Formulary
Granisetron: Indications, Dosing, Side Effects and Interactions
Granisetron is a specific 5HT 3 -receptor antagonist which blocks 5HT 3 receptors in the gastro-intestinal tract and in the CNS.
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Granisetron: Indications, Dosing, Side Effects and Interactions
Granisetron is a specific 5HT 3 -receptor antagonist which blocks 5HT 3 receptors in the gastro-intestinal tract and in the CNS.
Drug action
Granisetron is a specific 5HT 3 -receptor antagonist which blocks 5HT 3 receptors in the gastro-intestinal tract and in the CNS.
Indications and dose
**Nausea and vomiting induced by cytotoxic chemotherapy**
- **Adult** (By Transdermal Application Using Patches): for planned duration of 3-5 days where oral antiemetics cannot be used Apply 3.1 mg/24 hours, apply patch 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.
**Prevention of postoperative nausea and vomiting**
- **Adult** (By Intravenous Injection): 1 mg, to be administered before induction of anaesthesia, dose to be diluted to 5 mL and given over 30 seconds.
**Treatment of postoperative nausea and vomiting**
- **Adult** (By Intravenous Injection): 1 mg, dose to be diluted to 5 mL and given over 30 seconds; maximum 3 mg per day.
**Management of nausea and vomiting induced by cytotoxic chemotherapy or radiotherapy**
- **Adult** (By Mouth): 1-2 mg, to be taken within 1 hour before start of treatment, then 2 mg daily in 1-2 divided doses for up to 1 week following treatment, when intravenous route also used, maximum combined total dose 9 mg in 24 hours.
- **Adult** (By Intravenous Injection, Or By Intravenous Infusion): 10-40 micrograms/kg (max. per dose 3 mg), to be given 5 minutes before start of treatment, dose may be repeated if necessary, further maintenance doses must not be given less than 10 minutes apart, for intravenous injection, each 1 mg granisetron diluted to 5 mL and given over not less than 30 seconds, for intravenous infusion, to be given over 5 minutes; maximum 9 mg per day.
**Management of nausea and vomiting induced by cytotoxic chemotherapy for granisetron**
- **Child 12-17 years** (By mouth): 1-2 mg, to be taken within 1 hour before start of treatment, then 2 mg daily in 1-2 divided doses for up to 1 week following chemotherapy.
- **Child 2-17 years** (By intravenous infusion): 10-40 micrograms/kg (max. per dose 3 mg), repeated if necessary, to be given before start of chemotherapy, for treatment, dose may be repeated within 24 hours if necessary, not less than 10 minutes after initial dose; maximum 2 doses per day.
Cautions
Subacute intestinal obstruction; susceptibility to QT-interval prolongation (including electrolyte disturbances)
Side effects
General side-effects: Common or very common Constipation; headache Specific side-effects: Common or very common With intravenous use Diarrhoea; insomnia With oral use Diarrhoea; insomnia Uncommon With intravenous use Extrapyramidal symptoms; QT interval prolongation; serotonin syndrome With oral use Extrapyramidal symptoms; QT interval prolongation; serotonin syndrome With transdermal use Appetite decreased; arthralgia; dry mouth; flushing; generalised oedema; vertigo Rare or very rare With transdermal use Dystonia
Interactions
**Other interactions (9):**
- SSRIs and SNRIs, buprenorphine, opiods or other serotonergic medicinal products), there have been reports of serotonin syndrome following concomitant use of 5HT 3 antagonists and other serotonergic...
- Co-administration of intravenous 5HT3 receptor antagonists with oral paracetamol in human subjects has been reported to result in a block in the analgesic effect via a pharmacodynamic mechanism.
- As granisetron is metabolised by hepatic cytochrome P450 active substance-metabolising enzymes (CYP1A1 and CYP3A4), inducers or inhibitors of these enzymes may change the clearance and, hence, the...
- In human subjects, hepatic enzyme induction by phenobarbital has led to an increase in total plasma clearance (approximately 25%) following intravenous administration of granisetron.
- In vitro studies have shown that ketoconazole may inhibit the metabolism of granisetron via the cytochrome P450 3A isoenzyme family.
- In vitro studies using human microsomes indicate that granisetron neither stimulates nor inhibits the cytochrome P450 enzyme system.
Pregnancy
Manufacturer advises avoid.
Breast feeding
Avoid-no information available.
Hepatic impairment
Manufacturer advises caution.
Medicinal forms
Tablet,Solution,Patch
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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