Granisetron
Granisetron is a 5-HT3 receptor antagonist used to prevent and treat nausea and vomiting, primarily prescribed for patients undergoing chemotherapy or radiation therapy.
Granisetron is a 5-HT3 antagonist antiemetic used to prevent chemotherapy, surgery, and radiation-induced nausea and vomiting.
Key facts at a glance
- ATC
- A04AA02
- RxNorm
- 26237
- Generic
- Granisetron
- Class
- atc-a04
- Brands
- Sustol, Granisol, Sancuso
- Availability
- rx
- Pregnancy
- B
- Lactation
- safe
- Routes
- oral
- Forms
- prefilled syringe, injection, solution, tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 1 mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 10 mcg/kg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 1 mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
9 groupspregnancy
first trimesteruse lowest effective dose
use only if clearly needed and benefits outweigh potential risks
regular prenatal monitoring
Use with caution and monitor for adverse effects.
pregnancy
second third trimesterstandard dosing
considered safe for chemotherapy-induced nausea in later pregnancy
standard prenatal care
lactation
breastfeedinguse with caution
consider discontinuing breastfeeding or pumping and discarding milk for 24 hours after administration
monitor infant for unusual drowsiness or feeding changes
Use with caution and monitor for adverse effects.
pediatric_age
under 2 yearsdose based on body weight
use only in clinical setting for chemotherapy-induced emesis
close vital sign monitoring
Use with caution and monitor for adverse effects.
pediatric_age
2 to 17 yearsweight-based dosing up to adult maximum
approved for chemotherapy and radiotherapy-induced nausea
standard pediatric monitoring
geriatric
65 years and olderno adjustment needed
standard dosing appropriate
standard geriatric monitoring for adverse effects
renal_impairment
mild moderateno adjustment needed
standard dosing recommended
standard monitoring
hepatic_impairment
mild moderateno adjustment needed
standard dosing for mild to moderate impairment
standard liver function monitoring
hepatic_impairment
severeconsider dose reduction
monitor for increased adverse effects, consider lowering dose
close monitoring of liver function and drug response
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
First FDA approval for Granisetron
Drug class
ATC code A04AA02 - Serotonin (5-HT3) antagonists
Primary indication
Primary therapeutic use
Secondary indication
Additional therapeutic use
Prevention of acute nausea and vomiting associated with emetogenic cancer chemotherapy, radiation therapy, and surgery. It is particularly effective for moderate to highly emetogenic chemotherapy regimens.
Granisetron works by selectively blocking 5-hydroxytryptamine (5-HT3) receptors in the chemoreceptor trigger zone and on vagal afferent neurons in the gastrointestinal tract, inhibiting the vomiting reflex signal.
Available in oral, intravenous, and transdermal formulations. Common side effects include headache, constipation, and dizziness. Should be administered before chemotherapy or surgery for optimal effect. May interact with other serotonergic medications.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy