The Sound of Evolution
Granisetron
Mechanism of action:
Granisetron is a selective 5-HT₃ receptor antagonist. Chemotherapy or radiotherapy stimulates enterochromaffin cells in the gut to release large amounts of serotonin (5-HT). After serotonin activates 5-HT₃ receptors on the vagus nerve, vomiting signals are transmitted to the central nervous system. Granisetron binds to and blocks 5-HT₃ receptors, suppressing 5-HT₃ receptor-mediated vagal afferent signaling and reducing activation of the vomiting reflex pathway.
Reference(s):
1. Gan TJ et al. (2005). Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs.
2. Tan M et al. (2003). Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother.
3. Feyer P et al. (2005). Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer.