The Sound of Evolution
Sumatriptan
Mechanism of action:
Sumatriptan is a selective 5-HT1B/5-HT1D receptor agonist and belongs to the triptan class. Its action is focused on the trigeminovascular system, including intracranial trigeminal nerves and surrounding blood vessels. Sumatriptan stimulates 5-HT1B receptors on vascular smooth muscle in intracranial vessels, especially those of 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-related neuropeptides such as calcitonin gene-related peptide and substance P, thereby decreasing neurogenic inflammation and pain transmission.
Reference(s):
1. Nikai T et al. (2008). Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain.
2. Ferrari MD et al. (1992). Clinical effects and mechanism of action of sumatriptan in migraine. Clin Neurol Neurosurg.
3. Duquesnoy C et al. (1998). Comparative clinical pharmacokinetics of single doses of sumatriptan following subcutaneous, oral, rectal and intranasal administration. Eur J Pharm Sci.