Granisetron

Granisetron
Names
Trade namesKytril, Sancuso, others
IUPAC name
  • 1-Methyl-N-((1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1H-indazole-3-carboxamide
Clinical data
Drug class5-HT3 receptor antagonist.[1]
Main usesChemotherapy, radiation, and postoperative nausea and vomiting[2]
Side effectsHeadache, constipation, fever, abdominal pain, heart burn[3]
Pregnancy
category
  • AU: B1
    Routes of
    use    		By mouth, intravenous, transdermal
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa601211
    Legal
    License data
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    Pharmacokinetics
    Bioavailability60%
    Protein binding65%
    MetabolismLiver
    Elimination half-life3–14 hours
    ExcretionKidney 11–12%, faecal 38%
    Chemical and physical data
    FormulaC18H24N4O
    Molar mass312.417 g·mol−1
    3D model (JSmol)
    SMILES
    • CN4[C@@H]1CCC[C@H]4C[C@H](C1)NC(=O)c3nn(C)c2ccccc23
    InChI
    • InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14- checkY
    • Key:MFWNKCLOYSRHCJ-BTTYYORXSA-N checkY

    Granisetron, sold under the brand name Sancuso among others, is a medication used to treat chemotherapy, radiation, and postoperative nausea and vomiting.[2] It may be taken by mouth, injected into a vein, or used as a skin patch.[2] It is not useful for nausea due to motion sickness or opioids.[4]

    Common side effects include headache, constipation, fever, abdominal pain, and heart burn.[3] Other side effects may include allergic reactions.[3] While there is no evidence of harm in pregnancy, such use has not been well studied.[5] It is a 5-HT3 receptor antagonist.[1]

    Granisetron was patented in 1985 and approved for medical use in 1991.[6] It is on the World Health Organization's List of Essential Medicines as an alternative to ondansetron.[7] It is available as a generic.[2] In the United Kingdom 10 vials of 1 mg costs the NHS about £20 as of 2021.[2] This amount in the United States costs about 36 USD.[8]

    Medical uses

    Chemotherapy

    It may be used for chemotherapy-induced nausea and vomiting and appears to work about the same as ondansetron.[9] 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).[10] It is unclear if it is more or less effective than other agents such as droperidol, metoclopramide, or ondansetron.[10]

    Gastroparesis

    The granisetron patch (Sancuso) has been studied for use in gastroparesis,[11] though it is not FDA approved for this indication.[12]

    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.

    Dosage

    By mouth it is used at a dose of 1 to 2 mg an hour before chemotherapy followed by 2 mg per day.[2]

    The patch is used at a dose of 3.1 mg per day.[2] And by injection it is generally given at a dose of 1 mg.[2]

    Side 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.

    Society and culture

    Extended release

    An extended release injectable version of granisetron, known as Sustol is also available in the United States as of 2016.[13] 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.[14]

    References

    1. 1 2 "Sancuso". Archived from the original on January 8, 2021. Retrieved December 9, 2021.
    2. 1 2 3 4 5 6 7 8 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 454. ISBN 978-0857114105.
    3. 1 2 3 "Granisetron Monograph for Professionals". Drugs.com. Archived from the original on January 25, 2021. Retrieved December 9, 2021.
    4. ↑ Frogge, Margaret Hansen; Goodman, Michelle (April 1999). Cancer Symptom Management. Jones & Bartlett Learning. p. 243. ISBN 978-0-7637-0864-1. Archived from the original on December 11, 2021. Retrieved December 9, 2021.
    5. ↑ "Granisetron Use During Pregnancy". Drugs.com. Archived from the original on January 25, 2021. Retrieved December 9, 2021.
    6. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495. Archived from the original on September 30, 2021. Retrieved October 19, 2021.
    7. ↑ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
    8. ↑ "Granisetron Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved December 9, 2021.
    9. ↑ Billio A, Morello E, Clarke MJ (January 2010). Billio A (ed.). "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. (Retracted, see doi:10.1002/14651858.cd006272.pub3)
    10. 1 2 Carlisle JB, Stevenson CA (July 2006). Carlisle J (ed.). "Drugs for preventing postoperative nausea and vomiting". The Cochrane Database of Systematic Reviews (3): CD004125. doi:10.1002/14651858.CD004125.pub2. PMC 6463839. PMID 16856030. (Retracted, see doi:10.1002/14651858.cd004125.pub3)
    11. ↑ 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.
    12. ↑ "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.
    13. ↑ 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
    14. ↑ FDA.gov Sustol Prescribing Information Archived April 9, 2021, at the Wayback Machine.
    Identifiers:
    • Aapro M (2004). "Granisetron: an update on its clinical use in the management of nausea and vomiting". The Oncologist. 9 (6): 673–86. doi:10.1634/theoncologist.9-6-673. PMID 15561811.
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