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Sumatriptan

Brand and Other Names: IMITREX
Mechanism of Action:

Sumatriptan binds with high affinity to human cloned 5‑HT receptors. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine headache through agonist effects at the 5‑HT receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro‑inflammatory neuropeptide release.

Indications:

IMITREX is a serotonin (5-HT ) receptor agonist (triptan) indicated for acute treatment of migraine with or without aura in adults. 

Limitations of Use:

  • Use only if a clear diagnosis of migraine headache has been established.
  • Not indicated for the prophylactic therapy of migraine attacks.
  • Not indicated for the treatment of cluster headache.
Route: Oral
Dose:
  • Single dose of 25-mg, 50-mg, or 100-mg tablet. 
  • A second dose should only be considered if some response to the first dose was observed. Separate doses by at least 2 hours. 
  • Maximum dose in a 24-hour period: 200 mg. 
  • Maximum single dose should not exceed 50 mg in patients with mild to moderate hepatic impairment. 
Adverse Reactions:

Most common adverse reactions (≥2% and >placebo) were paresthesia, warm/cold sensation, chest pain/tightness/pressure and/or heaviness, neck/throat/jaw pain/tightness/pressure, other sensations of pain/pressure/tightness/heaviness, vertigo, and malaise/fatigue.

Contraindication:
  • History of coronary artery disease or coronary artery vasospasm
  • Wolff-Parkinson-White syndrome or other cardiac accessory conduction pathway disorders 
  • History of stroke, transient ischemic attack, or hemiplegic or basilar migraine 
  • Peripheral vascular disease 
  • Ischemic bowel disease 
  • Uncontrolled hypertension 
  • Recent (within 24 hours) use of another 5-HT agonist (e.g., another triptan) or of an ergotaminecontaining medication 
  • Concurrent or recent (past 2 weeks) use of monoamine oxidase-A inhibitor 
  • Hypersensitivity to IMITREX (angioedema and anaphylaxis seen) 
  • Severe hepatic impairment 
Warnings and Precautions:
  • Myocardial ischemia/infarction and Prinzmetal’s angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors.
  • Arrhythmias: Discontinue IMITREX if occurs.
  • Chest/throat/neck/jaw pain, tightness, pressure, or heaviness: Generally not associated with myocardial ischemia; evaluate for coronary artery disease in patients at high risk. 
  • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue IMITREX if occurs. 
  • Gastrointestinal ischemic reactions and peripheral vasospastic reactions: Discontinue IMITREX if occurs. 
  • Medication overuse headache: Detoxification may be necessary. 
  • Serotonin syndrome: Discontinue IMITREX if occurs. 
  • Seizures: Use with caution in patients with epilepsy or a lowered seizure threshold. 
See package insert for full prescribing information.