Ondansetron: A Selective 5‐HT3Receptor Antagonist and Its Applications in CNS‐Related Disorders
Open accessAbstract
Ondansetron is a selective 5‐hydroxytryptamine3 (5‐HT 3) receptor antagonist that has been introduced to clinical practice as an antiemetic for cancer treatment‐induced and anesthesia‐related nausea and vomiting. Its use under these circumstances is both prophylactic and therapeutic. It has a superior efficacy, safety and pharmacoeconomic profile compared with other groups of antiemetics, namely antidopaminergics, antihistamines and anticholinergics. However, its place in the management of anticipatory and delayed vomiting in cancer treatment and as a rescue antiemetic in surgical patients needs to be further explored. Furthermore, recent animal and human research also reflects its possible novel application in the treatment of other disease states, such as alcoholism, cocaine addiction, opioid withdrawal syndrome, anxiety disorders, gastrointestinal motility disorders, Tourette's syndrome and pruritus. This review revisits the widespread physiological and pathological effects of 5‐HT and discusses both the basic science literature and the clinical developments responsible for the conventional and novel uses of ondansetron. In addition, new discoveries relating to the effects of ondansetron on other receptors/channels and their possible therapeutic applications are presented.
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Single high doses of ondansetron reduce activation in the insula, precentral and postcentral gyri, and cingulate cortex.
“Single high doses of ondansetron, a 5-HT3 receptor antagonist FDA approved for severe nausea and vomiting [104], reduce activation in the insula, precentral and postcentral gyri, and cingulate cortex [105].”
From Toward a neurocircuit-based taxonomy to guide treatment of obsessive-compulsive disorder (2021) · cites this paper as [104]
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- Authors
- Ye, J., Ponnudurai, R., & Schaefer, R.
- Affiliations
- Rutgers New Jersey Medical School (US)
- Venue
- CNS Drug Reviews
- Publisher
- Wiley
- Published
- 2001-06
- Volume
- 7
- Issue
- 2
- Pages
- 199-213
- ISSN
- 1080-563X (ISSN-L)
- 1527-3458
- PMC
- PMC6741689
- OpenAlex
- W2067758452
- Cited by
- 162
- References
- 75
- Citations by year
- 2026: 3 · 2025: 11 · 2024: 10 · 2023: 11 · 2022: 13 · 2021: 9 · 2020: 4 · 2019: 5 · 2018: 5 · 2017: 4 · 2016: 11 · 2015: 9 · 2014: 9 · 2013: 12 · 2012: 5
- FWCI
- 1.03
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- CNS Drug Reviews (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute on Alcohol Abuse and Alcoholism (AA11989, R01AA011989)
- Topics
- Health Sciences › Medicine › Surgery › Nausea and vomiting management
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Health Sciences › Medicine › Gastroenterology › Gastrointestinal motility and disorders
- Keywords
- ondansetron, 5-HT3 receptor antagonists, serotonin, antiemetics, chemotherapy-induced nausea and vomiting, postoperative nausea and vomiting, alcoholism, cocaine dependence, opioid withdrawal, anxiety disorders, gastrointestinal motility disorders, Tourette syndrome, pruritus, off-label drug use, rescue antiemetics
- MeSH terms
- Animals, Colonic Diseases, Functional, Humans, Ion Channels, Nausea, Receptors, Serotonin, Serotonin Antagonists, Vomiting, Ondansetron
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