Palonosetron

Generic Details

Generic Name

Palonosetron

Other Names

  • Aloxi

Drug Class

  • 5-HT3 receptor antagonist

Chemical Formula

C19H24N2O

Molecular Weight

296.406 g/mol

Mechanism of Action

  • Selective inhibition of serotonin (5-HT3) receptors

Indications

  • Prevention of chemotherapy-induced nausea and vomiting (CINV)
  • Prevention of postoperative nausea and vomiting (PONV)

Common Dosage Forms

  • Oral tablets
  • Injection

Typical Dosage

  • 0.25 mg as a single dose prior to chemotherapy

Pediatric Dosage

  • Safety and efficacy not established in children

Geriatric Dosage

  • No dosage adjustment is necessary based on age alone

Side Effects

  • Headache
  • Fatigue
  • Constipation
  • Diarrhea
  • Dizziness

Contraindications

  • Hypersensitivity to palonosetron or any component of the formulation

Pregnancy Category

  • B - Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women

Lactation Safety

  • It is not known whether palonosetron is excreted in human milk, caution is advised

Drug Interactions

  • Concomitant use with apomorphine may result in profound hypotension and loss of consciousness

Overdose Symptoms

  • There is limited information on overdose, symptoms may include headache and mild hypertension

Antidote for Overdose

  • No specific antidote, symptomatic and supportive treatment should be given

Storage Conditions

  • Store at room temperature away from moisture and heat

Pharmacokinetics

  • Absorption: Well absorbed after oral administration
  • Distribution: Extensively distributed in tissues
  • Metabolism: Metabolized in the liver primarily by CYP2D6 and to a lesser extent by CYP3A4
  • Excretion: Primarily eliminated in the feces

Precautions

  • Use with caution in patients with a history of cardiac conduction abnormalities
  • Monitor for serotonin syndrome symptoms if used concomitantly with serotonergic drugs

Warnings

  • May cause QT interval prolongation and serotonin syndrome

Others

  • It has a long half-life making it suitable for single-dose regimens.