|Trade names||Kytril, Sancuso, others|
|Drug class||5-HT3 receptor antagonist.|
|Main uses||Chemotherapy, radiation, and postoperative nausea and vomiting|
|Side effects||Headache, constipation, fever, abdominal pain, heart burn|
|By mouth, intravenous, transdermal|
|Elimination half-life||3–14 hours|
|Excretion||Kidney 11–12%, faecal 38%|
|Chemical and physical data|
|Molar mass||312.417 g·mol−1|
|3D model (JSmol)|
Granisetron, sold under the brand name Sancuso among others, is a medication used to treat chemotherapy, radiation, and postoperative nausea and vomiting. It may be taken by mouth, injected into a vein, or used as a skin patch. It is not useful for nausea due to motion sickness or opioids.
Common side effects include headache, constipation, fever, abdominal pain, and heart burn. Other side effects may include allergic reactions. While there is no evidence of harm in pregnancy, such use has not been well studied. It is a 5-HT3 receptor antagonist.
Granisetron was patented in 1985 and approved for medical use in 1991. It is on the World Health Organization's List of Essential Medicines as an alternative to ondansetron. It is available as a generic. In the United Kingdom 10 vials of 1 mg costs the NHS about £20 as of 2021. This amount in the United States costs about 36 USD.
It may be used for chemotherapy-induced nausea and vomiting and appears to work about the same as ondansetron. The most common side-effects of chemotherapy treatment are nausea, vomiting and diarrhea. This is one type of drug that a doctor can prescribe to prevent, lessen, or relieve discomfort.
A number of medications including granisetron appear to be effective in controlling post-operative nausea and vomiting (PONV). It is unclear if it is more or less effective than other agents such as droperidol, metoclopramide, or ondansetron.
- Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis
- Treatment of cyclic vomiting syndrome although there are no formal trials to confirm efficacy.
By mouth it is used at a dose of 1 to 2 mg an hour before chemotherapy followed by 2 mg per day.
Granisetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipation are the most commonly reported side effects associated with its use. There have been no significant drug interactions reported with this drug's use. It is broken down by the liver's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.
Society and culture
An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016. The long acting form is used for the treatment of both acute and delayed CINV in moderately emetogenic chemotherapy and anthrocycline and/or cyclophosphamide (AC) highly emetogenic regimens. In its review, the FDA did not grant the broad HEC label to the drug citing the focus on AC regimens, primarily breast-cancer, and lack of data.
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- Midani D, Parkman HP (October 2016). "Granisetron Transdermal System for Treatment of Symptoms of Gastroparesis: A Prescription Registry Study". Journal of Neurogastroenterology and Motility. 22 (4): 650–655. doi:10.5056/jnm15203. PMC 5056574. PMID 27400689.
- "Sancuso Full Prescribing Information" (PDF). U.S. Food and Drug Administration. September 2015. Archived (PDF) from the original on April 15, 2021. Retrieved November 29, 2019.
- Drugs.com Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting Archived September 14, 2021, at the Wayback Machine
- FDA.gov Sustol Prescribing Information Archived April 9, 2021, at the Wayback Machine.