Tropisetron

Structural formula
General
Non-proprietary name	Tropisetron
other names	1 αH , 5 αH- tropane-3 α -yl-3-indole carboxylate; (1 R , 3 endo , 5 S ) -8-Methyl-8-azabicyclo [3.2.1] octan-3-yl-1 H -indole-3-carboxylate; Navoban;
Molecular formula	C 17 H 20 N 2 O 2
External identifiers / databases
PubChem	72165
ChemSpider	16736476
DrugBank	DB11699
Wikidata	Q29428
Drug information
ATC code	A04 AA03
Drug class	Antiemetic
Mechanism of action	selective blockade of central 5-HT 3 receptors
properties
Molar mass	284.35 g mol −1
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances	no GHS pictograms
	no GHS pictograms
H and P phrases	H: no H-phrases
	P: no P-phrases
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Tropisetron is a 5-HT3 antagonist and is mainly used as an antiemetic , but is now also used in pain therapy .

application areas

Tropisetron is as a remedy for vomiting , nausea and nausea used. This is particularly true in connection with chemotherapy and radiation therapy , where it can also be used preventively. It is also used for the prophylaxis of postoperative nausea and vomiting . A superiority of ondansetron , another 5-HT3 antagonist, over tropisetron compared to costs and prophylactic effect in high-risk patients was proven.

Several studies have shown a significant reduction in pain in some of the patients with fibromyalgia syndrome . The effect lasts for a relatively long time in these patients, without the need to take it permanently. In another part of the patients, however, no effect at all can be observed. Tropisetron is now widely recommended as a drug for treating fibromyalgia.

An analgesic effect has also been found in some rheumatic diseases and myofascial syndromes . The effect in these clinical pictures should be comparable to that of local anesthetics such as lidocaine or prilocaine . An anti-inflammatory effect was also found here. Evidence of effectiveness against pain is available for myofascial syndrome, osteoarthritis and rheumatoid arthritis .

It can be administered orally and intravenously.

Mechanism of action

Tropisetron blocks the action of the neurotransmitter serotonin on its receptors in the nervous system. The analgesic effect probably arises from the stimulation of the nociceptors, which arises when the activation of the 5-HT3 receptors is prevented.

Tropisetron is broken down by the enzyme CYP2D6.

Side effects

The most common side effects include headache , constipation, and diarrhea . High blood pressure , tremors , hives and shortness of breath are less common .

Interactions

Medicines taken at the same time such as antiarrhythmics , antibiotics and some drugs from the group of antidepressants can cause prolonged heart muscle excitation. Rifampicin and phenobarbital make tropisetron less effective.

Trade names

Navoban

Individual evidence

↑ Data sheet Tropisetron monohydrochloride from Sigma-Aldrich , accessed on April 2, 2011 ( PDF ).
↑ Roya Moazami-Benab: Ondansetron versus tropisetron for the prophylaxis of postoperative nausea and vomiting in high-risk patients with an abdominal and urological procedure under general anesthesia. (PDF; 336 kB). Dissertation . 2008, p 59. urn : nbn: de: gbv: 18-40289
↑ Definition, pathophysiology, diagnosis and treatment of fibromyalgia syndrome. ( Memento from March 1, 2011 in the Internet Archive ) (PDF; 1.0 MB) German Interdisciplinary Association for Pain Therapy (DIVS), 2012.
↑ D. Pongratz: Fibromyalgia - A current location determination. (PDF; 155 kB). 2006, p. 10.
^ P. Harten: Fibromyalgia syndrome: new developments in pharmacotherapy . doi: 10.1007 / s00393-007-0216-y . PMID 17924124
^ EP Calandre, F. Rico-Villademoros, M. Slim: An update on pharmacotherapy for the treatment of fibromyalgia . doi: 10.1517 / 14656566.2015.1047343 . PMID 26001183
↑ ^a ^b Th. Stratz, W. Müller: Local treatment of rheumatic diseases with the 5-HT3 receptor antagonist tropisetron . ( Memento of April 18, 2016 in the Internet Archive ) (PDF) In: The Pain , Volume 17, Issue 3, June 2003, pp. 200–203.
↑ W. Müller, BL Fiebich, T. Stratz: New treatment options using 5-HT3 receptor antagonists in rheumatic diseases . PMID 17017973

[Sigma-1] Data sheet Tropisetron monohydrochloride from Sigma-Aldrich , accessed on April 2, 2011 ( PDF ).

[RM-2] Roya Moazami-Benab: Ondansetron versus tropisetron for the prophylaxis of postoperative nausea and vomiting in high-risk patients with an abdominal and urological procedure under general anesthesia. (PDF; 336 kB). Dissertation . 2008, p 59. urn : nbn: de: gbv: 18-40289

[QZ-3] Definition, pathophysiology, diagnosis and treatment of fibromyalgia syndrome. ( Memento from March 1, 2011 in the Internet Archive ) (PDF; 1.0 MB) German Interdisciplinary Association for Pain Therapy (DIVS), 2012.

[VZ-4] D. Pongratz: Fibromyalgia - A current location determination. (PDF; 155 kB). 2006, p. 10.

[5] P. Harten: Fibromyalgia syndrome: new developments in pharmacotherapy . doi: 10.1007 / s00393-007-0216-y . PMID 17924124

[6] EP Calandre, F. Rico-Villademoros, M. Slim: An update on pharmacotherapy for the treatment of fibromyalgia . doi: 10.1517 / 14656566.2015.1047343 . PMID 26001183

[Stratz-7] Th. Stratz, W. Müller: Local treatment of rheumatic diseases with the 5-HT3 receptor antagonist tropisetron . ( Memento of April 18, 2016 in the Internet Archive ) (PDF) In: The Pain , Volume 17, Issue 3, June 2003, pp. 200–203.

[8] W. Müller, BL Fiebich, T. Stratz: New treatment options using 5-HT3 receptor antagonists in rheumatic diseases . PMID 17017973