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Zofran: Applications in Medicine as a Serotonin Blocker

Chemotherapy induced nausea and vomiting, CINV, has been a significant problem with oncology patients over past years.As a result much research was done and has lead to the creation of Zofran (Bernstein and Ong 2002).Ondansetron, marketed as Zofran was thefirst of its kind; it is a serotonin 5-HT3 receptor blocker, otherwise know as an antiemetic agent.Ondansetron is a tremendous breakthrough and is much more effective than older antiemetics, in some cases by almost 50% (Ramsook 2002).Ondansetron was FDA approved in January 1991 as a treatment for chemotherapy-induced nausea and vomiting with parenteraly administered dosage. It was later approved in oral dosage forms as a treatment for post-operative nausea and vomiting in April 1995.In 1999 ondansetron was approved for use as an “orally disintegrating tablet,” Zofran ODT®.This form of ondansetron does not require water to assist in swallowing (Clinical Pharmacology 2002).Now ondansetron is used primarily as a treatment for chemotherapy-induce and post-operative nausea and vomiting; however, it is also being recently used to treat drug dependencies such as alcoholism and to treat gastrointestinal disorders such as acute gastroenteritis.
Ondansetron blocks the serotonin 5-HT3 receptors centrally and peripherally.5-HT3 receptors are found centrally in the chemoreceptor trigger zone and peripherally in the lining of the small intestines.Most emesis, often associated with chemotherapy and/or radiation therapy, appears to be connected with the release of serotonin 5-HT3 from enterochromaffin cells that line the small intestine walls.By blocking these nerves signals to the central nervous system can no longer be sent.Ondansetron has also been identified as a small combatant of the serotonin 5-HT4 receptor (Physician’s Desk Reference 1993).Research is continuing to be done on what other agents ondansetron combats and if its action is mediated centrally or per…

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