Flupirtine in pain management: Pharmacological properties and clinical use

CNS Drugs

Volumn 24, Issue 10, 2010, Pages 867-881

  Devulder, Jacques ^a  

^a GHENT UNIVERSITY HOSPITAL   (Belgium)

Author keywords

Analgesics, general; Cancer pain; Flupirtine, general; Headache; Musculoskeletal pain; Neurogenic pain; NMDA receptor antagonists, general; Pain

Indexed keywords

ACETYLSALICYLIC ACID; BUPRENORPHINE; CARBAMAZEPINE; CHLORMEZANONE; DICLOFENAC; DRUG METABOLITE; DULOXETINE; FLUPIRTINE; MILNACIPRAN; MORPHINE; MUSCLE RELAXANT AGENT; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; NALOXONE; NONSTEROID ANTIINFLAMMATORY AGENT; OPIATE; PARACETAMOL; PENTAZOCINE; POTASSIUM CHANNEL; PREGABALIN; RETIGABINE; TRAMADOL;

ACTION POTENTIAL; ANALGESIA; ANTINOCICEPTION; ANTIOXIDANT ACTIVITY; ANXIETY DISORDER; ATAXIA; CANCER PAIN; CELL PROTECTION; CHEMICAL BURN; CLINICAL TRIAL; CONFUSION; CONSTIPATION; DIGESTIVE SYSTEM PERFORATION; DIGESTIVE SYSTEM ULCER; DIZZINESS; DROWSINESS; DRUG ABSORPTION; DRUG ACTIVITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG FORMULATION; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG TOLERABILITY; DYSMENORRHEA; FATIGUE; FIBROMYALGIA; GASTROINTESTINAL HEMORRHAGE; GASTROINTESTINAL OBSTRUCTION; GASTROINTESTINAL SYMPTOM; HEADACHE; HEARTBURN; HUMAN; INJURY; LOW BACK PAIN; MIGRAINE; MUSCULOSKELETAL PAIN; MYOFASCIAL PAIN; NAUSEA; NERVE CELL EXCITABILITY; NEURALGIA; NEURITIS; NEUROPATHIC PAIN; NONHUMAN; PAIN; PARESTHESIA; POSTOPERATIVE PAIN; POSTTRAUMATIC PAIN; PRIORITY JOURNAL; PRURITUS; RESPIRATION DEPRESSION; REVIEW; SEDATION; SIDE EFFECT; SPINAL ROOT IRRITATION SYNDROME; SPINE DISEASE; SWEATING; SYSTEMATIC REVIEW; TENSION HEADACHE; TREATMENT INDICATION; TREMOR; URINE RETENTION; VERTIGO; VOMITING; XEROSTOMIA;

AMINOPYRIDINES; ANALGESICS; HUMANS; PAIN;

EID: 77956685284     PISSN: 11727047     EISSN: 11791934     Source Type: Journal    
DOI: 10.2165/11536230-000000000-00000     Document Type: Review

References (54)

1. Friedel HA, Fitton A. Flupirtine: a review of its pharmaco-logical properties, and therapeutic efficacy in pain states. Drugs 1993; 45 (4): 548-569
2. Kornhuber J, Maler M, Wiltfang J, et al. Neuronal po-tassium channel opening with flupirtine. Fortschr Neurol Psychiatr 1999; 67 (10): 466-475
3. Nickel B. The antinociceptive activity of flupirtine: a structu-rally new analgesic. Postgrad Med J 1987; 63 Suppl. 3: 19-28
4. Szelenyi I, Nickel B, Borbe HO, et al. Mode of antinocicep-tive action of flupirtine in the rat. Br J Pharmacol 1989; 97 (3): 835-842
5. Darius H, Schror K. The action of flupirtine on pros-taglandin formation and platelet aggregation in vitro. Arzneimittelforschung 1985; 35 (1): 55-59
6. Kornhuber J, Bleich S, Wiltfang J, et al. Flupirtine shows functional NMDA receptor antagonism by enhancing Mg2+ block via activation of voltage independent potassium channels: rapid communication. J Neural Transm 1999; 106 (9-10): 857-867
7. Jakob R, Krieglstein J. Influence of flupirtine on a G-protein coupled inwardly rectifying potassium current in hippo-campal neurones. Br J Pharmacol 1997; 122 (7): 1333-1338
8. Methling K, Reszka P, Lalk M, et al. Investigation of the in vitro metabolism of the analgesic flupirtine. Drug Metab Dispos 2009 Mar; 37 (3): 479-493
9. Miceli F, Soldovieri MV, Martire M, et al. Molecular pharmacology and therapeutic potential of neuronal Kv7-modulating drugs. Curr Opin Pharmacol 2008; 8 (1): 65-74
10. Blackburn-Munro G, Dalby-Brown W, Mirza NR, et al. Retigabine: chemical synthesis to clinical application. CNS Drug Rev 2005; 11 (1): 1-20
11. Szelenyi I, Nickel B. Putative site(s) and mechanism(s) of action of flupirtine, a novel analgesic compound. Postgrad Med J 1987; 63 Suppl. 3: 57-60
12. Abrams SM, Baker LR, Crome P, et al. Pharmacokinetics of flupirtine in elderly volunteers and in patients with moderate renal impairment. Postgrad Med J 1988; 64 (751): 361-363
13. Hlavica P, Niebch G. Pharmacokinetics and biotransfor-mation of the analgesic flupirtine in humans. Arzneimittelforschung 1985; 35 (1): 67-74
14. Hummel T, Friedmann T, Pauli E, et al. Dose-related anal-gesic effects of flupirtine. Br J Clin Pharmacol 1991; 32 (1): 69-76
15. Schuster M, Schwarz M, Block F, et al. Flupirtine: a review of its neuroprotective and behavioral properties. CNS Drug Rev 1998; 4 (2): 149-164
16. Metanor® [flupirtine maleate 100 mg]: summary of product characteristics. Lisbon: Meda Pharmaceuticals 2006
17. Efiret® [flupirtine maleate 100mg capsule]: summary of pro-duct characteristics. Milan: Meda Pharmaceuticals 2007
18. Mueller-Schwefe G. Flupirtine in acute and chronic pain associated with muscle tenseness: results of a postmarket surveillance study. Fortschr Med Orig 2003; 121 (1): 11-18
19. Luben V, Muller H, Lobisch M, et al. Treatment of tumor pain with flupirtine: results of a double-blind study versus tramadol. Fortschr Med 1994; 112 (19): 282-286
20. Li C, Ni J, Wang Z, et al. Analgesic efficacy and tolerability of flupirtine vs. tramadol in patients with subacute low back pain: a double-blind multicentre trial. Curr Med Res Opin 2008; 24 (12): 3523-3530
21. Ringe JD, Miethe D, Pittrow D, et al. Analgesic efficacy of flupirtine in primary care of patients with osteoporosis related pain: a multivariate analysis. Arzneimittelforschung 2003; 53 (7): 496-502
22. Worz R, Bolten W, Heller B, et al. Flupirtine in comparison with chlormezanone in chronic musculoskeletal back pain: results of a multicenter randomized double-blind study. Fortschr Med 1996; 114 (35-36): 500-504
23. Worz R. Flupirtine in chronic myofascial pain conditions. Fortschr Med 1991; 109 (6): 158-160
24. Worz R, Lobisch M, Schwittmann B, et al. Effectiveness of flupirtine in chronic tension headache: results of a double-blind study versus placebo. Fortschr Med 1995; 113 (32): 463-468
25. Heusinger JH. Efficacy and tolerance of flupirtine and pen-tazocine in two multicentre trials. Postgrad Med J 1987; 63 Suppl. 3: 71-79
26. Goodchild CS, Kolosov A, Tucker AP, et al. Combination therapy with flupirtine and opioid: studies in rat pain models. Pain Med 2008; 9 (7): 928-938
27. Nickel B, Jakovlev V, Szelenyi I. The effect of flupirtine, various analgesics and muscle relaxants on skeletal muscle tonein the conscious rat. Arzneimittelforschung 1990; 40(8): 909-911
28. Sitzer G. Einfacblindstudie mit Flupirtin gegen Acetyl-salicylsaure bei Patienten mit spinalem Wurzelreizsyndrom. Orthopadie/Traumatologie 1991; 6: 37-42
29. Mastronardi P, D'Onofrio M, Scanni E, et al. Analgesic activity of flupirtine maleate: a controlled double-blind study with diclofenac sodium in orthopaedics. J Int Med Res 1988; 16 (5): 338-348
30. Marczyk LRS. Avaliacao comparativa do maleato de flu-pirtina versus diclofenaco potassico em afeccoes musculo-esqueleticas. Arq Bras Med 1992; 66 (3): 269-275
31. Million R, Finlay BR, Whittington JR. Clinical trial of flu-pirtine maleate in patients with migraine. Curr Med Res Opin 1984; 9 (3): 204-212
32. Muller-Schwefe GH, Uberall MA. Analgesic and muscle tonus normalizing effect of flupirtine retard in chronic back pain: results of a standardized therapeutic evaluation applying objective methods for measuring pain pressure threshold, pain pressure tolerance and muscle tension. MMW Fortschr Med 2008; 149 Suppl. 4: 153-161
33. Scheef W. Analgesic efficacy and safety of oral flupirtine in the treatment of cancer pain. Postgrad Med J 1987; 63 Suppl. 3: 67-70
34. Goodchild CS, Nelson J, Cooke I, et al. Combination ther-apy with flupirtine and opioid: open-label case series in the treatment of neuropathic pain associated with cancer. Pain Med 2008; 9 (7): 939-949
35. Belgrade MJ. Following the clues to neuropathic pain: dis-tribution and other leads reveal the cause and the treatment approach. Postgrad Med 1999; 106 (6): 127-32, 135-140
36. Gassen M, Pergande G, Youdim MB. Antioxidant proper-ties of the triaminopyridine, flupirtine. Biochem Pharmacol 1998; 56 (10): 1323-1329
37. Osborne NN, Cazevieille C, Pergande G, et al. Induction of apoptosis in cultured human retinal pigment epithelial cells is counteracted by flupirtine. Invest Ophthalmol Vis Sci 1997; 38 (7): 1390-1400 (Pubitemid 27278558)
38. Wood JP, Pergande G, Osborne NN. Prevention of glutathione depletion-induced apoptosis in cultured human RPE cells by flupirtine. Restor Neurol Neurosci 1998; 12 (2-3): 119-125
39. Boscia F, Annunziato L, Taglialatela M. Retigabine and flupirtine exert neuroprotective actions in organotypic hippocampal cultures. Neuropharmacology 2006; 51 (2): 283-294
40. Sattler MB, Williams SK, Neusch C, et al. Flupirtine as neuroprotective add-on therapy in autoimmune optic neuritis. Am J Pathol 2008; 173 (5): 1496-1507
41. Zimmer G, Balakirev M, Zwicker K, et al. Effect of the triaminopyridine flupirtine on calcium uptake, membrane potential and ATP synthesis in rat heart mitochondria. Br J Pharmacol 1998; 123 (6): 1154-1158
42. Stoll AL. Fibromyalgia symptoms relieved by flupirtine: an open-label case series. Psychosomatics 2000; 41 (4): 371-372
43. US FDA. News release: FDA approves first drug for treat-ing fibromyalgia [online]. Available from URL: http://www. fda.gov/NewsEvents/Newsroom/ PressAnnouncements/2007/ ucm108936.htm [Accessed 2010 May 21]
44. Eli Lilly. News release: FDA approves Cymbalta® for the management of fibromyalgia [online]. Available from URL: http://www2.prnewswire.com/cgi-bin/ micro-stories.pl?ACCT= 916306&TICK=LLY&STORY=/www/story/06-16-2008/ 0004832743&EDATE=Jun+16,+2008 [Accessed 2010 May 21]
45. Forest Laboratories, Inc. News release: Forest and Cypress announce FDA approval of Savella™ for the management of fibromyalgia [online]. Available from URL: http://www. frx.com/news/PressRelease.aspx?ID=1244788 [Accessed 2010 May 21]
46. Herrmann WM, Hiersemenzel R, Aigner M, et al. Long-term tolerance of flupirtine: open multicenter study over one year. Fortschr Med 1993; 111 (15): 266-270
47. Herrmann WM, Kern U, Aigner M. On the adverse reac-tions and efficacy of long-term treatment with flupirtine: preliminary results of an ongoing twelve-month study with 200 patients suffering from chronic pain states in arthrosis or arthritis. Postgrad Med J 1987; 63 Suppl. 3: 87-103
48. McMahon FG, Arndt Jr WF, Newton JJ, et al. Clinical experience with flupirtine in the U.S. Postgrad Med J 1987; 63 Suppl. 3: 81-85
49. Hirschowitz BI. Nonsteroidal antiinflammatory drugs and the gastrointestinal tract. Gastroenterologist 1994; 2 (3): 207-223
50. Theifin G, Flipo RM, Schaeverbeke T, et al. Upper gastro-intestinal symptoms in patients treated with NSAIDs: evaluation of physician-patient agreement and impact in the COMPLAINS study. 14th United European Gastro-enterology Week; 2006 Oct 21-25; Berlin
51. Laine L. Approaches to nonsteroidal anti-inflammatory drug use in the high-risk patient. Gastroenterology 2001; 120 (3): 594-606
52. Schug SA, Zech D, Grond S. Adverse effects of systemic opioid analgesics. Drug Saf 1992; 7 (3): 200-213
53. Powell-Jackson P, Williams R. Use of flupirtine maleate as an analgesic in patients with liver disease. Br J Clin Pract 1985; 39 (2): 63-66
54. Data on file, Degussa Pharma, 1987