Article thumbnail

Tapentadol in the management of chronic low back pain: a novel approach to a complex condition?

By Joseph Pergolizzi, Eli Alon, Ralf Baron, Cesare Bonezzi, Jan Dobrogowski, Rafael Gálvez, Troels Jensen, Hans-Georg Kress, Marco AE Marcus, Bart Morlion, Serge Perrot and Rolf-Detlef Treede

Abstract

Chronic pain affects approximately 1 in 5 people in Europe, and around half of sufferers receive inadequate pain management. The most common location is the lower back. Pharmacological treatment of this condition is challenging because of the range of causative mechanisms and the difficulty of balancing analgesic efficacy and tolerability. An international panel of clinical pain specialists met in September, 2009, to discuss the treatment of chronic low back pain, and to review preclinical and clinical data relating to the new analgesic, tapentadol. A lack of consensus exists on the best treatment for low back pain. The range of regularly prescribed pharmacological agents extends from nonopioids (paracetamol, NSAIDs, and COX-2 inhibitors) to opioids, antidepressants and anticonvulsants. Pain relief may be compromised, however, by an undetected neuropathic component or intolerable side effects. Treatment is potentially life-long and effective analgesics are urgently needed, with demonstrable long-term safety. Combining separate agents with different mechanisms of action could overcome the limitations of present pharmacological therapy, but clinical evidence for this approach is currently lacking. Tapentadol combines μ-opioid agonism with noradrenaline reuptake inhibition in a single molecule. There is strong evidence of synergistic antinociception between these two mechanisms of action. In preclinical and clinical testing, tapentadol has shown efficacy against both nociceptive and neuropathic pain. Preclinical data indicate that tapentadol’s μ-opioid agonism makes a greater contribution to analgesia in acute pain, while noradrenaline reuptake inhibition makes a greater contribution in chronic neuropathic pain models. Tapentadol also produces fewer adverse events than oxycodone at equianalgesic doses, and thus may have a ‘μ-sparing effect’. Current evidence indicates that tapentadol’s efficacy/tolerability ratio may be better than those of classical opioids. However, further research is needed to establish its role in pain management

Topics: Expert Opinion
Publisher: Dove Medical Press
OAI identifier: oai:pubmedcentral.nih.gov:3160833
Provided by: PubMed Central

To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.

Suggested articles

Citations

  1. (–)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties.
  2. (2000). A Clinical Guide to Neuropathic Pain.
  3. (1995). Antinociception induced by simultaneous intrathecal and intraperitoneal administration of low doses of morphine. Anesth Analg.
  4. (1989). Antinociceptive interactions between alpha 2-adrenergic and opiate agonists at the spinal level in rodents. Anesth Analg.
  5. (2005). Combination pharmacotherapy for neuropathic pain: current evidence and future directions. Expert Rev Neurotherapeutics.
  6. Definition and assessment of pain.
  7. (2010). Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic
  8. Efficacy and safety of tapentadol extended release for the management of chronic low back pain: results of a prospective, randomized, double-blind, placeboand active-controlled Phase III study. Expert Opin Pharmacother.
  9. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain. Adv Ther.
  10. (1999). Epidemiological features of chronic low-back pain.
  11. Epidemiology of chronic pain in Denmark: an update.
  12. (2009). European Guidelines For the Management of Chronic Non-Specific Low Back Pain (Amended Version). http:// www.backpaineurope.org/web/files/WG2_Guidelines.pdf. Accessed
  13. Evidence for the involvement of the mu but not the delta opioid receptor subtype in the synergistic interaction between opioid and alpha 2 adrenergic antinociception in the rat spinal cord.
  14. Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Pain Pract.
  15. Lost productive time and cost due to common pain conditions in the US workforce.
  16. (2004). Low back pain: an economic assessment in the United States. Orthop Clin North Am.
  17. (2002). Low back pain. Best Pract Res Clin Rheumatol.
  18. Mechanisms of opioid tolerance: emerging evidence and therapeutic implications.
  19. (2000). Modeling of the in vivo antinociceptive interaction between an opioid agonist, (+)-O-desmethyltramadol, and a monoamine reuptake inhibitor, (‑)-O-desmethyltramadol, in rats. J Pharmacol Exp Ther.
  20. Molecular insights into mu opioid pharmacology: from the clinic to the bench.
  21. Multimodal postoperative pain management.
  22. Opioid therapy for chronic pain.
  23. (2001). Pain terms and taxonomies of pain.
  24. Peripheral nerve injury-induced changes in spinal α2-adrenoceptor-mediated modulation of mechanically evoked dorsal horn neuronal responses.
  25. Pharmacoeconomic impact of adverse events of longterm opioid treatment for the management of persistent pain. Clin Drug Investig.
  26. pharmacy, and outpatient costs for osteoarthritis and chronic back pain.
  27. (1995). Physician office visits for low back pain: frequency, clinical evaluation, and treatment patterns from a US national survey.
  28. (2004). Prevalence and characteristics of chronic pain in the general Norwegian population.
  29. Problems of polypharmacy.
  30. (1999). Psychologic and psychosocial factors contributing to chronic pain. Curr Rev Pain.
  31. Quality of life in chronic pain is more associated with beliefs about pain, than with pain intensity.
  32. Safety and tolerability of tapentadol extended release in patients with painful diabetic peripheral neuropathy: Results of a randomizedwithdrawal phase 3 study.
  33. (2006). Survey of chronic pain
  34. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia.
  35. (2007). Systematic review: opioid treatment for chronic back pain: prevalence, efficacy, and association with addiction. Ann Intern Med.
  36. Tapentadol and its two mechanisms of action: Is there a new pharmacological class of centrally acting analgesics on the horizon? Eur
  37. (2009). Tapentadol immediate release for the relief of moderate-tosevere acute pain. Expert Opin Pharmacother.
  38. The 10-minute examination for low back pain.
  39. The determination and application of fixed-dose analgesic combinations for treating multimodal pain.
  40. The economic cost of low back pain
  41. (2009). Tolerability of tapentadol prolonged release based on discontinuations due to adverse events in a 1-Year Randomized Phase 3 Safety Study.
  42. Tölle TR. painDETECT: a new screening questionnaire to identify neuropathic components in patients with back pain. Curr Med Res Opin.
  43. Unmet needs in the management of neuropathic pain.