Pharm

Rolapitant

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Rolapitant, Varubi

  • See Also
  1. Neurokinin-1 Receptor Antagonist
  2. Aprepitant
  3. Antiemetic
  4. Chemotherapy Induced Nausea and Vomiting
  • 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
  • Dosing
  1. Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
    1. Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
    2. Take 180 mg orally 1 to 2 hours prior to Chemotherapy
  2. Postoperative Nausea and Vomiting Prevention (off-label)
    1. Give 90 to 180 mg orally at Anesthesia induction
  • Adverse Effects
  1. Asthenia or Fatigue
  2. Hiccups
  • Safety
  1. Unknown safety in pregnancy
  2. Unknown safety in Lactation
  • Drug Interactions
  1. May effect drugs metabolized by CYP2D6
  2. Thioridazine
    1. Avoid with NK1 Receptor Antagonist
  3. Strong CYP3A4 Inducers (e.g. Rifampin)
    1. May decrease Rolapitant effectiveness
  • 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. Rolapitant (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a52896cd-4a98-49b8-82db-bf1985a64d97
  • References
  1. (2023) Postoperative Nausea and Vomiting Management, Presc Lett, #390431
  2. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  3. (2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]