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Pregabalin

Abstract

In July 2004, pregabalin (Lyrica; Pfizer) was approved in Europe for the treatment of peripheral neuropathic pain and as an adjunctive therapy for partial seizures in patients with epilepsy. Approval by the US FDA for the management of neuropathic pain associated with diabetic peripheral neuropathy and post-herpetic neuralgia followed in December 2004.

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Figure 1: Chemical structures of GABA, gabapentin and pregabalin.

References

  1. Woolf, C. J. & Mannion, R. J. Neuropathic pain: aetiology, symptoms, mechanisms, and management. Lancet 353, 1959–1964 (1999).

    CAS  PubMed  Google Scholar 

  2. Dworkin, R. H. et al. Advances in neuropathic pain: diagnosis, mechanisms, and treatment recommendations. Arch. Neurol. 60, 1524–1534 (2003).

    Article  Google Scholar 

  3. Bryans, J. S. & Wustrow, D. J. 3-substituted GABA analogs with central nervous system activity: a review. Med. Res. Rev. 19, 149–177 (1999).

    Article  CAS  Google Scholar 

  4. Belliotti, T. R. et al. Structure–activity relationships of pregabalin and analogues that target the α2-δ protein. J. Med. Chem. 48, 2294–2307 (2005).

    Article  CAS  Google Scholar 

  5. Bramwell, S. R. et al. The analgesic actions of pregabalin are mediated through its binding to the α2δ-1 subunit of voltage-gated calcium channels. Abs. Soc. Neurosci. Ann. Meeting program 523.19 (2004).

  6. Electronic medicines compendium [online], <http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=14651> (2004).

  7. Lesser, H. et al. Pregabalin relieves symptoms of painful diabetic neuropathy: a randomized controlled trial. Neurology 63, 2104–2110 (2004).

    Article  CAS  Google Scholar 

  8. Rosenstock, J. et al. Pregabalin for the treatment of painful diabetic peripheral neuropathy: a double-blind, placebo-controlled trial. Pain 110, 628–638 (2004).

    Article  CAS  Google Scholar 

  9. Richter, R. W. et al. Relief of painful diabetic peripheral neuropathy with pregabalin: a randomized, placebo-controlled trial. J. Pain 6, 253–260 (2005).

    Article  CAS  Google Scholar 

  10. Dworkin, R. H. et al. Pregabalin for the treatment of postherpetic neuralgia: a randomized, placebo-controlled trial. Neurology 60, 1274–1283 (2003).

    Article  CAS  Google Scholar 

  11. Sabatowski, R. et al. Pregabalin reduces pain and improves sleep and mood disturbances in patients with post-herpetic neuralgia: results of a randomised, placebo-controlled clinical trial. Pain 109, 26–35 (2004).

    Article  CAS  Google Scholar 

  12. Beydoun, A. et al. Safety and efficacy of two pregabalin regimens for add-on treatment of partial epilepsy. Neurology 64, 475–480 (2005).

    Article  CAS  Google Scholar 

  13. Arroyo, S. et al. Pregabalin add-on treatment: a randomized, double-blind, placebo-controlled, dose–response study in adults with partial seizures. Epilepsia 45, 20–27 (2004).

    Article  CAS  Google Scholar 

  14. Drugs@FDA [online], <http://www.fda.gov/cder/foi/appletter/2004/21723ltr.pdf> (2004).

  15. Sawynok, J. et al. Antidepressants as analgesics: an overview of central and peripheral mechanisms of action. J. Psychiatry Neurosci. 26, 21–29 (2001).

    CAS  PubMed  PubMed Central  Google Scholar 

  16. Kalso, E. et al. (eds). Opioid Sensitivity of Chronic Noncancer Pain (IASP, Seattle, 1999).

    Google Scholar 

  17. Woolf, C. J. Pain: moving from symptom control toward mechanism-specific pharmacologic management. Ann. Intern. Med. 140, 441–451 (2004).

    Article  Google Scholar 

  18. Raja, S. N. et al. Opioids versus antidepressants in postherpetic neuralgia: a randomized, placebo-controlled trial. Neurology 59, 1015–1021 (2002).

    Article  CAS  Google Scholar 

  19. Gilron, I. et al. Morphine, gabapentin, or their combination for neuropathic pain. N. Engl. J. Med. 352, 1324–1334 (2005).

    Article  CAS  Google Scholar 

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Correspondence to Robert H. Dworkin or Peter Kirkpatrick.

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Dworkin, R., Kirkpatrick, P. Pregabalin. Nat Rev Drug Discov 4, 455–456 (2005). https://doi.org/10.1038/nrd1756

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