Drug information of Palonosetron

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Palonosetron is an antagonist of 5-HT3 receptors that is indicated for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Mechanism of effect

Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.


Palonosetron has a high affinity for 5-HT3 receptors, but has little to no affinity for other receptors.


Half-life: 40 hr

Peak plasma: 5.6±5.5 ng/mL (dose-proportional)

AUC: 35.8±20.9 ng.hr/mL (dose-proportional)

Protein bound: 62%

Vd: 8.3±2.5 L/kg

Metabolism: CYP2D6, CYP3A and CYP1A2

Metabolites: N-oxide-palonosetron and 6-S-hydroxy-palonosetron (<1% parent activity)

Excretion: Urine (80-93%); feces (5-8%)

Clearance: 160±35 mL/hr/kg (total)



Prevention of Chemotherapy-induced Nausea & Vomiting

0.25 mg IV over 30 seconds x1, beginning 30 minutes before chemotherapy

Prevention of Postoperative Nausea & Vomiting

0.075 mg IV infused over 10 seconds immediately before anesthesia



Prevention of Chemotherapy-induced Nausea & Vomiting

Indicated for prevention of acute N/V associated with initial and repeat courses of emetogenic cancer chemotherapy, including highly emetogenic cancer chemotherapy

<1 month: Safety and efficacy not established

1 month to 17 years: 20 mcg/kg IV infused over 15 minutes x1, beginning 30 minutes before chemotherapy; not to exceed 1.5 mg/dose

Prevention of Postoperative Nausea & Vomiting

<18 years: Safety and efficacy not established


Use caution in patients with congenital long QT syndrome or other factors that may prolong QT interval

Serotonin syndrome reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs including SSRIs, SNRIs, MAO inhibitors, lithium, tramadol, methylene blue IV, and mirtazapine

Hypersensitivity reactions, including anaphylaxis, reported with or without known hypersensitivity to other 5-HT3 receptor antagonists

For chemotherapy, the drug should follow a specific schedule, and not be administered as needed

Drug is not recommended in PONV if expectation for nausea or vomiting is very small; use only if the expectation is low or it is essential to avoid nausea and vomiting in the postoperative period

Points of recommendation

  • Tell all of your health care providers that you take palonosetron. This includes your doctors, nurses, pharmacists, and dentists.
  • Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

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