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Tropisetron



Tropisetron
Systematic (IUPAC) name
[(1S,5S)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl] 1H-indole-3-carboxylate
Identifiers
CAS number	89565-68-4
ATC code	A04AA03
PubChem	72165
Chemical data
Formula	C₁₇H₂₀N₂O₂
Mol. mass	284.353 g/mol
SMILES	search in eMolecules, PubChem
Pharmacokinetic data
Bioavailability	~60–80%
Protein binding	71%
Metabolism	Hepatic (CYP3A4, CYP1A2, CYP2D6)
Half life	6–8 hours
Excretion	Renal, Fecal
Therapeutic considerations
Pregnancy cat.	X(AU)
Legal status	Prescription Only (S4)(AU) POM(UK)
Routes	Oral, IM

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 and New Zealand as Navoban, but is not available in the U.S.

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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. 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.

References

^ Muller, W.; T. Stratz (2004). "Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron". Scand J Rheumatic Suppl. 119: 44–48. PMID 15515413. Retrieved on 2007-05-17.

v • d • e Antiemetics and antinauseants (A04)
Serotonin (5-HT₃) antagonists	Ondansetron • Granisetron • Tropisetron • Dolasetron • Palonosetron
Other	Scopolamine • Cerium oxalate • Chlorobutanol • Metopimazine • Cannabinoids (Dronabinol, Nabilone) • NK1 receptor antagonist (Aprepitant)