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General information

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.[1][2][3][4][5][6][7][8]
Route: PO, IV, transdermal (Sancuso), SC (Sustol extended release injection)
Extravasation: no information available

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1][3][6]

Patient drug information

History of changes in FDA indication

  • 2001-06-27: 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."
  • 2008-09-12: 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."
  • 2016-08-09: 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, granisetron hydroxychloride extended release, granisetron transdermal system, granisetronum
  • Brand names: Gramatic, Granicip, Graniset, Granisev, Granisol, Granitero, Graniz, Granney, Granny, Granovell, Gratryl, Kytril, Naurif, Sancuso, Sustol