5HT3 serotonin receptor antagonist
ATC code: A04AA02 (Granisetron)
Brand names
Kytril, Sancuso
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.
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.
First line
First-line option for postoperative nausea and vomiting prophylaxis and treatment, alongside ondansetron.
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FDA Category B. Pregnancy data are limited. Registries have not shown an excess of major malformations. SEOM recommends ondansetron as the best-studied antiemetic for chemotherapy-induced vomiting during pregnancy; granisetron is considered when ondansetron fails.
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.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
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.
Common side effects of Granisetron (≥ 1 in 100): Headache, Constipation, Elevated hepatic transaminases, Insomnia. See the Safety section for uncommon and serious reactions.
FDA category B. FDA Category B. Pregnancy data are limited. Registries have not shown an excess of major malformations. SEOM recommends ondansetron as the best-studied antiemetic for chemotherapy-induced vomiting during pregnancy; granisetron is considered when ondansetron fails.
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.
Granisetron is contraindicated in: Hypersensitivity to granisetron; Concomitant use of apomorphine. Full list in the Safety section.