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Granisetron

Antiemetic

AntiemeticATC A04AA02
CDSCO approvedATC A04AA02
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Manufacturer advises avoid unless potential benefit outweighs risk—limited information available.
FDA category + note
Top interactionssee all 12
  • AlfentanilSevereDatabaseDDInter
  • AlmotriptanSevereDatabaseDDInter
  • AmiodaroneSevereDatabaseDDInter
  • AmisulprideSevereDatabaseDDInter

Mechanism

Granisetron is a specific 5HT3-receptor antagonist which blocks 5HT3 receptors in the gastrointestinal tract and in the CNS.

Indications

Management of nausea and vomiting in patients receiving cytotoxicsPrevention of postoperative nausea and vomitingTreatment of postoperative nausea and vomitingNausea and vomiting induced by cytotoxic chemotherapy for planned duration of 3–5 days where oral antiemetics cannot be used (transdermal)Management of nausea and vomiting induced by cytotoxic chemotherapy or radiotherapyNauseaChemotherapy-induced nausea and vomitingPostoperative nausea and vomiting (PONV)Nausea secondary to upper abdominal irradiationHyperemesis of pregnancychemotherapy induced nausea and vomiting (CINV)Prevention of chemotherapy-induced nausea and vomiting

Dosing

Adult
By transdermal application using patches: Apply 3.1 mg/24 hours, to clean, dry, non-irritated, non-hairy skin on upper arm (or abdomen if upper arm cannot be used) 24–48 hours before treatment; patch may be worn for up to 7 days; remove at least 24 hours after completing chemotherapy.…
Renal adjustment
Manufacturer advises use with caution in severe impairment—limited information available.
Hepatic adjustment
Manufacturer advises caution in severe impairment (no information available).
Max dose
9 mg per day (combined total dose for oral and intravenous routes, or for IV injection/infusion in chemotherapy/radiotherapy management).

Pharmacokinetics

Half-life
6 to 9 h (depending on route)
Metabolism
Metabolized predominantly by the liver by the CYP3A family

Contraindications

  • Subacute intestinal obstruction
  • Susceptibility to QT-interval prolongation (including electrolyte disturbances)

Side effects

Common
ConstipationHeadacheConstipation or diarrheaLight-headednessdizzinessmild constipationabdominal discomfort
Serious
  • ECG interval changes (QT prolongation)
  • Serotonin syndrome

Pregnancy & lactation

Pregnancy

Manufacturer advises avoid unless potential benefit outweighs risk—limited information available.

Lactation

Manufacturer advises avoid—present in milk in animal studies.

Drug interactions

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Almotriptan
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Increased risk of QT prolongation and Torsades de Pointes. Amiodarone is a potent QT prolonging agent.

Avoid concomitant use if possible. If co-administration is necessary, monitor ECG for QT prolongation very closely. Consider alternative antiemetics or antiarrhythmics if feasible. Correct electrolyte imbalances.

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Apomorphine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Arsenic Trioxide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bedaquiline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bepridil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bupropion
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Related guidelines

Other Antiemetic drugs

Ask House about Granisetron

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-13 · House clinical team