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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

Also called: Sumatriptan succinate

Quick facts

Group
Triptans (5-HT1B/1D agonists)
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.

Mechanism of action

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

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.

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

Indications

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

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

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).

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Connections

← Back to the class: Triptans (5-HT1B/1D agonists)

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 - SUMATRIPTAN SUCCINATE injection (DailyMed (U.S. National Library of Medicine), 2026); Sumatriptan: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).

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Representative model, for educational purposes only.