Aprepitant

Aprepitant prevents nausea and vomiting associated with cancer chemotherapy. Is taken as 3 doses over 3 days, starting on the day you have chemotherapy, and the two days after chemotherapy.

Aprepitant Overview

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Aprepitant is a prescription medication used to prevent nausea and vomiting that may occur within 24 hours after receiving chemotherapy treatment. It is also used with other medications to prevent delayed nausea and vomiting that may occur several days after receiving chemotherapy medications. Aprepitant is also used to prevent nausea and vomiting caused by surgery. Aprepitant belongs to a group of drugs called antiemetics. These work by blocking the action of neurokinin, a natural substance in the brain that causes nausea and vomiting.

This medication comes as a capsule and an injection.

The capsule is taken by mouth usually once daily, with or without food. To prevent nausea and vomiting due to chemotherapy, you will probably take aprepitant 1 hour before your first dose of chemotherapy, and then each morning for the next 2 days. To prevent nausea and vomiting caused by surgery, aprepitant is usually taken as one dose within 3 hours before the start of surgery.

The injection is given either on day 1 with the capsule taken on days 2 and 3 or the injection is given on day 1 and no capsules are taken on the following days. 

Common side effects of the capsule include constipation, itching, and tiredness. Common side effects of the injection include hiccups, tiredness, and changes in liver function blood tests. Do not drive or operate heavy machinery until you know how aprepitant affects you.

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Uses of Aprepitant

Aprepitant is a prescription medicine used in adults to prevent nausea and vomiting:

Capsule:

  • prevent nausea and vomiting that may occur within 24 hours after receiving chemotherapy treatment
  • prevent delayed nausea and vomiting that may occur several days after receiving chemotherapy medications
  • prevent nausea and vomiting caused by surgery

​Injection:

  • prevent nausea and vomiting that may occur within 24 hours after receiving chemotherapy treatment
  • prevent delayed nausea and vomiting that may occur several days after receiving chemotherapy medications

Aprepitant is not used to treat nausea and vomiting that you already have.

Aprepitant should not be used continuously for a long time (chronic use).

It is not known if aprepitant is safe and effective in children.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.
 

Aprepitant Brand Names

Aprepitant may be found in some form under the following brand names:

Aprepitant Drug Class

Aprepitant is part of the drug class:

Side Effects of Aprepitant

In people taking aprepitant to prevent nausea and vomiting caused by chemotherapy, the most common side effects include:

  • tiredness
  • nausea
  • hiccups
  • constipation
  • diarrhea
  • loss of appetite
  • headache
  • hair loss

In people taking aprepitant to prevent nausea and vomiting after surgery, the most common side effects are:

  • constipation
  • nausea
  • itching
  • fever
  • low blood pressure
  • headache

This is not a complete list of this medication’s side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Aprepitant Interactions

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

  • anticoagulants ('blood thinners') such as warfarin (Coumadin)
  • antifungals such as itraconazole (Sporanox), ketoconazole (Nizoral), and lansoprazole
  • benzodiazepines such as alprazolam (Xanax), diazepam (Valium), midazolam (Versed), and triazolam (Halcion)
  • diltiazem (Cardizem, Dilacor, Tiazac)
  • cancer chemotherapy medications such as docetaxel (Taxotere), etoposide (Toposar, VePesid), ifosfamide (Ifex), imatinib (Gleevec), irinotecan (Camptosar), paclitaxel (Taxol), tamoxifen (Nolvadex), vinblastine, vincristine (Vincasar), and vinorelbine (Navelbine)
  • carbamazepine (Tegretol)
  • clarithromycin (Biaxin)
  • diltiazem (Cardizem, Dilacor, Tiazac)
  • HIV protease inhibitors such as nelfinavir (Viracept) and ritonavir (Norvir)
  • hormonal contraceptives (birth control pills, patches, rings, and injections)
  • nefazodone (Serzone)
  • oral steroids such as dexamethasone (Decadron, Dexone)
  • methylprednisolone (Medrol)
  • paroxetine (Paxil, Pexeva)
  • phenytoin (Dilantin)
  • rifampin (Rifadin, Rimactane)
  • tolbutamide (Orinase)
  • troleandomycin (TAO)
  • pimozide (Orap)
  • terfenadine (Seldan)
  • astemizole (Hismanal)
  • cisapride (Propulsid)

This is not a complete list of all drug interactions. Ask your doctor or pharmacist for more information.

Aprepitant Precautions

Aprepitant may cause serious side effects, including:

  • Serious allergic reactions. Allergic reactions can happen with aprepitant and may be serious. Stop taking aprepitant and call your doctor right away if you have any of these signs or symptoms of an allergic reaction:
    • hives
    • rash
    • itching
    • trouble breathing or swallowing.
  • Severe skin reactions may occur rarely.

Do not take aprepitant if you:

  • are allergic to any of the ingredients in aprepitant
  • are taking any of the following medicines:
    • pimozide (Orap)
    • terfenadine (Seldan)
    • astemizole (Hismanal)
    • cisapride (Propulsid)

Taking aprepitant with any of these medicines could cause serious or life-threatening problems.

Aprepitant Food Interactions

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of this medication, there are no specific foods that you must exclude from your diet.

Inform MD

Before you take aprepitant, tell your doctor if you:

  • have liver problems
  • are pregnant or plan to become pregnant. It is not known if aprepitant can harm your unborn baby. Women who use birth control medicines containing hormones to prevent pregnancy (birth control pills, skin patches, implants, and certain IUDs) should also use a back-up method of birth control during treatment with EMEND and for up to 1 month after using EMEND to prevent pregnancy.
  • are breastfeeding

Tell your doctor about all the medicines you are taking or plan to take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Aprepitant and Pregnancy

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category B. There are no well-done studies that have been done in humans with aprepitant. In animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

Aprepitant and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if aprepitant crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using this medication.

Aprepitant Usage

Take aprepitant exactly as prescribed.

Aprepitant is given for 3 days as part of the chemotherapy induced nausea and vomiting (CINV) regimen that includes a corticosteroid and a 5-HT3 antagonist. 

  • The recommended dose of aprepitant is 125 mg orally 1 hour prior to chemotherapy treatment (Day 1) and 80 mg orally once daily in the morning on Days 2 and 3. 
  • The injection may be substituted for oral aprepitant (125 mg) on Day 1 only as part of the CINV regimen. 

High emetogenic cancer (Single Dose Regimen): The injection (150 mg) is administered on Day 1 only as an infusion over 20-30 minutes initiated approximately 30 minutes prior to chemotherapy. No capsules of aprepitant are administered on Days 2 and 3. The injection is part of a regimen to prevent nausea and vomiting induced by chemotherapy that includes a corticosteroid and a 5-HT3 antagonist. 

High and moderate emetogenic cancer (3-Day Dosing Regimen): The injection (115 mg) is administered on Day 1 as an infusion over 15 minutes initiated approximately 30 minutes prior to chemotherapy. Emend capsules (80 mg) are given orally on Days 2 and 3. The injection and capsules are part of a regimen to prevent nausea and vomiting induced by chemotherapy that includes a corticosteroid and a 5-HT3 antagonist. 

For prevention of Postoperative Nausea and Vomiting (PONV): Aprepitant capsules will be given 3 hours prior to administration of anesthesia.

If you take the blood thinner medicine warfarin (Coumadin, Jantoven), your doctor may do blood tests after you take aprepitant to check your blood clotting.

 

Aprepitant Dosage

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

  • the condition being treated
  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight
  • your height
  • your age
  • your gender

Aprepitant Capsules:

If you are receiving cancer chemotherapy, aprepitantis taken as 3 doses over 3 days - starting on the day you have chemotherapy, and the two days after chemotherapy. There are two ways that your doctor may prescribe aprepitant for you:

  1. Aprepitant capsules by mouth for all 3 doses:
    • You should get a package that has three aprepitant capsules.
    • Day 1 (Day of chemotherapy): Take one aprepitant 125-mg capsule (white and pink) by mouth 1 hour before you start your chemotherapy treatment.
    • Day 2 and Day 3 (the two days after chemotherapy): Take one aprepitant 80-mg capsule (white) by mouth, each morning for the 2 days after your chemotherapy treatment.
      Or 
  2. Intravenous (IV) injection into a vein the first day, then capsules by mouth on the two days after chemotherapy:
    • Day 1 (Day of chemotherapy): The injection will be given to you by intravenous (IV) injection in your vein 30 minutes before you start your chemotherapy treatment.
    • You should get a package that has two aprepitant capsules.
    • Day 2 and Day 3 (the two days after chemotherapy): Take one 80-mg capsule (white) by mouth, each morning for the 2 days after your chemotherapy treatment.

If you are receiving chemotherapy, aprepitant may be taken with or without food.

If you are having surgery:  Your doctor will prescribe a 40-mg aprepitant capsule for you before surgery. You take aprepitant within three hours before surgery. Follow your doctor’s instructions about restrictions on eating and drinking before surgery.

Injection:

You will receive the injection in one of two ways:

1. 150 mg injection given on Day 1 only.

  • Day 1 (Day of chemotherapy): Injection 150 mg will be given to you by infusion in your vein (intravenous) about 30 minutes before you start your chemotherapy treatment.

Or

2. 115 mg injection given along with aprepitant capsules.

  • Day 1 (Day of chemotherapy): The Injection (115 mg) will be given to you by infusion in your vein (intravenous) about 30 minutes before you start your chemotherapy treatment.
  • You will get a prescription for two aprepitant capsules.
  • Day 2 and Day 3 (the two days after chemotherapy): Take one aprepitant 80-mg capsule (white) by mouth, each morning for the 2 days after your chemotherapy treatment.

The recommended oral dosage of aprepitant for the postoperative nausea and vomiting (PONV) indication is 40 mg within 3 hours prior to induction of anesthesia.

Aprepitant Overdose

If you take too much this medication, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If this medication is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Other Requirements

  • Storage requirements:
    • Capsule: Store at room temperature, between 68°F and 77°F (20°C and 25°C).
    • Injection: Store at 36-46°F (2-8°C)
  • Keep aprepitant and all medicines out of the reach of children.