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Granisetron

Brand and Other Names: Kytril
Mechanism of Action:
Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT1; 5-HT1A; 5-HT1B/C; 5-HT2; for alpha1-, alpha2- or beta-adrenoreceptors; for dopamine-D2; or for histamine-H1; benzodiazepine; picrotoxin or opioid receptors. Serotonin receptors of the 5-HT3 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-HT3 receptors. This evokes vagal afferent discharge and may induce vomiting. See package insert for complete information.
Indications:

KYTRIL 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.
Route: Intravenous
Dose:

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.
  • Treatment of postoperative nausea and vomiting:
    Recommended dosage is 1 mg, undiluted, administered intravenously over 30 seconds.
Adverse Reactions:

Most common adverse reactions:

  • Chemotherapy-induced nausea and vomiting (≥3%): Headache, and constipation.
  • Postoperative nausea and vomiting (≥2%): Pain, headache, fever, abdominal pain and hepatic enzymes increased.
Contraindication:
Hypersensitivity to granisetron or to any of its components.
Warnings and Precautions:
  • KYTRIL does not stimulate gastric or intestinal peristalsis and should not be used instead of nasogastric suction.
  • QT prolongation has been reported with KYTRIL. 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-HT3 receptor antagonists.
  • Contains benzyl alcohol.
See package insert for full prescribing information.