Extended-release formulations of tramadol in the treatment of chronic pain

Expert Opinion on Pharmacotherapy

Volumn 12, Issue 11, 2011, Pages 1757-1768

  Pergolizzi Jr , Joseph V ^a,b,c   Taylor Jr , Robert ^c   Raffa, Robert B ^d  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b GEORGETOWN UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c NEMA Research   (United States)

^d TEMPLE UNIVERSITY   (United States)

Author keywords

Analgesia; Extended release formulation; Pain; Pain management; Tramadol; Tramadol extended release

Indexed keywords

'TRAVEL'; ALCOHOL; AMITRIPTYLINE; ANTIDEPRESSANT AGENT; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE; BUPRENORPHINE; CLOPIDOGREL; CODEINE; CYTOCHROME P450 2D6; DICLOFENAC; DIHYDROCODEINE; METHADONE; METOCLOPRAMIDE; MONOALGIC; MONOAMINE OXIDASE INHIBITOR; MONOTRAMAL; NALOXONE; NOAX; NONSTEROID ANTIINFLAMMATORY AGENT; PHENYTOIN; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR; SEROTONIN UPTAKE INHIBITOR; TACROLIMUS; TIPAROL; TIPAROL RETARD; TRADOREC; TRAMADOL; TRAMADOL CONTRAMID; TRAMADOLOR; TRAMAL RETARD; TRICYCLIC ANTIDEPRESSANT AGENT; TRIPTAN DERIVATIVE; UNCLASSIFIED DRUG; UNITRAMA; WARFARIN; ZYTRAM;

ANALGESIC ACTIVITY; CANCER PAIN; CENTRAL NERVOUS SYSTEM DISEASE; CHRONIC PAIN; CONSTIPATION; CONTROLLED DRUG RELEASE; DISEASE SEVERITY; DIZZINESS; DRUG ALCOHOL INTERACTION; DRUG COATING; DRUG EFFICACY; DRUG FORMULATION; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; EXTENDED DRUG RELEASE; FIBROMYALGIA; FLUSHING; GENETIC POLYMORPHISM; GERIATRIC PATIENT; HEMODYNAMIC PARAMETERS; HUMAN; LOW DRUG DOSE; NARCOTIC DEPENDENCE; NAUSEA; NEUROPATHIC PAIN; NONHUMAN; OSTEOARTHRITIS; PAIN ASSESSMENT; PHANTOM PAIN; PHARMACOGENETICS; PRURITUS; RECOMMENDED DRUG DOSE; RESPIRATION DEPRESSION; REVIEW; SEIZURE; SEROTONIN SYNDROME; SIDE EFFECT; SLEEP QUALITY; SOMNOLENCE; TABLET COMPRESSION; VOMITING; XEROSTOMIA;

ANALGESICS, OPIOID; ANIMALS; CHRONIC DISEASE; DELAYED-ACTION PREPARATIONS; HUMANS; MEDICATION ADHERENCE; PAIN; TRAMADOL;

EID: 79960234767     PISSN: 14656566     EISSN: 17447666     Source Type: Journal    
DOI: 10.1517/14656566.2011.576250     Document Type: Review

References (95)

1. Claxon A, Cramer J, Pierce C. A systematic review of the associations between dose regimens and medication compliance. Clin Ther 2001;23:1296-301
2. Richter A, Anton S, Koch P, Dennett S. The impact of reducing dose frequency on health outcomes. Clin Ther 2003;25:2307-35 (Pubitemid 37076322)
3. Altman RD, Hochberg MC, Moskowitz RW, Schnitzer TJ. Recommendations for the medical management of osteoarthritis of the hip and knee: 2000 update. American College of Rheumatology Subcommittee on Osteoarthritis Guidelines. Athritis Rheum 2000;43:1905-15
4. Mongin G. Tramadol extended-release formulations in the management of pain due to osteoarthritis. Expert Rev Neurother 2007;7:1775-84 (Pubitemid 350260673)
5. Zehr L. Cipher gets U.S. patent for tramadol. 2010. Available from: http:// biotuesday.ca/2010/10/07/ciphergets- u-s-patent-for-tramadol/. [Last accessed 17 January 2010]
6. Zhang W, Doherty M, Leeb B, et al. EULAR evidence based recommendations for the management of hand osteoarthritis: report of a task force of the EULAR Standing Committee for International Clinical Studies including Therapeutics (ESCISIT). Ann Rheum Dis 2007;66:377-88 (Pubitemid 46579641)
7. Zhang W, Doherty M, Arden N, et al. EULAR evidence based recommendations for the management of hip osteoarthritis: report of a task force of the EULAR Standing Committee for Inerantional Clinical Studies including Therapuetics (ESCISIT). Ann Rheum Dis 2005;64:669-81 (Pubitemid 40559291)
8. Chou R, Qasseem A, Snow V, et al. Diagnosis and treatment of low back pain: a joint clinical practice guideline from the American College of Physicians and the American Pain Society. Ann Intern Med 2007;147:478-91 (Pubitemid 351688341)
9. Airaksinen O, Brox J, Cedraschi C, et al. European guidelines for the management of chronic nonspecifc low back pain. Eur Spine J 2006;15(Suppl 2):S192-300
10. Dworkin R, OConnor A, Backonja M, et al. Pharmacological management of neuropathic pain: evidence-based recommendations. Pain 2007;132:237-51 (Pubitemid 350051570)
11. Buckhardt C, Goldenberg D, Crofford L, et al. Guideline for the management of fibromyalgia syndrome pain in adults and children. Guidelines 2005. Available from: http://www.guidelines.gov/content. aspx?id=14869. [Last accessed 26 January 2011]
12. Carville S, Arendt-Nielsen S, Bliddal H, et al. EULAR evidence-based recommendations for the management of fibromyalgia syndrome. Ann Rheum Dis 2008;67:536-41 (Pubitemid 351498437)
13. Grond S, Sablotzki A. Clinical pharmacology of tramadol. Clin Pharmacokinet 2005;43:879-923 (Pubitemid 39447033)
14. Lee C, McTavish D, Sorkin E. Tramadol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute and chronic pain states. Drugs 1993;46:313-40 (Pubitemid 23244649)
15. Mattia C, Coluzzi F. Once-daily tramadol in rheumatological pain. Expert Opin Pharmacother 2006;7:1811-23
16. Mongin G, Yakusevich V, Kope A, et al. Efficacy and safety assessment of a novel once-daily tablet formulation of tramadol: a randomised, controlled study versus twice-daily tramadol in patients with osteoarthritis of the knee. Clin Drug Investig 2004;24:545-8
17. Adler L, McDonald C, OBrien C, Wilson M. A comparison of once-daily tramadol with normal release tramadol in the treatment of pain in osteoarthritis. J Rheumatol 2002;29:2196-9
18. Bodalia B, McDonald C, Smith K, et al. A comparison of the pharmacokinetics, clinical efficacy, and tolerability of once-daily tramadol tablets with normal release tramadol capsules. J Pain Symptom Manage 2003;25:142-9 (Pubitemid 36183292)
19. Beaulieu A, Peloso P, Bensen W, et al. A randomized, double-blind, 8-week crossover study of once-daily controlledrelease tramadol versus immediate-release tramadol taken as needed for chronic noncancer pain. Clin Ther 2007;29:49-60 (Pubitemid 46414025)
20. Raffa R, Friderichs E, Reimann W, et al. Complementary and synergistic antinociceptive interaction between the enantiomers of tramadol. J Pharmacol Exp Ther 1993;267:331-40 (Pubitemid 23325025)
21. Raffa R, Pergolizzi J, Tallarida R. The determination and application of fixed-dose analgesic combinations for treating multimodal pain. J Pain 2010;11:701-9
22. Ide S, Minami M, Ishihara K, et al. Mu opioid receptor-dependent and independent components in effects of tramadol. Neuropharmacol 2006;51:651-8 (Pubitemid 44215970)
23. Raffa R, Friderichs E, Reimann W, et al. Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an atypical opioid analgesic. J Pharmacol Exp Ther 1992;260:275-84
24. Friderichs E, Reimann W, Selve N. Contribution of both enantiomers to antinociception of the centrally acting analgesic tramadol. Naunyn Schmiedebergs Arch Pharmacol 1992;346(Suppl 1):R36
25. Gillen C, Haurand M, Kobelt D, Wendt S. Affinity, potency and efficacy of tramadol and its metabolites at the cloned human mu-opioid receptor. Naunyn Schmiedebergs Arch Pharmacol 2000;362:116-21 (Pubitemid 30640039)
26. Wu W, McKown L, Liao S. Metabolism of the analgesic drug ULTRAM (tramadol hydrochloride) in humans: API-MS and MS/MS characterization of metabolites. Xenobiotica 2002;32:411-25 (Pubitemid 34620945)
27. Hennies H-H, Friderichs E, Schneider J. Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids. Arzneim Forsch 1988;38:877-80
28. Lai J, Ma S-W, Porreca F, Raffa R. Tramadol, M1 metabolite and enantiomer affinities for cloned human opioid receptors expressed in transfected HN9.10 neuroblastoma cells. Eur J Pharmacol 1996;316:369-72 (Pubitemid 27008172)
29. Codd E, Shank R, Schupsky J, Raffa R. Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception. J Pharmacol Exp Ther 1995;274:1263-70
30. Driessen B, Reimann W. Effects of tramadol on noradrenaline release from rat brain cortex slices. Naunyn Schmiedebergs Arch Pharmacol 1989;339(Suppl):R89
31. Friderichs E, Reimann W, Selve N. Investigations on opioid and non-opioid components in tramadol antinociception. Naunyn Schmiedebergs Arch Pharmacol 1991;344(Suppl 1):R72
32. Driessen B, Reimann W. Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro. Br J Pharmacol 1992;105:147-51
33. Kayser V, Besson J-M, Guilbaud G. Evidence for a noradrenergic component in the antinociceptive effect of the analgesic agent tramadol in an animal model of clinical pain, the arthritic rat. Eur J Pharmacol 1992;224:83-8
34. Sora I, Takahashi N, Funada M, et al. Opiate receptor knockout mice define mu receptor roles in endogenous nociceptive responses and morphine-induced analgesia. Proc Natl Acad Sci USA 1997;94:1544-9 (Pubitemid 27087888)
35. Collart L, Luthy C, Dayer P. Multimodal analgesic effect of tramadol. Annual meeting of the American Society of Clinical Pharmacology and Therapeutics, Honolulu, March 1993. Clin Pharmacol Ther 1993;53:223
36. Yanarates O, Dogrul A, Yildirim V, et al. Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, O-Desmethyltramadol, via activation of descending serotonergic pathways. Anesthesiology 2010;112:696-710
37. Desmeules J, Piguet V, Collart L, Dayer P. Contribution of monoaminergic modulation to the analgesic effect of tramadol. Br J Clin Pharmacol 1996;41:7-12 (Pubitemid 26009905)
38. Christoph T, Kogel B, Strassburger W, Schug S. Tramadol has a better potency ratio relative to morphine in neuropathic than in nociceptive pain models. Drugs R D 2007;8:51-7 (Pubitemid 46191807)
39. Stamer U, Musshoff F, Kobilay M, et al. Concentrations of tramadol and O-desmethyltramadol enantiomers in different CYP2D6 genotypes. Clin Pharmacol Ther 2007;82:41-7 (Pubitemid 46944194)
40. Stamer U, Stuber F, Muders T, Musshoff F. Respiratory depression with tramadol in a patient with renal impairment and CYP2D6 gene duplication. Anesth Analg 2008;107:926-9
41. Kleine-Brueggeney M, Musshoff F, Stuber F, Stamer U. Pharmacogenetics in palliative care. Forensic Sci Intern 2010;203:63-70
42. Johansson I, Ingelman-Sundberg M. Genetic polymorphisms and toxicology - with emphasis on cytochrome P450. Toxicol Sci Advance 2010;120(1):1-13
43. Kim E, Choi C-B, Kang C, Bae S-C. Adverse events in analgesic treatment with tramadol associated with CYP2D6 extensive-metaboliser and OPRM1 high-expression variants. Ann Rheum Dis 2010;69:1889-90
44. Roth S. Efficacy and safety of tramadol HCl in breakthrough musculoskeletal pain attributed to osteoarthritis. J Rheumatol 1998;25:1358-63 (Pubitemid 28312355)
45. Bird H, Hill J, Stratford M, et al. A double-blind cross-over study comparing the analgesic efficacy of tramadol with pentazocine in patients with osteoarthritis. J Drug Dev Clin Pract 1995;7:181-8
46. Jensen E, Ginsberg F. Tramadol versus dextropropoxyphene in the treatment of osteoarthritis. A short term double-blind study. Drug Invest 1994;8:211-18 (Pubitemid 24319459)
47. Katz W. Pharmacology and clinical experience with tramadol in osteoarthritis. Drugs 1996;52(Suppl 3):39-47 (Pubitemid 26366543)
48. Schnitzer T, Kamin M, Olson W. Tramadol allows reduction of naproxen dose among patients with naproxen-responsive osteoarthritis pain: a randomized, double-blind, placebo-controlled study. Athritis Rheum 1999;42:1370-7 (Pubitemid 30265594)
49. Wilder-Smith C, Schimke J, Osterwalder B, Senn H-J. Oral tramadol, a mu-opioid agonist and monoamine reuptake-blocker, and morphine for strong cancer-related pain. Ann Oncol 1994;5:141-6
50. Russell I, Kamin M, Bennett R, et al. Efficacy of tramadol in treatment of pain in fibromyalgia. J Clin Rheumatol 2000;6:250-7
51. Schnitzer T, Gray W, Paster R, Kamin M. Efficacy of tramadol in treatment of chronic low back pain. J Rheumatol 2000;27:772-8 (Pubitemid 30151361)
52. Hair P, Curran M, Keam S. Tramadol extended-release tablets in moderate to moderately severe chronic pain in adults: profile report. CNS Drugs 2007;21:259-63 (Pubitemid 46425630)
53. Contramid. Labopharm 2011. Available from: http://www.labopharm.com/ default.aspx?id=31. [Last accessed 26 January 2011]
54. CIP Tramadol ER. 2011. Available from:http://www.cipherpharma.com/ products/cip-tramadol-er/. [Last accessed 26 January 2011]
55. Rosenberg M. The role of tramadol ER in the treatment of chronic pain. Int J Clin Pract 2009;53:1531-43
56. Smith B, Torrance N, Bennett M, Lee A. Health and quality of life associated with chronic pain of predominantly neuropathic origin in the community. Clin J Pain 2007;23:143-9 (Pubitemid 46145461)
57. Bouhassira D, Lanteri-Minet M, Attal N, et al. Prevalence of chronic pain with neuropathic characteristics in the general population. Pain 2008;136:380-7 (Pubitemid 351680253)
58. Attal N, Cruccu G, Haanpaa M, et al. EFNS guidelines on pharmacological treatment of neuropathic pain. Eur J Neurol 2006;13:1153-69 (Pubitemid 44581463)
59. Ho T, Backonja M, Ma J, et al. Efficient assessment of neuropathic pain drugs in patients with small fiber sensory neuropathies. Pain 2009;141:19-24
60. Jensen T, Madsen C, Finnerup N. Pharmacology and treatment of neuropathic pains. Curr Opin Neurol 2009;22:467-74
61. Dworkin R, OConnor A, Audette J, et al. Recommendations for the pharmacological management of neuropathic pain: an overview and literature update. Mayo Clin Proc 2010;85(Suppl):S3-14
62. Sindrup S, Madsen C, Brosen K, Jensen T. The effect of tramadol in painful polyneuropathy in relation to serum drug and metabolite levels. Clin Pharmacol Ther 1999;66:636-41 (Pubitemid 30014092)
63. Harati Y, Gooch C, Swenson M, et al. Double-blind randomized trial of tramadol for the treatment of the pain of diabetic neuropathy. Neurology 1998;50:1842-6 (Pubitemid 28283262)
64. Kroenke K, Krebs E, Bair M. Pharmacotherapy of chronic pain: a synthesis of recommendations from systematic reviews. Gen Hosp Psychiatry 2009;31:206-19
65. Marcus D. Fibromyalgia: diagnosis and treatment options. Gender Med 2009;6:139-51
66. Attal N, Mazaltarine G, Perrouin-Verbe B, Albert T. Chronic neuropathic pain management in spinal cord injury patients. What is the efficacy of pharmacological treatments with a general mode of administration? (Oral, transdermal, intravenous). Ann Phys Rehab Med 2009;52:124-41
67. Wilder-Smith C, Hill L, Laurent S. Postamputation pain and sensory changes in treatment-naive patients: characteristics and responses to treatment with tramadol, amitriptyline, and placebo. Anesthesiology 2005;103:619-28 (Pubitemid 41258162)
68. Sindrup S, Andersen G, Madsen C, et al. Tramadol relieves pain and allodynia in polyneuropathy: a randomised, double-blind, controlled trial. Pain 1999;83:85-90 (Pubitemid 29446160)
69. Kraychete D, Sakata R, Issy A, et al. Proinflammatory cytokines in patients with neuropathic pain treated with tramadol. Rev Bras Anestesiol 2009;59:297-303
70. Cepeda M, Camargo F, Zea C, Valencia L. Tramadol for osteoarthritis: a systematic review and meta-analysis. J Rheumatol 2007;34:543-55 (Pubitemid 46364009)
71. Babul N, Noveck R, Chipman H, et al. Efficacy and safety of extended-release, once-daily tramadol in chronic pain: a randomized 12-week clinical trial in osteoarthritis of the knee. J Pain Symptom Manage 2004;28:59-71 (Pubitemid 38829673)
72. Gana T, Pascual M, Fleming R, et al. Extended-release tramadol in the treatment of osteoarthritis: a multicenter, randomized, double-blind, placebo-controlled clinical trial. Curr Med Res Opin 2006;22:1391-401 (Pubitemid 44085591)
73. Vorsanger G, Xiang J, Jordan D, Farrell J. Post hoc analysis of a randomized, double-blind, placebo-controlled efficacy and tolerability study of tramadol extended release for the treatment of osteoarthritis pain in geriatric patients. Clin Ther 2007;29:2520-35 (Pubitemid 350299463)
74. Malonne H, Coffiner M, Sonet B, et al. Efficacy and tolerability of sustained-release tramadol in the treatment of symptomatic osteoarthritis of the hip or knee: a multicenter, randomized, double-blind, placebo-controlled study. Clin Ther 2004;26:1774-82 (Pubitemid 40089490)
75. Fishman R, Kistler C, Ellerbusch M, et al. Efficacy and safety of 12 weeks of osteoarthritic pain therapy with once-daily tramadol (Tramadol Contramid OAD). J Opioid Manag 2007;3:273-80 (Pubitemid 350268071)
76. Burch F, Fishman R, Messina N, et al. A comparison of the analgesic efficacy of tramadol Contramid OAD versus placebo in patients with pain due to osteoarthritis. J Pain Symptom Manage 2007;34:328-38 (Pubitemid 47371077)
77. Kean W, Bouchard S, Roderich-Gossen E. Women with pain due to osteoarthritis: the efficacy and safety of a once-daily formulation of tramadol. Pain Med 2009;10:1001-11
78. Beaulieu A, Peloso P, Haraoui B, et al. Once-daily, controlled-release tramadol and sustained-release diclofenac relieve chronic pain due to osteoarthritis: a randomized controlled trial. Pain Res Manage 2008;13:103-10 (Pubitemid 351865292)
79. Karlsson M, Berggren A-C. Efficacy and safety of low-dose transdermal buprenorphine patches (5, 10, and 20 μg/h) versus prolonged-release tramadol tablets (75, 100, 150, and 200 mg) in patients with chronic osteoarthritis pain: a 12-week randomized, open-label, controlled, parallel-group noninferiority study. Clin Ther 2009;31:503-13
80. Wilder-Smith CH, Hill L, Spargo K, Kalla A. Treatment of severe pain from osteoarthritis with slow-release tramadol or dihydrocodeine in combination with NSAIDs: a randomized study comparing analgesia, antinociception and gastrointestinal effects. Pain 2001;91:3-31
81. Leppert W, Majkowicz M. The impact of tramadol and dihydrocodeine treatment on quality of life of patients with cancer pain. Int J Clin Pract 2010;64:1681-7
82. Langley P, Patkar A, Boswell K, et al. Adverse event profile of tramadol in recent clinical studies of chronic osteoarthritis pain. Curr Med Res Opin 2010;26:239-51
83. Thorne C, Beaulieu A, Callaghan D, et al. A randomized, double-blind, crossover comparison of the efficacy and safety of oral controlled-release tramadol and placebo in patients with painful osteoarthritis. Pain Res Manage 2008;13:93-102 (Pubitemid 351865291)
84. Wilder-Smith C, Bettiga A. The analgesic tramadol has minimal effect on gastrointestinal motor function. Br J Clin Pharmacol 1997;43:71-5 (Pubitemid 27060273)
85. Murphy D, Sutton A, Prescott L, Murphy M. A comparison of the effects of tramadol and morphine on gastric emptying in man. Anaesthesia 1997;52:1224-9 (Pubitemid 27511267)
86. Staritz M, Poralla T, Manns M, Buschenfelde K. Effect of modern analgesic drugs (Tramadol, pentazocine, and buprenorphine) on the bile duct sphincter in man. Gut 1986;27:567-9 (Pubitemid 16079758)
87. Hair P, Curran M, Keam S. Tramadol extended-release tablets. Drugs 2006;66:2017-27 (Pubitemid 44771942)
88. Teppema L, Nieuwenhuijs D, Olievier C, Dahan A. Respiratory depression by tramadol in the cat: involvement of opioid receptors. Anesthesiology 2003;98:420-7 (Pubitemid 36592811)
89. Leppert W. Tramadol as an analgesic for mild to moderate cancer pain. Pharmacol Rep 2009;61:978-92
90. Pascual M, Fleming R, Gana T, Vorsanger G. Open-label study of the safety and effectiveness of long-term therapy with extended-release tramadol in the management of chronic nonmalignant pain. Curr Med Res Opin 2007;23:2531-42 (Pubitemid 350033455)
91. Malonne H, Coffiner M, Fontaine D, et al. Long-term tolerability of tramadol LP, a new once-daily formulation, in patients with osteoarthritis or low back pain. J Clin Pharm Ther 2005;30:113-20 (Pubitemid 41583605)
92. ULTRAM ER (tramadol HCl) extended-release tablets. US prescribing information 2006. Available from: http://www.ortho-mcneil.com/orthomcneil/ shared/pi/ultramer.pdf. [Last accessed 15 January 2010]
93. Morin C, Gibson D, Wade J. Self-reported sleep and mood disturbance in chronic pain patients. Clin J Pain 1998;14:311-14 (Pubitemid 28560153)
94. Kosinski M, Janagap C, Gajria K, et al. Pain relief and pain-related sleep disturbance with extended-release tramadol in patients with osteoarthritis. Curr Med Res Opin 2007;23:1615-26 (Pubitemid 47122171)
95. Florete O, Xiang J, Vorsanger G. Effects of extended-release tramadol on pain-related sleep parameters in patients with osteoarthritis. Expert Opin Pharmacother 2008;9:1817-27