Flupirtine in Pain Management Pharmacological Properties and Clinical Use

Devulder, Jacques
October 2010
CNS Drugs;2010, Vol. 24 Issue 10, p867
Academic Journal
Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain. Although large-scale clinical trials are lacking, the clinical trial database available to date from smaller-scale studies, together with extensive clinical experience, indicate that flupirtine effectively reduces chronic musculoskeletal pain, migraine and neuralgias, amongst other types of pain. In addition, flupirtine produces, at recommended clinical doses, muscle-relaxing effects in the presence of abnormally increased muscle tension. Its analgesic and muscle-relaxant properties were comparable to tramadol and chiormezanone, respectively, in two prospective trials in patients with lower back pain. Cytoprotective, anti-apoptotic and antioxidant properties have also been associated with flupirtine use in a small number of studies to date. When provided as combination therapy with morphine, flupirtine increases the antinociceptive activity of morphine 4-fold. Flupirtine displays superior tolerability when compared with tramadol and pentazocine. The most common adverse effects associated with flupirtine use are drowsiness, dizziness, heartburn, dry mouth, fatigue and nausea. With respect to its molecular structure, mechanism of action and adverse event profile, flupirtine is a unique drug. Flupirtine is an analgesic with many potential therapeutic benefits that may prove useful in the treatment of many disease states.


Related Articles

  • Tapentadol potentiates descending pain inhibition in chronic pain patients with diabetic polyneuropathy. Niesters, M.; Proto, P. L.; Aarts, L.; Sarton, E. Y.; Drewes, A. M.; Dahan, A. // BJA: The British Journal of Anaesthesia;Jul2014, Vol. 113 Issue 1, p148 

    Background Tapentadol is an analgesic agent for treatment of acute and chronic pain that activates the µ-opioid receptor combined with inhibition of neuronal norepinephrine reuptake. Both mechanisms are implicated in activation of descending inhibitory pain pathways. In this study, we...

  • TREATING PAIN. REED, JENNIFER // Gulfshore Life;Jun2014 Supplement Health, p20 

    The article reports that physicians are taking a different approach to the treatment of pain. Doctors know more about the roots of chronic pain, will less likely write a prescription for a painkiller and will encourage a combination of therapies, both medical and nonmedical. Doctors have found...

  • Chronic non-specific low back pain -- sub-groups or a single mechanism? Wand, Benedict Martin; O'Connell, Neil Edward // BMC Musculoskeletal Disorders;2008, Vol. 9, Special section p1 

    Background: Low back pain is a substantial health problem and has subsequently attracted a considerable amount of research. Clinical trials evaluating the efficacy of a variety of interventions for chronic non-specific low back pain indicate limited effectiveness for most commonly applied...

  • The impact on sleep of a multidisciplinary cognitive behavioural pain management programme: a pilot study. Cunningham, Jennifer M.; Blake, Catherine; Power, Camillus K.; O'Keeffe, Declan; Kelly, Valerie; Horan, Sheila; Spencer, Orla; Fullen, Brona M. // BMC Musculoskeletal Disorders;2011, Vol. 12 Issue 1, p1 

    Background: Reduced sleep quality is a common complaint among patients with chronic pain, with 50-80% of patients reporting sleep disturbance. Improvements in pain and quality of life measures have been achieved using a multidisciplinary cognitive behavioural therapy pain management programme...

  • The effect of local anaesthetic wound infiltration on chronic pain after lower limb joint replacement: A protocol for a double-blind randomised controlled trial. Wylde, Vikki; Gooberman-Hill, Rachael; Horwood, Jeremy; Beswick, Andrew; Noble, Sian; Brookes, Sara; Smith, Alison J.; Pyke, Mark; Dieppe, Paul; Blom, Ashley W. // BMC Musculoskeletal Disorders;2011, Vol. 12 Issue 1, p53 

    Background: For the majority of patients with osteoarthritis (OA), joint replacement is a successful intervention for relieving chronic joint pain. However, between 10-30% of patients continue to experience chronic pain after joint replacement. Evidence suggests that a risk factor for chronic...

  • Systematic review of topical rubefacients containing salicylates for the treatment of acute and chronic pain. Mason, Lorna; Moore, R. Andrew; Edwards, Jayne E.; McQuay, Jenry J.; Derry, Sheena; Wiffen, Philip J. // BMJ: British Medical Journal (International Edition);4/24/2004, Vol. 328 Issue 7446, p995 

    Objectives To determine the efficacy and safety of topical rubefacients containing salicylates in acute and chronic pain. Data sources Electronic databases and manufacturers of salicylates. Study selection Randomised double blind trials comparing topical rubefacients with placebo or another...

  • The efficacy of different pre- and post-operative analgesics in the management of pain after orthodontic separator placement: A randomized clinical trial. Sudhakar, V.; Vinodhini, T. S.; Mohan, A. Mathan; Srinivasan, B.; Rajkumar, B. K. // Journal of Pharmacy & Bioallied Sciences;Jul2014 Dental Supplement, Vol. 6 Issue S1, pS80 

    Introduction: Pain-free treatment to the patients is considered as an important treatment objective for orthodontic health care providers. However, many orthodontists underestimate the degree of pain experienced by the patients. Hence, this study was conducted as a randomized, double-blinded...

  • Concerns over opioid analgesic use in spinal pain not warranted.  // PharmacoEconomics & Outcomes News;2/26/2005, Issue 472, p11 

    Discusses research being done on the use of opioid analgesic by patients with pain related to defined spinal diseases. Reference to a study by M. L. Mahowald and colleagues published in a January 2005 issue of "Arthritis and Rheumatism"; Assessment of the tolerance and dependence associated...

  • Update on prescription extended-release opioids and appropriate patient selection. Brennan, Michael J. // Journal of Multidisciplinary Healthcare;2013, Vol. 6, p265 

    Chronic pain is largely underdiagnosed, often undertreated, and expected to increase as the American population ages. Many patients with chronic pain require long-term treatment with analgesic medications, and pain management may involve use of prescription opioids for patients whose pain is...


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics