Rizatriptan

Selective 5-HT1B/1D serotonin receptor agonist

ATC code: N02CC04

Brand names: Maxalt-MLT, Maxalt, Rizalt

Updated 24 Sep 2026 · Methodology

Indications

Acute migraine attack

First line

First-line for acute moderate-to-severe migraine per AHS 2021 and EFNS 2009. The 2016 Cochrane systematic review showed pain-free response at 2 hours with rizatriptan 10 mg in 40% versus 19% on placebo. Among triptans, one of the fastest onsets (especially the MLT orally disintegrating tablet when nausea is present). Take at the first sign of pain, not during aura. If no response at 2 hours, repeat dosing is not recommended.

Sources

ICD-10: G43.9 · ICD-11: 8A80.Z

Migraine during breastfeeding

Second line

Migraine in nursing mothers. Per AHS 2024 – alternative to sumatriptan during breastfeeding. Dose 5–10 mg orally, repeat at 2 h. Max 30 mg/day. Fast onset (30 min).

Sources

ICD-10: G43.9 · ICD-11: 8A80.Z

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Memory and concentration enhancement

Not recommended

Rizatriptan is a triptan with indications similar to sumatriptan. It is prescribed for migraine and cluster headache ( NG150 2021 and AHS 2021 guidelines). For severe tension-type headache, premenstrual headache, or hangover headache without confirmed migraine, rizatriptan is not used: regular use for non-migraine pain provokes medication-overuse headache. Triptans are contraindicated in ischemic heart disease, prior stroke, and uncontrolled hypertension. If rizatriptan was prescribed for any severe headache without confirmed migraine, consider seeking a second opinion.

Sources

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

A selective 5-HT1B and 5-HT1D agonist. Via 5-HT1B it constricts dilated cranial vessels; via 5-HT1D it blocks release of inflammatory neuropeptides (CGRP, substance P) from trigeminal nerve endings. Onset 30–60 minutes after orally disintegrating tablets (MLT) or 60–90 minutes after standard tablets. Half-life 2–3 hours.

Safety

Contraindications

Rizatriptan hypersensitivity
Coronary artery disease, prior MI
Uncontrolled hypertension
History of cerebrovascular events (stroke, TIA)
Peripheral arterial disease
Hemiplegic, basilar, or ophthalmoplegic migraine
Severe hepatic or renal impairment
Concurrent MAO inhibitors, ergotamines, other triptans
Age under 18 (most formulations)

Serious adverse effects

Coronary spasm, myocardial infarction (rare, in predisposed patients)
Cerebrovascular events
Serotonin syndrome with SSRIs/SNRIs
Anaphylaxis
Medication-overuse headache with overuse

Common adverse effects

Drowsiness
Dizziness
Chest, neck, or jaw tightness or pressure
Nausea
Dry mouth
Flushing

Pregnancy: can you take Rizatriptan?

AEMPS summary of product characteristics (section 4.6): data from 300–1,000 pregnancies show no sign that first-trimester exposure to rizatriptan causes malformations. Animal studies have shown no reproductive toxicity. Data on use in the second and third trimesters are limited. When clinically needed, rizatriptan may be considered during pregnancy.

Breastfeeding: can you take Rizatriptan?

Hale L3 · Probably compatible, limited data

Compatible. Hale L3, limited RID data. Short T½ 2 h gives rapid clearance. Wait 4–8 h before feeding to minimize exposure.

Maternal half-life: 2 h
Maternal peak time: 1.3 h

Calculate RID Safe feeding window Full profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Take at the first sign of pain, not during aura. Standard dose 10 mg; reduce to 5 mg in patients on propranolol (which raises rizatriptan levels). Maximum 2 doses per day with at least 2 hours apart. Use exceeding 10 days per month risks medication-overuse headache. Do not combine with other triptans on the same day, with MAO inhibitors, or with ergotamines; with SSRIs and SNRIs there is a serotonin syndrome risk.

Drug–drug interactions

2 pairs found. Sorted from critical to minor.

CriticalPhenelzineAntidepressant, irreversible non-selective monoamine oxidase inhibitor (MAO-A and MAO-B)

Mechanism

Rizatriptan is a MAO-A substrate. With phenelzine accumulation and fatal serotonin syndrome.

Symptoms

Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.

Management

Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.

Sources

Pair details →Phenelzine →

CriticalTranylcypromineAntidepressant, irreversible non-selective monoamine oxidase inhibitor (MAO-A and MAO-B), amphetamine derivative

Mechanism

MAO-A inhibition by tranylcypromine + rizatriptan – fatal serotonin syndrome.

Symptoms

Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.

Management

Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.

Sources

Pair details →Tranylcypromine →

Label mentions19 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

CriticalDihydroergotamine
«Ergot-Containing Drugs: Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type…»
FDA, section 7 · Open on DailyMed
CriticalErgotamine
«Uso concomitante de rizatriptán y ergotamina, derivados de la ergotamina (entre ellos la metisérgida) u otros agonistas del receptor 5-HT 1B/1D (ver sección 4.5).»
AEMPS, section 4.3 · Open on CIMA
CriticalErgotamine
«Ergot-Containing Drugs: Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type…»
FDA, section 7 · Open on DailyMed
CriticalIMAOclass named in the label
«Administración simultánea de inhibidores de la monoaminooxidasa (MAO) o uso en un periodo de dos semanas siguientes a la discontinuación de la terapia con inhibidores de la MAO (ver sección 4.5).»
AEMPS, section 4.3 · Open on CIMA
CriticalLinezolid
«Inhibidores de la monoaminooxidasa: El rizatriptán se metaboliza principalmente por la monoaminooxidasa, subtipo A (MAO-A). Las concentraciones plasmáticas de rizatriptán y su metabolito activo…»
AEMPS, section 4.5 · Open on CIMA
CriticalMAO inhibitorsclass named in the label
«Monoamine Oxidase Inhibitors: Rizatriptan benzoate is contraindicated in patients taking MAO-A inhibitors and non-selective MAO inhibitors. A specific MAO-A inhibitor increased the systemic exposure…»
FDA, section 7 · Open on DailyMed
CriticalNaratriptan
«Ergotamina, derivados de la ergotamina (incluyendo metisérgida) y otros agonistas de los receptores 5 HT 1B/1D : Debido a un efecto aditivo, el uso concomitante de rizatriptán y ergotamina, derivados…»
AEMPS, section 4.5 · Open on CIMA
CriticalSumatriptan
«Ergotamina, derivados de la ergotamina (incluyendo metisérgida) y otros agonistas de los receptores 5 HT 1B/1D : Debido a un efecto aditivo, el uso concomitante de rizatriptán y ergotamina, derivados…»
AEMPS, section 4.5 · Open on CIMA
CriticalZolmitriptan
«Ergotamina, derivados de la ergotamina (incluyendo metisérgida) y otros agonistas de los receptores 5 HT 1B/1D : Debido a un efecto aditivo, el uso concomitante de rizatriptán y ergotamina, derivados…»
AEMPS, section 4.5 · Open on CIMA
ModerateISRSclass named in the label
«Se ha informado de síndrome serotoninérgico (incluyendo estado mental alterado, inestabilidad autonómica y anomalías neuromusculares) tras el tratamiento concomitante de triptanos con inhibidores…»
AEMPS, section 4.4 · Open on CIMA
Moderatemedicamentos serotoninérgicosclass named in the label
«Se ha informado de síndrome serotoninérgico (incluyendo estado mental alterado, inestabilidad autonómica y anomalías neuromusculares) tras el tratamiento concomitante de triptanos con inhibidores…»
AEMPS, section 4.4 · Open on CIMA
betabloqueantesclass named in the label
«Beta bloqueantes: Las concentraciones plasmáticas de rizatriptán pueden aumentar con la administración concomitante de propranolol. Este aumento se debe, con gran probabilidad, a la interacción…»
AEMPS, section 4.5 · Open on CIMA
Metoprolol
«En un estudio de interacción farmacológica, el nadolol y metoprolol no alteraron las concentraciones plasmáticas de rizatriptán.»
AEMPS, section 4.5 · Open on CIMA
Propranolol
«Beta bloqueantes: Las concentraciones plasmáticas de rizatriptán pueden aumentar con la administración concomitante de propranolol. Este aumento se debe, con gran probabilidad, a la interacción…»
AEMPS, section 4.5 · Open on CIMA
Propranolol
«Propranolol: The dose of rizatriptan benzoate should be adjusted in propranolol-treated patients, as propranolol has been shown to increase the plasma AUC of rizatriptan by 70% [see Dosage and…»
FDA, section 7 · Open on DailyMed
SSRIs/SNRIsclass named in the label
«SSRIs/SNRIs and Serotonin Syndrome: Cases of serotonin syndrome have been reported during co-administration of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine…»
FDA, section 7 · Open on DailyMed

From other drugs’ labels

CriticalMoclobemide
«La administración conjunta de Manerix con triptanos está contraindicada ya que éstos son potentes receptores agonistas serotoninérgicos metabolizados por las monoaminooxidasas (MAOs) y varios enzimas…»
AEMPS, section 4.5 · Open on CIMA
CriticalSelegiline
«Agonistas de la serotonina: La selegilina no debe utilizarse en combinación con agonistas de la serotonina (por ejemplo, sumatriptán, naratriptán, zolmitriptán, rizatriptán, lasmiditán) debido al…»
AEMPS, section 4.5 · Open on CIMA
Propranolol
«Combinación no recomendada: Durante el tratamiento concomitante con propranolol inhibió el metabolismo de primer paso de rizatriptán cuyo AUC aumenta en un 70-80%. Se recomienda una dosis de 5 mg de…»
AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Rizatriptan used for?

Rizatriptan is evaluated for the following indications with varying evidence strength: Acute migraine attack (evidence tier A), Migraine during breastfeeding (evidence tier B), Memory and concentration enhancement (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Rizatriptan?

Common side effects of Rizatriptan (≥ 1 in 100): Drowsiness, Dizziness, Chest, neck, or jaw tightness or pressure, Nausea, Dry mouth, Flushing. See the Safety section for uncommon and serious reactions.

Is Rizatriptan safe during pregnancy?

Is Rizatriptan compatible with breastfeeding?

Compatible. Hale L3, limited RID data. Short T½ 2 h gives rapid clearance. Wait 4–8 h before feeding to minimize exposure.

Who should not take Rizatriptan?

Rizatriptan is contraindicated in: Rizatriptan hypersensitivity; Coronary artery disease, prior MI; Uncontrolled hypertension; History of cerebrovascular events (stroke, TIA); Peripheral arterial disease. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMALabel dated 09/30/2025
FDA / DailyMedLabel dated 11/05/2025

Other drugs in this group

Sumatriptan, Tapentadol, Tramadol, Tramadol + Paracetamol, Dihydroergotamine, Frovatriptan, Naratriptan, Zolmitriptan