|
EMEND (aprepitant) capsules
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use EMEND CAPSULES safely and effectively. See full prescribing information for EMEND.
EMEND (aprepitant) capsules, for oral use
Initial U.S. Approval: 2003
RECENT MAJOR CHANGES
|
Indications and Usage (1.1) |
08/2015 |
|
Dosage and Administration |
|
|
Prevention of CINV (2.1) |
08/2015 |
INDICATIONS AND USAGE
EMEND® is a substance P/neurokinin 1 (NK1) receptor antagonist, indicated:
-
in combination with other antiemetic agents in patients 12 years of age and older and patients less than 12 years of age who weigh at least 30 kg for prevention of:
-
acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin (1.1)
-
nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC) (1.1)
-
for prevention of postoperative nausea and vomiting (PONV) in adults (1.2)
Limitations of Use: (1.3)
-
EMEND has not been studied for treatment of established nausea and vomiting.
-
Chronic continuous administration of EMEND is not recommended.
DOSAGE AND ADMINISTRATION
Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) (2.1)
-
Recommended dosage of EMEND in adults and pediatric patients 12 years of age and older and patients less than 12 years of age who weigh at least 30 kg, and who can swallow oral capsules, is 125 mg on Day 1 and 80 mg on Days 2 and 3.
-
Administer EMEND orally 1 hour prior to chemotherapy on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer EMEND in morning.
-
See Full Prescribing Information for recommended dosages of concomitant dexamethasone and 5-HT3 antagonist for HEC and MEC.
PONV (2.2)
-
Recommended oral EMEND dosage in adults is 40 mg within 3 hours prior to induction of anesthesia.
DOSAGE FORMS AND STRENGTHS
EMEND capsules: 40 mg; 80 mg; 125 mg (3)
CONTRAINDICATIONS
-
Known hypersensitivity to any component of this drug. (4)
-
Concurrent use with pimozide. (4)
WARNINGS AND PRECAUTIONS
-
CYP3A4 Interactions: Aprepitant is a substrate, weak-to-moderate inhibitor and inducer of CYP3A4; See Full Prescribing Information for recommendations regarding contraindications, risk of adverse reactions, and dosage adjustments of EMEND and concomitant drugs. (4, 5.1, 7.1, 7.2)
-
Warfarin (a CYP2C9 substrate): Risk of decreased INR of prothrombin time; monitor INR in 2-week period, particularly at 7 to 10 days, following initiation of EMEND. (5.2, 7.1)
-
Hormonal Contraceptives: Efficacy of contraceptives may be reduced during administration of and for 28 days following the last dose of EMEND. Use alternative or back-up methods of contraception. (5.3, 7.1)
ADVERSE REACTIONS
Most common adverse reactions are (6.1):
Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
-
Adults (≥3%): fatigue, diarrhea, asthenia, dyspepsia, abdominal pain, hiccups, white blood cell count decreased, dehydration, and alanine aminotransferase increased.
-
Pediatrics (≥3%): neutropenia, headache, diarrhea, decreased appetite, cough, fatigue, hemoglobin decreased, dizziness, and hiccups.
PONV
-
Adults (≥3%): constipation and hypotension.
To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
See Full Prescribing Information for a list of clinically significant drug interactions. (4, 5.1, 5.2, 5.3, 7.1, 7.2)
See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.
Revised: 8/2015
FULL PRESCRIBING INFORMATION: CONTENTS*
1 INDICATIONS AND USAGE
1.1 Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
EMEND®, in combination with other antiemetic agents, is indicated in patients 12 years of age and older and patients less than 12 years who weigh at least 30 kg for the prevention of:
-
acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin [see Dosage and Administration (2.1)].
-
nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC) [see Dosage and Administration (2.1)].
1.2 Prevention of Postoperative Nausea and Vomiting (PONV)
EMEND capsules are indicated in adults for the prevention of postoperative nausea and vomiting [see Dosage and Administration (2.2)].
1.3 Limitations of Use
-
EMEND has not been studied for the treatment of established nausea and vomiting.
-
Chronic continuous administration of EMEND is not recommended because it has not been studied, and because the drug interaction profile may change during chronic continuous use.
2 DOSAGE AND ADMINISTRATION
2.1 Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Adults and Pediatric Patients 12 Years of Age and Older and Patients Less Than 12 Years of Age who Weigh at least 30 kg
The recommended oral dosage of EMEND capsules, dexamethasone, and a 5-HT3 antagonist in adults and pediatric patients 12 years of age and older and patients less than 12 years of age who weigh at least 30 kg, who can swallow oral capsules, for the prevention of nausea and vomiting associated with administration of HEC or MEC is shown in Table 1 or Table 2, respectively.
In adults only, EMEND for injection (115 mg), a prodrug of aprepitant, may be substituted for EMEND capsules (125 mg), 30 minutes prior to chemotherapy, on Day 1 of the CINV regimen as an intravenous infusion administered over 15 minutes, followed by oral EMEND (80 mg) on Days 2 and 3. See the prescribing information for EMEND for injection.
2.2 Prevention of Postoperative Nausea and Vomiting (PONV)
The recommended oral dosage of EMEND capsules in adults is 40 mg within 3 hours prior to induction of anesthesia.
2.3 Administration Instructions
-
Take with or without food.
-
Swallow capsules whole.
3 DOSAGE FORMS AND STRENGTHS
EMEND capsules:
-
40 mg: white body and mustard yellow cap with "464" and "40 mg" printed radially in black ink on the body.
-
80 mg: white body and cap with "461" and "80 mg" printed radially in black ink on the body.
-
125 mg: white body and pink cap with "462" and "125 mg" printed radially in black ink on the body.
4 CONTRAINDICATIONS
EMEND is contraindicated in patients:
-
who are hypersensitive to any component of the product. Hypersensitivity reactions including anaphylactic reactions have been reported [see Adverse Reactions (6.2)].
-
taking pimozide. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of this drug which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide [see Warnings and Precautions (5.1)].
5 WARNINGS AND PRECAUTIONS
5.1 Clinically Significant CYP3A4 Drug Interactions
Aprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4.
-
Use of EMEND with other drugs that are CYP3A4 substrates, may result in increased plasma concentration of the concomitant drug.
-
Use of pimozide with EMEND is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide [see Contraindications (4)].
-
Use of EMEND with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to EMEND.
-
Use of EMEND with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of EMEND.
See Table 8 and Table 9 for a listing of potentially significant drug interactions [see Drug Interactions (7.1, 7.2)].
5.2 Decrease in INR with Concomitant Warfarin
Coadministration of EMEND with warfarin, a CYP2C9 substrate, may result in a clinically significant decrease in International Normalized Ratio (INR) of prothrombin time [see Clinical Pharmacology (12.3)]. Monitor the INR in patients on chronic warfarin therapy in the 2-week period, particularly at 7 to 10 days, following initiation of the 3-day regimen of EMEND with each chemotherapy cycle, or following administration of a single 40-mg dose of EMEND for the prevention of postoperative nausea and vomiting [see Drug Interactions (7.1)].
|
|
