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 Tapentadol

Tapentadol hydrochloride ER is an orally active, extended-release preparation of the hydrochloride salt of tapentadol with analgesic activity. Tapentadol is a synthetic, centrally acting analgesic with a dual mechanism of action involving mu-opioid receptor agonism and norepinephrine reuptake inhibition. This agent may be effective in the management of pain, cancer-related and other. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Tapentadol (trade name Nucynta, Palexia, In India - ZYNTAP)  is a centrally acting analgesic with a dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor. While its analgesic actions have been compared to tramadol and oxycodone, its general potency is somewhere between tramadol and morphine in effectiveness. Tapentadol is a new molecular entity that is structurally similar to Tramadol (Tramal). It has opioid and nonopioid acitivity in a single compound. In the US, Tapentadol is FDA approved for the treatment of moderate to severe acute pain. Due to the dual mechanism of action as an opioid agonist and norepinephrine reuptake inhibitor, there is potential for off label use in chronic pain. (source: http://en.wikipedia.org/wiki/Tapentadol).

Grunenthal (Achen, Germany) and Johnson & Johnson Pharmaceutical Research & Development (Raritan, NL)  are currently developing tapentadol hydrochloride (controlled release) for cancer pain.

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2: Etropolski M, Kelly K, Okamoto A, Rauschkolb C. Comparable efficacy and superior gastrointestinal tolerability (nausea, vomiting, constipation) of tapentadol compared with oxycodone hydrochloride. Adv Ther. 2011 May;28(5):401-17. Epub 2011 Apr 13. PubMed PMID: 21494892.

3: Guay DR. Oral hydromorphone extended-release. Consult Pharm. 2010 Dec;25(12):816-28. Review. PubMed PMID: 21172762.

4: Schwartz S, Etropolski M, Shapiro DY, Okamoto A, Lange R, Haeussler J, Rauschkolb C. 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 Jan;27(1):151-62. PubMed PMID: 21162697.

5: Schwartz S, Etropolski M, Shapiro DY, Okamoto A, Lange R, Haeussler J, Rauschkolb C. 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 Dec 2. [Epub ahead of print] PubMed PMID: 21126106.

6: Oh C, Rengelshausen J, Mangold B, Etropolski M, Rauschkolb C, Wang SS, Upmalis D, Häufel T. A thorough QT/QTc study of multiple doses of tapentadol immediate release in healthy subjects. Int J Clin Pharmacol Ther. 2010 Oct;48(10):678-87. PubMed PMID: 20875374.

7: Vorsanger G, Xiang J, Okamoto A, Upmalis D, Moskovitz B. Evaluation of study discontinuations with tapentadol inmmediate release and oxycodone immediate release in patients with low back or osteoarthritis pain. J Opioid Manag. 2010 May-Jun;6(3):169-79. PubMed PMID: 20642246.

8: Wild JE, Grond S, Kuperwasser B, Gilbert J, McCann B, Lange B, Steup A, Häufel T, Etropolski MS, Rauschkolb C, Lange R. Long-term safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Pain Pract. 2010 Sep-Oct;10(5):416-27. doi: 10.1111/j.1533-2500.2010.00397.x. PubMed PMID: 20602712.

9: Afilalo M, Etropolski MS, Kuperwasser B, Kelly K, Okamoto A, Van Hove I, Steup A, Lange B, Rauschkolb C, Haeussler J. 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. doi: 10.2165/11533440-000000000-00000. PubMed PMID: 20586515.

10: Buynak R, Shapiro DY, Okamoto A, Van Hove I, Rauschkolb C, Steup A, Lange B, Lange C, Etropolski M. 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 Aug;11(11):1787-804. Erratum in: Expert Opin Pharmacother. 2010 Nov;11(16):2773. PubMed PMID: 20578811.

11: Lange B, Kuperwasser B, Okamoto A, Steup A, Häufel T, Ashworth J, Etropolski M. Efficacy and safety of tapentadol prolonged release for chronic osteoarthritis pain and low back pain. Adv Ther. 2010 Jun;27(6):381-99. Epub 2010 Jun 11. Erratum in: Adv Ther. 2010 Dec;27(12):981. PubMed PMID: 20556560.

12: Vadivelu N, Mitra S, Narayan D. Recent advances in postoperative pain management. Yale J Biol Med. 2010 Mar;83(1):11-25. Review. PubMed PMID: 20351978; PubMed Central PMCID: PMC2844689.

13: Etropolski MS, Okamoto A, Shapiro DY, Rauschkolb C. Dose conversion between tapentadol immediate and extended release for low back pain. Pain Physician. 2010 Jan-Feb;13(1):61-70. PubMed PMID: 20119464.

14: Smit JW, Oh C, Rengelshausen J, Terlinden R, Ravenstijn PG, Wang SS, Upmalis D, Mangold B. Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010 Jan;30(1):25-34. PubMed PMID: 20030470.

15: Daniels S, Casson E, Stegmann JU, Oh C, Okamoto A, Rauschkolb C, Upmalis D. A randomized, double-blind, placebo-controlled phase 3 study of the relative efficacy and tolerability of tapentadol IR and oxycodone IR for acute pain. Curr Med Res Opin. 2009 Jun;25(6):1551-61. Erratum in: Curr Med Res Opin. 2009 Jun;25(6):1561. Dosage error in article text. PubMed PMID: 19445652.

16: Hartrick C, Van Hove I, Stegmann JU, Oh C, Upmalis D. 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 Feb;31(2):260-71. PubMed PMID: 19302899.

17: Hale M, Upmalis D, Okamoto A, Lange C, Rauschkolb C. 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 May;25(5):1095-104. PubMed PMID: 19301989.

18: Daniels SE, Upmalis D, Okamoto A, Lange C, Häeussler J. A randomized, double-blind, phase III study comparing multiple doses of tapentadol IR, oxycodone IR, and placebo for postoperative (bunionectomy) pain. Curr Med Res Opin. 2009 Mar;25(3):765-76. PubMed PMID: 19203298.

19: Stegmann JU, Weber H, Steup A, Okamoto A, Upmalis D, Daniels S. 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 Nov;24(11):3185-96. Epub 2008 Oct 15. PubMed PMID: 18851776.