Treatment of migraine with drugs related to 5-hydroxytryptamine

  • P. Tfelt-Hansen
  • T. H. Nielsen
Part of the Developments in CardioCardiovascular Pharmacology of 5-Hydroxytryptamine book series (DICM, volume 106)


The 5-hydroxytryptamine (5-HT) antagonist methysergide was introduced in the prophylaxis of migraine in 1959 [1] and later proved to be quite effective [2]. Ergotamine, one of the traditional drugs used in the treatment of migraine attacks, was later found to act on 5-HT receptors [3]. Recently GR43175, a 5-HT1-like receptor agonist, has been introduced as a new treatment for migraine attacks [4].


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  1. 1.
    Sicuteri F (1959): Prophylactic and therapeutic properties of 1-methyl-lysergic acid butanolamide in migraine. Int Arch Allergy 15: 300–307.PubMedCrossRefGoogle Scholar
  2. 2.
    Pedersen E, Moller CE (1966): Methysergide in migraine prophylaxis. Clin Pharmacol Ther 7: 520–526.PubMedGoogle Scholar
  3. 3.
    Müller-Scweinitzer E (1976): Evidence for stimulation of 5-HT receptors in canine saphenous arteries by ergotamine. Naunyn-Schmiedeberg’s Arch Pharmacol 295: 41–44.CrossRefGoogle Scholar
  4. 4.
    Humphrey PPA, Feniuk W, Perren MJ, Connor, HE, Oxford AW (1989): The pharmacology of the novel 5-HT1-like receptor agonist GR43175. Cephalalgia 9 (Suppl. 9): 23–33.PubMedGoogle Scholar
  5. 5.
    Fanchamps A, Doepfner W, Weidman H, Cerletti A (1960): Pharmakologische Charak- terisierung von Deseril, einem Serotonin-Antagonisten. Schweiz Med Wschr 51: 1040–1046.Google Scholar
  6. 6.
    Saxena PR (1974): Selective vasoconstriction in carotid vascular bed by methysergide: possible relevance to its antimigraine effect. Eur J Pharmacol 27: 99–105.PubMedCrossRefGoogle Scholar
  7. 7.
    Saxena PR, Verdouw PD (1984): Effects of methysergide and 5-hydroxytryptamine on carotid blood flow distribution in pigs: further evidence for the presence of atypical 5-HT receptors. BrJPharmac 82: 817–826.Google Scholar
  8. 8.
    Bianchine JR (1968): Metabolism of methysergide (MS) in the rabbit and man. Fed Proc 27: 238.Google Scholar
  9. 9.
    Bredberg U, Eyjolfdottir GS, Paalzow L, Tfelt-Hansen P, Tfelt-Hansen V (1986): Pharmacokinetics of methysergide and its metabolite methylergometrine in man. Eur J Clin Pharmacol 30: 75–77.PubMedCrossRefGoogle Scholar
  10. 10.
    Berde B, Sturmer E (1978): Introduction to the pharmacology of ergot alkaloids and related compounds as a basis of their therapeutic application, pp. 1–28 in: Berde B, Schild HO (eds), Ergot alkaloids and related compounds. Handbook Exp Pharmacol 49.CrossRefGoogle Scholar
  11. 11.
    Tfelt-Hansen P, Jansen I, Edvinsson L (1987): Methylergometrine antagonizes 5 HT in the temporal artery. Eur J Clin Pharmacol 33: 77–79.PubMedCrossRefGoogle Scholar
  12. 12.
    Flückiger E, del Pozo E (1978): Influence on the endocrine system pp. 615–690 in: Berde B, Schild HO (eds), Ergot alkaloids and related compounds. Handbook Exp Pharmacol 49.CrossRefGoogle Scholar
  13. 13.
    Graham JR, Wolff HG (1938): Mechanism of migraine headache and action of ergotamine tartrate. Arch Neurol Psychiatr 39: 737–763.CrossRefGoogle Scholar
  14. 14.
    Raskin NH (1981): Pharmacology of migraine. Ann Rev Pharmacol Toxicol 21: 463–478.CrossRefGoogle Scholar
  15. 15.
    Markowitz S, Saito K, Moskowitz MA (1988): Neurogenically mediated plasma extravasation in dura mater: Effect of ergot alkaloids. A possible mechanism of action in vascular headache. Cephalalgia 8: 83–91.PubMedCrossRefGoogle Scholar
  16. 16.
    Saxena PR, de Vlaam-Schluter GM (1974): Role of some biogenic substances in migraine and relevant mechanism in antimigraine action of ergotamine-studies in an experimental model for migraine. Headache 13: 142–163.PubMedCrossRefGoogle Scholar
  17. 17.
    Johnston BM, Saxena PR (1978): The effect of ergotamine on tissue blood flow and the arteriovenous shunting of radioactive microspheres in the head. Br J Pharmacol 63: 541–549.PubMedCrossRefGoogle Scholar
  18. 18.
    Bom AH, Heiligers J, Saxena PR, Verdouw, PD (1989): Ergotamine-induced reduction in arteriovenous shunting is not mediated by 5-HT1-like or 5-HT2 receptors. Br J Pharmacol 97: 383–390.PubMedCrossRefGoogle Scholar
  19. 19.
    Olsen TS, Olesen J (1988): Regional cerebral blood flow in migraine and cluster headache, pp. 377–391 in: Olesen J, Edvinsson L (eds), Basic mechanisms of headache . Amsterdam: Elsevier.Google Scholar
  20. 20.
    Andersen AR, Tfelt-Hansen P, Lassen NA (1987): The effect of ergotamine and dihydroergotamine on cerebral blood flow in man. Stroke 18: 120–123.PubMedCrossRefGoogle Scholar
  21. 21.
    Ibraheem JJ, Paalzow L, Tfelt-Hansen P (1982): Kinetics of ergotamine after intravenous and intramuscular administration to migraine sufferers. Eur J Clin Pharmacol 23: 235–240.PubMedCrossRefGoogle Scholar
  22. 22.
    Ibraheem JJ, Paalzow L, Tfelt-Hansen P (1983): Low bioavailability of ergotamine tartrate after oral and rectal administration in migraine sufferers. Br J Clin Pharmacol 16: 695–699.PubMedCentralPubMedCrossRefGoogle Scholar
  23. 23.
    Tfelt-Hansen P (1986): The effect of ergotamine on the arterial system in man. Acta Pharmacol Toxicol 59 suppl. 3: 1–30.Google Scholar
  24. 24.
    Parsons AA, Whalley ET (1989): Characterization of the 5-HT receptor which mediates contraction of the human basilar artery. Cephalalgia 9 (Suppl 9): 47–51.PubMedGoogle Scholar
  25. 25.
    Nielsen TH, Tfelt-Hansen P (1989): Lack of effect of GR43175 on peripheral arteries in man. Cephalalgia 9 (Suppl. 9): 93–95.PubMedGoogle Scholar
  26. 26.
    Doenicke A, Brand J, Perrin VL (1988): Possible benefit of GR43175, a novel 5-HT1- like receptor agonist, for the acute treatment of severe migraine. Lancet 1: 1309–11.PubMedCrossRefGoogle Scholar
  27. 27.
    Perrin VL, Färkkilä M, Goasguen J, Docnicke A, Brand J, Tfilt-Hansen P (1989): Overview of initial clinical studies with intravenous and oral GR43175 in acute migraine. Cephalalgia 9 (Suppl. 9): 63–72.PubMedGoogle Scholar
  28. 28.
    Tfelt-Hansen P, Brand J, Dano P, Doenicke A, Findley LJ, Iversen HK, Melchart D, Sahlender HM (1989): Early clinical experience with subcutaneous GR43175 in acute migraine: an overview. Cephalalgia 9(Suppl 9): 63–72.PubMedGoogle Scholar

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© Springer Science+Business Media Dordrecht 1990

Authors and Affiliations

  • P. Tfelt-Hansen
  • T. H. Nielsen

There are no affiliations available

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