Tapentadol a New Therapeutic Option
Keywords:
Tramadol, pain, receptors, opioid, opioid analgesics, neuralgia.
Abstract
Introduction: The peripheral dysfunction or illness is associated to the sensory phenomenon that includes both symptoms of loss of function as well as pain generation. Opioids provide relief from many pain settings; however they have reduced potency and efficacy for neuropathic pain.
Objective. Provide a current review of the literature about tapentadol that could be used as a guide.
Methodology. A literature search on the Cochrane, PubMed and Embase databases retrieved 66 papers, and from these, the papers with relevant information about tapentadol were selected.
Results and Conclusions. The therapeutic combination of the μ opioid receptor agonists with inhibitors of the norepinephrine reuptake have become more popular recently as an alternative to treat the mechanisms responsible for neuropathic pain. However, even though the inhibitors of the norepinephrine reuptake are well tolerated, their analgesic efficacy is usually unsatisfactory, and opioids usually have tolerability problems; the recent introduction of tapentadol, which combines in the same molecule both mechanisms of action can represent a novel, improved and efficient alternative for analgesia.
References
1. Tuchman M, Barrett JA, Donevan S, et al. Central sensitization and Ca(V)alphadelta ligands in chronic pain syndromes: pathologic processes and pharmacologic effect. J Pain. 2010;11:1241-9.
2. Uchitel OD, Di Guilmi MN, Urbano FJ, et al. Acute modulation of calcium currents and synaptic transmission by gabapentinoids. Channels (Austin). 2010;4:490-6.
3. Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009;31:2804-18.
4. Bee LA, Bannister K, Rahman W, et al. Mu-opioid and noradrenergic alpha(2)-adrenoceptor contributions to the effects of tapentadol on spinal electrophysiological measures of nociception in nerve-injured rats. Pain. 2011;152:131-9.
5. Camilleri M. Opioid-induced constipation: challenges and therapeutic opportunities. Am J Gastroenterol. 2011;106:835-42.
6. Rich JD, Green TC, McKenzie MS. Opioids and deaths. N Engl J Med. 2011;364:686.
7. Prommer EE. Tapentadol: an initial analysis. J Opioid Manag. 2010;6:223-6.
8. Jackson M, Dubose L. Pain medications: what you need to know. Todays FDA. 2010;22:60-3.
9. Hussar DA. New drugs: tapentadol hydrochloride, tolvaptan, and benzyl alcohol. J Am Pharm Assoc (2003). 2009;49:704-8.
10. Nossaman VE, Ramadhyani U, Kadowitz PJ, et al. Advances in perioperative pain management: use of medications with dual analgesic mechanisms, tramadol & tapentadol. Anesthesiol Clin. 2010;28:647-66.
11. Thompson CA. Tapentadol approved as pain reliever. Am J Health Syst Pharm. 2009;66:8.
12. Ravikumar K, Sridhar B, Pradhan N, et al. Four stereoisomers of the novel mu-opioid receptor agonist tapentadol hydrochloride. Acta Crystallogr C. 2011;67:o71-6.
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 mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007;323:265-76.
14. 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;14:814-21.
15. Guay DR. Is tapentadol an advance on tramadol? Consult Pharm. 2009;24:833-40.
16. Abasolo L, Carmona L. Systematic review: are major opioids effective in the treatment of musculoskeletal pain?. Med Clin (Barc). 2007;128:291-301.
17. Nelson T, Brett V. Tapentadol: an initial analysis-- follow-up. J Opioid Manag. 2011;7:87-8, 90-1; author reply 92.
18. Sloan P. Tapentadol for acute and chronic pain. Expert Opin Pharmacother. 2010;11:1783-5.
19. Tzschentke TM, Jahnel U, Kogel B, et al. Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule. Drugs Today (Barc). 2009;45:483-96.
20. Tapentadol (Nucynta)-a new analgesic. Med Lett Drugs Ther. 2009;51:61-2.
21. Kress HG. Tapentadol and its two mechanisms of action: is there a new pharmacological class of centrally- acting analgesics on the horizon? Eur J Pain. 2010;14:781-3.
22. Schroder W, Tzschentke TM, Terlinden R, et al. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia. J Pharmacol Exp Ther. 2011;337:312-20.
23. Guay DR. Oral hydromorphone extended-release. Consult Pharm. 2010;25:816-28.
24. 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, doubleblind, placebo- and active-controlled phase III study. Clin Drug Investig. 2010;30:489-505.
25. Fredheim OM, Borchgrevink PC, Nordstrand B, et al. Prescription of analgesics to patients in opioid maintenance therapy: A pharmacoepidemiological study. Drug Alcohol Depend. 2011. Epub ahead of print.
26. Terlinden R, Kogel BY, Englberger W, et al. In vitro and in vivo characterization of tapentadol metabolites. Methods Find Exp Clin Pharmacol. 2010;32:31-8.
27. Hersh EV, Golubic S, Moore PA. Analgesic update: tapentadol hydrochloride. Compend Contin Educ Dent. 2010;31:594-9.
28. Weichel C, Hecht B. Tapentadol. Opioid analgesic and norepinephrine reuptake inhibitors. Med Monatsschr Pharm. 2010;33:454-60.
29. Xu XS, Smit JW, Lin R, et al. Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010;49:671-82.
30. Terlinden R, Ossig J, Fliegert F, et al. Absorption, metabolism, and excretion of 14C-labeled tapentadol HCl in healthy male subjects. Eur J Drug Metab Pharmacokinet. 2007;32:163-9.
31. Pinn S. Tapentadol a 'realistic alternative' to strong opioids for severe pain. Br J Hosp Med (Lond). 2008;69:499.
32. Varrassi G, Marinangeli F, Piroli A, et al. Strong analgesics: working towards an optimal balance between efficacy and side effects. Eur J Pain. 2010;14:340-2.
33. Kögel B, De Vry J, Tzschentke TM, et al. The antinociceptive and antihyperalgesic effect of tapentadol is partially retained in OPRM1 (mu-opioid receptor) knockout mice. Neurosci Lett. 2011;491:104-7.
34. Hartrick CT, Rozek RJ. tapentadol in pain management: a mu-opioid receptor agonist and noradrenaline reuptake inhibitor. CNS Drugs. 2011;25:359-70.
35. Hussar DA. New Drugs2010, PART 1. Nursing. 2010;40:36,45; quiz 45-7.
36. Frampton JE. Tapentadol immediate release: a review of its use in the treatment of moderate to severe acute pain. Drugs. 2010;70:1719-43.
37. Tzschentke TM, Christoph T, Schröder W, et al. Tapentadol: with two mechanisms of action in one molecule effective against nociceptive and neuropathic pain : Preclinical overview. Schmerz. 2011;25:19-25.
38. 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;27:151-62.
39. 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 2010; s. d.
40. Kneip C, Terlinden R, Beier H, et al. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008;2:67-75.
41. Smit JW, Oh C, Rengelshausen J, et al. Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010;30:25-34.
42. Hartrick CT. Tapentadol immediate-release for acute pain. Expert Rev Neurother. 2010;10:861-9.
43. Gloth FM,3rd. Pharmacological management of persistent pain in older persons: focus on opioids and nonopioids. J Pain. 2011;12:S14-20.
44. Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010;32:675-703.
45. Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009;31:597-633.
46. Tomillero A, Moral MA. Gateways to clinical trials. December 2008. Methods Find Exp Clin Pharmacol. 2008;30:761-82.
47. Kleinert R, Lange C, Steup A, et al. Single dose analgesic efficacy of tapentadol in postsurgical dental pain: the results of a randomized, double-blind, placebocontrolled study. Anesth Analg. 2008;107:2048-55.
48. Vadivelu N, Mitra S, Narayan D. Recent advances in postoperative pain management. Yale J Biol Med. 2010;83:11-25.
49. Ngian GS, Guymer EK, Littlejohn GO. The use of opioids in fibromyalgia. Int J Rheum Dis. 2011;14:6-11.
50. Vorsanger G, Xiang J, Okamoto A, et al. Evaluation of study discontinuations with tapentadol inmmediate release and oxycodone immediate release in patients with low back or osteoarthritis pain. J Opioid Manag. 2010;6:169-79.
51. 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;11:1787-804.
52. Stegmann JU, Weber H, Steup A, et al. The efficacy and tolerability of multiple-dose tapentadol immediate release for the relief of acute pain following orthopedic (bunionectomy) surgery. Curr Med Res Opin. 2008;24:3185-96.
53. Hale M, Upmalis D, Okamoto A, et al. Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Curr Med Res Opin. 2009;25:1095-104.
54. Tzschentke TM, Christoph T, Schröder W, et al. Tapentadol: with two mechanisms of action in one molecule effective against nociceptive and neuropathic pain. Preclinical overview. Schmerz. 2011;25:19-25.
55. Hartrick C, Van Hove I, Stegmann JU, et al. Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary joint replacement surgery for end-stage joint disease: a 10-day, phase III, randomized, double- blind, active- and placebo-controlled study. Clin Ther. 2009;31:260-71.
56. Kwong WJ, Ozer-Stillman I, Miller JD, et al. Costeffectiveness analysis of tapentadol immediate release for the treatment of acute pain. Clin Ther. 2010;32:1768-81.
2. Uchitel OD, Di Guilmi MN, Urbano FJ, et al. Acute modulation of calcium currents and synaptic transmission by gabapentinoids. Channels (Austin). 2010;4:490-6.
3. Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009;31:2804-18.
4. Bee LA, Bannister K, Rahman W, et al. Mu-opioid and noradrenergic alpha(2)-adrenoceptor contributions to the effects of tapentadol on spinal electrophysiological measures of nociception in nerve-injured rats. Pain. 2011;152:131-9.
5. Camilleri M. Opioid-induced constipation: challenges and therapeutic opportunities. Am J Gastroenterol. 2011;106:835-42.
6. Rich JD, Green TC, McKenzie MS. Opioids and deaths. N Engl J Med. 2011;364:686.
7. Prommer EE. Tapentadol: an initial analysis. J Opioid Manag. 2010;6:223-6.
8. Jackson M, Dubose L. Pain medications: what you need to know. Todays FDA. 2010;22:60-3.
9. Hussar DA. New drugs: tapentadol hydrochloride, tolvaptan, and benzyl alcohol. J Am Pharm Assoc (2003). 2009;49:704-8.
10. Nossaman VE, Ramadhyani U, Kadowitz PJ, et al. Advances in perioperative pain management: use of medications with dual analgesic mechanisms, tramadol & tapentadol. Anesthesiol Clin. 2010;28:647-66.
11. Thompson CA. Tapentadol approved as pain reliever. Am J Health Syst Pharm. 2009;66:8.
12. Ravikumar K, Sridhar B, Pradhan N, et al. Four stereoisomers of the novel mu-opioid receptor agonist tapentadol hydrochloride. Acta Crystallogr C. 2011;67:o71-6.
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 mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007;323:265-76.
14. 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;14:814-21.
15. Guay DR. Is tapentadol an advance on tramadol? Consult Pharm. 2009;24:833-40.
16. Abasolo L, Carmona L. Systematic review: are major opioids effective in the treatment of musculoskeletal pain?. Med Clin (Barc). 2007;128:291-301.
17. Nelson T, Brett V. Tapentadol: an initial analysis-- follow-up. J Opioid Manag. 2011;7:87-8, 90-1; author reply 92.
18. Sloan P. Tapentadol for acute and chronic pain. Expert Opin Pharmacother. 2010;11:1783-5.
19. Tzschentke TM, Jahnel U, Kogel B, et al. Tapentadol hydrochloride: a next-generation, centrally acting analgesic with two mechanisms of action in a single molecule. Drugs Today (Barc). 2009;45:483-96.
20. Tapentadol (Nucynta)-a new analgesic. Med Lett Drugs Ther. 2009;51:61-2.
21. Kress HG. Tapentadol and its two mechanisms of action: is there a new pharmacological class of centrally- acting analgesics on the horizon? Eur J Pain. 2010;14:781-3.
22. Schroder W, Tzschentke TM, Terlinden R, et al. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia. J Pharmacol Exp Ther. 2011;337:312-20.
23. Guay DR. Oral hydromorphone extended-release. Consult Pharm. 2010;25:816-28.
24. 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, doubleblind, placebo- and active-controlled phase III study. Clin Drug Investig. 2010;30:489-505.
25. Fredheim OM, Borchgrevink PC, Nordstrand B, et al. Prescription of analgesics to patients in opioid maintenance therapy: A pharmacoepidemiological study. Drug Alcohol Depend. 2011. Epub ahead of print.
26. Terlinden R, Kogel BY, Englberger W, et al. In vitro and in vivo characterization of tapentadol metabolites. Methods Find Exp Clin Pharmacol. 2010;32:31-8.
27. Hersh EV, Golubic S, Moore PA. Analgesic update: tapentadol hydrochloride. Compend Contin Educ Dent. 2010;31:594-9.
28. Weichel C, Hecht B. Tapentadol. Opioid analgesic and norepinephrine reuptake inhibitors. Med Monatsschr Pharm. 2010;33:454-60.
29. Xu XS, Smit JW, Lin R, et al. Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010;49:671-82.
30. Terlinden R, Ossig J, Fliegert F, et al. Absorption, metabolism, and excretion of 14C-labeled tapentadol HCl in healthy male subjects. Eur J Drug Metab Pharmacokinet. 2007;32:163-9.
31. Pinn S. Tapentadol a 'realistic alternative' to strong opioids for severe pain. Br J Hosp Med (Lond). 2008;69:499.
32. Varrassi G, Marinangeli F, Piroli A, et al. Strong analgesics: working towards an optimal balance between efficacy and side effects. Eur J Pain. 2010;14:340-2.
33. Kögel B, De Vry J, Tzschentke TM, et al. The antinociceptive and antihyperalgesic effect of tapentadol is partially retained in OPRM1 (mu-opioid receptor) knockout mice. Neurosci Lett. 2011;491:104-7.
34. Hartrick CT, Rozek RJ. tapentadol in pain management: a mu-opioid receptor agonist and noradrenaline reuptake inhibitor. CNS Drugs. 2011;25:359-70.
35. Hussar DA. New Drugs2010, PART 1. Nursing. 2010;40:36,45; quiz 45-7.
36. Frampton JE. Tapentadol immediate release: a review of its use in the treatment of moderate to severe acute pain. Drugs. 2010;70:1719-43.
37. Tzschentke TM, Christoph T, Schröder W, et al. Tapentadol: with two mechanisms of action in one molecule effective against nociceptive and neuropathic pain : Preclinical overview. Schmerz. 2011;25:19-25.
38. 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;27:151-62.
39. 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 2010; s. d.
40. Kneip C, Terlinden R, Beier H, et al. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008;2:67-75.
41. Smit JW, Oh C, Rengelshausen J, et al. Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010;30:25-34.
42. Hartrick CT. Tapentadol immediate-release for acute pain. Expert Rev Neurother. 2010;10:861-9.
43. Gloth FM,3rd. Pharmacological management of persistent pain in older persons: focus on opioids and nonopioids. J Pain. 2011;12:S14-20.
44. Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010;32:675-703.
45. Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009;31:597-633.
46. Tomillero A, Moral MA. Gateways to clinical trials. December 2008. Methods Find Exp Clin Pharmacol. 2008;30:761-82.
47. Kleinert R, Lange C, Steup A, et al. Single dose analgesic efficacy of tapentadol in postsurgical dental pain: the results of a randomized, double-blind, placebocontrolled study. Anesth Analg. 2008;107:2048-55.
48. Vadivelu N, Mitra S, Narayan D. Recent advances in postoperative pain management. Yale J Biol Med. 2010;83:11-25.
49. Ngian GS, Guymer EK, Littlejohn GO. The use of opioids in fibromyalgia. Int J Rheum Dis. 2011;14:6-11.
50. Vorsanger G, Xiang J, Okamoto A, et al. Evaluation of study discontinuations with tapentadol inmmediate release and oxycodone immediate release in patients with low back or osteoarthritis pain. J Opioid Manag. 2010;6:169-79.
51. 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;11:1787-804.
52. Stegmann JU, Weber H, Steup A, et al. The efficacy and tolerability of multiple-dose tapentadol immediate release for the relief of acute pain following orthopedic (bunionectomy) surgery. Curr Med Res Opin. 2008;24:3185-96.
53. Hale M, Upmalis D, Okamoto A, et al. Tolerability of tapentadol immediate release in patients with lower back pain or osteoarthritis of the hip or knee over 90 days: a randomized, double-blind study. Curr Med Res Opin. 2009;25:1095-104.
54. Tzschentke TM, Christoph T, Schröder W, et al. Tapentadol: with two mechanisms of action in one molecule effective against nociceptive and neuropathic pain. Preclinical overview. Schmerz. 2011;25:19-25.
55. Hartrick C, Van Hove I, Stegmann JU, et al. Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary joint replacement surgery for end-stage joint disease: a 10-day, phase III, randomized, double- blind, active- and placebo-controlled study. Clin Ther. 2009;31:260-71.
56. Kwong WJ, Ozer-Stillman I, Miller JD, et al. Costeffectiveness analysis of tapentadol immediate release for the treatment of acute pain. Clin Ther. 2010;32:1768-81.
How to Cite
1.
Leotau Rodríguez MA. Tapentadol a New Therapeutic Option. Colomb. J. Anesthesiol. [Internet]. 2011 Jul. 1 [cited 2024 Apr. 29];39(3):375-8. Available from: https://www.revcolanest.com.co/index.php/rca/article/view/843
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2011-07-01
How to Cite
1.
Leotau Rodríguez MA. Tapentadol a New Therapeutic Option. Colomb. J. Anesthesiol. [Internet]. 2011 Jul. 1 [cited 2024 Apr. 29];39(3):375-8. Available from: https://www.revcolanest.com.co/index.php/rca/article/view/843
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Systematic review
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