Triptans (5-HT1B/1D agonists)
Serotonin 5-HT1B/1D agonists that stop a migraine attack. They narrow vessels, so they are not used in coronary or cerebrovascular disease.
What they are
Triptans are indole derivatives used for the acute treatment of migraine with or without aura; they are not preventive. They differ mainly in speed, duration, route (tablet, orally disintegrating tablet, nasal spray, injection) and metabolism. Subcutaneous sumatriptan is also used for cluster headache.
Mechanism of action
Triptans stimulate 5-HT1B/1D receptors on intracranial blood vessels, which constrict, and on sensory endings of the trigeminal nerve, which release less pro-inflammatory neuropeptide (successful treatment goes with lower CGRP levels). Pain signalling through the trigeminovascular system falls.
Target: Serotonin 5-HT1B and 5-HT1D receptors
Drugs in this class
- SumatriptanThe first triptan: a 5-HT1B/1D agonist that stops migraine attacks, by mouth, nose or injection; the injection also…Serotonin 5-HT1B and 5-HT1D receptors
- RizatriptanA fast oral triptan, also as an orally disintegrating tablet, for migraine attacks; propranolol raises its levels and…Serotonin 5-HT1B and 5-HT1D receptors
- EletriptanAn oral triptan for migraine attacks, metabolized by CYP3A4: strong CYP3A4 inhibitors such as clarithromycin or…Serotonin 5-HT1B and 5-HT1D receptors
Others in the class
- Naratriptan
- Zolmitriptan
- Almotriptan
- Frovatriptan
Test yourself
Think of the answer, then tap the question to see it.
Which receptors do triptans stimulate?
Serotonin 5-HT1B (vessels) and 5-HT1D (trigeminal nerve endings).
Which three cardiovascular conditions contraindicate triptans?
Coronary artery disease, previous stroke or TIA, and uncontrolled hypertension (also Prinzmetal angina, peripheral vascular disease).
Are triptans used to prevent migraine?
No; they treat attacks. Prevention uses other medicines (e.g., propranolol, topiramate, CGRP antibodies).
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - SUMATRIPTAN tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); DailyMed - RIZATRIPTAN BENZOATE tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.