Tapentadol hydrochloride: A centrally acting oral analgesic

Clinical Therapeutics

Volumn 31, Issue 12, 2009, Pages 2804-2818

  Wade, William E ^a   Spruill, William J ^a  

^a UNIVERSITY OF GEORGIA   (United States)

Author keywords

acute pain; analgesic; norepinephrine reuptake inhibitor; opioid receptor agonist; tapentadol hydrochloride

Indexed keywords

GABAPENTIN; IBUPROFEN; MORPHINE; MORPHINE SULFATE; MU OPIATE RECEPTOR; NORADRENALIN UPTAKE INHIBITOR; OMEPRAZOLE; OXYCODONE; PLACEBO; TAPENTADOL; TRAMADOL;

ANALGESIC ACTIVITY; ANTINOCICEPTION; AREA UNDER THE CURVE; ARTICLE; BUNIONECTOMY; CHRONIC PAIN; CLINICAL TRIAL; CONSTIPATION; CONTROLLED RELEASE FORMULATION; DIARRHEA; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG COST; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG EXCRETION; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG OVERDOSE; DRUG RECEPTOR BINDING; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; GASTROINTESTINAL SYMPTOM; HEAT SENSATION; HIP OSTEOARTHRITIS; HIP PAIN; HUMAN; HYPERHIDROSIS; KNEE OSTEOARTHRITIS; KNEE PAIN; LOW BACK PAIN; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NEUROPATHIC PAIN; NONHUMAN; OFF LABEL DRUG USE; PAIN; PAIN ASSESSMENT; PLASMA CONCENTRATION-TIME CURVE; PLASMA PROTEIN BINDING; POSTOPERATIVE PAIN; PRURITUS; RECOMMENDED DRUG DOSE; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; TIME TO MAXIMUM PLASMA CONCENTRATION; TOOTH EXTRACTION; TOOTH PAIN; VERTIGO; VISCERAL PAIN; VOMITING; XEROSTOMIA;

ACUTE DISEASE; ADMINISTRATION, ORAL; ADRENERGIC UPTAKE INHIBITORS; ANALGESICS; ANIMALS; CLINICAL TRIALS AS TOPIC; DRUG INTERACTIONS; HUMANS; PAIN; PAIN MEASUREMENT; PHENOLS; RECEPTORS, OPIOID, MU; SEVERITY OF ILLNESS INDEX; TREATMENT OUTCOME;

EID: 74549207680     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2009.12.003     Document Type: Article

References (65)

1. Tzschentke T.M., De Vry J., Terlinden R., et al. Tapentadol hydrochloride: Analgesic mu-opioid receptor agonist noradrenaline reuptake inhibitor. Drugs Future 31 (2006) 1053-1061
2. Tzschentke T.M., 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 Exper Ther. 323 (2007) 265-276
3. Tzschentke T.M., De Vry J., Christoph T., et al. Tapentadol, a novel centrally acting analgesic: Preclinical evidence for a dual mode of action underlying its broad efficacy profile. Eur J Pain. 10 Suppl 1 (2006) S54 Abstract 196.
4. Tzschentke T., De Vry J., Christoph T., et al. Tapentadol HCl: In vitro and in vivo studies on the dual mechanism of action underlying its broad analgesic profile. J Pain. 7 Suppl 1 (2006) S25 Abstract 686.
5. Tzschentke T., De Vry J., Christoph T., et al. Tapentadol: Preclinical evidence for a dual mode of action. Poster presented at: 18th Annual Clinical Meeting of the American Academy of Pain Management. Las Vegas, Nev (September 27-30, 2007)
6. Tzschentke T.M., De Vry J., Christoph T., et al. Tapentadol, a novel centrally acting analgesic: Preclinical evidence for a dual mode of action underlying its broad efficacy profile. Poster presented at: 3rd International Forum on Pain Medicine. Montreal, Canada (June 28-July 1, 2007)
7. Tzschentke T.M., De Vry J., Christoph T., et al. Tapentadol HCl: In vitro and in vivo studies on the dual mechanism of action underlying its broad analgesic profile. Presented at: 23rd Annual Meeting of the American Academy of Pain Medicine. New Orleans, La. (February 7-10, 2007)
8. Bahrenberg G., De Vry J., Christoph T., et al. Evidence for a combined mode of action underlying the broad efficacy profile of tapentadol, a novel centrally acting analgesic. J Pain. 9 Suppl 2 (2008) 31 Abstract 223.
9. Bahrenberg G., De Vry J., Christoph T., et al. Evidence for a combined mode of action underlying the broad efficacy profile of tapentadol, a novel centrally acting analgesic. Poster presented at: 37th Annual Meeting of the Society for Neuroscience. San Diego, Calif. (November 3-7, 2007)
10. Tzschentke T., De Vry J., Christoph T., et al. Tapentadol HCl: Analgesic profile of a novel centrally active analgesic with a dual mode of action in animal models of nociception, inflammatory, and neuropathic pain. J Pain. 7 Suppl 1 (2006) S26 Abstract 687.
11. Tzschentke T., Christoph T., Meen M., et al. Efficacy profile of tapentadol, a novel centrally active analgesic with a combined mode of action, in animal pain models. Abstract presented at: 37th Annual Meeting of the Society for Neuroscience. San Diego, Calif. (November 3-7, 2007)
12. Tzschentke T., Christoph T., Méen M., et al. Efficacy profile of tapentadol, a novel centrally active analgesic with a combined mode of action, in animal pain models. J Pain. 9 Suppl 2 (2008) 32 Abstract 227.
13. De Vry J., Tzschentke T.M., Christoph T., et al. Tapentadol: Efficacy profile of a novel centrally active analgesic with a dual mode of action in animal pain models. Eur J Pain. 10 Suppl 1 (2006) S62 Abstract 230.
14. Christoph T., Meen M., De Vry J., and Tzschentke T.M. Efficacy of tapentadol, a novel centrally acting analgesic with dual mode of action, in animal models of chronic neuropathic pain. Eur J Pain. 11 Suppl 1 (2007) 61 Abstract 140.
15. Christoph T., Meen M., De Vry J., and Tzschentke T.M. Efficacy of tapentadol, a novel centrally acting analgesic with dual mode of action, in animal models of chronic neuropathic pain. Poster presented at: 60th Annual Meeting of the American Academy of Neurology. Chicago, Ill (April 12-19, 2008)
16. Christoph T., Meen M., De Vry J., et al. Tapentadol: Efficacy in animal models of neuropathic pain. Poster presented at: 18th Annual Clinical Meeting of the American Academy of Pain Management. Las Vegas, Nev. (September 27-30, 2007)
17. Schiene K., Kogel B., Tzschentke T., et al. Efficacy of tapentadol, a novel centrally active analgesic with a dual mode of action, in animal models of visceral pain. Pain Practice. 7 Suppl 1 (2007) 23 Abstract
18. Schiene K., Kogel B., Tzschentke T., et al. Efficacy of tapentadol, a novel centrally acting analgesic with a dual mode of action, in animal models of visceral pain. Poster presented at: 60th Annual Meeting of the American Academy of Neurology. Chicago, Ill. (April 12-19, 2008)
19. Schiene K., Kogel B., Tzschentke T., et al. Efficacy of tapentadol, a novel centrally active analgesic with a dual mode of action, in animal models of visceral pain. Poster presented at: 24th Annual Meeting of the American Academy of Pain Medicine. Orlando, Fla. (February 12-16, 2008)
20. Terlinden R., Ossig J., Fliegert F., and Gohler K. Pharmacokinetics, excretion, and metabolism of tapentadol HCl, a novel centrally acting analgesic, in healthy subjects. J Pain. 7 Suppl 1 (2006) S26 Abstract 689.
21. Terlinden R., Ossig J., Fliegert F., et al. Tapentadol: Pharmacokinetics, excretion, and metabolism. Poster presented at: 18th Annual Clinical Meeting of the American Academy of Pain Management. Las Vegas, Nev. (September 27-30, 2007)
22. Terlinden R., Ossig J., Fliegert F., et al. Pharmacokinetics, excretion and metabolism of tapentadol HCl, a novel centrally acting analgesic in healthy subjects. Poster presented at: 23rd Annual Meeting of the American Academy of Pain Medicine. New Orleans, La. (February 7-10, 2007)
23. 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. 32 (2007) 163-169
24. Mangold B., Oh C., Jager D., et al. The pharmacokinetics of tapentadol are not affected by omeprazole: Results of a 2-way crossover drug-interaction study in healthy subjects. Pain Practice 7 Suppl 1 (2007) 55 Abstract
25. Mangold B., Oh C., Jager D., et al. The pharmacokinetics of tapentadol are not affected by omeprazole: Results of a 2-way crossover druginteraction study in healthy subjects. Poster presented at: 24th Annual Meeting of the American Academy of Pain Medicine. Orlando, Fla. (February 12-16, 2007)
26. Kneip C., Terlinden R., Beier H., and Chen G. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett 2 (2008) 67-75
27. Kneip C., Terlinden R., Chen G., et al. Evaluation of the inhibitory potential of tapentadol on the activities of CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4. Ann Rheum Dis. 66 Suppl 2 (2007) i Abstract
28. Kneip C., Terlinden R., Chen G., et al. Evaluation of the induction potential of tapentadol on the activities of CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4. Ann Rheum Dis. 66 Suppl 2 (2007) 618 Abstract
29. 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, placebo-controlled study. Anesth Analg. 107 (2008) 2048-2055
30. Kleinert R., Hallmann C., Steup A., et al. Efficacy of a single dose of tapentadol HCl for analgesia after third molar surgery. J Pain. 7 Suppl 1 (2006) S44 Abstract 773
31. Kleinert R., Steup A., Black P., et al. Tapentadol: Efficacy in a postsurgical pain model. Poster presented at: 18th Annual Clinical Meeting of the American Academy of Pain Management. Las Vegas, Nev. (September 27-30, 2007)
32. Kleinert R., Hallmann C., Steup A., et al. Efficacy of a single dose of tapentadol HCl for analgesia after third molar surgery. Poster presented at: 23rd Annual Meeting of the American Academy of Pain Medicine. New Orleans, La. (February 7-10, 2007)
33. Lange C., Steup A., Black P., and Desjardins P. Rapid pain relief after bunionectomy with tapentadol, a novel centrally acting analgesic. Eur J Pain 10 Suppl 1 (2006) S165 Abstract 629
34. Lange C., Steup A., Black P., and Desiardins P. Analgesic efficacy and tolerability of tapentadol, a new centrally acting analgesic, following bunionectomy. Poster presented at: 8th European Federation of National Associations of Orthopaedics and Traumatology Congress. Florence, Italy (May 11-15, 2007)
35. Stegmann J.U., Engels C., Steup A., et al. Tapentadol, a novel centrally acting analgesic with a dual mode of action: Efficacy and safety in clinical acute pain models. Eur J Pain 10 Suppl 1 (2006) S167 Abstract 639
36. Stegmann J., Engels C., Steup A., et al. Tapentadol, a novel centrally acting analgesic with a dual mode of action: Efficacy and safety in clinical acute pain models. Poster presented at: Third International Forum on Pain Medicine. Montreal, Canada (June 28-July 1, 2007)
37. Stegmann J.U., 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. 24 (2008) 3185-3196
38. Stegmann J., Weber H., Steup A., et al. Tapentadol: Efficacy using a bunionectomy pain model. Poster presented at: 18th Annual Clinical Meeting of the American Academy of Pain Management. Las Vegas, Nev. (September 27-30, 2007)
39. Stegmann J., Weber H., Steup A., et al. The efficacy and tolerability of tapentadol immediate release for the treatment of acute pain following bunionectomy. Pain Practice 7 Suppl 1 (2007) 84 Abstract
40. Stegmann J., Weber H., Steup A., et al. The efficacy and tolerability of tapentadol immediate release for the treatment of acute pain following bunionectomy. Poster presented at: 24th Annual Meeting of the American Academy of Pain Medicine. Orlando, Fla. (February 12-16, 2008)
41. Weber H., Stegmann J., and Upmalis D. Tapentadol immediate release for the relief of acute pain following orthopedic surgery of the forefoot: Efficacy and tolerability results from a randomized, double blind, phase II study. Eur J Anaesthesiol 25 Suppl 44 (2008) 14AP11-3. Abstract
42. Weber H., Hallmann C., Steup A., et al. Efficacy and safety of tapentadol HCl in patients with pain after bunionectomy. J Pain 7 Suppl 1 (2006) S3 Abstract 312/776
43. 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. 25 (2009) 1095-1104
44. Oh C., Upmalis D., Okamoto A., and Stegmann J. Flexible use of tapentadol immediate release for 90 days for the treatment of low back pain and osteoarthritis pain: A safety study. Ann Rheum Dis. 67 Suppl 2 (2008) 389 Abstract FRI0335
45. Upmalis D., Okamoto A., Oh C., et al. Symptoms of opioid withdrawal after discontinuation of tapentadol immediate release, an analgesic with mu-opioid receptor agonism. J Pain 9 Suppl 1 (2008) 29 Abstract 214
46. Hartrick C., Van Hove I., Stegmann J.U., et al. Efficacy and tolerability of tapentadol immediate release and oxycodone HCl immediate release in patients awaiting primary ioint replacement surgery for end-stage ioint disease: A 10-day, phase III, randomized, double-blind, active-and placebo-controlled study. Clin Ther. 31 (2009) 260-271
47. Hartrick C., Okamoto A., Oh C., et al. Analgesic efficacy of tapentadol immediate release in patients with pain from end stage joint disease. J Pain 9 Suppl 2 (2008) 31 Abstract 222
48. Afilalo M., Oh C., Okamoto A., et al. Tapentadol immediate release compared with oxycodone immediate release for the relief of moderateto-severe pain in patients with end stage ioint disease. J Pain 9 Suppl 2 (2008) 32 Abstract 224
49. Upmalis D., Okamoto A., Oh C., et al. Tapentadol immediate release provides effective pain relief in patients with end-stage disease of the hip or knee. Poster presented at: 12th World Congress on Pain. Glasgow, Scotland (August 17-22, 2008)
50. Upmalis D., Okamoto A., Oh C., et al. Efficacy and tolerability data supporting the use of tapentadol immediate release for the relief of pain from end-stage ioint disease. Ann Rheum Dis. 67 Suppl 2 (2008) 632 Abstract AB0744
51. Haeussler J., Oh C., Okamoto A., et al. Efficacy and tolerability of ta- pentadol immediate release: Pain relief in patients with end-stage joint disease. Poster presented at: 12th World Congress on Pain. Glasgow, Scotland (August 17-22, 2008)
52. Rauschkolb-Loeffler C., Okamoto A., Steup A., and Lange C. Efficacy and tolerability of tapentadol for relief of moderate-to-severe chronic pain due to osteoarthritis of the knee. Ann Rheum Dis. 66 Suppl 2 (2007) 507 Abstract
53. Rauschkolb-Loeffler C., Okamoto A., Steup A., and Lange C. Efficacy and tolerability of tapentadol for relief of moderate-to-severe chronic pain due to osteoarthritis of the knee. Poster presented at: 60th Annual Meeting of the American Academy of Neurology. Chicago, Ill. (April 12-19, 2008)
54. Rauschkolb-Loeffler C., Oh C., Upmalis D., et al. Safety and efficacy of tapentadol IR over 90 days for relief of low back pain or osteoporosis pain. Poster presented at: 12th World Congress on Pain of the International Association for the Study of Pain. Glasgow, Scotland (August 12-17, 2008)
55. Okamoto A., Upmalis D., Oh C., and Stegmann J. Safety and tolerability of tapentadol IR for opioid experienced and non-experienced patient populations after 90 days of exposure in patients with low back pain or osteoporosis pain. Poster presented at: 12th World Congress on Pain of the International Association for the Study of Pain. Glasgow, Scotland (August 12-17, 2008)
56. Rauschkolb-Loeffler C., Okamoto A., Steup A., and Lange C. Tapentadol extended release (ER) for the relief of moderate-to-severe chronic pain due to osteoarthritis of the knee. Pain Practice 7 Suppl 1 (2007) 55 Abstract
57. Rauschkolb-Loeffler C., Okamoto A., Steup A., and Lange C. Tapentadol extended release (ER) for management of moderate-to-severe chronic pain due to osteoarthritis of the knee. Poster presented at: 24th An- nual Meeting of the American Academy of Pain Medicine. Orlando, Fla. (February 12-16, 2008)
58. Rauschkolb-Loeffler C., Oh C., Steup A., and Lange C. Tapentadol extended release (ER) is effective for the relief of chronic pain due to osteoarthritis (OA) of the knee. Arthritis Rheum 56 Suppl S (2007) S660 Abstract
59. Lange C., Upmalis D., Okamoto A., and Ma Y. Relief of acute pain following orthopedic surgery: Efficacy and tolerability of tapentadol immediate release in a randomized, double blind, phase III study. Eur J Anaesthesiol 25 Suppl 44 (2008) 14AP11-5. Abstract
60. Oh C., Upmalis D., Okamoto A., et al. Efficacy of tapentadol immediate release in patients with pain after bunionectomy. J Pain 9 Suppl 2 (2008) 33 Abstract 229
61. Upmalis D., Okamoto A., Oh C., et al. Safety and tolerability of tapentadol immediate release in patients with pain after bunionectomy. Poster presented at: Annual Meeting of the American Podiatric Medical Association. Honolulu, Hawaii (July 24-27, 2008)
62. Oh C., Okamoto A., Ma Y., and Lange C. Effective relief of acute pain following orthopedic surgery: Efficacy and tolerability of tapentadol immediate release in a randomized, doubleblind, placebo-controlled, phase III study. Poster presented at: 12th World Congress on Pain of the International Association for the Study of Pain. Glasgow, Scotland (August 17-22, 2008)
63. Gottlieb I., Oh C., Upmalis D., et al. Efficacy of tapentadol immediate release in patients with pain after bunionectomy. Poster presented at: Annual Meeting of the American Podiatric Medical Association. Honolulu, Hawaii (July 24-27, 2008)
64. Upmalis D., Okamoto A., Ma Y., et al. Tapentadol immediate release provides effective acute pain relief following bunionectomy surgery in a randomized, double-blind, active-and placebo-controlled phase III study. Poster presented at: 33rd Annual Regional Anesthesia Meeting and Workshops. Playa Del Carmen, Mexico (May 1-4, 2008)
65. NUCYNTA (tapentadol hydrochloride) tablet, film coated [Ortho-McNeil-Janssen Pharmaceuticals, Inc.]. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10273 Accessed October 2, 2009