Pharm

Palonosetron

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Palonosetron, Aloxi, Akynzeo

  • Indications
  1. Prevention of Postoperative Nausea and Vomiting
  2. Chemotherapy associated Nausea
    1. Not effective in treating Nausea after it occurs
    2. Most effective in preventing delayed Emesis
      1. Longer Half-Life (>40 hours) and higher 5-HT affinity than other 5HT3 Antagonists
  • Mechanism
  1. Blocks peripheral and central 5HT3 receptors
    1. Peripheral 5HT3 receptors at vagal nerve terminals
    2. Central 5HT3 receptors at ChemoreceptorTrigger Zone in Medulla (area postrema controls Vomiting)
  • Dosing
  • Palonosetron (Aloxi)
  1. Precautions
    1. Do NOT repeat dose more than once weekly
  2. Prevention of Nausea with Chemotherapy
    1. Adult: 0.25 mg IV over 30 seconds, given 30 min before Chemotherapy
    2. Child: 20 mcg/kg up to 1.5 mg IV over 15 min, given 30 min before Chemotherapy
  3. Prevention of Surgery Related Nausea
    1. Give 0.075 mg IV over 10 seconds, before Anesthesia
  1. Palonosetron is combined with the NK1 Antagonist Netupitant (Akynzeo)
    1. See Netupitant
    2. Pregnancy Category C
    3. Avoid in severe Chronic Kidney Disease or hepatic dysfunction
  2. Prevention of Nausea with Chemotherapy (adults only)
    1. Typically combined with Dexamethasone
    2. Capsules: 0.5 mg Palonosetron AND 300 mg Netupitant
      1. Take 1 capsule orally 1 hour prior to Chemotherapy
    3. Injection: 0.25 mg Palonosetron AND 235 mg fosNetupitant per vial
      1. Inject 1 vial in 50 ml IV over 30 minutes prior to Chemotherapy
  • Safety
  1. Pregnancy Category B
  2. Unknown safety in Lactation