Clinical Pharmacokinetics

, Volume 27, Issue 5, pp 337–344 | Cite as

Sumatriptan Clinical Pharmacokinetics

  • Andrew K. Scott
Review Articles Drug Disposition


Sumatriptan is a novel serotonini (5-hydroxytryptamine1; 5-HT1)-like agonist which has been shown to be effective in the treatment of acute migraine. Single-dose pharmacokinetic studies reflect the way that sumatriptan will be used in routine practice, but relatively few studies have been published.

Bioavailability is high (96%) following subcutaneous injection, but low (14%) following oral administration because of first-pass metabolism. Absorption is rapid after subcutaneous injection, with peak concentration reached in 10 minutes. After oral administration, multiple peak concentrations are observed, but a concentration that is 75% of the final peak concentration is usually reached within 45 minutes. Less than 20% of the drug is protein bound. The volume of distribution is greater than total body water at 170L. Total plasma clearance is rapid, with an elimination half-life of around 2 hours. There is one major metabolite (an indole acetic acid analogue) which is excreted in the urine as the free acid and its ester glucuronide conjugate.

The pharmacokinetic profile of sumatriptan is not significantly affected by an acute migraine attack (absorption phase), old age or gender. Pharmacokinetic studies in individuals with hepatic and renal disease have not been published; however, care should be taken when sumatriptan is administered to patients with liver disease until such information is available. No significant interaction was found between sumatriptan and propranolol, flunarizine, pizotifen or alcohol (ethanol).


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Graham JR, Wolff HG. Mechanism of migraine headache and action of ergotamine tartrate. Arch Neurol Psychiatry 1938; 39: 737–63Google Scholar
  2. 2.
    Humphrey PPA, Feniuk W, Perren MJ, et al. The pharmacology of the novel 5-HTl-like receptor agonist, GR43175. Cephalalgia 1989; 9 Suppl. 9: 23–33PubMedGoogle Scholar
  3. 3.
    Lance JW. 5-Hydroxytryptamine and its role in migraine. Eur Neurol 1991; 31: 279–81PubMedCrossRefGoogle Scholar
  4. 4.
    Oral Sumatriptan Dose Defining Study Group. Sumatriptan — an oral dose-defining study. Eur Neurol 1991; 31: 300–5CrossRefGoogle Scholar
  5. 5.
    Sumatriptan Auto-Injector Study Group. Self treatment of acute migraine with subcutaneous sumatriptan using an auto-injector device. Eur Neurol 1991; 31: 323–31CrossRefGoogle Scholar
  6. 6.
    Fowler PA, Lacey LF, Thomas M, et al. The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan. Eur Neurol 1991; 31: 291–4PubMedCrossRefGoogle Scholar
  7. 7.
    Andrew PD, Birch HL, Phillpot DA. Determination of sumatriptan succinate in plasma and urine by high-performance liquid chromatography with electrochemical detection. J Pharm Sci 1993: 82: 73–6PubMedCrossRefGoogle Scholar
  8. 8.
    Bateman DN. Sumatriptan. Lancet 1993; 341: 221–4PubMedCrossRefGoogle Scholar
  9. 9.
    Gutterman DL, Plachetka JR, Donn K, et al. Evaluation of the safety and pharmacokinetic properties of single subcutaneous doses of GR43175c in healthy, adult, male volunteers. Cephalalgia 1989; 9 Suppl. 10: 412–3Google Scholar
  10. 10.
    Busch MA, Plachetka JR, Donn KH, et al. Evaluation of the pharmacokinetics and safety of ascending single oral doses of GR 43175 administered to healthy male volunteers. Cephalalgia 1989; 9 Suppl. 10: 414–5Google Scholar
  11. 11.
    Scott AK, Walley T, Breckenridge AM, et al. Lack of an interaction between propranolol and sumatriptan. Br J Clin Pharmacol 1991; 32: 581–4PubMedCrossRefGoogle Scholar
  12. 12.
    Van Hecken AM, Depre M, De Schepper PJ, et al. Lack of effect of flunarizine on the pharmacokinetics and pharmacodynamics of sumatriptan in healthy volunteers. Br J Clin Pharmacol 1992; 34: 82–4PubMedCrossRefGoogle Scholar
  13. 13.
    Scott AK, Grimes S, Ng K, et al. Sumatriptan and cerebral perfusion in healthy volunteers. Br J Clin Pharmacol 1992; 33: 401–4PubMedCrossRefGoogle Scholar
  14. 14.
    Dixon CM, Saynor DA, Halliday TJ, et al. The disposition of sumatriptan in animals and man. Poster presented at Imigran: planning a revolution. Imigran Medical Marketing Symposium: 1990 Sept; Westminster, LondonGoogle Scholar
  15. 15.
    Cutler NR, Hussey EK, Sramek JJ, et al. Pharmacokinetics of oral sumatriptan in migraine patients during an attack and while pain free [abstract]. Biol Psychiatry 1992; 31: 180AGoogle Scholar
  16. 16.
    Glaxo. Sumatriptan prescribing information, United Kingdom, 1994Google Scholar
  17. 17.
    Bax NDS, Lennard MS, Tucker GT. Inhibition of antipyrine metabolism by beta-adrenoceptor antagonists. Br J Clin Pharmacol 1981; 12: 779–84PubMedCrossRefGoogle Scholar
  18. 18.
    Fowler PA, Lacey LF, Keene ON, et al. Effect of prophylactic migraine medications on the pharmacokinetic and pharmacodynamic profiles of sumatriptan. Cephalalgia 1991; 11 Suppl. 11: 228–9Google Scholar
  19. 19.
    Kempsford RD, Lacey LF, Thomas M, et al. The effect of alcohol on the pharmacokinetic profile of oral sumatriptan [abstract]. Fundam Clin Pharmacol 1991; 5: 470Google Scholar
  20. 20.
    Friberg L, Olesen J, Iversen HK, et al. Migraine pain associated with middle cerebral artery dilation: reversal by sumatriptan. Lancet 1991; 338: 13–7PubMedCrossRefGoogle Scholar

Copyright information

© Adis International Limited 1994

Authors and Affiliations

  • Andrew K. Scott
    • 1
  1. 1.Department of Geriatric MedicineUniversity of Manchester, Clinical Sciences Building, Hope HospitalSalfordEngland

Personalised recommendations