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Neurokinin-1 Receptor Antagonist

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Neurokinin-1 Receptor Antagonist, NK1 Receptor Antagonist, Netupitant

  • Indications
  1. Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
    1. Typically used in combination with 5-HT3 Antagonists and Dexamethasone 20 mg daily
  • Mechanism
  1. Blocks the neurokinin-1 receptor (a tachykinin)
  2. Cross the blood brain barrier to inhibit CNS substance-P activity
  3. Effects
    1. Antiemetic (synergistic with 5-HT3 Antagonists)
    2. Anxiolysis and Antidepressant properties
  1. Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
  2. Oral (Emend) before Chemotherapy
    1. Adult: 125 mg orally 1 hour before Chemotherapy, then 80 mg orally daily in AM on days 2 and 3
    2. Child (age >6 months): 3 mg/kg (up to 125 mg), then 2 mg/kg (up to 80 mg) orally daily in AM on days 2 and 3
  3. Oral (Emend) post-op Vomiting prophylaxis
    1. Adult: 40 mg orally given 3 hours or less prior to Anesthesia
  4. IV before Chemotherapy
    1. Fosaprepitant (Aprepitant prodrug)
      1. Adult: 150 mg infused over 20 to 30 minutes
      2. Child: 3 mg/kg (up to 125 mg) IV over 20 to 30 minutes, followed by oral Emend on days 2, 3 (see dose above)
    2. Cinvanti
      1. Adult: 130 mg IV over 2 minutes (or infused over 30 min) OR 100 mg IV followed by oral Emend on days 2, 3
  1. Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
  2. Take 180 mg orally 1 to 2 hours prior to Chemotherapy
  1. See Akynzeo
  2. Combined 5HT-3 Antagonist (Palonosetron) with the NK1 Antagonist Netupitant
  3. Contraindicated in severe renal disease (including ESRD) and severe hepatic disease
  4. Oral: Take 1 capsule orally one hour before Chemotherapy
  5. IV: Give one injectable vial diluted in 50 ml over 30 min prior to Chemotherapy
  • Adverse Effects
  • Drug Interactions
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]