Skip to main content
Log in

Oral Sumatriptan Pharmacokinetics in the Migraine State

  • Clinical Pharmacokinetics
  • Published:
Clinical Drug Investigation Aims and scope Submit manuscript

Abstract

Objective: This double-blind, parallel, multicentre study investigated the effect of migraine on absorption of oral sumatriptan (25, 50 and 100mg) compared with placebo.

Design: Patients received sumatriptan or placebo in the clinic during an acute migraine and at least 7 days later, when pain-free. Pharmacokinetic and efficacy (n = 192) and safety (n = 259) parameters were assessed for 4 hours after administration of study medication.

Results: Absorption of sumatriptan from 50 and 100mg tablets was not significantly different between the migraine and pain-free periods. There was however a statistically significant decrease (approximately 23%) and delay (35 minutes) in absorption of sumatriptan from the 25mg tablet during a migraine compared with the pain-free period. Sumatriptan pharmacokinetics exhibited dose proportionality during the migraine and pain-free periods. All doses of sumatriptan were significantly superior to placebo in reducing headache pain. Adverse events were comparable among the sumatriptan groups and placebo group.

Conclusions: Absorption of sumatriptan, administered at therapeutic doses, was not statistically significantly impaired during migraine versus the pain-free state. These data suggest that coadministration of drugs that improve the absorption of sumatriptan is not necessary during sumatriptan treatment.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Connor HE, Feniuk W, Humphrey PPA. Characterization of 5-HT receptors mediating contraction of canine and primate basilar artery by use of GR43175, a selective 5-HT1-like receptor agonist. Br J Pharmacol 1989; 96: 379–87

    Article  PubMed  CAS  Google Scholar 

  2. Humphrey PPA, Feniuk W, Perren MJ, et al. The pharmacology of the novel 5-HT1-like receptor agonist, GR43175. Cephalalgia 1989; 9 Suppl. 9: 23–33

    PubMed  Google Scholar 

  3. Parsons AA, Whalley ET. Characterization of the 5-hydroxy-tryptamine receptor which mediates contraction of the human isolated basilar artery. Cephalalgia 1989; 9 Suppl. 9: 47–51

    PubMed  Google Scholar 

  4. Van Es NM, Bruning TA, Camps J, et al. Assessment of peripheral vascular effects of antimigraine drugs in humans. Cephalalgia 1995; 15(4): 288–91

    Article  Google Scholar 

  5. Dechant KL, Clissold SP. Sumatriptan: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache. Drugs 1992; 43(5): 776–98

    Article  PubMed  CAS  Google Scholar 

  6. Scott AK. Sumatriptan: clinical pharmacokinetics. Clin Pharmacokinet 1994; 27: 337–44

    Article  PubMed  CAS  Google Scholar 

  7. Friberg L, Olesen J, Iversen HK, et al. Migraine pain associated with middle cerebral artery dilation: reversal by sumatriptan. Lancet 1991; 338: 13–7

    Article  PubMed  CAS  Google Scholar 

  8. Moskowitz MA. Neurogenic versus vascular mechanisms of sumatriptan and ergot alkaloids in migraine. Trends Pharmacol Sci 1992; 13:307–12

    Article  PubMed  CAS  Google Scholar 

  9. Goadsby PJ, Hoskin KL. Serotonin inhibits trigeminal nucleus activity evoked by craniovascular stimulation through a 5HT1b/1d receptor: a central action in migraine? Ann Neurol 1998; 43(6): 711–8

    Article  PubMed  CAS  Google Scholar 

  10. Buzzi MG, Moskowitz MA. The antimigraine drug, sumatriptan (GR43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater. Br J Pharmacol 1990; 99: 202–6

    Article  PubMed  CAS  Google Scholar 

  11. Pearce JMS. Sumatriptan: efficacy and contribution to migraine mechanisms. J Neurol Neurosurg Psychiatry 1992; 55: 1103–5

    Article  PubMed  CAS  Google Scholar 

  12. Plosker GL, McTavish D. Sumatriptan: a reappraisal of its pharmacology and therapeutic efficacy in the acute treatment of migraine and cluster headache. Drugs 1994; 47(4): 622–51

    Article  PubMed  CAS  Google Scholar 

  13. May A, Shepheard SL, Knorr M, et al. Retinal plasma extravasation in animals but not humans: implications for the pathophysiology of migraine. Brain 1998; 121: 1231–7

    Article  PubMed  Google Scholar 

  14. Cady RK, Wendt JK, Kirchner JR, et al. Treatment of acute migraine with subcutaneous sumatriptan. JAMA 1991; 265: 2831–5

    Article  PubMed  CAS  Google Scholar 

  15. The Oral Sumatriptan Dose-Defining Study Group. Sumatriptan — an oral dose defining study. Eur Neurol 1991; 31: 300–5

    Article  Google Scholar 

  16. Carpay HA, Matthijsse P, Steinbuch M, et al. Oral and subcutaneous sumatriptan in the acute treatment of migraine: an open randomized cross-over study. Cephalalgia 1997; 17(5): 591–5

    Article  PubMed  CAS  Google Scholar 

  17. Kelly AM, Ardagh M, Curry C, et al. Intravenous chlorpromazine versus intramuscular sumatriptan for acute migraine. J Accid Emerg Med 1997; 14(4): 209–11

    Article  PubMed  CAS  Google Scholar 

  18. Eckborn K, Monstad I, Prusinski A, et al. Subcutaneous sumatriptan in the acute treatment of cluster headache: a dose comparison study. Acta Neurol Scand 1993; 88: 63–9

    Google Scholar 

  19. Ryan R, Elkind A, Baker CC, et al. Sumatriptan nasal spray for the acute treatment of migraine. Results of two clinical studies. Neurology 1997; 49(5): 1225–30

    Article  PubMed  CAS  Google Scholar 

  20. Perry CM, Markham A. Sumatriptan. An updated review of its use in migraine. Drugs 1998; 55(6): 889–922

    Article  PubMed  CAS  Google Scholar 

  21. Boyle R, Behan PO, Sutton JA. Acorrelation between severity of migraine and delayed gastric emptying measured by an epigastric impedance method. Br J Clin Pharmacol 1990; 30: 405–9

    Article  PubMed  CAS  Google Scholar 

  22. Volans GN. Research review — Migraine and drug absorption. Clin Pharmacokinet 1978; 3: 313–8

    Article  PubMed  CAS  Google Scholar 

  23. Ross-Lee LM, Eadie MJ, Heazlewood V, et al. Aspirin pharmacokinetics in migraine. The effect of metoclopramide. Eur J Clin Pharmacol 1983; 24: 777–85

    Article  PubMed  CAS  Google Scholar 

  24. Tokola RA, Neuvonen PJ. Effect of migraine attacks on paracetamol absorption. Br J Clin Pharmacol 1984; 18: 867–71

    Article  PubMed  CAS  Google Scholar 

  25. Tokola RA. The effect of metoclopramide and prochlorperazine on the absorption of effervescent paracetamol in migraine. Cephalalgia 1988; 8: 139–47

    Article  PubMed  CAS  Google Scholar 

  26. Tokola RA, Neuvonen PJ. Effects of migraine attack and metoclopramide on the absorption of tolfenamic acid. Br J Clin Pharmacol 1984; 17: 67–75

    Article  PubMed  CAS  Google Scholar 

  27. Pini LA, Bertolotti M, Trenti T, et al. Disposition of naproxen after oral administration during and between migraine attacks. Headache 1993; 33(4): 191–4

    Article  PubMed  CAS  Google Scholar 

  28. Houghton LA, Fowler P, Keene ON, et al. Effect of sumatriptan, a new selective 5HT-1-like agonist, on gastric emptying in man. Aliment Pharmacol Ther 1992; 6(6): 685–91

    Article  PubMed  CAS  Google Scholar 

  29. Headache Classification Committee of the International Headache Society. Classification and diagnostic criteria for headache disorders, cranial neuralgias and facial pain. Cephalalgia 1988; 8 Suppl. 7: 19–28

    Google Scholar 

  30. Busch MA, Plachetka JR, Donn KH, et al. Evaluation of the pharmacokinetics and safety of ascending single oral doses of GR43175 administered to healthy male volunteers. Cephalalgia 1989; 9 Suppl. 10: 414–5

    Google Scholar 

  31. Pini L-A, Bertolotti M, Bergonzini G, et al. Pharmacokinetics of tiaprofenic acid after oral administration in fasting patients during and between migraine attacks. Headache 1990; 30: 672–5

    Article  PubMed  CAS  Google Scholar 

  32. Fowler PA, Lacey LF, Thomas M, et al. The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan. Eur Neurol 1991; 31: 291–4

    Article  PubMed  CAS  Google Scholar 

  33. Fowler PA, Lacey LF. The effect of food on the pharmacokinetic profile of sumatriptan. Abstract XVth World Congress of Neurology, Vancouver, September 5–10, 1993

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Sramek, J.J., Hussey, E.K., Clements, B. et al. Oral Sumatriptan Pharmacokinetics in the Migraine State. Clin. Drug Investig. 17, 137–144 (1999). https://doi.org/10.2165/00044011-199917020-00008

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00044011-199917020-00008

Keywords

Navigation