Rizatriptan
Triptans (5-HT1B/1D agonists)
Triptans (5-HT1B/1D agonists)
A fast oral triptan, also as an orally disintegrating tablet, for migraine attacks; propranolol raises its levels and MAO inhibitors are excluded.
Also called: Rizatriptan benzoate
Quick facts
- Group
- Triptans (5-HT1B/1D agonists)
- Target
- Serotonin 5-HT1B and 5-HT1D receptors
- Used for
- Acute treatment of migraine
- Key effects
- Weakness or tiredness · Sensations of pain or pressure
- Monitor
- Cardiovascular evaluation · Blood pressure
- ATC
- N02CC04
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; rizatriptan binds the same pocket.
Rizatriptan is a 5-HT1B/1D receptor agonist. It constricts intracranial vessels and reduces the release of inflammatory neuropeptides from trigeminal nerve endings, relieving the headache and associated nausea and light sensitivity of an attack.
- Rizatriptan activates 5-HT1B/1D receptors
- Intracranial vessels constrict; trigeminal endings quiet down
- Headache and associated symptoms improve
Indications
- Acute treatment of migraine with or without aura in adults and children 6 to 17 years old Migraine →
Adverse effects
Common
- Weakness or tiredness, drowsiness and dizziness
- Sensations of pain or pressure (chest, throat, neck or jaw)
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
- An MAO-A inhibitor now or in the past 2 weeks
- Hypersensitivity to rizatriptan or excipients
Key interactions
- Propranolol
- Raises rizatriptan levels (by about 70%); a lower dose is used
- MAO-A inhibitors
- Block its metabolism; contraindicated
- Ergot alkaloids or other triptans within 24 hours
- Additive vasospasm; contraindicated
- SSRIs, SNRIs, tricyclics
- Serotonin syndrome
What is monitored
- Cardiovascular evaluation in triptan-naive patients with several risk factors
- Blood pressure
- Days of acute treatment per month
Administration and safety
- The orally disintegrating tablet dissolves on the tongue without water
- The dose is adjusted in patients on propranolol
- For attacks only; not a preventive
Pregnancy and breastfeeding
Human data are not sufficient to define the risk; animal studies showed developmental toxicity at high exposure.
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
- Completely absorbed; bioavailability about 45%; peak in about 1 to 1.5 hours (slightly later with the orally disintegrating tablet)
- Metabolism
- Oxidative deamination by MAO-A
- Half-life
- About 2 to 3 hours
Test yourself
Think of the answer, then tap the question to see it.
Which migraine-preventive drug raises rizatriptan levels?
Propranolol.
Which enzyme mainly metabolizes rizatriptan?
MAO-A, so MAO-A inhibitors are contraindicated.
Can rizatriptan be used in children?
Yes, for acute migraine from 6 to 17 years of age.
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 - RIZATRIPTAN BENZOATE tablet (DailyMed (U.S. National Library of Medicine), 2026); Rizatriptan: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).
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Representative model, for educational purposes only.