title: Drugs targeting 5-hydroxytryptamine receptors in acute treatments of migraine attacks. A review of new drugs and new administration forms of established drugs.
abstract: BACKGROUND
  The development of sumatriptan, more than 20 years ago, added substantially to the characterization of 5-hydroxytryptamine (5-HT) receptors and their relevance to acute migraine therapy. Recently, 5-HT1F receptor agonists, with no vascular effects, have shown efficacy in the treatment of migraines.
  
  
  METHODS
  This evaluation reviews the recent advances in acute migraine therapy targeting the 5-HT receptor. Specifically, the authors review the pharmacokinetics, pharmacodynamics, clinical efficacy and safety of 5-HT1F receptor agonists and new formulations of sumatriptan and dihydroergotamine (DHE).
  
  
  CONCLUSIONS
  Lasmiditan, a non-vascular acting 5-HT1F receptor agonist, is effective in migraine but causes central nervous system-related adverse events, which may considerably limit its clinical use. The efficacy of transdermal sumatriptan is too low for general use in migraine. Intranasal sumatriptan powder could be a step forward compared with oral sumatriptan, but comparative trials are needed. Orally inhaled DHE has a very quick systemic absorption but the onset of effect in migraine is relatively slow with a maximum effect after 2 h. In contrast, orally inhaled DHE results in a low incidence of recurrence. None of these reviewed treatments are likely to fulfill patients' expectations, and the advancement of acute migraine drugs should likely depend on different mechanisms from current 5-HT-related drugs.
authors.affiliation: University of Copenhagen, Glostrup Hospital, Danish Headache Center, Department of Neurology , N39, DK-2600, Glostrup , Denmark ptha@regionh.dk.
authors.forename: Peer C
authors.initials: PC
authors.lastname: Tfelt-Hansen
authors.forename: Thomas
authors.initials: T
authors.lastname: Pihl
authors.forename: Anders
authors.initials: A
authors.lastname: Hougaard
authors.forename: Dimos D
authors.initials: DD
authors.lastname: Mitsikostas
mesh_terms: D000818:Animals; D001549:Benzamides / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D004333:Drug Administration Routes; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy* / Q000378:metabolism; D010880:Piperidines / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011725:Pyridines / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011985:Receptors, Serotonin / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D014363:Tryptamines / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D001549:Benzamides; D010880:Piperidines; D011725:Pyridines; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; C554777:lasmiditan