Zolmitriptan

Mechanism of action:
Zolmitriptan is a serotonin 5-HT₁B/5-HT₁D receptor agonist belonging to the triptan class. Its action is focused on the trigeminovascular system, including intracranial trigeminal nerves and surrounding blood vessels. It stimulates 5-HT₁B receptors on the smooth muscle of intracranial blood vessels, especially those in the dura mater, increasing vascular tone and inducing vasoconstriction. It also stimulates 5-HT₁D receptors at trigeminal nerve terminals, reducing the release of pro-inflammatory and pain-mediating neuropeptides such as calcitonin gene-related peptide and substance P, thereby decreasing neurogenic inflammation and pain transmission.
Reference(s):
1. Martin GR et al. (1997). Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia.
2. Rubio-Beltran E et al. (2018). Is selective 5-HT1F receptor agonism an entity apart from that of the triptans in antimigraine therapy? Pharmacol Ther.
3. Goadsby PJ et al. (2017). Pathophysiology of Migraine: A Disorder of Sensory Processing. Physiol Rev.
