5-HT3 antagonist

5-HT ₃ receptor antagonists are active substances that occupy 5-HT ₃ receptors as inhibitors . An essential area of application is antiemesis. They suppress nausea and vomiting that occur during tumor chemotherapy or radiation therapy or after surgical operations . The receptor inhibition can be competitive or non-competitive in nature. Setrons are a chemically defined class of medicinally used antiemetics with the active principle of 5-HT ₃ receptor inhibition.

Alosetron is approved in the United States under the trade name Lotronex for the treatment of irritable bowel syndrome . For the representative tropisetron there are indications from several studies for a reduction of the pain in the hitherto difficult to treat fibromyalgia syndrome . However, this only applies to some of the patients, as other patients are classified as therapy-resistant for the drug.

Setron-class drugs

EU and Switzerland:
- Dolasetron (trade name Anemet )
- Granisetron ( Kevatril , Kytril , Sancuso )
- Ondansetron ( Axisetron , Cellondan , Ondansan , Zofran , Zotrix )
- Palonosetron ( Aloxi )
- Tropisetron ( Navoban )
additionally in the USA:
- Alosetron ( Lotronex )
only in Japan and certain parts of Southeast Asia:
- Ramosetron ( Nasea )

literature

Ernst Mutschler u. a .: drug effects . 8th edition. Scientific publishing company. Stuttgart 2001. ISBN 3-8047-1763-2

References

^ Robin Herbrechte, Paul M. Ziemba a. a .: Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids. In: Frontiers in Pharmacology. 6, 2015, doi: 10.3389 / fphar.2015.00130 .
↑ Christiane Berg: Alosetron relieves symptoms of irritable bowel syndrome. In: Pharmazeutische Zeitung , 2000.
↑ German Interdisciplinary Association for Pain Therapy (DIVS): Definition, pathophysiology, diagnosis and therapy of fibromyalgia syndrome ( Memento of October 31, 2012 in the Internet Archive ) 2008, p. 67.
↑ D. Pongratz: Fibromyalgia - A current location determination . In: R. Dengler, D. Pongratz (Eds.): Management of neuromuscular diseases . tape 11 , letter no. 32 , 2006, pp. 1–12 ( full text [PDF; 154 kB ] Here: p. 10).
↑ Abriged prescribing information - Nasea (MIMS Philippines) . Retrieved June 13, 2008.

[1] Robin Herbrechte, Paul M. Ziemba a. a .: Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids. In: Frontiers in Pharmacology. 6, 2015, doi: 10.3389 / fphar.2015.00130 .

[PZ-2] Christiane Berg: Alosetron relieves symptoms of irritable bowel syndrome. In: Pharmazeutische Zeitung , 2000.

[QZ-3] German Interdisciplinary Association for Pain Therapy (DIVS): Definition, pathophysiology, diagnosis and therapy of fibromyalgia syndrome ( Memento of October 31, 2012 in the Internet Archive ) 2008, p. 67.

[VZ-4] D. Pongratz: Fibromyalgia - A current location determination . In: R. Dengler, D. Pongratz (Eds.): Management of neuromuscular diseases . tape 11 , letter no. 32 , 2006, pp. 1–12 ( full text [PDF; 154 kB ] Here: p. 10).

[5] Abriged prescribing information - Nasea (MIMS Philippines) . Retrieved June 13, 2008.