Neurokinin-1 Receptor Antagonist

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

Blocks the neurokinin-1 receptor (a tachykinin)
Cross the blood brain barrier to inhibit CNS substance-P activity
Effects
1. Antiemetic (synergistic with 5-HT3 Antagonists)
2. Anxiolysis and Antidepressant properties

Typically administered with 5-HT3 Antagonists and Dexamethasone before Chemotherapy
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
Oral (Emend) post-op Vomiting prophylaxis
1. Adult: 40 mg orally given 3 hours or less prior to Anesthesia
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

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

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

May affect drugs metabolized by CYP3A4
CYP2C9 Inducer
Pimozide
1. Avoid with NK1 Receptor Antagonist
Oral Contraceptives (OCP)
1. Aprepitant may reduce OCP efficacy (use second form of Contraception)
Warfarin
1. Aprepitant may affect INR