Aprepitant

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)

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