Tropisetron

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Tropisetron
Tropisetron structure.svg
Tropisetron3Dan.gif
Clinical data
Trade namesNavoban
SynonymsICS 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
Chemical and physical data
FormulaC17H20N2O2
Molar mass284.353 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Tropisetron (INN) 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] The drug is available in a 5 mg oral preparation or in 2 mg intravenous form. 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[edit]

Tropisetron acts as both a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist.[2][3]

Adverse effects[edit]

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[edit]

As a biological stain and as trypanocide[citation needed]

See also[edit]

References[edit]

  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. ^ 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.
  3. ^ 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.

External links[edit]