacy and safety of tapentadol prolonged release for moderate-to-severe chronic osteoarthritis knee pain: a pooled analysis of two double-blind, randomized, placebo- and oxycodone controlled release-controlled studies. Curr Med Res Opin. 2017;33(8):1413–22.CrossRefGoogle Scholar
  32. 32.
    Sanchez Del Aguila MJ, Schenk M, Kern KU, et al. Practical considerations for the use of tapentadol prolonged release for the management of severe chronic pain. Clin Ther. 2015;37(1):94–113.CrossRefGoogle Scholar
  33. 33.
    Merchant S, Provenzano D, Mody S, et al. 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.CrossRefGoogle Scholar
  34. 34.
    Buynak R, Rappaport SA, Rod K, et al. Long-term safety and efficacy of tapentadol extended release following up to 2 years of treatment in patients with moderate to severe, chronic pain: results of an open-label extension trial. Clin Ther. 2015;37(11):2420–38.CrossRefGoogle Scholar
  35. 35.
    Etropolski MS, Okamoto A, Shapiro DY, et al. Dose conversion between tapentadol immediate and extended release for low back pain. Pain Physician. 2010;13(1):61–70.PubMedGoogle Scholar
  36. 36.
    Schwartz S, Etropolski M, Shapiro DY, et al. Safety and efficacy of tapentadol ER in patients with painful diabetic peripheral neuropathy: results of a randomized-withdrawal, placebo-controlled trial. Curr Med Res Opin. 2011;27(1):151–62.CrossRefGoogle Scholar
  37. 37.
    Vinik AI, Shapiro DY, Rauschkolb C, et al. A randomized withdrawal, placebo-controlled study evaluating the efficacy and tolerability of tapentadol extended release in patients with chronic painful diabetic peripheral neuropathy. Diabetes Care. 2014;37(8):2302–9.CrossRefGoogle Scholar
  38. 38.
    Schwartz S, Etropolski MS, Shapiro DY, et al. A pooled analysis evaluating the efficacy and tolerability of tapentadol extended release for chronic, painful diabetic peripheral neuropathy. Clin Drug Investig. 2015;35(2):95–108.CrossRefGoogle Scholar
  39. 39.
    Kress HG, Koch ED, Kosturski H, et al. Tapentadol prolonged release for managing moderate to severe, chronic malignant tumor-related pain. Pain Physician. 2014;17(4):329–43.PubMedGoogle Scholar
  40. 40.
    Imanaka K, Tominaga Y, Etropolski M, et al. Efficacy and safety of oral tapentadol extended release in Japanese and Korean patients with moderate to severe, chronic malignant tumor-related pain. Curr Med Res Opin. 2013;29(10):1399–409.CrossRefGoogle Scholar
  41. 41.
    Imanaka K, Tominaga Y, Etropolski M, et al. Ready conversion of patients with well-controlled, moderate to severe, chronic malignant tumor-related pain on other opioids to tapentadol extended release. Clin Drug Investig. 2014;34(7):501–11.CrossRefGoogle Scholar
  42. 42.
    Galvez R, Schafer M, Hans G, et al. Tapentadol prolonged release versus strong opioids for severe, chronic low back pain: results of an open-label, phase 3b study. Adv Ther. 2013;30(3):229–59.CrossRefGoogle Scholar
  43. 43.
    Steigerwald I, Schenk M, Lahne U, et al. Effectiveness and tolerability of tapentadol prolonged release compared with prior opioid therapy for the management of severe, chronic osteoarthritis pain. Clin Drug Investig. 2013;33(9):607–19.CrossRefGoogle Scholar
  44. 44.
    Kress HG, Koch ED, Kosturski H, et al. Direct conversion from tramadol to tapentadol prolonged release for moderate to severe, chronic malignant tumour-related pain. Eur J Pain. 2016;20(9):1513–8.CrossRefGoogle Scholar
  45. 45.
    Schwittay A, Schumann C, Litzenburger BC, et al. Tapentadol prolonged release for severe chronic pain: results of a noninterventional study involving general practitioners and internists. J Pain Palliat Care Pharmacother. 2013;27(3):225–34.CrossRefGoogle Scholar
  46. 46.
    Baron R, Jansen JP, Binder A, et al. Tolerability, safety, and quality of life with tapentadol prolonged release (PR) compared with oxycodone/naloxone PR in patients with severe chronic low back pain with a neuropathic component: a randomized, controlled, open-label, phase 3b/4 trial. Pain Pract. 2016;16(5):600–19.CrossRefGoogle Scholar
  47. 47.
    Volkow ND, McLellan AT. Opioid abuse in chronic pain - misconceptions and mitigation strategies. N Engl J Med. 2016;374(13):1253–63.CrossRefGoogle Scholar
  48. 48.
    Centers for Disease Control and Prevention. CDC guideline for prescribing opioids for chronic pain - United States, 2016. MMWR Morb Mortal Wkly Rep. 2016.  https://doi.org/10.15585/mmwr.rr6501e1.CrossRefGoogle Scholar
  49. 49.
    Caraceni A, Hanks G, Kaasa S, et al. Use of opioid analgesics in the treatment of cancer pain: evidence-based recommendations from the EAPC. Lancet Oncol. 2012;13(2):e58–68.CrossRefGoogle Scholar
  50. 50.
    American Academy of Pain Medicine. Use of opioids for the treatment of chronic pain. 2013. http://www.painmed.org. Accessed 30 Oct 2018.
  51. 51.
    Leppert W. The impact of opioid analgesics on the gastrointestinal tract function and the current management possibilities. Contemp Oncol (Pozn). 2012;16(2):125–31.PubMedPubMedCentralGoogle Scholar
  52. 52.
    Salwan AJ, Hagemeier NE, Harirforoosh S. Abuse-deterrent opioid formulations: a key ingredient in the recipe to prevent opioid disasters? Clin Drug Investig. 2018;38(7):573–7.CrossRefGoogle Scholar
  53. 53.
    Vosburg SK, Severtson SG, Dart RC, et al. Assessment of tapentadol API abuse liability with the Researched Abuse, Diversion and Addiction-Related Surveillance System. J Pain. 2018;19(4):439–53.CrossRefGoogle Scholar
  54. 54.
    Baron R, Kern U, Muller M, et al. 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. 2015;15(5):471–86.CrossRefGoogle Scholar

Copyright information

© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.SpringerAucklandNew Zealand

Personalised recommendations