Palonosetron

Products

Palonosetron is commercially available as a solution for injection and as soft capsules (Aloxi, generic). It has been approved in many countries since 2006. The capsules were registered in 2013. Also approved is a fixed combination of netupitant and palonosetron in capsule form; see netupitant palonosetron.

Structure and properties

Palonosetron (C19H24N2O, Mr = 296.4 g/mol) is present in drugs as palonosetron hydrochloride, a white crystalline powder that is soluble in water.

Effects

Palonosetron (ATC A04AA05) has antiemetic properties. The effects are due to selective antagonism at serotonin 5HT3 receptors. Palonosetron has a long half-life of approximately 40 hours.

Indications

For prevention of nausea and vomiting associated with cytostatic chemotherapy.

Dosage

According to the SmPC. Capsules are taken one hour before chemotherapy, independent of meals.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Palonosetron is metabolized primarily by CYP2D6. CYP3A4 and CYP1A2 are involved to a minor extent. Corresponding drug-drug interactions are possible.

Adverse effects

The most common possible adverse effects include headache, dizziness, constipation, and diarrhea.