Chemistry:Tropisetron

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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.[1]

It was patented in 1982 and approved for medical use in 1992.[2] Tropisetron is a therapeutic alternative on the World Health Organization's List of Essential Medicines.[3] It is sold by Novartis in Europe, Australia, New Zealand, Japan, South Korea and the Philippines as Navoban, but is not available in the US. It is also available from Novell Pharmaceutical Laboratories and sold in several Asian countries as Setrovel.

Pharmacology

Tropisetron acts as both a selective 5-HT3 receptor antagonist and α7-nicotinic receptor partial agonist.[4][5]

Tropisetron have been shown to sensitise human α7-nicotinic receptors to low concentrations of acetylcholine, indicative of a possible co-agonist or other modulatory action of tropisetron at these receptors.[6]

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.[7][8][9] Hypotension, transient liver enzyme elevation, immune hypersensitivity syndromes and extrapyramidal side effects have also been associated with its use on at least one occasion.[7] 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.[10]

Other uses

As a biological stain and as trypanocide.[11][12]

References

  1. ↑ "Local treatment of tendinopathies and myofascial pain syndromes with the 5-HT3 receptor antagonist tropisetron". Scandinavian Journal of Rheumatology. Supplement 119 (119): 44–48. 2004. doi:10.1080/03009740410007032. PMID 15515413. 
  2. ↑ Analogue-based Drug Discovery. John Wiley & Sons. 2006. pp. 448. ISBN 978-3-527-60749-5. https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA448. 
  3. ↑ The selection and use of essential medicines, 2025: WHO Model List of Essential Medicines, 24th list. Geneva: World Health Organization. 2025. 
  4. ↑ "The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist". Bioorganic & Medicinal Chemistry Letters 11 (3): 319–321. February 2001. doi:10.1016/S0960-894X(00)00670-3. PMID 11212100. 
  5. ↑ "Tropisetron attenuates naloxone-induced place aversion in single-dose morphine-treated rats: role of alpha7 nicotinic receptors". European Journal of Pharmacology 609 (1–3): 74–77. May 2009. doi:10.1016/j.ejphar.2008.12.051. PMID 19374878. 
  6. ↑ "Tropisetron sensitizes α7 containing nicotinic receptors to low levels of acetylcholine in vitro and improves memory-related task performance in young and aged animals". Neuropharmacology 117: 422–433. May 2017. doi:10.1016/j.neuropharm.2017.02.025. PMID 28259598. 
  7. ↑ 7.0 7.1 "5-HT(3)-receptor antagonists for the treatment of nausea and vomiting: a reappraisal of their side-effect profile". The Oncologist 7 (5): 424–436. 2002. doi:10.1634/theoncologist.7-5-424. ISSN 1083-7159. PMID 12401905. 
  8. ↑ "Tropisetron, ondansetron, and granisetron for control of chemotherapy-induced emesis in Turkish cancer patients: a comparison of efficacy, side-effect profile, and cost". Cancer Investigation 25 (3): 135–139. 2007. doi:10.1080/07357900701208709. ISSN 0735-7907. PMID 17530482. 
  9. ↑ "Comparative Pharmacology and Guide to the Use of the Serotonin 5-HT3 Receptor Antagonists for Postoperative Nausea and Vomiting". Drugs 76 (18): 1719–1735. December 2016. doi:10.1007/s40265-016-0663-3. ISSN 1179-1950. PMID 27988869. 
  10. ↑ "Patient-tailored antiemetic treatment with 5-hydroxytryptamine type 3 receptor antagonists according to cytochrome P-450 2D6 genotypes". Journal of Clinical Oncology 20 (12): 2805–2811. 2002-06-15. doi:10.1200/JCO.2002.09.064. ISSN 0732-183X. PMID 12065557. 
  11. ↑ "In vitro effects of tropisetron and granisetron against Echinococcus granulosus (s.s.) protoscoleces by involvement of calcineurin and calmodulin" (in en). Parasites & Vectors 14 (1). 2021-04-12. doi:10.1186/s13071-021-04691-9. ISSN 1756-3305. PMID 33845889. 
  12. ↑ "Renoprotective effects of tropisetron through regulation of the TGF-β1, p53 and matrix metalloproteinases in streptozotocin-induced diabetic rats". Chemico-Biological Interactions 335. 2021-02-01. doi:10.1016/j.cbi.2020.109332. ISSN 0009-2797. PMID 33387473. Bibcode: 2021CBI...33509332P. https://www.sciencedirect.com/science/article/pii/S0009279720315519. 



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