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

# Sumatriptan

## Triptans (5-HT1B/1D agonists)?

Triptans (5-HT1B/1D agonists)

The first triptan: a 5-HT1B/1D agonist that stops migraine attacks, by mouth, nose or injection; the injection also treats cluster headache.

Updated Nov 1, 2026

Also called: Sumatriptan succinate

## Quick facts

**Group**
[Triptans (5-HT1B/1D agonists)](https://durgical.com/en/pharmacology/classes/triptans/)

**Target**
Serotonin 5-HT1B and 5-HT1D receptors

**Used for**
Acute treatment of migraine

**Key effects**
Tightness · Tingling · Dizziness

**Monitor**
Blood pressure · Number of treated days per month

**ATC**
N02CC01

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

◎**Serotonin 5-HT1B and 5-HT1D receptors**Sumatriptan

ⓘ The figure shows donitriptan, an experimental triptan, in the serotonin-binding pocket of the human 5-HT1B receptor; sumatriptan binds the same pocket.

**Target in 3D:** Serotonin 5-HT1B and 5-HT1D receptors. PDB structure 6G79 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6G79) · Drag to rotate · pinch to zoom

Sumatriptan is a serotonin analogue that binds 5-HT1B and 5-HT1D receptors with high affinity. On intracranial blood vessels it causes constriction; on sensory endings of the trigeminal nerve it inhibits the release of pro-inflammatory neuropeptides. Together these effects interrupt the pain of a migraine attack. It treats attacks and does not prevent them.

- Sumatriptan activates 5-HT1B/1D receptors
- Dilated intracranial vessels constrict
- Trigeminal endings release less inflammatory neuropeptide
- The migraine attack eases

## Indications

- Acute treatment of migraine with or without aura [Migraine →](https://durgical.com/en/conditions/migraine/)
- Acute treatment of cluster headache (subcutaneous injection) [Cluster headache →](https://durgical.com/en/conditions/cluster-headache/)

## Adverse effects

### Common

- Tightness, pressure or pain in the chest, throat, neck or jaw (usually not cardiac)
- Tingling, numbness, warm or cold sensations and flushing
- Dizziness, vertigo and tiredness
- Pain, burning or redness at the injection site

### Serious (rare, important)

- Myocardial ischaemia, infarction and coronary vasospasm, sometimes in people without known heart disease
- Life-threatening arrhythmias (ventricular tachycardia, ventricular fibrillation)
- Stroke and brain haemorrhage; bowel or peripheral ischaemia
- Serotonin syndrome, especially with SSRIs, SNRIs, tricyclics or MAO inhibitors
- Medication overuse headache with frequent use
- Rise in blood pressure, rarely hypertensive crisis; seizures

## Contraindications

- Ischaemic coronary artery disease or coronary vasospasm (including Prinzmetal angina)
- History of stroke or TIA; hemiplegic or basilar migraine
- Peripheral vascular disease and ischaemic bowel disease
- Uncontrolled hypertension
- Another triptan or an ergot alkaloid in the previous 24 hours
- Wolff-Parkinson-White syndrome or other accessory pathway arrhythmias
- An MAO-A inhibitor now or in the past 2 weeks
- Severe liver impairment

## Key interactions

**MAO-A inhibitors**
Much higher sumatriptan exposure; contraindicated

**Ergotamine, dihydroergotamine or another triptan within 24 hours**
Additive, prolonged vasospasm; contraindicated

**SSRIs, SNRIs, tricyclic antidepressants**
Serotonin syndrome

## What is monitored

- Cardiovascular evaluation before the first dose in people with several risk factors (age, diabetes, hypertension, smoking, obesity, family history)
- Blood pressure
- Number of treated days per month (medication overuse headache)

## Administration and safety

- Used at the start of the headache phase; it is not a preventive
- The injection is for subcutaneous use only; coronary vasospasm has followed intravenous use
- If the first attack does not respond, the diagnosis is reconsidered before treating more attacks

## Pregnancy and breastfeeding

Pregnancy registry and epidemiological data have not shown an increased rate of birth defects; the decision weighs the benefit for the mother.

## Nursing care

- Before the first dose, ask about chest pain, heart disease, stroke, high blood pressure and cardiovascular risk factors
- Check the medication list for ergots, other triptans, MAO inhibitors and serotonergic antidepressants
- Explain that chest or throat tightness is common, but crushing chest pain needs urgent care
- Encourage a headache diary to spot medication overuse
- Teach signs of serotonin syndrome: agitation, fever, sweating, tremor, muscle jerks

## Pharmacokinetics

**Absorption**
Low oral bioavailability because of first-pass liver metabolism; subcutaneous bioavailability is almost complete

**Metabolism**
Mainly MAO-A, to an inactive indoleacetic acid metabolite

**Half-life**
About 2 to 2.5 hours

**Onset and duration**
Subcutaneous injection: relief can begin within about 10 minutes

## Memory aid

«Triptan = Tight vessels»: sumatriptan narrows cranial vessels to stop the attack, so diseased coronary arteries are a hard stop.

## Test yourself

Think of the answer, then tap the question to see it.

## Which receptors does sumatriptan stimulate?

Serotonin 5-HT1B and 5-HT1D receptors.

## Why is sumatriptan contraindicated in coronary artery disease?

It can constrict coronary arteries and cause ischaemia, infarction or vasospasm.

## Which headache besides migraine does subcutaneous sumatriptan treat?

Cluster headache.

## How long must separate sumatriptan from an ergot alkaloid?

At least 24 hours.

## Which enzyme metabolizes sumatriptan, explaining the MAOI contraindication?

Monoamine oxidase A (MAO-A).

[Add to my cards (5)](https://durgical.app/estudiar/?add=/en/pharmacology/sumatriptan/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 5

- [Rizatriptan](https://durgical.com/en/pharmacology/rizatriptan/)
- [Eletriptan](https://durgical.com/en/pharmacology/eletriptan/)
- [Ergotamine](https://durgical.com/en/pharmacology/ergotamine/)
- [Erenumab](https://durgical.com/en/pharmacology/erenumab/)
- [Propranolol](https://durgical.com/en/pharmacology/propranolol/)

## Related conditions 2

- [Migraine](https://durgical.com/en/conditions/migraine/)
- [Cluster headache](https://durgical.com/en/conditions/cluster-headache/)

[← Back to the class: Triptans (5-HT1B/1D agonists)](https://durgical.com/en/pharmacology/classes/triptans/)

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 - SUMATRIPTAN SUCCINATE injection](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0e8b65f7-9d3b-42f2-8d7e-69b143365980) (DailyMed (U.S. National Library of Medicine), 2026); [Sumatriptan: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a601116.html) (MedlinePlus (U.S. National Library of Medicine), 2026).

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Representative model, for educational purposes only.

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