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Zolmitriptan

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An Erratum to this article was published on 01 July 1997

Abstract

  • ▲ Zolmitriptan is indicated for the acute treatment of migraine with and without aura.

  • ▲ The drug is a serotonin 5-HT1B/1D receptor agonist that has little or no affinity for other serotonin receptors or receptors of other neurotransmitters.

  • ▲ Preclinical studies indicate that zolmitriptan has a novel dual mechanism of action, having effects at both central (trigeminal nucleus caudalis) and peripheral (trigeminovascular system) targets.

  • ▲ Studies in volunteers demonstrate that zolmitriptan has relatively good oral bioavailability.

  • ▲ Zolmitriptan is effective in alleviating migraine headache and also nonheadache symptoms such as photophobia, phonophobia and nausea.

  • ▲ The tolerability of zolmitriptan is good, with the most common adverse experiences being paresthesia, asthenia, nausea, somnolence and dizziness. Heaviness, tightness or pressure in the chest have been reported, but have not been associated with ECG abnormalities.

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References

  1. Lipton RB, Stewart WF, von Korff M. Burden of migraine: societal costs and therapeutic opportunities. Neurology 1997; 48Suppl. 3: S4–9

    Article  PubMed  CAS  Google Scholar 

  2. Heachache Classification Committee of the International Headache Society. Classification and diagnostic criteria for headache disorders, cranial neuralgias and facial pain. Cephalalgia 1988; 8 Suppl. 11:87–8

    Google Scholar 

  3. Lance JW. Current concepts of migraine pathogenesis. Neurology 1995; 43Suppl. 3: S11–5

    Google Scholar 

  4. Martin GR. Pre-clinical profile of the novel 5-HT1D receptor agonist 311C90. New Advances in Headache Research. 10th Migraine Trust Symposium; 1994 Sep; London, Pt 4: 3–4

  5. Martin GR. 5-HT1D agonist drugs in acute migraine treatment: current perspectives [abstract]. 311C90: Potential for Improving Patient Care. 3rd European Headache Conference; 1996 Jun 5-8; Sardinia, 6–7

  6. Martin GR, Dixon R. Pre-clinical and clinical pharmacology of the novel antimigraine compound 311C90 [poster]. 37th Annual Scientific Meeting of the American Association for the Study of Headache; 1995 Jun 23-25; Boston

  7. Martin GR. Receptor pharmacology of 183C91, the N-desmethyl metabolite of 311C90. Zeneca Pharmaceuticals (Macclesfield). BB10/94/0005; Sep 12, 1994. (Data on file)

    Google Scholar 

  8. Ferrari MD, Martin GR, Earl NL, et al. Emerging preclinical and clinical profile of 311C90: a poster review and discussion. Eur Neurol 1996; 36Suppl. 2: 19–23

    Article  PubMed  CAS  Google Scholar 

  9. Knight YE, Goadsby PJ. Central nervous system distribution of [3H]-311C90 in cat [abstract no. P12]. Cephalalgia 1995; 15Suppl. 14: 214

    Google Scholar 

  10. Mills A, Rhodes P, Martin GR. [3H]311C90 binding sites in cat brain stem: implications for migraine treatment [abstract no. P201]. Cephalalgia 1995; 15Suppl. 14: 116

    Google Scholar 

  11. Mills A, Martin GR. Labelling of cat brainstem sections with [3H]311C90 and the 5-HT3 receptor ligand [3H]BRL43694 [abstract no. P11]. Cephalalgia 1995; 15Suppl. 14: 213

    Google Scholar 

  12. Martin GR. Inhibition of the trigemino-vascular system with 5-HT1D agonist drugs: selectively targeting additional sites of action. Eur Neurol 1996; 36Suppl. 2: 13–8

    Article  PubMed  CAS  Google Scholar 

  13. Goadsby PJ, Edvinsson L. Peripheral and central trigeminovascular activation in cat is blocked by the serotonin (5HT)-1D receptor agonist 311C90. Headache 1994 Jul-Aug; 34: 394–9

    Article  PubMed  CAS  Google Scholar 

  14. Martin GR, MacLennan SJ, Cambridge D, et al. Effect of 311C90 on regional blood flows and systemic haemodynamics in anaesthetised dogs and cats [abstract no. 27]. Cephalalgia 1994; 15Suppl. 14: 311

    Google Scholar 

  15. Shepheard SL, Williamson DJ, Cook D, et al. Studies of the sympatholytic effects of some 5-HT1D receptor agonists in pithed rats and guinea pigs [abstract no. 58]. Headache Treatment Trial Methodology and New Drugs. 6th International Headache Research Seminar: 1995 Nov 17-19; Copenhagen

  16. Seaber E, On N, Phillips S, et al. The tolerability and pharmacokinetics of the novel antimigraine compound 311C90 in healthy male volunteers. Br J Clin Pharmacol 1996 Feb; 41: 141–7

    Article  PubMed  CAS  Google Scholar 

  17. Dixon R, On N, Seaber E, et al. Lack of an interaction between 311C90, a novel antimigraine compound, and oral ergotamine in healthy subjects [poster]. 37th Annual Scientific Meeting of the American Association for the Study of Headache; 1995 Jun 23-25; Boston

  18. Seaber E, Mohanlal R, Gillotin C, et al. Lack of interaction between pizotifen and the novel anti-migraine compound 311C90 [poster]. 11th Migraine Trust International Symposium; 1996 Sep 9-12; London

  19. Seaber E, Dixon R, Gillotin C, et al. Study of the interaction between propranolol and the novel anti-migraine compound 311C90 [poster]. 11th Migraine Trust International Symposium; 1996 Sep 9-12; London

  20. Veronese L, Gillotin C, Marion-Gallois R, et al. Lack of an interaction between oral dihydroergotamine and the novel antimigraine compound [poster]. 3rd European Headache Conference; 1996 Jun 5-8; Sardina

  21. Seaber E, Dixon R, Jackson S, et al. The pharmacodynamic effects of 311C90, a novel antimigraine compound, in healthy young and elderly subjects [abstact no. 28b]. Functional Neurology 1996; 11(2-3): 153

    Google Scholar 

  22. Dixon R, Gillotin C, Posner J, et al. The pharmacokinetics and effects on blood pressure of multiple doses of the novel antimigraine drug zolmitriptan (311C90) in healthy volunteers. Br J Clin Pharmacol 1997; 43: 273–81

    Article  PubMed  CAS  Google Scholar 

  23. Smith DA, Phillips L, Fleck RJ, et al. 311C90 in normotensive and mild to moderate hypertensive volunteers: a pharmacodynamic and pharmacokinetic comparison [poster]. 7th International Headache Congress; 1995 Sep 16-20; Toronto

  24. Earl NL. Clinical safety of 311C90: aggregated data from patients and volunteers to date. Eur Neurol 1996; 36Suppl. 2: 8–12

    Article  PubMed  CAS  Google Scholar 

  25. Thomsen LL, Dixon R, Lassen LH, et al. 311C90 (zolmitriptan), a novel centrally and peripheral acting oral 5-hydroxytryptamine-lD agonist: a comparison of its absorption during a migraine attack and in a migraine-free period. Cephalalgia 1996 Jun; 16: 270–5

    Article  PubMed  CAS  Google Scholar 

  26. Mercer AJ, Lamb RJ, Gibbens M, et al. The effects of 311C90, a novel 5HT1D agonist, lorazepam and placebo on psychometric task performance in healthy volunteers [poster]. 37th Annual Scientific Meeting of the American Association for the Study of Headache; 1995 Jun 23-25; Boston

  27. Visser WH, Klein KB, Cox RC. 311C90, a new central and peripherally acting 5-HT1D receptor agonist in the acute oral treatment of migraine: a double-blind, placebo-controlled, dose-range finding study. Neurology 1996 Feb; 46: 522–6

    Article  PubMed  CAS  Google Scholar 

  28. Dahlof C, Diener HC, Goadsby PJ, et al. 311C90 in the acute oral treatment of migraine: a dose-range finding study to investigate the efficacy and safety in outpatients [poster]. 37th Annual Scientific Meeting of the American Association for the Study of Headache; 1995 Jun 23-25; Boston

  29. Dixon R, On N, Posner J. Oral bioavailability of the novel 5-HT1D agonist 311C90 [poster]. 7th International Headache Congress; 1995 Sep 16-20; Toronto

  30. Seaber E, Peck RW, Ridour G, et al. The minimal interaction between 311C90, a novel antimigraine compound, and oral paracetamol and metoclopramide, in healthy subjects [poster]. 3rd International Headache Conference; 1996 Jun 5-8; Sardinia

  31. Goadsby PJ, Hoskin KL. Inhibition of trigeminal neurons by intravenous administration of the serotonin (5HT)(1B/D) receptor agonist zolmitriptan (311C90): are brain stem sites therapeutic target in migraine? Pain 1996 Oct; 67: 355–9

    Article  PubMed  CAS  Google Scholar 

  32. Honey AC. Effect of 311C90 and sumatriptan on neurogenic plasma extravasation and extracranial blood flow in anaesthetised guinea-pigs. Zeneca Pharmaceuticals (Macclesfield). BBAH/93/0001; Dec 22 1993. (Data on file)

    Google Scholar 

  33. Hoskin KL, Knight YE, Goadsby PJ. Zolmitriptan inhibits c-fos expression in the dorsal horn of the medulla and upper cervical horn evoked by sagittal sinus stimulation in the cat [abstract]. Cephalalgia 1996 Aug; 16: 355

    Article  Google Scholar 

  34. Seaber E, On N, Dixon R, et al. The metabolic disposition of the novel antimigraine compound 311C90 [poster]. 7th International Headache Conference; 1995 Sep 16-30; Toronto

  35. Seaber E, On N, Jackson S, et al. Similar pharmacokinetics and tolerability of the novel anti-migraine compound 311C90 in young and elderly volunteers [poster]. 7th International Headache Congress; 1995 Sep 16-20; Toronto

  36. Ferrari MD. 311C90: increasing the options for therapy with effective acute antimigraine 5HT1B/1D receptor agonists. Neurology 1997; 48(3) Suppl. 3: S21–4

    Article  PubMed  CAS  Google Scholar 

  37. 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 

  38. Rapoport AM, Cady RK, Matthew NT, et al. Optimizing the oral dose of 311C90 in the acute treatment of migraine [abstract and poster]. 6th International Headache Research Seminar: 1995 Nov 17-19; Copenhagen

  39. Lowy M, Cady R. 2.5mg of 311C90 in acute treatment of migraine: efficacy and safety [abstract]. 2nd Congress of the European Federation of Neurological Societies; 1996 Oct 30-Nov 3; Rome

  40. Diener HC, Klein KB, for the Multinational Oral 311C90 and Sumatripan Comparative Study Group. The first comparison of the efficacy and safety of 311C90 and sumatriptan in the treatment of migraine [poster]. 3rd European Headache Conference; 1996 Jun 5-8; Sardinia

  41. Visser WH, Ferrari MD, Klein KB. An in-patient, placebo-controlled, dose-ranging study of oral 311C90 in the acute treatment of migraine [abstract]. Headache 1995 May; 35: 291

    Google Scholar 

  42. Zagami AS. 311C90: long term efficacy and tolerability profile of for the acute treatment of migraine. Neurology 1997; 48(3) Suppl. 3: S25–8

    Article  PubMed  CAS  Google Scholar 

  43. Sweet R, Klein KB. 311C90 is effective in good, fair and poor responders to existing therapies for acute migraine [abstract]. 6th International Headache Research Seminar: 1995 Nov 17-19; Copenhagen

  44. Dalessio DJ, Brown DL, Solbach P. Oral 311C90 is effective in treatment of menstrual migraine [abstract]. Cephalalgia 1996 Aug; 16: 400–1

    Google Scholar 

  45. Sweet RM, Brown DL, Walker A. The high efficacy of 311C90 in treating migraine headache is maintained in patients using oral contraceptives [abstract]. Cephalalgia 1996 Aug; 16: 396

    Google Scholar 

  46. Dowson A. Can oral 311C90, a novel 5-HT1D agonist, prevent migraine headache when taken during an aura? Eur Neurol 1996; 36Suppl. 2: 28–31

    Article  PubMed  CAS  Google Scholar 

  47. Tfelt-Hansen P. Experience with 311C90 in a long-term clinical setting [abstract]. 311C90: potenial for improving patient care. 3rd European Headache Conference; 1996 Jun 5-8; Sardinia, 16–7

  48. Earl NL. 311C90, a new acute treatment of migraine: an overview of safety [poster]. 7th International Headache Congress; 1995 Sep 16-20; Toronto

  49. Giorgi L, Dixon R, Touw K. Cardiovascular safety of the novel anti-migraine compound 311C90 [poster]. 7th International Headache Congress; 1996 Sep 16-20; Toronto

  50. Schoenen J, Klein KB, for the Multinational Oral 311C90 and Sumatriptan Comparative Study Group. 311C90 and sumatriptan produce indistinguishable CNS adverse event profiles [abstract]. Cephalalgia 1996 Aug; 16: 389–90

    Article  Google Scholar 

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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Katharine J. Palmer & Caroline M. Spencer

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  1. Katharine J. Palmer
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  2. Caroline M. Spencer
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Correspondence to Katharine J. Palmer.

Additional information

An erratum to this article is available at http://dx.doi.org/10.1007/BF03260135.

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Palmer, K.J., Spencer, C.M. Zolmitriptan. CNS Drugs 7, 468–478 (1997). https://doi.org/10.2165/00023210-199707060-00005

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  • DOI: https://doi.org/10.2165/00023210-199707060-00005

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