[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/) › Rizatriptan

# 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.

Updated Nov 1, 2026

Also called: Rizatriptan benzoate

## 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**
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.

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**Rizatriptan

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

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 →](https://durgical.com/en/conditions/migraine/)

## Adverse effects

### Common

- Weakness or tiredness, drowsiness and dizziness
- Sensations of pain or pressure (chest, throat, neck or jaw)

### 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

## 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

## Memory aid

«Riza-propra»: rizatriptan plus propranolol = more rizatriptan, so a smaller dose.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/rizatriptan/)

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

## Connections

## Related drugs 3

- [Sumatriptan](https://durgical.com/en/pharmacology/sumatriptan/)
- [Eletriptan](https://durgical.com/en/pharmacology/eletriptan/)
- [Propranolol](https://durgical.com/en/pharmacology/propranolol/)

## Related conditions 1

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

[← 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 - RIZATRIPTAN BENZOATE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=99c66300-bd75-4b31-9fab-88c6e4b12688) (DailyMed (U.S. National Library of Medicine), 2026); [Rizatriptan: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a601109.html) (MedlinePlus (U.S. National Library of Medicine), 2026).

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Representative model, for educational purposes only.

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