How do triptans relieve acute migraine symptoms?

How do triptans relieve acute migraine symptoms?

• A. They are 5-HT1B/1D receptor agonists that cause cranial vasoconstriction and inhibit release of pro-inflammatory peptides from trigeminal nerve endings, reducing pain signaling.
• B. They block CGRP signaling.
• C. They inhibit COX enzymes.
• D. They antagonize adrenergic receptors.

Answer: (A)

Triptans relieve acute migraine by acting on the trigeminovascular system through selective serotonin receptor activation. They bind to 5-HT1B and 5-HT1D receptors. Activation of 5-HT1B receptors on cranial blood vessels causes vasoconstriction, countering migraine-related vasodilation. Activation of 5-HT1D receptors on trigeminal nerve endings inhibits the release of pro-inflammatory peptides like CGRP, reducing neurogenic inflammation and pain signaling. Together, these actions decrease nociceptive transmission and alleviate migraine symptoms. This mechanism is distinct from blocking CGRP signaling, inhibiting COX enzymes, or antagonizing adrenergic receptors, which explains why the receptor-mediated vasoconstriction and peptide-release inhibition best describes how triptans work.

Triptans relieve acute migraine by acting on the trigeminovascular system through selective serotonin receptor activation. They bind to 5-HT1B and 5-HT1D receptors. Activation of 5-HT1B receptors on cranial blood vessels causes vasoconstriction, countering migraine-related vasodilation. Activation of 5-HT1D receptors on trigeminal nerve endings inhibits the release of pro-inflammatory peptides like CGRP, reducing neurogenic inflammation and pain signaling. Together, these actions decrease nociceptive transmission and alleviate migraine symptoms. This mechanism is distinct from blocking CGRP signaling, inhibiting COX enzymes, or antagonizing adrenergic receptors, which explains why the receptor-mediated vasoconstriction and peptide-release inhibition best describes how triptans work.