5-HT3 Receptor Antagonists (Antiemetics)
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Overview
Serotonin 5-HT3 receptor antagonists are among the most effective antiemetic agents available, primarily used for prevention and treatment of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery.
How do 5-ht3 receptor antagonists (antiemetics) work?
5-HT3 antagonists selectively block serotonin type 3 receptors located on vagal nerve terminals in the gastrointestinal tract and in the chemoreceptor trigger zone of the central nervous system. Chemotherapy and radiation cause enterochromaffin cells in the gut to release serotonin, which activates these receptors to trigger the vomiting reflex. By blocking this pathway, 5-HT3 antagonists prevent emesis at both peripheral and central sites.
Drugs in this class
- Ondansetron (Zofran, Zofran ODT, Zuplenz)