What is the mechanism of action of triptans in migraine treatment?

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Multiple Choice

What is the mechanism of action of triptans in migraine treatment?

Triptans treat migraine by acting as agonists at serotonin 5-HT1B and 5-HT1D receptors. Activation of 5-HT1B receptors on intracranial blood vessels causes vasoconstriction, countering the abnormal dilation linked to migraine. Activation of 5-HT1D receptors on presynaptic trigeminal nerve terminals reduces the release of pain-promoting neuropeptides like CGRP, which dampens trigeminal nerve signaling to the brain. This combination — constricting dilated vessels and inhibiting the neural transmission that drives migraine pain — explains why triptans are effective for acute relief. They are not acting through dopamine D2 antagonism, COX inhibition, or histamine H1 blockade, which underlie other drug classes. Note the vasoconstrictive action means they’re used with care in patients with cardiovascular disease or uncontrolled hypertension.

Triptans treat migraine by acting as agonists at serotonin 5-HT1B and 5-HT1D receptors. Activation of 5-HT1B receptors on intracranial blood vessels causes vasoconstriction, countering the abnormal dilation linked to migraine. Activation of 5-HT1D receptors on presynaptic trigeminal nerve terminals reduces the release of pain-promoting neuropeptides like CGRP, which dampens trigeminal nerve signaling to the brain. This combination — constricting dilated vessels and inhibiting the neural transmission that drives migraine pain — explains why triptans are effective for acute relief. They are not acting through dopamine D2 antagonism, COX inhibition, or histamine H1 blockade, which underlie other drug classes. Note the vasoconstrictive action means they’re used with care in patients with cardiovascular disease or uncontrolled hypertension.

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