Class/mechanism: Selective serotonin 5-HT3 receptor antagonist. Chemotherapy medications can cause nausea and vomiting by stimulating release of serotonin from the enterochromaffin cells of the small intestine, and serotonin triggers the vomiting reflex by binding to and activating 5-HT3 receptors. Granisetron prevents nausea and vomiting by binding with high affinity to 5-HT3 receptors and blocking their activation by serotonin. Granisetron does not block 5-HT1, 5-HT1A, 5-HT1B/C, 5-HT2, dopamine-D2, or histamine-H1 receptors.
Route: PO, IV, transdermal (Sancuso), SC (Sustol extended release injection)
Extravasation: no information available
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Patient drug information
History of changes in FDA indication
- 6/27/2001: Initial FDA approval "for the prevention of: 1) nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. 2) nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation."
- 9/12/2008: FDA approved as Sancuso "for the prevention of nausea and vomiting in patients receiving moderately and/or highly emetogenic chemotherapy for up to 5 consecutive days."
- 08/09/2016: FDA approved as Sustol "in combination with other antiemetics in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy (MEC) or anthracycline and cyclophosphamide (AC) combination chemotherapy regimens."
Also known as
- Generic names: granisetron extended-release injection for subcutaneous use, granisetron hydrochloride tablets, granisetron transdermal system, granisetronum
- Brand names: Gramatic, Granicip, Graniset, Granisev, Granisol, Granitero, Graniz, Granney, Granny, Granovell, Gratryl, Kytril, Naurif, Sancuso, Sustol
- Granisetron (Kytril) package insert
- Granisetron (Kytril) package insert (locally hosted backup)
- Granisetron (Sancuso) package insert
- Granisetron (Sancuso) package insert (locally hosted backup)
- Sancuso manufacturer's website
- Granisetron (Sustol) package insert
- Granisetron (Sustol) package insert (locally hosted backup)
- Sustol manufacturer's website
- Granisetron (Kytril) patient drug information (UpToDate)