The hydrochloride salt of an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
Granisetron hydrochloride nasal spray
Upon administration to the nostril, granisetron selectively binds to and inhibits 5-HT3R located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting.
Granisetron transdermal system
Upon application of the transdermal system (patch) to the skin and the subsequent sustained release of granisetron into the bloodstream, granisetron selectively binds to and inhibits 5-HT3 receptors located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting.
Adult
PO
Nausea and vomiting associated w/ cancer chemotherapy: 1-2 mg w/in 1 hr prior to start of chemotherapy, then 2 mg/day as a single or in 2 divided doses for up to 1 wk after chemotherapy. Max: 9 mg/day.
Prophylaxis of nausea and vomiting associated w/ radiation therapy: 2 mg once daily w/in 1 hr of irradiation.
IV
Nausea and vomiting associated w/ cancer chemotherapy or radiotherapy: 1-3 mg 5 min prior to start of therapy; further doses may be given at least 10 min apart. Max: 9 mg/day.
Treatment and prophylaxis of post-op nausea and vomiting: 1 mg before induction of anesth.
Transdermal
Nausea and vomiting associated w/ cancer chemotherapy: apply 1 patch at the upper arm 24-48 hr prior to chemotherapy; remove at least 24 hr after the end of chemotherapy. May be worn for up to 7 days.