Ondansetron blocks serotonin 5-HT3 receptors to prevent nausea and vomiting associated with various medical treatments. Genetic variability in CYP2D6 can alter the drug's elimination rate and contribute to individual differences in its efficacy.
Ondansetron (Dosage)
Ondansetron is a medication used primarily for the prevention and treatment of nausea and vomiting associated with chemotherapy, radiotherapy, and surgical procedures. It belongs to the group of selective serotonin 5-HT3 receptor antagonists.
Ondansetron works by blocking serotonin 5-HT3 receptors located in the central nervous system and in the nerve endings of the gastrointestinal tract. During chemotherapy or radiotherapy, serotonin release in the intestine can activate these receptors and trigger the vomiting reflex. By inhibiting this signaling, ondansetron reduces the occurrence of nausea and vomiting.
The response to treatment can vary between individuals due to clinical and genetic factors. Among the genetic factors studied, CYP2D6 stands out, a liver enzyme involved in the metabolism of numerous medications, including ondansetron.
Side effects
- Headache
- Constipation
- Feeling of warmth or facial flushing
- Dizziness
- Fatigue
- Gastrointestinal disturbances
Precautions
Ondansetron has a good safety profile, although it should be used with caution in patients with cardiac risk factors due to the possibility of QT interval prolongation. The activity of the CYP2D6 enzyme can modify the rate of drug metabolism, potentially affecting its plasma concentrations and clinical response.
Drug interactions
CYP2D6 inhibitors can reduce the metabolism of ondansetron and increase its concentrations. The combination with drugs that prolong the QT interval should also be monitored.
Brand names
- Zofran®
- Ondansetron Normon®
- Ondansetron Teva®
- Ondansetron Accord®
Genes analyzed
Bibliography
Bell GC, Caudle KE, Whirl-Carrillo M, et al. Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline for CYP2D6 genotype and use of ondansetron and tropisetron. Clin Pharmacol Ther. 2017 Aug;102(2):213-218.
Moore C, Williams E, Dyas R, et al. CYP2D6 genotype and associated 5-HT3 receptor antagonist outcomes: A systematic review and meta-analysis. Clin Transl Sci. 2025 Feb;18(2):e70108..
