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Aprepitant

    Brands

    DEA Class; Rx

    Common Brand Names; Cinvanti, Aponvie, Emend PO

    • Antiemetic Agents; 
    • NK1 Receptor Antagonists

    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

    Indicated for chemotherapy-induced nausea/vomiting prophylaxis (CINV prophylaxis).

    Hypersensitivity

    Concomitant pimozide or cisapride

    • 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

    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

    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

    Adults

    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.

    Geriatric

    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.

    Adolescents

    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.

    Children

    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.

    Infants

    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.

    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)