Zolmitriptan is a selective agonist of serotonin 5HT1B / 1D receptors, the stimulation of which leads to vasoconstriction. It has a high affinity for recombinant human serotonin 5HT1B / 1D receptors and a moderate affinity for serotonin 5HT1A receptors. Zolmitriptan has no affinity and does not show significant pharmacological activity in relation to serotonin 5HT2, 5HT3, 5HT4, adrenergic, histamine, muscarinic and dopaminergic receptors.
Zolmitriptan administration to laboratory animals resulted in vasoconstriction in the carotid artery basin. In addition, the results of studies in laboratory animals indicate that zolmitriptan blocks the central and peripheral activity of the trigeminal nerve by inhibiting the release of the peptide associated with the calcitonin gene, vasoactive intestinal peptide and substance P.
In clinical studies, the effect of zolmitriptan on headache and other migraine symptoms (such as nausea, photophobia, phonophobia) was observed after 1 hour and increased in the period from 2 to 4 hours after taking the drug.
Zolmitriptan is equally effective for migraine with aura, migraine without aura, and migraine associated with menstruation. Taking zolmitriptan during aura did not prevent migraine headache, so the drug should be taken after the onset of a painful attack.