Granisetron

5HT3 serotonin receptor antagonist

ATC code: A04AA02

Brand names: Kytril, Sancuso

Updated 27 May 2026 · Methodology

Indications

Chemotherapy-induced nausea and vomiting

First line

First-line selective 5-HT3 antagonist for prophylaxis of nausea and vomiting in highly and moderately emetogenic chemotherapy. SEOM places granisetron in the triple regimen with dexamethasone and an NK-1 antagonist.

Sources

AEMPS: Ficha técnica de Granisetrón (2024)
Journal of Clinical Oncology: Antiemetics: ASCO Guideline Update (2020)
Supportive Care in Cancer: 2023 updated MASCC/ESMO consensus recommendations: prevention of nausea and vomiting following high-emetic-risk antineoplastic agents (2023)
Cochrane Database Syst Rev: Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis. (2021)

ICD-10: R11.0 · ICD-11: MD90

Postoperative nausea and vomiting

First line

First-line option for postoperative nausea and vomiting prophylaxis and treatment, alongside ondansetron.

Sources

ICD-10: R11 · ICD-11: MD90

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

Blocks 5HT3 receptors in the gut wall and the vomiting center trigger zone, suppresses nausea and emesis from chemotherapy, radiation and surgery. CYP3A4 metabolism. Prolongs the QT interval in a dose-dependent way, so use with caution in electrolyte disturbances and with other QT-prolonging agents.

Safety

Contraindications

Hypersensitivity to granisetron
Concomitant use of apomorphine

Serious adverse effects

QT prolongation and ventricular arrhythmias
Hypersensitivity reactions including anaphylaxis
Serotonin syndrome when combined with serotonergic drugs

Common adverse effects

Headache
Constipation
Elevated hepatic transaminases
Insomnia

Pregnancy: can you take Granisetron?

AEMPS summary of product characteristics (section 4.6): data on granisetron in pregnant women are limited. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precaution, it is preferable to avoid granisetron during pregnancy.

Breastfeeding: can you take Granisetron?

Compatible with caution. Hale L3. No data on transfer into human milk; animal data show small amounts in milk. With single-dose use (postoperative or chemotherapy-induced vomiting prophylaxis) infant exposure is minimal.

Calculate RID Full profile on NIH LactMed ↗

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

Label mentions10 mentions

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

From this drug’s label

Moderateantineoplásicosclass named in the label
«Al igual que otros antagonistas del receptor 5-HT 3 , se han notificado modificaciones del ECG (electrocardiograma) incluyendo prolongación del intervalo QT con granisetrón. Esto puede tener…»
AEMPS, section 4.4 · Open on CIMA
ModerateISRSclass named in the label
«Síndrome serotoninérgico: Se han notificado casos de síndrome serotoninérgico con el uso de antagonistas de 5-HT 3 en monoterapia, pero sobre todo en combinación con otros medicamentos…»
AEMPS, section 4.4 · Open on CIMA
Moderatemedicamentos serotoninérgicosclass named in the label
«Síndrome serotoninérgico: Se han notificado casos de síndrome serotoninérgico con el uso de antagonistas de 5-HT 3 en monoterapia, pero sobre todo en combinación con otros medicamentos…»
AEMPS, section 4.4 · Open on CIMA
Moderateserotonergic drugsclass named in the label
«Serotonergic Drugs: Serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular symptoms) has been described following the concomitant use of 5-HT 3 receptor…»
FDA, section 7 · Open on DailyMed
ModerateSSRIs/SNRIsclass named in the label
«Serotonergic Drugs: Serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular symptoms) has been described following the concomitant use of 5-HT 3 receptor…»
FDA, section 7 · Open on DailyMed
antipsicóticosclass named in the label
«En estudios en sujetos sanos, no se ha indicado evidencia de interacción alguna entre granisetrón y benzodiazepinas (lorazepam), neurolépticos (haloperidol) o medicamentos antiulcerosos (cimetidina)…»
AEMPS, section 4.5 · Open on CIMA
benzodiazepinasclass named in the label
«En estudios en sujetos sanos, no se ha indicado evidencia de interacción alguna entre granisetrón y benzodiazepinas (lorazepam), neurolépticos (haloperidol) o medicamentos antiulcerosos (cimetidina)…»
AEMPS, section 4.5 · Open on CIMA
Haloperidol
«En estudios en sujetos sanos, no se ha indicado evidencia de interacción alguna entre granisetrón y benzodiazepinas (lorazepam), neurolépticos (haloperidol) o medicamentos antiulcerosos (cimetidina)…»
AEMPS, section 4.5 · Open on CIMA
Lorazepam
«En estudios en sujetos sanos, no se ha indicado evidencia de interacción alguna entre granisetrón y benzodiazepinas (lorazepam), neurolépticos (haloperidol) o medicamentos antiulcerosos (cimetidina)…»
AEMPS, section 4.5 · Open on CIMA
medicamentos que prolongan el QTclass named in the label
«Al igual que otros antagonistas 5-HT 3 , se han notificado con granisetrón casos de modificaciones del ECG incluyendo prolongación del intervalo QT. Esto puede tener consecuencias clínicas en…»
AEMPS, section 4.5 · Open on CIMA

Check interaction with another drug

Opens the checker prefilled with this drug. Pick the second one from your regimen.

Open checker

Summary of a multi-drug list →

Medicine list: everything you take in one place →

Frequently asked

What is Granisetron used for?

Granisetron is evaluated for the following indications with varying evidence strength: Postoperative nausea and vomiting (evidence tier A), Chemotherapy-induced nausea and vomiting (evidence tier A). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Granisetron?

Common side effects of Granisetron (≥ 1 in 100): Headache, Constipation, Elevated hepatic transaminases, Insomnia. See the Safety section for uncommon and serious reactions.

Is Granisetron safe during pregnancy?

Is Granisetron compatible with breastfeeding?

Who should not take Granisetron?

Granisetron is contraindicated in: Hypersensitivity to granisetron; Concomitant use of apomorphine. Full list in the Safety section.

Official sources

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

AEMPS / CIMALabel dated 08/11/2022
FDA / DailyMedLabel dated 04/30/2026

Other drugs in this group

Doxylamine, Ondansetron