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Antiemetics
Tropisetron
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Tropisetron

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Not to be confused with Tropanserin.
Tropisetron
Tropisetron structure.svg
Tropisetron3Dan.gif
Clinical data
Trade names Navoban
Other names ICS 205-930
AHFS/Drugs.com International Drug Names
Pregnancy
category
  • AU: B3
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 binding 71%
Metabolism Hepatic (CYP3A4, CYP1A2, CYP2D6)
Elimination half-life 6–8 hours
Excretion Renal, Fecal
Identifiers
  • (1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 1methyl-indole-3-carboxylate
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C17H20N2O2
Molar mass 284.359 g·mol−1
3D model (JSmol)
  • CN4[C@@H]1CC[C@H]4C[C@H](C1)OC(=O)c3c[nH]c2ccccc23
  • InChI=1S/C17H20N2O2/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16/h2-5,10-13,18H,6-9H2,1H3/t11-,12+,13+ checkY
  • Key:ZNRGQMMCGHDTEI-ITGUQSILSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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.

It was patented in 1982 and approved for medical use in 1992. It is on the World Health Organization's List of Essential Medicines. 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.

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

External links


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