Emend

Generic name: aprepitant (oral/injection)
Drug class: NK1 receptor antagonists

Medically reviewed by  A Ras MD.

What is Emend?

Emend for oral suspension is a prescription medicine used with other medicines that treat nausea and vomiting in patients 6 months of age and older to prevent nausea and vomiting caused by certain anti-cancer (chemotherapy) medicines

Emend capsules is a prescription medicine used with other medicines that treat nausea and vomiting in patients 12 years of age and older to prevent nausea and vomiting caused by certain anti-cancer (chemotherapy) medicines

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

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

Description

EMEND capsules contain the active ingredient, aprepitant. Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist, an antiemetic agent, chemically described as 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one.

Its empirical formula is C23H21F7N4O3, and its structural formula is:

Aprepitant is a white to off-white crystalline solid, with a molecular weight of 534.43. It is practically insoluble in water. Aprepitant is sparingly soluble in ethanol and isopropyl acetate and slightly soluble in acetonitrile.

Each capsule of EMEND for oral administration contains either 80 mg or 125 mg of aprepitant and the following inactive ingredients: sucrose, microcrystalline cellulose, hydroxypropyl cellulose and sodium lauryl sulfate. The capsule shell excipients are gelatin, titanium dioxide, and may contain sodium lauryl sulfate and silicon dioxide. The 125-mg capsule also contains red ferric oxide and yellow ferric oxide.

Each pouch of EMEND for oral suspension 125 mg contains 125 mg of aprepitant and the following inactive ingredients: sucrose, lactose, hydroxypropyl cellulose, sodium lauryl sulfate, red iron oxide, and sodium stearyl fumarate.

Mechanism of Action

Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV).

Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.

Who should not take Emend?

Do not take Emend if you:

• are allergic to aprepitant or any of the ingredients in Emend See the end of this leaflet for a complete list of ingredients in Emend.
• are taking pimozide (Orap)

What should I tell my healthcare provider before taking Emend?

Before you take Emend, tell your healthcare provider if you:

• have liver problems
• are pregnant or plan to become pregnant. It is not known if Emend 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 that does not contain hormones, such as condoms and spermicides, during treatment with Emend and for 1 month after your last dose of Emend.
• are breastfeeding or plan to breastfeed. It is not known if Emend passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby if you take Emend.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Emend may affect the way other medicines work, and other medicines may affect how Emend works causing serious side effects.

Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine.

How should I take Emend?

• Take Emend exactly as prescribed.
• Swallow Emend capsules whole.
• Emend may be taken with or without food.
• If you take too much Emend, call your healthcare provider, or go to the nearest hospital emergency room.
• Emend is taken as 3 doses over 3 days – starting on the day you have chemotherapy, and for the following 2 days.
• In adults, there are 2 ways your healthcare provider may prescribe Emend for you:

1. Capsules of Emend by mouth for all 3 doses:

• You should get a package that has 3 capsules of Emend.
• Day 1 (Day of chemotherapy): Take one 125 mg capsule of Emend (white and pink) by mouth 1 hour before you start your chemotherapy treatment.
• Day 2 and Day 3: Take one 80 mg capsule of Emend (white) by mouth 1 hour before you start your chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, Emend should be taken in the morning.

2. Oral suspension of Emend by mouth for all 3 doses, for adults who are not able to swallow capsules:

• For each dose of Emend for oral suspension, you will get a pre-filled oral dosing dispenser that contains your prescribed dose.
• See the detailed Instructions for Use that comes with Emend for oral suspension for information about the correct way to take a dose of Emend for oral suspension. If you have questions about how to take Emend for oral suspension, talk to your healthcare provider.
• Day 1 (Day of chemotherapy): Take 1 dose of Emend for oral suspension by mouth 1 hour before you start your chemotherapy treatment.
• Day 2 and Day 3: Take 1 dose of Emend for oral suspension by mouth 1 hour before you start your chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, Emend for oral suspension should be taken in the morning.

• In children 12 years of age and older who can swallow capsules by mouth, Emend is prescribed as capsules of Emend by mouth for all 3 doses:
  • You should get a package that has 3 capsules of Emend.
  • Day 1 (Day of chemotherapy): Take one 125 mg capsule of Emend (white and pink) by mouth 1 hour before you start your chemotherapy treatment.
  • Day 2 and Day 3: Take one 80 mg capsule of Emend (white) by mouth 1 hour before you start your chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, Emend should be taken in the morning.
• In children 6 months to less than 12 years of age or in children 12 years of age and older who are not able to swallow capsules, Emend is prescribed as oral suspension of Emend by mouth for all 3 doses:
  • For each dose of Emend, you will get a pre-filled oral dosing dispenser that contains your child’s prescribed dose.
  • See the detailed Instructions for Use that comes with Emend for oral suspension, for information about the correct way to give a dose of Emend for oral suspension. If you have questions about how to give Emend for oral suspension, talk to your child’s healthcare provider.
  • Day 1 (Day of chemotherapy): Give 1 dose of Emend for oral suspension to your child by mouth 1 hour before they start their chemotherapy treatment.
  • Day 2 and Day 3: Give 1 dose of Emend for oral suspension to your child by mouth 1 hour before they start their chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, Emend should be given in the morning.
• If you take the blood thinner medicine warfarin sodium (Coumadin, Jantoven), your healthcare provider may do blood tests after you take Emend to check your blood clotting.

What are the possible side effects of Emend?

• In adults taking Emend, the most common side effects include tiredness, diarrhea, weakness, indigestion, stomach (abdominal) pain, hiccups, decrease in white blood cell count, dehydration, and changes in liver function tests.
• In children 6 months to 17 years of age, the most common side effects include decrease in white blood cell count, headache, diarrhea, decreased appetite, cough, tiredness, decrease in red blood cell count, dizziness, and hiccups.

Tell your healthcare provider if you have any side effect that bothers you or that does not go away. These are not all of the possible side effects of EMEND. For more information ask your healthcare provider or pharmacist.

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

General information about the safe and effective use of Emend

Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet. Do not use Emend for a condition for which it was not prescribed. Do not give Emend to other people, even if they have the same symptoms you have. It may harm them. You can ask your healthcare provider or pharmacist for information about Emend that is written for health professionals. For more information about Emend call 1-800-622-4477 or go to www.emend.com.

How should I store Emend?

Emend capsules

• Store Emend capsules at room temperature, between 68°F to 77°F (20°C to 25°C).

Emend for oral suspension

• Store Emend for oral suspension in the refrigerator, between 36°F to 46°F (2°C to 8°C).
• Use Emend for oral suspension within 2 days of getting the medicine from your healthcare provider.
• When ready to use, Emend for oral suspension can be kept at room temperature, between 68°F to 77°F (20°C to 25°C) for up to 3 hours.

Keep Emend and all medicines out of the reach of children.

What are the ingredients in Emend?

Active ingredient: aprepitant

Inactive ingredients:

Capsules: sucrose, microcrystalline cellulose, hydroxypropyl cellulose and sodium lauryl sulfate. The capsule shell excipients are gelatin, titanium dioxide, and may contain sodium lauryl sulfate and silicon dioxide. The 125 mg capsule shell also contains red ferric oxide and yellow ferric oxide.

Oral suspension: sucrose, lactose, hydroxypropyl cellulose, sodium lauryl sulfate, red iron oxide, and sodium stearyl fumarate.

Label

PRINCIPAL DISPLAY PANEL – 80 MG CAPSULE DOSE PACK

• NDC 0006-0461-02
• BiPack
  2 capsules
• EMEND®
  (aprepitant) capsules
• 80mg
• For Adults and
  Pediatric Patients
  12 years of Age and Older
• You have already been given
  a capsule of EMEND (aprepitant) to
  prevent nausea and vomiting before
  your chemotherapy on Day 1.
• The two capsules in this package
  are to be taken on Days 2 and 3.
• Each capsule contains 80 mg
  of aprepitant.

SRC: NLM .