Serotonin Receptor Agonists

Antimigrene Agents

Sumatriptan

Rizatriptan

• 5-HT1B/1D receptor agonists that cause:

  • Vasoconstriction of (dilated) cranial and basilar arteries

  • Inhibition of trigeminal nerve nociception

  • Inhibition of vasoactive peptide secretion

• Most effective if taken at the onset of headache

• Migraine headaches

• Cluster headaches

• Vasospasm of coronary vessels → coronary ischemia (rare)

• Paresthesia and sensation of cold in the extremities

• Serotonin syndrome (if taken with other 5-HT agonists)

• Temporary blood pressure increase (very common)

• Dizziness, malaise, flashes

• Frequent intake (≥ 10 x/month) can lead to headaches.

• Hypertension

• Coronary artery disease

• Vasospastic angina

• Peripheral artery disease

• Hypertension

Remember to check for drug interactions (e.g., with SSRIs or macrolides) before starting triptans or ergotamines to avoid adverse events. Coronary spasm and/or serotonin syndrome can occur if triptans and ergotamines are combined.

A SUMo wrestler TRIPs ANd falls on his head: SUMaTRIPtANs are used for headaches (cluster and migraine).