tified during post-marketing use of aprepitant. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to the drug.
Skin and subcutaneous tissue disorders: pruritus, rash, urticaria
Immune system disorders: hypersensitivity reactions including anaphylactic reactions
OVERDOSAGE
No specific information is available on the treatment of overdosage. Single doses up to 200 mg of fosaprepitant I.V. and 600 mg of oral aprepitant were generally well tolerated in healthy subjects.
Three out of 33 subjects receiving 200 mg of fosaprepitant experienced mild injection site thrombosis. Aprepitant was generally well tolerated when administered as 375 mg once daily for up to 42 days to patients in non-CINV studies. In 33 cancer patients, administration of a single 375-mg dose of aprepitant on Day 1 and 250 mg once daily on Days 2 to 5 was generally well tolerated.
Drowsiness and headache were reported in one patient who ingested 1440 mg of aprepitant.
In the event of overdose, oral aprepitant should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of aprepitant, drug-induced emesis may not be effective.
Aprepitant cannot be removed by hemodialysis.
DOSAGE AND ADMINISTRATION
EMEND for Injection is a sterile, lyophilized prodrug of aprepitant containing polysorbate 80 (PS80), to be administered intravenously as an infusion. Aprepitant is available as capsules (EMEND2) for oral administration.
EMEND for Injection (115 mg) may be substituted for EMEND (125 mg) 30 minutes prior to chemotherapy, on Day 1 only of the CINV regimen as an infusion administered over 15 minutes.
EMEND for Injection should not be mixed or reconstituted with solutions for which physical and chemical compatibility have not been established. EMEND for Injection is incompatible with any solutions containing divalent cations (e.g., Ca2+, Mg2+), including Lactated Ringer’s Solution and Hartmann's Solution.
The 3-day CINV regimen includes EMEND for Injection (115 mg) or EMEND (125 mg orally) on Day 1; EMEND (80 mg orally) on Days 2 and 3; in addition to a corticosteroid and a 5-HT3 antagonist as specified in the tables below.
In clinical studies with EMEND, the following regimen was used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy
Day 1 Day 2 Day 3 Day 4
EMEND was administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3.
Dexamethasone was administered 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4. The dose of dexamethasone was chosen to account for drug interactions.
Ondansetron was administered 30 minutes prior to chemotherapy treatment on Day 1.
EMEND* 125 mg orally 80 mg orally 80 mg orally none
Dexamethasone† 12 mg orally 8 mg orally 8 mg orally 8 mg orally
Ondansetron‡ 32 mg I.V. none none none
In a clinical study with EMEND, the following regimen was used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Day 1 Day 2 Day 3
EMEND was administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3.
Dexamethasone was administered 30 minutes prior to chemotherapy treatment on Day 1. The dose of dex |
