Neurokinin-1 Receptor Antagonist

Aka: Neurokinin-1 Receptor Antagonist, NK1 Receptor Antagonist, Netupitant

advertisement

II. Indications

  1. Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
    1. Typically used in combination with 5-HT3 Antagonists and Dexamethasone 20 mg daily

III. 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

IV. Dosing: Aprepitant

  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

V. Dosing: Rolapitant (Varubi)

  1. Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
  2. Take 180 mg orally 1 to 2 hours prior to Chemotherapy

VI. Dosing: Netupitant/Palonosetron (Akynzeo)

  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

VII. Adverse Effects

  1. Asthenia or Fatigue
  2. Hiccups

VIII. Drug Interactions

  1. See Aprepitant (Emend, Fosaprepitant, Cinvanti)
  2. See Rolapitant (Varubi)

IX. Resources

  1. NK1 Receptor Antagonist (Wikipedia)
    1. https://en.wikipedia.org/wiki/NK1_receptor_antagonist
  2. Antiemetic Neurokinin-1 Receptor Blockers (Stat Pearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK470394
  3. Aprepitant - Emend (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f58b8944-93ee-4be1-a238-cc0061ddd93a
  4. Aprepitant - Cinvanti (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4c218d3a-a508-4abc-9ed8-a6e8e191d1b4
  5. Rolapitant (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a52896cd-4a98-49b8-82db-bf1985a64d97

X. References

  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]

Images: Related links to external sites (from Bing)

These images are a random sampling from a Bing search on the term "Neurokinin-1 Receptor Antagonist." Click on the image (or right click) to open the source website in a new browser window. Search Bing for all related images

Related Studies

Related Topics in Pharmacology

advertisement