Contraindicated in:
Use Cautiously in:
CV: dizziness, fatigue, weakness.
Derm: STEVENS-JOHNSON SYNDROME.
GI: diarrhea.
Neuro: headache.
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), hiccups, infusion reactions (fosaprepitant IV only).
Drug-Drug:
(Generic available)
Prevention of Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy
12 yr): Capsules 125 mg given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 80 mg once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 3 days [Days 24]).
6 kg): Singleday chemotherapy regimen 150 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 115 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 80 mg PO once daily (capsules) for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
6 kg): Singleday chemotherapy regimen 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
6 kg): Singleday chemotherapy regimen 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].Prevention of Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy
12 yr): Capsules 125 mg given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist), then 80 mg once daily for 2 days (Days 2 and 3).
6 kg): Singleday chemotherapy regimen 150 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 115 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 80 mg PO once daily (capsules) for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
6 kg): Singleday chemotherapy regimen 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
6 kg): Singleday chemotherapy regimen 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multiday chemotherapy regimen 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT3 antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].Absorption: 6065% absorbed following oral administration. Following IV administration, fosaprepitant is rapidly converted to aprepitant, the active component. IV administration results in complete bioavailability.
Distribution: Crosses the blood brain barrier; remainder of distribution unknown.
Protein Binding: 9599%.
Metabolism/Excretion: Mostly metabolized by the liver (CYP3A4 enzyme system); not renally excreted.
Half-life: Aprepitant 913 hr.
NDC Code*