Tropisetron

Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy, although it has been used experimentally as an analgesic in cases of fibromyalgia.[1]

Tropisetron
Clinical data
Trade namesNavoban
Other namesICS 205-930
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
    Routes of
    administration    		Oral, IV
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: Not available or approved
    Pharmacokinetic data
    Bioavailability~60–80%
    Protein binding71%
    MetabolismHepatic (CYP3A4, CYP1A2, CYP2D6)
    Elimination half-life6–8 hours
    ExcretionRenal, Fecal
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC17H20N2O2
    Molar mass284.353 g/mol g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    It was patented in 1982 and approved for medical use in 1992.[2] It is marketed by Novartis in Europe, Australia, New Zealand, Japan, South Korea and the Philippines as Navoban, but is not available in the U.S. It is also available from Novell Pharmaceutical Laboratories and marketed in several Asian countries as Setrovel.

    Pharmacology

    Tropisetron acts as both a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist.[3][4]

    Adverse effects

    Tropisetron is a well-tolerated drug with few side effects. Headache, constipation, and dizziness are the most commonly reported side effects associated with its use. Hypotension, transient liver enzyme elevation, immune hypersensitivity syndromes and extrapyramidal side effects have also been associated with its use on at least one occasion. There have been no significant drug interactions reported with this drug's use. It is broken down by the hepatic cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.

    Other uses

    As a biological stain and as trypanocide

    See also

    References
    1. Müller, W.; Stratz, T. (2004). "Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron". Scand J Rheumatic Suppl. 119 (119): 44–48. PMID 15515413. Retrieved 2007-05-17.
    2. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495.
    3. Macor, J.E.; Gurley, D.; Lanthorn, T.; Loch, J.; Mack, R.A.; Mullen, G.; Tran, O.; Wright, N.; Gordon, J.C. (February 2001). "The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist". Bioorganic & Medicinal Chemistry Letters. 11 (3): 319–21. doi:10.1016/S0960-894X(00)00670-3. PMID 11212100.
    4. Cui, R.; Suemaru, K.; Li, B.; Kohnomi, S.; Araki, H. (May 2009). "Tropisetron attenuates naloxone-induced place aversion in single-dose morphine-treated rats: role of alpha7 nicotinic receptors". European Journal of Pharmacology. 609 (1–3): 74–7. doi:10.1016/j.ejphar.2008.12.051. PMID 19374878.


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