Rationale for the use of 5-HT1-like agonists in the treatment of migraine.
Migraine headache is thought to be associated with a dilatation of cranial blood vessels, particularly those in the dura mater, and an accompanying localized sterile inflammatory response. Sumatriptan is a highly selective 5-HT1-like receptor agonist which selectively constricts cranial blood vessels (including those in the dura mater). It also inhibits neurogenically-mediated plasma protein extravasation in the dura mater. Haemodynamic studies in anaesthetized animals have shown that sumatriptan selectively constricts the carotid arterial circulation and this effect appears to be restricted to an effect on carotid arteriovenous anastomoses. Sumatriptan has a much more selective pharmacological profile than ergot preparations which are also used in the acute treatment of migraine. The development of sumatriptan has been based on a vascular theory of migraine and its high degree of efficacy in the treatment of migraine strengthens the argument that dilatation of cranial blood vessels is the cause of vascular headache.
Feniuk
W
W
Pharmacology Division, Glaxo Group Research Ltd., Ware, UK.
Humphrey
P P
PP
Perren
M J
MJ
Connor
H E
HE
Whalley
E T
ET
D000818:Animals; D001798:Blood Proteins / Q000187:drug effects; D002339:Carotid Arteries / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000627:therapeutic use*; D008881:Migraine Disorders / Q000188:drug therapy*; D011985:Receptors, Serotonin / Q000187:drug effects; D012039:Regional Blood Flow / Q000187:drug effects; D013449:Sulfonamides / Q000737:chemistry / Q000627:therapeutic use*; D018170:Sumatriptan; D014662:Vasoconstrictor Agents / Q000627:therapeutic use*
D001798:Blood Proteins; D007211:Indoles; D011985:Receptors, Serotonin; D013449:Sulfonamides; D014662:Vasoconstrictor Agents; D018170:Sumatriptan