Granisetron

Indications
 Oral
Nausea and vomiting associated with cancer chemotherapy
Adult: 1-2 mg within 1 hr before the start of chemotherapy, then 2 mg daily in 1-2 divided doses during treatment.
Child: 1 mth-12 yr: 20 mcg/kg (max: 1 mg) within 1 hr before chemotherapy, then 20 mcg/kg (max: 1 mg) bid for up to 5 days during treatment.
Oral
Prophylaxis of nausea and vomiting associated with radiation therapy
Adult: 2 mg daily within 1 hr of irradiation.
Intravenous
Nausea and vomiting associated with cancer chemotherapy
Adult: 3 mg diluted to 20-50 ml with a suitable infusion solution, given over 5 minutes before the start of chemotherapy. Alternatively, 3 mg given in 15 ml of infusion solution given as bolus over at least 30 sec. May repeat dose up to twice within 24 hr. Doses should be given at least 10 minutes apart. Max: 9 mg daily.
Child: 40 mcg/kg (max 3 mg), in 10-30 ml of infusion fluid given over 5 minutes, may repeat once within 24 hr, at least 10 minutes apart from the 1st dose. 1st dose should be given within 1 hr of the start of chemotherapy.
Intravenous
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 1 mg diluted to 5 ml, injected over 30 sec. To be completed before induction of anaesthesia. May be given up to bid for the treatment of postoperative nausea and vomiting.

Special Populations: Dosage should be reduced in moderate to severe hepatic impairment.
Contraindications
 Hypersensitivity.
Warnings / Precautions
 Subacute intestinal obstruction or ileus. Moderate to severe hepatic impairment. Congenital long QT syndrome or other risk factors for QT prolongation (e.g. electrolyte abnormalities and cumulative high-dose anthracycline therapy). Pregnancy, lactation.
Adverse Reactions
 Headache; sensation of flushing; constipation; hypersensitivity reactions; chest pain; CV disturbances; dizziness; transient visual disturbances. Rarely, liver disorders; development of seizures; extrapyramidal reactions.
Overdose Reactions
 Treatment is symptomatic.
Drug Interactions
 Phenobarbital may induce metabolism of granisetron.
See Below for More granisetron Drug Interactions
Lab Interactions
 Transient rise in liver enzymes.
Mechanism of Actions
 Granisetron is a selective 5-HT3-receptor antagonist with little or no affinity for other serotonin receptors. It blocks serotonin in the chemoreceptor zone.
Duration: 24 hr.
Absorption: Rapidly absorbed after oral admin. Oral bioavailability: About 60%.
Distribution: Protein binding: About 65%.
Metabolism: Hepatically metabolised, mainly by N-demethylation.
Excretion: IV admin: Elimination half-life: 4-5 hr in healthy subjects; 9-12 hr in cancer patients.
Administration
 May be taken with or without food. (Take up to 1 hr before chemotherapy.)
Storage Conditions
 Intravenous: Store at 25°C. Oral: Store at 25°C.
ATC Classification
 A04AA02 - granisetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
Storage
 Intravenous: Store at 25°C. Oral: Store at 25°C.
Available As
  • Granisetron 0.025%
  • Granisetron 1 mg
  • Granisetron 2 mg

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