5-HT1B/1D agonist
5-HT1B and 5-HT1D serotonin receptor agonist
- 5-HT1B → cranial vasoconstriction
- 5-HT1D → ↓ trigeminal CGRP release
- Together abort migraine without requiring central action
- 5-HT1B → coronary vasoconstriction → chest tightness, ischemia risk
- ➔ antimigraine effect is peripheral, not CNS
- ➔ vasoconstriction via 5-HT1B
- ➔ inhibition of CGRP release via 5-HT1D
- 1B & 1D are structurally and functionally homologous, making their roles hard to separate
Drugs with this mechanism (12)
- Almotriptan — Triptan (5-HT1B/1D agonist) for acute migraine.
- Dihydroergotamine — Injectable or intranasal ergot for refractory migraine; never combine closely with a triptan.
- Eletriptan — Triptan for acute migraine.
- Ergotamine — Ergot alkaloid for migraine; vasoconstrictive, largely supplanted by triptans.
- Frovatriptan — The longest-acting triptan; useful for menstrual migraine.
- Naratriptan — A slower, longer-acting triptan with fewer side effects.
- Rizatriptan — A fast-acting triptan for migraine.
- Serotonin — The endogenous ligand at fourteen receptor subtypes; the home of serotonicity — synaptic serotonin elevation.
- Sumatriptan — The first triptan; the migraine benchmark, with an injectable form.
- Sumatriptan SC injection — Fastest-acting triptan formulation for migraine and cluster-headache attacks.
- Sumatriptan nasal — Nasal triptan for acute migraine; useful when nausea makes tablets impractical.
- Zolmitriptan — A triptan for migraine, with nasal and orally-dissolving forms.
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