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Palonosetron: Uses, Dosage, Side Effects & Brands | MedexInfo

Palonosetron: Uses, Dosage, Side Effects & Brands | MedexInfo

Palonosetron

Rx Only
Generic NamePalonosetron
Therapeutic Class5-HT3 Antagonist
Common Dose0.25 mg IV single dose
Max / 24h0.75 mg
PregnancyCategory B
Indications ▼
Prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV)
Prevention of postoperative nausea and vomiting (PONV)
Radiation-induced nausea and vomiting (off-label)
Mechanism & Pharmacokinetics ▼
Mechanism: Selective serotonin (5-HT3) receptor antagonist that blocks serotonin receptors centrally (chemoreceptor trigger zone) and peripherally in the GI tract.
Pharmacokinetics: High receptor binding affinity and long half-life (~40 hours). Metabolized mainly by CYP2D6 (also CYP3A4 & CYP1A2). Eliminated via urine and feces.
Dosage & Administration ▼
Patient CategoryRecommended DoseMax / 24h
Adults (CINV)0.25 mg IV single dose 30 minutes before chemotherapy0.75 mg
Adults (PONV)0.075 mg IV immediately before induction of anesthesia0.075 mg
Oral (Combination therapy)0.5 mg capsule prior to chemotherapy0.5 mg
ElderlyNo dose adjustment requiredSame as adults
Note: Administer IV slowly over 30 seconds. Often combined with dexamethasone for enhanced antiemetic effect.
Side Effects ▼
Common: Headache, constipation
Occasional: Dizziness, fatigue
Rare: QT prolongation, hypersensitivity reactions
Contraindications ▼
Hypersensitivity to palonosetron or other 5-HT3 antagonists
Use cautiously in patients with cardiac conduction disorders
Drug Interaction ▼
Serotonergic drugs (SSRIs, SNRIs, tramadol): risk of serotonin syndrome
QT-prolonging agents: monitor ECG
CYP2D6 inhibitors: may increase levels
Pregnancy & Lactation ▼
Category B; no adequate human studies, use if clearly needed
Unknown if excreted in breast milk; caution advised
Clinical / Research Summary ▼
Superior control of delayed CINV compared to first-generation 5-HT3 antagonists.
Long half-life allows single-dose therapy per chemotherapy cycle.
Effective in combination with corticosteroids and NK1 receptor antagonists.
Well tolerated with minimal cardiac risk compared to older agents.
Patient Counseling Points ▼
Usually given before chemotherapy or surgery.
Report persistent constipation or severe headache.
Inform doctor about antidepressants or other serotonergic medicines.
Storage & Handling ▼
Store injection at 20–25°C
Protect from light
Do not freeze
Medical Disclaimer: This information is for educational purposes only. Always consult a registered healthcare professional for medical advice.

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