Tropisetron Explained

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] It is on the World Health Organization's List of Essential Medicines.^[3] 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 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. 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

• 5-HT₃ receptor antagonist: Drug discovery and development
• Zatosetron
• Ricasetron
• Bemesetron
• Tropanserin
• Granisetron

External links

• Official site
• Navoban data sheet

Notes and References

1. Müller W, Stratz T . 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 . 15515413 . 10.1080/03009740410007032 . 24916914 .
2. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 9783527607495 . 448 . en.
3. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 22nd list (2021) . 2021 . 10665/345533 . World Health Organization . World Health Organization . Geneva . WHO/MHP/HPS/EML/2021.02 . free .
4. Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC . 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 . 11212100 . 10.1016/S0960-894X(00)00670-3 .
5. Cui R, Suemaru K, Li B, Kohnomi S, Araki H . 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 . 19374878 . 10.1016/j.ejphar.2008.12.051 .
6. Callahan PM, Bertrand D, Bertrand S, Plagenhoef MR, Terry AV . 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 . 28259598 . 10.1016/j.neuropharm.2017.02.025 . 9400277 .