Generic
Palonosetron
44 brands available in the market
At a glance
Palonosetron is a 5-HT3 receptor antagonist used for prevention of nausea and vomiting associated with chemotherapy, radiotherapy and surgery. It blocks serotonin receptors to prevent the vomiting reflex.
Description
Palonosetron is a 5-HT3 receptor antagonist with strong binding affinity for this receptor. Chemotherapeutic agents release serotonin from enterochromaffin cells of the small intestine which activates 5-HT3 receptors on vagal nerve terminals to initiate the vomiting reflex. Palonosetron blocks this reflex.
Indications
- Chemotherapy-induced nausea and vomiting (acute and delayed)
- Radiotherapy-induced nausea and vomiting
- Postoperative and post-discharge nausea and vomiting
Therapeutic class
Anti-emetic Drugs
Pharmacological class
5-HT3 Receptor Antagonist
Pharmacology
Palonosetron binds to 5-HT3 receptors to block serotonin action, preventing the vomiting reflex initiated by 5-HT release from the small intestine during chemotherapy and radiotherapy.
Mechanism of action
Controls nausea and vomiting by blocking serotonin receptors.
Dosage
Adult Dose:
- IV (CINV): 0.25 mg IV single dose (over 30 seconds), 30 minutes before chemotherapy; do not repeat within 7 days
- Oral (CINV): 0.5 mg tablet/capsule, 1 hour before chemotherapy
- IV (PONV): 0.075 mg IV single dose (over 10 seconds), before anesthesia induction
Pediatric Dose (1 month-17 years): 20 mcg/kg IV (over 15 minutes), 30 minutes before chemotherapy; max 1.5 mg/dose
Administration
- Oral: May be taken with or without food
- IV: Administered by doctor or nurse slowly
- Oral soluble film: Place on tongue
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Headache
- Constipation
Precautions & warnings
- Caution while driving (may cause dizziness and drowsiness)
- Avoid alcohol
- Caution in heart or liver problems, stomach or intestinal obstruction
Contraindications
- Hypersensitivity
Drug interactions
- Additive effect on QT prolongation with QT-prolonging drugs (moxifloxacin, erythromycin, antipsychotics, TCAs)
Food interactions
Safety with alcohol not known; consult doctor.
Use in pregnancy
Use in Pregnancy: Palonosetron is considered safe during pregnancy; animal studies show low or no adverse effects.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Palonosetron is probably safe during breastfeeding; no significant risk to baby.
Pediatric use
Dose established for children 1 month-17 years (CINV); safety not established in <18 years for PONV.
Geriatric use
No dose adjustment needed in elderly.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed.
Hepatic Impairment: Safe in liver disease; no dose adjustment needed.
Overdose effects
No specific antidote for overdose; supportive care.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Palonosetron