Triptans

Summary

Triptans, which include the archetypal drug sumatriptan, are a class of drugs used to treat headaches. They act as agonists or activators of Serotonin receptors, specifically the serotonin 1B and 1D receptors in the trigeminal nerve and blood vessels in the brain. This agonist activity inhibits the release and delivery of vasoactive peptides that cause inflammation associated with headache disorders. Specifically, triptans are used in the acute treatment of migraine and cluster headaches. An important side effect of taking triptans is the development of coronary vasospasms. As such, these drugs are contraindicated in patients with a history of coronary artery disease or Prinzmetal angina. Another important side effect to remember is serotonin syndrome, which is more common if triptans are given with other serotonin-modulating drugs.

Key Points

• Triptans (Sumatriptan)
  • Mechanism
    • Serotonin 5-HT1B/1D agonists
      • Inhibits the release of vasoactive peptides, promoting vasoconstriction
      • Inhibits trigeminal nerve activation
      • Blocks pain pathways in the brainstem
  • Clinical Use
    • Abortion of acute migraine
      • Involved in the abortive therapy of migraine headaches
      • Ergotamine can be used as an alternative
    • Cluster headache
      • First-line in the treatment of acute cluster headaches, along with 100% oxygen
  • Adverse Effects
    • Coronary vasospasm
      • Contraindicated in patients with CAD or vasospastic angina
    • Mild paresthesia
    • Serotonin syndrome (in combination with other 5-HT agonists)
      • Any drug that alters serotonin signaling can cause serotonin syndrome