Dihydroergotamine, ergotamine, methysergide and sumatriptan - basic science in relation to migraine treatment

Headache. 2012 Apr;52(4):707-14. doi: 10.1111/j.1526-4610.2012.02124.x. Epub 2012 Mar 22.

Abstract

The 5-hydroxytryptamine (5-HT) receptor family mediates the effects of several drugs highly effective in migraine primarily by activating 5-HT(1B) , 5-HT(1D) , and 5-HT(1F) receptors. Ergotamine, dihydroergotamine, and methysergide, as well as the "triptan" sumatriptan, are all agonists for these receptors. The receptor profile and degree of selectivity of these four drugs differ, which is reflected by their side effects that limit their use in the acute and prophylactic treatment of migraine. The acute antimigraine efficacy of these remedies is very much dependent on the formulation used where, in general, parenteral formulations are more effective in reliving the symptoms of a migraine attack.

Publication types

  • Review

MeSH terms

  • Animals
  • Dihydroergotamine / chemistry
  • Dihydroergotamine / pharmacokinetics
  • Dihydroergotamine / therapeutic use*
  • Ergotamine / chemistry
  • Ergotamine / pharmacokinetics
  • Ergotamine / therapeutic use*
  • Humans
  • Methysergide / chemistry
  • Methysergide / pharmacokinetics
  • Methysergide / therapeutic use*
  • Migraine Disorders / drug therapy*
  • Migraine Disorders / metabolism
  • Sumatriptan / chemistry
  • Sumatriptan / pharmacokinetics
  • Sumatriptan / therapeutic use*
  • Treatment Outcome

Substances

  • Dihydroergotamine
  • Sumatriptan
  • Ergotamine
  • Methysergide