Granisetron

What it is and how it works

Mechanism of Action Granisetron is a selective 5-hydroxytryptamine 3 (5-HT 3 ) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT 1 ; 5-HT 1A ; 5-HT 1B/C ; 5-HT 2 ; for alpha 1 -, alpha 2 - or beta-adrenoreceptors; for dopamine-D 2 ; or for histamine-H 1 ; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy-induced vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT 3 receptors. This evokes vagal afferent discharge and may induce vomiting.

Indications

Granisetron hydrochloride injection is a serotonin-3 (5-HT 3 ) receptor antagonist indicated for: • The prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. • The prevention and treatment of postoperative nausea and vomiting in adults. As with other antiemetics, routine prophylaxis is not recommended in patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively. In patients where nausea and/or vomiting must be avoided during the postoperative period, granisetron hydrochloride injection is recommended even where the incidence of postoperative nausea and/or vomiting is low. Granisetron hydrochloride injection is a serotonin-3 (5-HT3) receptor antagonist indicated for: • Prevention of nausea and/or vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. • Prevention and treatment of postoperative nausea and vomiting in adults.

Dosage and administration (summary)

Prevention of chemotherapy-induced nausea and vomiting : • Recommended dosage is 10 mcg/kg intravenously within 30 minutes before initiation of chemotherapy • Pediatric patients (2 to 16 years): Recommended dosage is 10 mcg/kg Prevention of postoperative nausea and vomiting : • Recommended dosage is 1 mg, undiluted, administered intravenously over 30 seconds, before anesthetic induction or immediately before reversal of anesthesia.

Contraindications

Granisetron hydrochloride injection is contraindicated in patients with known hypersensitivity (eg. anaphylaxis, shortness of breath, hypotension, urticaria) to the drug or to any of its components. • Hypersensitivity to granisetron or to any of its components.

Warnings and precautions

• Granisetron hydrochloride does not stimulate gastric or intestinal peristalsis and should not be used instead of nasogastric suction. • QT prolongation has been reported with granisetron hydrochloride. Use with caution in patients with pre-existing arrhythmias or cardiac conduction disorders. • Hypersensitivity reactions, such as anaphylaxis, shortness of breath, hypotension, and urticaria, may occur in patients with known hypersensitivity to other selective 5-HT 3 receptor antagonists.

Pregnancy

Pregnancy Teratogenic Effects Pregnancy Category B Reproduction studies have been performed in pregnant rats at intravenous doses up to 9 mg/kg/day (54 mg/m 2 /day, 146 times the recommended human dose based on body surface area) and pregnant rabbits at intravenous doses up to 3 mg/kg/day (35.4 mg/m 2 /day, 96 times the recommended human dose based…

Storage and supply

Granisetron Hydrochloride Injection, USP is supplied as follows: NDC Granisetron Hydrochloride Injection, USP Package Factor 67457-861-01 0.1 mg per mL Single-Dose Vial 5 vials per carton 67457-863-01 1 mg per mL Single-Dose Vial 1 vial per carton Single-dose vials contain no preservative.

Source: Granisetron Hydrochloride (Granisetron Hydrochloride) — US FDA prescribing information, 2017-08-31, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.