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[An outline of 5-HT3 receptor antagonists (1)--In pharmacological actions]
S Tsukagoshi1, J Ohta, T Taguchi
1Cancer Chemotherapy Center, Japanese Foundation for Cancer Research.
Abstract:
This paper described an outline of pharmacological studies of 5-HT3 receptor antagonists, mainly on ondansetron, which control nausea and vomiting associated with cancer chemotherapy. Administration of cytotoxic drugs is known to increase serotonin (5-HT) concentrations, and when released, 5-HT provokes the emetic responses via two routes; 1) 5-HT acts as an intrinsic transmitter substance and stimulates the emetic response via 5-HT3 receptors on vagal afferent terminals; 2) 5-HT transmits impulses to the vomiting center via 5-HT3 receptors on the chemoreceptor trigger zone in the area postrema of the central nervous system. 5-HT3 receptor antagonists are thought to exert an antiemetic action by specifically and competitively blocking 5-HT3 receptors.
Insights
Ondansetron and other 5-HT3 receptor antagonists effectively control chemotherapy-induced nausea and vomiting. These drugs work by blocking serotonin (5-HT) pathways involved in triggering emetic responses.
Area of Science:
- Pharmacology
- Neuroscience
- Oncology
Context:
- Chemotherapy often causes nausea and vomiting.
- Serotonin (5-HT) plays a key role in these side effects.
- The 5-HT3 receptor is implicated in the emetic pathway.
Purpose:
- To outline pharmacological studies of 5-HT3 receptor antagonists.
- To detail the mechanism of action for controlling chemotherapy-induced nausea and vomiting.
- To highlight the role of ondansetron.
Summary:
- Cytotoxic drugs increase serotonin (5-HT) levels, stimulating emesis.
- 5-HT acts on vagal afferent terminals and the central nervous system's chemoreceptor trigger zone.
- 5-HT3 receptor antagonists competitively block these receptors to prevent nausea and vomiting.
Impact:
- Provides a framework for understanding antiemetic drug action.
- Supports the clinical use of 5-HT3 antagonists in cancer care.
- Offers insights into managing chemotherapy side effects.