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Triptan

Sumatriptan

A 5-HT1B/1D agonist that relieves migraine and cluster headache attacks, given as tablets, nasal spray or injection.

Drug card

Class
Triptan
How it works
Activating 5-HT1B/1D receptors to constrict cranial vessels in migraine
Used for
  • Acute migraine attacks, with or without aura
  • Cluster headache attacks
Known for
  • Tightness in the chest, throat, neck or jaw
  • Coronary spasm, heart attack or stroke
Its name
-triptan means a 5-HT1B/1D agonist for migraine (triptan)

Study it as a flashcard, and it comes back before you forget it.

Mechanism of action

How does sumatriptan work?

Binds strongly to 5-HT1B and 5-HT1D receptors on intracranial vessels and trigeminal sensory nerves, so the cranial vessels constrict and less pro-inflammatory neuropeptide is released. It is broken down by monoamine oxidase, mainly MAO-A, so MAO-A inhibitors roughly double the amount in the blood.

Uses

What is sumatriptan used for?

  • Acute migraine attacks, with or without aura
  • Cluster headache attacks

Side effects

Side effects of sumatriptan

  • Tightness in the chest, throat, neck or jawKnown for
  • Coronary spasm, heart attack or strokeKnown forSerious
  • Tingling, numbness or burning
  • Warm or hot sensations and flushing
  • Dizziness and vertigo
  • Nausea and vomiting
  • Pain and redness at the injection site
  • Dangerous heart rhythmsSerious
  • Vasospasm in the gut or limbs (Raynaud's)Serious
  • Serotonin syndrome with SSRIs or SNRIsSerious
  • Rise in blood pressureSerious
  • Medication overuse headache

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Contraindicated in coronary artery disease, past stroke or TIA, peripheral vascular disease and uncontrolled hypertension.
  • Not taken within 24 hours of an ergot drug or another triptan, as their vasospasm adds up.
  • MAO-A inhibitors are contraindicated with it, now or in the past 2 weeks, because they raise its levels.
  • People with several cardiac risk factors are checked for coronary disease before a first dose.

Good to know: It treats an attack once it has begun; it does not prevent migraine, and the injection is also licensed for cluster headache.

Remember it

A way to remember it

Triptans tighten.

They tighten (constrict) swollen cranial vessels to stop a migraine, can tighten the coronary arteries too, which is why heart disease rules them out, and a feeling of chest tightness is a common side effect.

Written for biofideX

Its name

  • -triptan means 5-HT1B/1D agonist for migraine (triptan)

    Sumatriptan stimulates serotonin 5-HT1B/1D receptors to stop migraine and cluster headache attacks; rizatriptan and zolmitriptan share the stem. Don't confuse it with -triptyline.

  • Every drug name stem

Its class

Triptans

Triptans activate serotonin 5-HT1B and 5-HT1D receptors on cranial blood vessels and on the sensory endings of the trigeminal nerve. The swollen vessels constrict and the nerves release fewer of the inflammatory neuropeptides that drive migraine pain. They treat attacks that have started and do not prevent them; because they can also constrict coronary arteries, heart disease rules them out.

Easily mixed up with 5-HT3 antagonists.

Sources

Checked against

Written for biofideX in plain words, after checking these references:

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.

Practice it

Parkinson's, dementia and migraine

Sumatriptan is one of 9 drugs practiced together here: their classes, how they work, what they treat and what they're known for.

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