Granisetron

Granisetron
Clinical data
Trade names Kytril, Sancuso, others
AHFS/Drugs.com Monograph
MedlinePlus a601211
License data
Pregnancy
category
    Routes of
    administration    		 by mouth, intravenous, transdermal
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    Pharmacokinetic data
    Bioavailability 60%
    Protein binding 65%
    Metabolism Hepatic
    Elimination half-life 3–14 hours
    Excretion Renal 11–12%, faecal 38%
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.212.327 Edit this at Wikidata
    Chemical and physical data
    Formula C18H24N4O
    Molar mass 312.42 g·mol−1
    3D model (JSmol)
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    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and Radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

    Granisetron was developed by chemists working at the British drug company Beecham around 1988 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA.

    A granisetron transdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008.[1] Sancuso is manufactured by 3M Drug Delivery Systems Division for ProStrakan.

    Granisetron is metabolized slowly by the liver, giving it a longer than average half-life. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.

    Medical uses

    Chemotherapy

    It may be used for chemotherapy-induced nausea and vomiting and appears to work about the same as ondansetron.[2] 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.

    Post operative

    A number of medications including granisetron appear to be effective in controlling post-operative nausea and vomiting (PONV).[3] It is unclear if it is more or less effective than other agents such as droperidol, metoclopramide, ondansetron or cyclizine.[3]

    Its efficacy has also been questioned with a research Dr. Yoshitaka Fujii having 12 published papers on this topic in Canadian Journal of Anesthesia retracted. A further five papers in the same journal on the same drug by Dr Fujii are considered indeterminate.

    Other

    • 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.

    Adverse effects

    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.

    Extended release

    An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016.[4] 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.[5]

    References

    1. ↑ "FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy". PRNewswire. September 12, 2008.
    2. ↑ Billio, A; Morello, E; Clarke, MJ (January 20, 2010). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults". The Cochrane Database of Systematic Reviews (1): CD006272. doi:10.1002/14651858.CD006272.pub2. PMID 20091591.
    3. 1 2 Carlisle, JB; Stevenson, CA (July 19, 2006). "Drugs for preventing postoperative nausea and vomiting". The Cochrane Database of Systematic Reviews (3): CD004125. doi:10.1002/14651858.CD004125.pub2. PMID 16856030.
    4. ↑ Drugs.com Heron Therapeutics Announces FDA Approval of Sustol (granisetron) Extended-Release Injection for the Prevention of Chemotherapy-Induced Nausea and Vomiting
    5. ↑ FDA.gov Sustol Prescribing Information.

    Further reading

    • Aapro, M. (2004). "Granisetron: an update on its clinical use in the management of nausea and vomiting". The Oncologist. 9 (6): 673–686. doi:10.1634/theoncologist.9-6-673. ISSN 1083-7159. PMID 15561811.
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