[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › Triptans (5-HT1B/1D agonists)

# 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.

Updated Nov 1, 2026

## 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

## Key points

- Contraindicated in coronary artery disease, coronary vasospasm, previous stroke or TIA, peripheral vascular disease, ischaemic bowel disease, uncontrolled hypertension and hemiplegic or basilar migraine.
- Not within 24 hours of an ergot alkaloid or another triptan.
- Serotonin syndrome is possible with SSRIs, SNRIs, tricyclics and MAO inhibitors; MAO-A inhibitors are contraindicated with sumatriptan and rizatriptan.
- Chest, throat or jaw tightness is common and usually not cardiac, but high-risk patients get a cardiac evaluation.
- Frequent use (10 or more days a month) can cause medication overuse headache.

## Drugs in this class

- [**Sumatriptan** The 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](https://durgical.com/en/pharmacology/sumatriptan/)
- [**Rizatriptan** A fast oral triptan, also as an orally disintegrating tablet, for migraine attacks; propranolol raises its levels and… Serotonin 5-HT1B and 5-HT1D receptors](https://durgical.com/en/pharmacology/rizatriptan/)
- [**Eletriptan** An oral triptan for migraine attacks, metabolized by CYP3A4: strong CYP3A4 inhibitors such as clarithromycin or… Serotonin 5-HT1B and 5-HT1D receptors](https://durgical.com/en/pharmacology/eletriptan/)

## 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).

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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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7a5f3bb3-147c-49b4-bd62-fdb4af775f8a) (DailyMed (U.S. National Library of Medicine), 2026); [DailyMed - RIZATRIPTAN BENZOATE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=99c66300-bd75-4b31-9fab-88c6e4b12688) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N02CC) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/classes/triptans/