5-HT3 antagonist
5-HT3 serotonin receptor antagonist
- Antiemetic effect
- ↓ enteric signaling → constipation/reduced GI motility
- Can lower seizure threshold (case reports)
- Release of neurotransmitters downstream with theoretical antidepressant and anxiolytic effect
- powerful disinhibitor of glutamate release
- Potential improvement of negative symptoms of schizophrenia
- Potential Improvement of OCD
- Theoretical mitigation of SRI-induced bipolar destabilization (El-Mallakh and Aydin, 2024)
- An effect of metoclopramide, mirtazapine, vortioxetine, clozapine, olanzapine, and loxapine
Drugs with this mechanism (9)
- Alosetron — 5-HT3 antagonist restricted to severe refractory IBS-D because of ischemic-colitis risk.
- Dolasetron — 5-HT3 antiemetic largely displaced because IV use carries marked QT risk.
- Granisetron — 5-HT3 antagonist antiemetic available as a multi-day transdermal patch.
- Memantine — NMDA antagonist for moderate-to-severe Alzheimer dementia; well tolerated.
- Metoclopramide — D2-antagonist prokinetic/antiemetic; tardive dyskinesia limits long use.
- Memantine XR — Extended-release NMDA antagonist for moderate-to-severe Alzheimer disease.
- Ondansetron — 5-HT3 antagonist antiemetic; QT prolongation at high dose.
- Palonosetron — Long-acting second-generation setron that covers delayed chemo nausea.
- Vortioxetine — Multimodal serotonergic antidepressant; cognitive benefits and less sexual dysfunction, but dose-related nausea.
Self-check
- What therapeutic effect follows 5-HT3 blockade?
Antiemesis. - What bowel adverse effect follows reduced enteric signaling with 5-HT3 blockade?
Constipation.
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