CV: dizziness, fatigue, weakness.
Derm: STEVENS-JOHNSON SYNDROME.
GI: diarrhea.
Neuro: headache.
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), hiccups, infusion reactions (fosaprepitant IV only).
Prevention of Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy
- PO (Adults): Capsules or suspension 125 mg given 1 hr prior to chemotherapy (Day 1) (with dexamethasone 12 mg PO 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 dexamethasone 8 mg once daily for 3 days [Days 24]).
- IV (Adults): Fosaprepitant 150 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist prior to chemotherapy). Continue dexamethasone on Days 24 (8 mg PO on Day 2, 8 mg twice daily on Days 3 and 4); Aprepitant 130 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist prior to chemotherapy). Continue dexamethasone on Days 24 (8 mg PO on Day 2, 8 mg twice daily on Days 3 and 4).
- PO (Children 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]).
- PO (Children 6 mo<12 yr and >6 kg): Suspension 3 mg/kg (max dose = 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 2 mg/kg (max dose = 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]).
- IV (Children 1217 yr and 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].
- IV (Children 2<12 yr and 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].
- IV (Children 6 mo-<2 yr and 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
- PO (Adults): Capsules or suspension 125 mg given 1 hr prior to chemotherapy (Day 1) (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist), then 80 mg once daily for 2 days (Days 2 and 3).
- IV (Adults): Fosaprepitant (for delayed nausea/vomiting) 150 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist prior to chemotherapy); Aprepitant (singledose regimen for delayed nausea/vomiting) 130 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist prior to chemotherapy). Aprepitant (3day regimen) 100 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT3 antagonist prior to chemotherapy). Continue aprepitant 80 mg PO on Days 2 and 3.
- PO (Children 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).
- PO (Children 6 mo<12 yr and >6 kg): Suspension 3 mg/kg (max dose = 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 2 mg/kg (max dose = 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]).
- IV (Children 1217 yr and 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].
- IV (Children 2<12 yr and 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].
- IV (Children 6 mo-<2 yr and 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].
Emend
Aprepitant (Injection): Cinvanti
fosaprepitant (Injection): Emend
Therapeutic Classification: antiemetics
Pharmacologic Classification: neurokinin antagonists
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.
a-PREP-i-tant
Aprepitant (Injection): a-PREP-i-tant
fosaprepitant (Injection): fos-a-PREP-i-tant