Classes
DEA Class; Rx
Common Brand Names; Cinvanti, Aponvie, Emend PO
- Antiemetic Agents;
- NK1 Receptor Antagonists
Description
Selective substance P (NK1) antagonist, fosaprepitant is prodrug of aprepitant
Used for prevention of chemotherapy-induced nausea/vomiting (CINV) due to highly and moderately emetogenic regimens; IV aprepitant (Aponvie) used for prevention of post-operative nausea/voming (PONV)
For CINV use with in combination with a 5HT3 antagonist and a corticosteroid: oral aprepitant is a 3-day regimen; IV aprepitant or IV fosaprepitant are given as a single dose
Indications
Indicated for chemotherapy-induced nausea/vomiting prophylaxis (CINV prophylaxis).
Contraindications
Hypersensitivity
Concomitant pimozide or cisapride
Adverse Effects
- Headache
- Asthenia/fatigue
- Anorexia
- Constipation
- Diarrhea
- Nausea
- Alopecia
- Hiccups
- Dizziness
- Insomnia
- Bradycardia
- Hypotension
- Pharyngolargeal pain
- Mucosal inflammation
- Stomatitis
- Dyspepsia
- Anemia
- Neutropenia
- Hot flash
- Pruritus
- Dehydration
- Fever
Warnings
Infusion site reactions (ISRs) reported with injection; majority of severe ISRs, including thrombophlebitis and vasculitis, were reported with concomitant vesicant (anthracycline-based) chemotherapy administration, particularly when associated with extravasation; necrosis was also reported in some patients with concomitant vesicant chemotherapy; if a severe ISR develops during infusion, discontinue infusion and administer appropriate medical treatment
Serious hypersensitivity reactions, including anaphylaxis, during or soon after administration of therapy reported; symptoms including dyspnea, eye swelling, flushing, pruritus and wheezing reported with IV infusion; monitor patients during and after administration; if hypersensitivity reactions occur, discontinue drug and administer appropriate medical therapy; do not reinitiate treatment in patients who experience these symptoms with previous use
Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate
Pregnancy and Lactation
Insufficient data on use in pregnant women to inform a drug associated risk
It is not known whether this drug is excreted in milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother
Maximum Dosage
125 mg/day PO (Day 1) and 80 mg/day PO (Days 2 and 3); 150 mg/day fosaprepitant IV (Day 1) (Emend products).
130 mg/day aprepitant IV emulsion (Cinvanti) (Day 1) for CINV prophylaxis.
32 mg/day aprepitant IV emulsion (Aponvie) for PONV prophylaxis.
125 mg/day PO (Day 1) and 80 mg/day PO (Days 2 and 3); 150 mg/day fosaprepitant IV (Day 1) (Emend products).
130 mg/day aprepitant IV emulsion (Cinvanti) (Day 1) for CINV prophylaxis.
32 mg/day aprepitant IV emulsion (Aponvie) for PONV prophylaxis.
125 mg/day PO (Day 1) and 80 mg/day PO (Days 2 and 3); 150 mg/day fosaprepitant IV (Day 1) for a single-dose CINV regimen; 115 mg/day fosaprepitant IV (Day 1) for a multiple-dose CINV regimen; safety and efficacy of the IV aprepitant emulsion have not been established.
12 years: 125 mg/day PO (Day 1) and 80 mg/day PO (Days 2 and 3); 150 mg/day fosaprepitant IV (Day 1) for a single-dose CINV regimen; 115 mg/day fosaprepitant IV (Day 1) for a multiple-dose CINV regimen; safety and efficacy of the IV aprepitant emulsion have not been established.
2 to 11 years: 3 mg/kg/day PO (Max: 125 mg/day – Day 1) and 2 mg/kg/day PO (Max: 80 mg/day – Days 2 and 3); 4 mg/kg/day fosaprepitant IV (Max: 150 mg/day – Day 1) for a single-dose CINV regimen; 3 mg/kg/day fosaprepitant IV (Max: 115 mg/day – Day 1) for a multiple-dose CINV regimen; safety and efficacy of the IV aprepitant emulsion have not been established.
1 year: 3 mg/kg/day PO (Max: 125 mg/day – Day 1) and 2 mg/kg/day PO (Max: 80 mg/day – Days 2 and 3); 5 mg/kg/day fosaprepitant IV (Max: 150 mg/day – Day 1) for a single-dose CINV regimen; 3 mg/kg/day fosaprepitant IV (Max: 115 mg/day – Day 1) for a multiple-dose CINV regimen; safety and efficacy of the IV aprepitant emulsion have not been established.
6 to 11 months: 3 mg/kg/day PO (Day 1) and 2 mg/kg/day PO (Days 2 and 3); 5 mg/kg/day fosaprepitant IV (Day 1) for a single-dose CINV regimen; 3 mg/kg/day fosaprepitant IV (Day 1) for a multiple-dose CINV regimen; safety and efficacy of the IV aprepitant emulsion have not been established.
1 to 5 months: Safety and efficacy have not been established for any dosage form.
How supplied
Aprepitant
capsule
- Emend PO, generic
- 40mg
- 80mg
- 125mg
oral suspension
- Emend PO
- 125mg/pouch (once pouch is mixed with 4.6 mL drinking water, resulting suspension yields 25mg/mL)
injection, emulsion
- 7.2mg/mL (130mg/18mL) (Cinvanti)
- 7.2mg/mL (32mg/4.4mL single-dose vial) (Aponvie)