Current Pain and Headache Reports

, Volume 9, Issue 3, pp 206–212

Non-oral formulations of triptans and their use in acute migraine

  • Carl G. H. Dahlöf
Article
  • 94 Downloads

Abstract

The introduction of triptans (5-HT 1B/1D agonists) into clinical practice has expanded the therapeutic options for doctors treating migraine sufferers. The triptans are available in several different formulations such as conventional oral tablets, orally disintegrating wafers, subcutaneous injections, nasal sprays, and suppositories, which provide an excellent opportunity to tailor therapy to individual patients’ needs. Although the oral formulations are the most popular with patients, they are not the most appropriate route of administration for drug delivery during the migraine attack. Due to gastrointestinal dysmotility, the intestinal absorption of any triptan administered orally may be impaired and treatment effects become inconsistent. For this reason, triptans preferably should be prescribed in a non-oral formulation (injection, nasal spray, or suppository). Parenteral administration of a triptan is more likely to provide relief of symptoms, even when it is used later in the course of the migraine attack.

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References and Recommended Reading

  1. 1.
    Campbell JK: Manifestations of migraine. Neurol Clin 1990, 8:841–855.PubMedGoogle Scholar
  2. 2.
    International Headache Society: The International Classification of Headache Disorders, edn 2. Cephalalgia 2004, 1:9–160.Google Scholar
  3. 3.
    Goadsby PJ, Lipton RB, Ferrari MD: Migraine: current understanding and treatment. N Engl J Med 2002, 346:257–270.PubMedCrossRefGoogle Scholar
  4. 4.
    Waeber C, Moskowitz MA: Therapeutic implications of central and peripheral neurologic mechanisms in migraine. Neurology 2003, 61(suppl 4):S9-S20.PubMedGoogle Scholar
  5. 5.
    Welch KM: Contemporary concepts of migraine pathogenesis. Neurology 2003, 61(suppl 4):S2-S8.PubMedGoogle Scholar
  6. 6.
    Murray CJ, Lopez AD: The global burden of disease: a comprehensive assessment of mortality and disability from diseases, injuries, and risk factors in 1990 and projected to 2020. In Global Burden of Disease and Injury Series. Cambridge, MA: Harvard School of Public Health on behalf of the World Health Organization and the World Bank; 1966.Google Scholar
  7. 7.
    Lopez AD, Murray CC: The global burden of disease: 1990–2020. Nat Med 1998, 4:1241–1243.PubMedCrossRefGoogle Scholar
  8. 8.
    Menken M, Munsat TL, Toole JF: The global burden of disease study: implications for neurology. The ambulatory workload of office-based neurologists: implications of the National Ambulatory Medical Care Survey. Arch Neurol 2000, 57:418–420.PubMedCrossRefGoogle Scholar
  9. 9.
    The World Health Report: Mental Health: New Understanding, New Hope. Geneva: World Health Organization; 2001.Google Scholar
  10. 10.
    Linde M, Dahlöf C: Attitudes and burden of disease among self-considered migraineurs: a nation-wide population-based survey in Sweden. Cephalalgia 2004, 24:455–465.PubMedCrossRefGoogle Scholar
  11. 11.
    Tepper SJ, Dahlöf CG, Dowson A, et al.: Prevalence and diagnosis of migraine in patients consulting their physician with a complaint of headache: data from the landmark study. Headache 2004, 44:856–864.PubMedCrossRefGoogle Scholar
  12. 12.
    Lipton RB, Stewart WF: Acute migraine therapy: Do doctors understand what patients with migraine want from therapy? Headache 1999, 39(suppl 2):S20-S26.CrossRefGoogle Scholar
  13. 13.
    Dahlöf CG: Characteristics of different routes of administration. In Frontiers in Headache Research. The Triptans: Novel Drugs for Migraine. Edited by Olesen J, Ferrari M, Humphrey PP. Oxford: Oxford University Press; 2001:80–90.Google Scholar
  14. 14.
    MacGregor EA, Brandes J, Eikermann A: Migraine prevalence and treatment patterns: the global Migraine and Zolmitriptan Evaluation Survey. Headache 2003, 43:19–26.PubMedCrossRefGoogle Scholar
  15. 15.
    MacGregor EA, Brandes J, Eikermann A, Giammarco R: Impact of migraine on patients and their families: the Migraine and Zolmitriptan Evaluation (MAZE) Survey, phase III. Curr Med Res Opin 2004, 20:1143–1150.PubMedCrossRefGoogle Scholar
  16. 16.
    Dahlöf C: Integrating the triptans into clinical practice. Curr Opin Neurol 2002, 15:317–322.PubMedCrossRefGoogle Scholar
  17. 17.
    Silberstein SD: Migraine. Lancet 2004, 363:381–391.PubMedCrossRefGoogle Scholar
  18. 18.
    Dahlöf CG, Hargreaves RJ: Pathophysiology and pharmacology of migraine. Is there a place for antiemetics in future treatment strategies? Cephalalgia 1998, 18:593–604.PubMedCrossRefGoogle Scholar
  19. 19.
    Kaufman JS, Levine I: Acute gastric dilatation of stomach during attack of migraine. Radiology 1936, 27:301–302.Google Scholar
  20. 20.
    Volans GN: Migraine and drug absorption. Clin Pharmacokinet 1978, 3:313–318.PubMedGoogle Scholar
  21. 21.
    Tokola RA, Kangasniemi P, Neuvonen PJ, Tokola O: Tolfenamic acid, metoclopramide, caffeine, and their combinations in the treatment of migraine attacks. Cephalalgia 1984, 4:253–263.PubMedCrossRefGoogle Scholar
  22. 22.
    Tokola RA, Neuvonen PJ: Effects of migraine attack and metoclopramide on the absorption of tolfenamic acid. Br J Clin Pharmacol 1984, 17:67–75.PubMedGoogle Scholar
  23. 23.
    Houghton LA, Fowler P, Keene ON, Read NW: Effect of sumatriptan, a new selective 5HT1-like agonist, on liquid gastric emptying in man. Aliment Pharmacol Ther 1992, 6:685–691.PubMedCrossRefGoogle Scholar
  24. 24.
    Cipolla G, Sacco S, Crema F, et al.: Gastric motor effects of triptans: open questions and future perspectives. Pharmacol Res 2001, 43:205–210.PubMedCrossRefGoogle Scholar
  25. 25.
    Tack J: The physiology and the pathophysiology of the gastric accommodation reflex in man. Verh K Acad Geneeskd Belg 2000, 62:183–207.PubMedGoogle Scholar
  26. 26.
    Dahlöf CG: Sumatriptan: pharmacological basis and clinical results. Curr Med Res Opin 2001, 17:s35-s45. A comprehensive review of the pharmacokinetics, efficacy, and tolerability of sumatriptan injection, nasal spray, conventional tablets, and suppository.PubMedCrossRefGoogle Scholar
  27. 27.
    Schoenen J: When should triptans be taken during a migraine attack? CNS Drugs 2001, 15:583–587.PubMedCrossRefGoogle Scholar
  28. 28.
    Burstein R, Cutrer MF, Yarnitsky D: The development of cutaneous allodynia during a migraine attack clinical evidence for the sequential recruitment of spinal and supraspinal nociceptive neurons in migraine. Brain 2000, 123:1703–1709.PubMedCrossRefGoogle Scholar
  29. 29.
    Burstein R, Yarnitsky D, Goor-Aryeh I, et al.: An association between migraine and cutaneous allodynia. Ann Neurol 2000, 47:614–624.PubMedCrossRefGoogle Scholar
  30. 30.
    Burstein R: Deconstructing migraine headache into peripheral and central sensitization. Pain 2001, 89:107–110.PubMedCrossRefGoogle Scholar
  31. 31.
    Burstein R, Collins B, Jakubowski M: Defeating migraine pain with triptans: a race against the development of cutaneous allodynia. Ann Neurol 2004, 55:19–26.PubMedCrossRefGoogle Scholar
  32. 32.
    Cady RK, Lipton RB, Hall C, et al.: Treatment of mild headache in disabled migraine sufferers: results of the Spectrum Study. Headache 2000, 40:792–797.PubMedCrossRefGoogle Scholar
  33. 33.
    Cady RK, Sheftell F, Lipton RB, et al.: Effect of early intervention with sumatriptan on migraine pain: retrospective analyses of data from three clinical trials. Clin Ther 2000, 22:1035–1048.PubMedCrossRefGoogle Scholar
  34. 34.
    Hu XH, Raskin NH, Cowan R, et al.: Treatment of migraine with rizatriptan: when to take the medication. Headache 2002, 42:16–20.PubMedCrossRefGoogle Scholar
  35. 35.
    Pascual J, Cabarrocas X: Within-patient early versus delayed treatment of migraine attacks with almotriptan: the sooner the better. Headache 2002, 42:28–31.PubMedCrossRefGoogle Scholar
  36. 36.
    Pascual J: Clinical benefits of early triptan therapy for migraine. Headache 2002, 1:10–17.CrossRefGoogle Scholar
  37. 37.
    Mathew NT: Early intervention with almotriptan improves sustained pain-free response in acute migraine. Headache 2003, 43:1075–1079.PubMedCrossRefGoogle Scholar
  38. 38.
    Winner P, Mannix LK, Putnam DG, et al.: Pain-free results with sumatriptan taken at the first sign of migraine pain: two randomized, double-blind, placebo-controlled studies. Mayo Clin Proc 2003, 78:1214–1222.PubMedCrossRefGoogle Scholar
  39. 39.
    Scholpp J, Schellenberg R, Moeckesch B, Banik N: Early treatment of a migraine attack while pain is still mild increases the efficacy of sumatriptan. Cephalalgia 2004, 24:925–933.PubMedCrossRefGoogle Scholar
  40. 40.
    Klapper J, Lucas C, Rosjo O, Charlesworth B: Benefits of treating highly disabled migraine patients with zolmitriptan while pain is mild. Cephalalgia 2004, 24:918–924.PubMedCrossRefGoogle Scholar
  41. 41.
    Dahlöf C, Hogenhuis L, Olesen J, et al.: Early clinical experience with subcutaneous naratriptan in the acute treatment of migraine: a dose-ranging study. Eur J Neurol 1998, 5:469–477.PubMedCrossRefGoogle Scholar
  42. 42.
    Diamond S, Freitag FG: Sumatriptan 6 mg subcutaneous as a successful treatment for migraine associated with allodynia. Presented at the 56th Annual Meeting of the American Academy of Neurology. San Francisco: April 24–May 1, 2004.Google Scholar
  43. 43.
    Freitag FG, Diamond S: Sumatriptan 6 mg subcutaneous as an effective migraine treatment in patients who historically fail to respond to oral triptans. Presented at the 56th Annual Meeting of the American Academy of Neurology. San Francisco: April 24–May 1, 2004.Google Scholar
  44. 44.
    Linde M, Mellberg A, Dahlof CG: Subcutaneous sumatriptan provides symptomatic relief at any pain intensity or time during the migraine attack. Cephalalgia 2005, in press.Google Scholar
  45. 45.
    Carpay J, Schoenen J, Ahmad F, et al.: Efficacy and tolerability of sumatriptan tablets in a fast-disintegrating, rapid-release formulation for the acute treatment of migraine: results of a multicenter, randomized, placebo-controlled study. Clin Ther 2004, 26:214–223.PubMedCrossRefGoogle Scholar
  46. 46.
    Walls C, Lewis A, Bullman J, et al.: Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers. Curr Med Res Opin 2004, 20:803–809.PubMedCrossRefGoogle Scholar
  47. 47.
    Yates R, Nairn K, Dixon R, et al.: Pharmacokinetics, dose proportionality, and tolerability of single and repeat doses of a nasal spray formulation of zolmitriptan in healthy volunteers. J Clin Pharmacol 2002, 42:1244–1250.PubMedCrossRefGoogle Scholar
  48. 48.
    Charlesworth BR, Dowson AJ, Purdy A, et al.: Speed of onset and efficacy of zolmitriptan nasal spray in the acute treatment of migraine: a randomized, double-blind, placebocontrolled, dose-ranging study versus zolmitriptan tablet. CNS Drugs 2003, 17:653–667.PubMedCrossRefGoogle Scholar
  49. 49.
    Dowson AJ, Charlesworth BR, Purdy A, et al.: Tolerability and consistency of effect of zolmitriptan nasal spray in a longterm migraine treatment trial. CNS Drugs 2003, 17:839–851.PubMedCrossRefGoogle Scholar
  50. 50.
    Syrett N, Abu-Shakra S, Yates R: Zolmitriptan nasal spray: advances in migraine treatment. Neurology 2003, 61(suppl 4):S27-S30.PubMedGoogle Scholar
  51. 51.
    Uemura N, Charlesworth B, Onishi T: Zolmitriptan is detectable in plasma 2–5 minutes after administration by nasal spray. Headache 2003, 43:S159.Google Scholar
  52. 52.
    Bergström M, Wall A, Kagedal M: An open-label positronemission tomography study to investigate the distribution of intranasally administered [11C]-zolmitriptan into the CNS. Neurology 2004, 62(suppl 5):A801.Google Scholar
  53. 53.
    Zingmark PH, Yates R, Hedlund C: True nasal absorption of zolmitriptan following administration of zolmitriptan nasal spray. Cephalalgia 2003, 23:700.Google Scholar
  54. 54.
    Anonymous: Treatment of migraine attacks with sumatriptan. The Subcutaneous Sumatriptan International Study Group. N Engl J Med 1991, 325:316–321.Google Scholar
  55. 55.
    Cady RK, Wendt JK, Kirchner JR, et al.: Treatment of acute migraine with subcutaneous sumatriptan. JAMA 1991, 265:2831–2835.PubMedCrossRefGoogle Scholar
  56. 56.
    Dahlöf C: Sumatriptan nasal spray in the acute treatment of migraine: a review of clinical studies. Cephalalgia 1999, 19:769–778.PubMedCrossRefGoogle Scholar
  57. 57.
    Dahlöf C, Kerekes E, Linde M: Zolmitriptan nasal spray provides fast relief of migraine symptoms and is preferred by patients: a Swedish study of preference in clinical practice. J Headache Pain 2004, 5(suppl 4):237–242.CrossRefGoogle Scholar
  58. 58.
    Dahlöf C: Clinical applications of new therapeutic deliveries in migraine. Neurology 2003, 61(suppl 4):S31-S34.PubMedGoogle Scholar
  59. 59.
    Limmroth V, Dowson A, Diener HC, Dahlöf C: Non-oral delivery systems in headache therapy: focus on intranasal delivery. Am J Drug Deliv 2004, 2:59–68.CrossRefGoogle Scholar
  60. 60.
    Dahlöf C, Ekbom K, Persson L: Clinical experiences from Sweden on the use of subcutaneously administered sumatriptan in migraine and cluster headache. Arch Neurol 1994, 51:1256–1261.PubMedGoogle Scholar
  61. 61.
    Dahlöf CG, Mathew N: Cardiovascular safety of 5-HT1B/1D agonists: Is there a cause for concern? Cephalalgia 1998, 18:539–545.PubMedCrossRefGoogle Scholar
  62. 62.
    Dodick D, Lipton RB, Martin V, et al.: Consensus statement: cardiovascular safety profile of triptans (5-HT agonists) in the acute treatment of migraine. Headache 2004, 44:414–425. Comprehensive review and expert assessment of preclinical and clinical data on the cardiovascular safety of triptans.PubMedCrossRefGoogle Scholar
  63. 63.
    Hall GC, Brown MM, Mo J, MacRae KD: Triptans in migraine: the risks of stroke, cardiovascular disease, and death in practice. Neurology 2004, 62:563–568. Comprehensive review on migraine, triptan treatment, and the risk of cardiovascular disease, stroke, and mortality.PubMedGoogle Scholar
  64. 64.
    Velentgas P, Cole JA, Mo J, et al.: Severe vascular events in migraine patients. Headache 2004, 44:642–651. Comprehensive review on migraine, triptan treatment, and the risk of cardiovascular disease, stroke, and mortality.PubMedCrossRefGoogle Scholar
  65. 65.
    Dodick D, Brandes J, Elkind A: Speed of onset, efficacy and tolerability of zolmitriptan nasal spray in the management of acute migraine. Headache 2004, 44:469.CrossRefGoogle Scholar
  66. 66.
    Gawel M, Aschoff J, May A, et al.: High levels of satisfaction in patients treating migraine with zolmitriptan nasal spray in a real life setting: results from phase 2 of the REALIZE study. Neurology 2004, 62(suppl 5):A151.Google Scholar
  67. 67.
    Dahlöf CG, Saiers J: Sumatriptan injection and tablets in clinical practice: results of a survey of 707 migraineurs. Headache 1998, 38:756–763.PubMedCrossRefGoogle Scholar
  68. 68.
    Dahlöf CG, Boes-Hansen S, Cederberg CG, et al.: How does sumatriptan nasal spray perform in clinical practice? Cephalalgia 1998, 18:278–282.PubMedCrossRefGoogle Scholar

Copyright information

© Current Science Inc 2005

Authors and Affiliations

  • Carl G. H. Dahlöf
    • 1
  1. 1.Gothenburg Migraine ClinicGothenburgSweden

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