II. Indications
- Prevention of Nausea, Vomiting with highly emetogenic Chemotherapy
- Typically used in combination with 5-HT3 Antagonists and Dexamethasone 20 mg daily
III. Mechanism
- Blocks the neurokinin-1 receptor (a tachykinin)
- Cross the blood brain barrier to inhibit CNS substance-P activity
- Effects
- Antiemetic (synergistic with 5-HT3 Antagonists)
- Anxiolysis and Antidepressant properties
IV. Dosing: Aprepitant
- Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
- Oral (Emend) before Chemotherapy
- Adult: 125 mg orally 1 hour before Chemotherapy, then 80 mg orally daily in AM on days 2 and 3
- 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
- Oral (Emend) post-op Vomiting prophylaxis
- Adult: 40 mg orally given 3 hours or less prior to Anesthesia
- IV before Chemotherapy
- Fosaprepitant (Aprepitant prodrug)
- Adult: 150 mg infused over 20 to 30 minutes
- 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)
- Cinvanti
- Adult: 130 mg IV over 2 minutes (or infused over 30 min) OR 100 mg IV followed by oral Emend on days 2, 3
- Fosaprepitant (Aprepitant prodrug)
V. Dosing: Rolapitant (Varubi)
- Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
- Take 180 mg orally 1 to 2 hours prior to Chemotherapy
VI. Dosing: Netupitant/Palonosetron (Akynzeo)
- Combined 5HT-3 Antagonist (Palonosetron) with the NK1 Antagonist Netupitant
- Contraindicated in severe renal disease (including ESRD) and severe hepatic disease
- Oral: Take 1 capsule orally one hour before Chemotherapy
- IV: Give one injectable vial diluted in 50 ml over 30 min prior to Chemotherapy
VII. Pharmacokinetics: Aprepitant
IX. Safety
- Aprepitant Pregnancy Category B
- Unknown safety in Lactation
X. Drug Interactions: Aprepitant (Emend, Fosaprepitant, Cinvanti)
- May affect drugs metabolized by CYP3A4
- CYP2C9 Inducer
-
Pimozide
- Avoid with NK1 Receptor Antagonist
-
Oral Contraceptives (OCP)
- Aprepitant may reduce OCP efficacy (use second form of Contraception)
-
Warfarin
- Aprepitant may affect INR
XI. Drug Interactions: Rolapitant (Varubi)
- May effect drugs metabolized by CYP2D6
-
Thioridazine
- Avoid with NK1 Receptor Antagonist
- Strong CYP3A4 Inducers (e.g. Rifampin)
- May decrease Rolapitant effectiveness
XII. Resources
- NK1 Receptor Antagonist (Wikipedia)
- Antiemetic Neurokinin-1 Receptor Blockers (Stat Pearls)
- Aprepitant - Emend (DailyMed)
- Aprepitant - Cinvanti (DailyMed)
- Rolapitant (DailyMed)
XIII. References
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
- (2003) Med Lett Drugs Ther 45(W1162B): 62-4 [PubMed]
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aprepitant (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
APREPITANT 40 MG CAPSULE | Generic | $52.79 each |