Tropisetron

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Tropisetron
Tropisetron2DACS2.svg
Tropisetron3Dan.gif
Systematic (IUPAC) name
(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl 1methyl-indole-3-carboxylate
Clinical data
Trade names Navoban
AHFS/Drugs.com International Drug Names
Pregnancy cat. B3 (AU)
Legal status Prescription Only (S4) (AU) POM (UK)
Routes Oral, IV
Pharmacokinetic data
Bioavailability ~60–80%
Protein binding 71%
Metabolism Hepatic (CYP3A4, CYP1A2, CYP2D6)
Half-life 6–8 hours
Excretion Renal, Fecal
Identifiers
CAS number 89565-68-4 N
ATC code A04AA03
PubChem CID 72165
IUPHAR ligand 260
ChemSpider 16736476 YesY
UNII 6I819NIK1W YesY
KEGG D02130 YesY
ChEMBL CHEMBL496980 N
Synonyms ICS 205-930
Chemical data
Formula C17H20N2O2 
Mol. mass 284.353 g/mol
 N (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.

See also[edit]

References[edit]

  1. ^ 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 (119): 44–48. PMID 15515413. Retrieved 2007-05-17. 
  2. ^ Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC (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]