Skip to main content

5HT3 receptor antagonists

Other names: 5hydroxytryptamine receptor antagonists, serotonin blockers, serotonin receptor antagonists

What are 5HT3 receptor antagonists?

5-HT3 receptor antagonists (also called serotonin receptor antagonists or serotonin blockers) are a class of medicines that are used for the prevention and treatment of nausea and vomiting, particularly that caused by chemotherapy, radiation therapy, or postoperatively. 5-HT3 is an abbreviation for serotonin that may also be written as 5-hydroxytryptamine.

Cells lining the gastrointestinal tract release serotonin when damaged by chemotherapy and radiation therapy. This serotonin binds to serotonin receptors on nerves that transmit impulses to the vomiting center within the brain, which in turn stimulates other nerves involved in the vomit reflex. 5-HT3 receptor antagonists prevent serotonin from binding to 5-HT3 receptors in the small intestine thereby reducing the likelihood of nausea and vomiting. The way 5-HT3 receptor antagonists work to prevent postoperative nausea and vomiting is less well understood.

The first generation 5-HT3 receptor antagonists include dolasetron, granisetron, and ondansetron. Despite variations in their chemical structures and absorption rates, they all work in the same way and are well tolerated. The oral formulations are just as effective at preventing nausea and vomiting as the intravenous forms.

Palonosetron is a second-generation serotonin blocker. It has a greater affinity for serotonin receptors than first generation agents, which increases its duration of effect. Palonosetron is also thought to have an effect on 5-HT3 receptors in the vomiting center and chemoreceptor trigger zone as well, not just the small intestine. It is approved for both acute and delayed chemotherapy-induced nausea and vomiting.

List of 5HT3 receptor antagonists

View by  Brand | Generic
Drug Name Avg. Rating Reviews
Zofran (Pro)
Generic name: ondansetron
263 reviews
Zofran ODT (Pro)
Generic name: ondansetron
58 reviews
Sancuso (Pro)
Generic name: granisetron
14 reviews
Generic name: granisetron
2 reviews
Aloxi (Pro)
Generic name: palonosetron
2 reviews
Sustol (Pro)
Generic name: granisetron
1 review
Zuplenz (Pro)
Generic name: ondansetron
No reviews
Anzemet (Pro)
Generic name: dolasetron
No reviews
For ratings, users were asked how effective they found the medicine while considering positive/adverse effects and ease of use (1 = not effective, 10 = most effective).

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.