Aprepitant

Aprepitant is a prescription medication used to treat nausea and vomiting associated with chemotherapy.

• Aprepitant is available under the following different brand names: Aponvie, Cinvanti, Emend, fosaprepitant

Adult and pediatric dosage

Capsule (aprepitant)

Emend, generic

• 40mg
• 80mg
• 125mg

Injection, powder for reconstitution (fosaprepitant)

Emend, generic

• 150mg/vial

Oral suspension (aprepitant)

Emend

• 125mg/pouch (once the pouch is mixed with 4.6 mL drinking water, resulting in suspension yields 25mg/mL)

Injection, emulsion (aprepitant)

Cinvanti

• 7.2mg/mL (130mg/18mL)

Chemotherapy-Induced Nausea & Vomiting

Adult dosage

IV (fosaprepitant)

HEC

• Day 1: 150 mg IV infused over 20-30 minutes ~30 minutes before chemotherapy plus dexamethasone 12 mg orally and a 5-HT3 antagonist
• Day 2: Dexamethasone 8 mg orally in the morning
• Days 3 and 4: Dexamethasone 8 mg orally twice daily (morning and evening)
• Note: A 50% dosage reduction of dexamethasone on Days 1 and 2 is recommended to account for drug interaction with aprepitant

MEC

• Day 1: 150 mg IV infused over 20-30 minutes ~30 minutes before chemotherapy plus dexamethasone 12 mg orally and a 5-HT3 antagonist
• IV emulsion (aprepitant - Cinvanti)

HEC

• Day 1: 130 mg IV infused over 30 minutes or as IV push over 2 min; complete infusion or injection ~30 minutes before chemotherapy plus dexamethasone 12 mg orally and a 5-HT3 antagonist
• Day 2: Dexamethasone 8 mg orally in the morning
• Days 3 and 4: Dexamethasone 8 mg orally twice daily (morning and evening)
• Note: A 50% dosage reduction of dexamethasone on Days 3 and 4 is recommended to account for drug interaction with aprepitant

MEC (single-dose regimen)

• Day 1: 130 mg IV infused over 30 minutes or as IV push over 2 min; complete infusion or injection ~30 minutes before chemotherapy plus dexamethasone 12 mg orally and a 5-HT3 antagonist
• Note: A 50% dosage reduction of dexamethasone is recommended to account for drug interaction with aprepitant

MEC (3-day regimen plus aprepitant orally)

• Day 1: 100 mg IV infused over 30 minutes or as IV push over 2 min; complete infusion or injection ~30 minutes before chemotherapy plus dexamethasone 12 mg orally and a 5-HT3 antagonist
• Days 2-3: 80 mg orally 1 hr before chemotherapy
• Note: A 50% dosage reduction of dexamethasone is recommended to account for drug interaction with aprepitant

Oral

HEC

• Day 1: 125 mg orally 1 hr before chemotherapy plus dexamethasone 12 mg orally (30 minutes before chemotherapy) and a 5-HT3 antagonist
• Days 2-3: 80 mg orally 1 hr before chemotherapy plus dexamethasone 8 mg orally every morning
• Day 4: Dexamethasone 8 mg orally in the morning

MEC

• Day 1: 125 mg orally 1 hr before chemotherapy plus dexamethasone 12 mg orally (30 minutes before chemotherapy) and a 5-HT3 antagonist
• Days 2-3: 80 mg orally 1 hr before chemotherapy

Pediatric dosage

• Oral suspension: Aged below 6 months: Safety and efficacy not established
• Capsule
• Aged below 12 years or weight below 30 kg: Safety and efficacy not established
• Aged above 12 years or below 12 years and weight above 30 kg
  • Day 1: 125 mg orally 1 hr before chemotherapy plus dexamethasone 12 mg orally (30 minutes before chemotherapy) and a 5-HT3 antagonist
  • Days 2 and 3: 80 mg orally 1 hr before chemotherapy plus dexamethasone 8 mg orally every morning
  • Day 4: Dexamethasone 8 mg orally in the morning
• Oral suspension
• Aged below 6 months: Safety and efficacy not established
• Aged above 6 months to 11  years
  • Day 1: 3 mg/kg orally 1 hr before chemotherapy
  • Days 2 and 3: 2 mg/kg orally 1 hr before chemotherapy
  • Administer with concomitant dexamethasone and 5-HT3 antagonist (e.g., ondansetron) IV emulsion (single-day chemotherapy regimens)
• Aged below 6 months or weight below 6 kg: Safety and efficacy not established
• 6 months to below 2 years: 5 mg/kg IV over 60 minutes ~30 minutes before chemotherapy; not to exceed 150 mg/dose

IV (single-day chemotherapy regimens)

Fosaprepitant only

• Aged below 6 months or weight below 6 kg: Safety and efficacy not established
• 6 months to below 2 years: 5 mg/kg IV over 60 minutes ~30 minutes before chemotherapy; not to exceed 150 mg/dose
• 2 to below 12 years: 4 mg/kg IV over 60 minutes ~30 minutes before chemotherapy; not to exceed 150 mg/dose
• 12-17 years: 150 mg IV over 30 minutes ~30 minutes before chemotherapy

In combination with dexamethasone and 5-HT3 antagonist (eg, ondansetron)

• Recommended dosing for 6 months to 17 years for the prevention of nausea and vomiting associated with single-day regimens of HEC or MEC
• Dexamethasone: If a corticosteroid (eg, dexamethasone) is coadministered, administer 50% of recommended corticosteroid dose on Days 1 and 2; administer 30 minutes before chemotherapy treatment on Day 1
• 5-HT3 antagonist: See selected 5-HT3 antagonist prescribing information for recommended dosage

IV (multiday chemotherapy regimens)

Fosaprepitant only

• Aged below 6 months or weight below 6 kg: Safety and efficacy not established
• 6 months to below 12 years
  • Day 1: 3 mg/kg IV over 60 minutes ~30 minutes before chemotherapy; not to exceed 115 mg/dose
  • Days 2 and 3 (oral suspension): 2 mg/kg orally ~30 minutes before chemotherapy; not to exceed 80 mg/dose
• 12-17 years
  • Day 1: 115 mg IV over 30 minutes ~30 minutes before chemotherapy
  • Days 2 and 3 (capsules): 80 mg orally ~30 minutes before chemotherapy

In combination with dexamethasone and 5-HT3 antagonist (eg, ondansetron)

• Recommended dosing for 6 months to 17 years for the prevention of nausea and vomiting associated with multiday regimens of HEC or MEC
• Dexamethasone: If a corticosteroid (e.g., dexamethasone) is coadministered, administer 50% of recommended corticosteroid dose on Days 1 and 2; administer 30 minutes before chemotherapy treatment on Day 1
• 5-HT3 antagonist: See selected 5-HT3 antagonist prescribing information for recommended dosage

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of the Aprepitant include:

• stomach pain,
• indigestion,
• burping,
• loss of appetite,
• low blood cell counts,
• diarrhea,
• constipation,
• hiccups,
• abnormal liver function tests,
• headache,
• dizziness,
• dehydration,
• pain in the arms or legs,
• pain, hardening, redness, swelling, or itching at the injection site,
• cough,
• weakness, and
• tiredness.

Serious side effects of the Aprepitant include:

• hives,
• difficulty breathing,
• swelling of the face, lips, tongue, or throat,
• fast heartbeat,
• wheezing,
• fever,
• sore throat,
• burning eyes,
• skin pain,
• red or purple skin rash with blistering and peeling,
• lightheadedness,
• pain or burning while urinating,
• sores or white patches in the mouth or throat,
• chills,
• tiredness,
• mouth sores,
• easy bruising,
• unusual bleeding,
• pale skin,
• cold hands and feet,
• shortness of breath,
• increased thirst,
• feeling hot,
• heavy sweating, and
• hot and dry skin

Rare side effects of the Aprepitant include:

• none

This is not a complete list of side effects and other serious side effects or health problems that may occur due to the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Aprepitant has severe interactions with the following drugs:
  • chloramphenicol
  • darunavir
  • flibanserin
  • lomitapide
  • lonafarnib
  • pimozide
  • ribociclib
  • tipranavir
• Aprepitant has serious interactions with at least 69 other drugs.
• Aprepitant has moderate interactions with at least 183 other drugs.
• Aprepitant has minor interactions with at least 51 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity
• Concomitant pimozide or cisapride (see Cautions)

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Aprepitant?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Aprepitant?”

Cautions

• Infusion site reactions (ISRs) were reported with injection; the 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 the 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 the drug and administer appropriate medical therapy; do not reinitiate treatment in patients who experience these symptoms with previous use
• Severe and disabling arthralgia was reported in patients taking DPP-4 inhibitors; considered a possible cause of severe joint pain and discontinue the drug if appropriate
• Drug interactions overview
  • Aprepitant is a substrate, weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4
  • Concomitant use of aprepitant and CYP3A4 substrates may result in increased plasma concentration of the CYP3A4 drugs
  • Concomitant use of pimozide with aprepitant is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, which may prolong QT interval (see Contraindications)
  • Avoid concomitant use of aprepitant with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations and the effects of aprepitant
  • Avoid concomitant use of aprepitant with strong CYP3A4 inducers (e.g., rifampin) may result in a substantial reduction in aprepitant plasma concentrations and decreased efficacy
  • Decreased corticosteroid dose by 25% (IV) or 50% (PO) on days aprepitant is administered
  • Coadministration with benzodiazepines metabolized by CYP3A4 may increase levels and/or effects of midazolam or other benzodiazepines (alprazolam, triazolam)
  • Coadministration with warfarin may decrease warfarin exposure and prolong prothrombin time (INR); patients on chronic warfarin therapy, monitor INR for 7-10 days following administration of aprepitant IV emulsion with each chemotherapy cycle
  • Coadministration with oral contraceptives may decrease estrogen and progestin exposure during the administration of and for 28 days after administration of the last dose of aprepitant (see Pregnancy)

Pregnancy and Lactation

• Insufficient data on use in pregnant women to inform a drug-associated risk; in animal reproduction studies, no adverse developmental effects were observed in rats or rabbits exposed during the period of organogenesis to systemic drug levels (AUC) ~1.5 times adult human exposure at 125-mg/80-mg/80-mg regimen
• Avoid the use of aprepitant IV emulsion in pregnant women due to the alcohol content
• Coadministration with aprepitant may reduce the efficacy of hormonal contraceptives; advise females of reproductive potential using hormonal contraceptives to use an effective alternative or back-up non-hormonal contraceptive (such as condoms or spermicides) during treatment and for 1 month following the last dose of aprepitant IV emulsion or oral aprepitant, whichever is administered last
• Lactation
  • 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