5-HT3 antagonist

5-HT3 receptor antagonist
Drug class
Skeletal formula of ondansetron, the prototypical 5-HT3 antagonist
Class identifiers
UseNausea and Vomiting
ATC codeA04AA
Biological target5-HT3 receptor
Clinical data
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External links
MeSHD058831
Legal status
In Wikidata

The 5-HT3 antagonists, informally known as "setrons", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain. With the notable exceptions of alosetron and cilansetron, which are used in the treatment of irritable bowel syndrome, all 5-HT3 antagonists are antiemetics, used in the prevention and treatment of nausea and vomiting. They are particularly effective in controlling the nausea and vomiting produced by cancer chemotherapy and are considered the gold standard for this purpose.[1]

The 5-HT3 antagonists may be identified by the suffix -setron,[2] and are classified under code A04AA of the WHO's Anatomical Therapeutic Chemical Classification System.

  1. ^ de Wit R, Aapro M, Blower PR (2005). "Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?". Cancer Chemother Pharmacol. 56 (3): 231–8. doi:10.1007/s00280-005-1033-0. PMID 15838653. S2CID 27576150.
  2. ^ World Health Organization (2006). "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances" (PDF). (703 KiB). Geneva: WHO Press. Retrieved on 2007-05-15.