In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan.


Zolmitriptan is a pharmaceutical medication utilized for managing and treating acute migraines. Zolmitriptan belongs to the triptan class of drugs that targets migraine symptoms and provides relief to patients. The underlying cause of migraines can be attributed to localized cranial vasodilatation coupled with the discharge of neuropeptides, including calcitonin gene-related peptide, vasoactive intestinal peptide (VIP), and substance P, within the trigeminal system. Zolmitriptan is a selective 5-hydroxytryptamine (5-HT) 1B/1D receptor agonist with moderate affinity for the 5-HT 1A receptor subtypes. Zolmitriptan's interaction with 5-HT 1B/1D receptors induces vasoconstriction of intracranial blood vessels, concurrently inhibiting the release of proinflammatory neuropeptides from trigeminal perivascular nerve endings. This educational activity provides insights into the applications, mechanism of action, and contraindications of zolmitriptan as a valuable agent in treating acute migraines. This activity also highlights the adverse events, toxicity concerns, and other pivotal considerations, including off-label applications, dosage guidelines, pharmacokinetics, monitoring procedures, and relevant interactions, which are crucial for healthcare practitioners when managing migraine issues and associated ailments in patients.

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