What it does
Palonsetron is a medication used to prevent nausea and vomiting, especially after surgery or chemotherapy.
Commonly used for: nausea and vomiting after chemotherapy, nausea and vomiting after surgery
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Source: Food and Drugs Authority · fetched 2026-05-12 08:01:04 · updated 2026-10-20 04:00:08
About this medicine
Palonsetron is a medication used to prevent nausea and vomiting, especially after surgery or chemotherapy.
What it treats
- nausea and vomiting after chemotherapy
- nausea and vomiting after surgery
How it works
Palonsetron works by blocking signals in the brain that cause nausea and vomiting.
Who it's for
It is for adults and children who need help managing nausea and vomiting due to medical treatments.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: palonsetron
Palonsetron is a selective serotonin 5-HT3 receptor antagonist used primarily for the prevention of nausea and vomiting associated with cancer chemotherapy and postoperative procedures. It is characterized by a longer half-life compared to other 5-HT3 antagonists, making it effective for delayed nausea and vomiting.
Indications
- Prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy
- Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy
- Prevention of postoperative nausea and vomiting
Dosage
Children: Refer to the BNF for Children for specific paediatric dosing recommendations.
Adults: Refer to the BNF for specific adult dosing recommendations.
Mechanism of action
Palonsetron works by selectively blocking the 5-HT3 receptors located in the central nervous system and gastrointestinal tract. By inhibiting these receptors, palonsetron prevents the action of serotonin, which is released in response to chemotherapy or surgical procedures, thereby reducing the sensation of nausea and the vomiting reflex.
Pharmacodynamics
Palonsetron exhibits dose-dependent antiemetic effects. The drug binds to the 5-HT3 receptors with high affinity, leading to effective inhibition of serotonin-induced emesis. It also has a longer duration of action compared to older 5-HT3 antagonists, which allows for extended protection against nausea and vomiting following chemotherapy and surgery.
Pharmacokinetics
Palonsetron is rapidly absorbed after intravenous administration, with a peak plasma concentration reached within 30 minutes. It has a half-life of approximately 40 hours, allowing for once-daily dosing. The drug is extensively metabolized in the liver, primarily by cytochrome P450 enzymes. The renal excretion of unchanged drug is minimal, indicating that hepatic metabolism is the main route of elimination.
Contra-indications
- Hypersensitivity to palonsetron or any of its components
- Concomitant use with apomorphine
Adverse effects
- Headache
- Constipation
- Dizziness
- Fatigue
- Injection site reactions
Interactions
- May enhance the effects of other serotonergic drugs, leading to an increased risk of serotonin syndrome
- Concomitant use with apomorphine may increase the risk of hypotension and loss of consciousness
Precautions
- Use with caution in patients with a history of cardiac arrhythmias
- Monitor for signs of serotonin syndrome when used with other serotonergic agents
- Caution in patients with renal impairment
Pregnancy
There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
It is not known whether palonsetron is excreted in human milk. Caution should be exercised when administering to a nursing woman.
Storage
Store at room temperature, away from light and moisture. Do not freeze.
Formulations
- Injection: 0.25 mg/5 mL vial
- Oral tablet: 0.5 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.