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Mechanisms of action of sumatriptan and ergotamine

Last reviewed dd mmm yyyy. Last edited dd mmm yyyy

Authoring team

Sumatriptan:

  • highly selective agonist of the D subtype of 5-HT1 - these are located on peripheral trigeminal-nerve terminals that supply pain-sensitive vascular and meningeal structures.
  • selective for a subtype of 5-HT1 receptors located on intracranial vessels, where it mediates contraction, particularly of large arteries - the direct vasoconstrictive action of sumatriptan may also alleviate headache.
  • calcitonin-gene-related peptide is released into jugular venous blood during a migraine attack - this release is blocked by sumatriptan.
  • blocks the neuropeptide-mediated inflammatory response after trigeminal stimulation.

Ergotamine:

  • has high affinity but less selectively for 5-HT1 receptors.
  • dihydroergotamine is a potent venoconstrictor - also has arterial vasoconstrictor effects, which may alleviate headache.

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