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Aprepitant

APREPITANT

Standard Dose

2 DOSAGE AND ADMINISTRATION Recommended Dosage for Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) ( 2.1 ) Aprepitant capsules in adults and pediatric patients 12 years of age and older: is 125 mg on Day 1 and 80 mg on Days 2 and 3. Administer aprepitant 1 hour prior to chemotherapy on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant in morning. See Full Prescribing Information for recommended dosages of concomitant dexamethasone and 5-HT 3 antagonist for HEC and MEC. Recommended Dosage for PONV ( 2.2 ) Adults: 40 mg aprepitant capsules within 3 hours prior to induction of anesthesia. Administration ( 2.4 ) Aprepitant capsules can be administered with or without food. Swallow aprepitant capsules whole. 2.1 Recommended Dosage For Chemotherapy Induced Nausea and Vomiting (CINV) Adults and Pediatric Patients 12 Years of Age and Older The recommended oral dosage of aprepitant capsules, dexamethasone, and a 5-HT 3 antagonist in adults and pediatric patients 12 years of age and older 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. Table 1: Recommended Dosing for the Prevention of Nausea and Vomiting Associated with HEC Population Day 1 Day 2 Day 3 Day 4 Aprepitant capsules * Adults and Pediatric Patients 12 Years and Older 125 mg orally 80 mg orally 80 mg orally none Dexamethasone Adults 12 mg orally 8 mg orally 8 mg orally 8 mg orally Pediatric Patients 12 Years and Older If a corticosteroid, such as dexamethasone, is co-administered, administer 50% of the recommended corticosteroid dose on Days 1 through 4 [see Clinical Studies (14.3) ] . 5-HT 3 antagonist Adults and Pediatric Patients 12 Years and Older See selected 5-HT 3 antagonist prescribing information for the recommended dosage none none none * Administer aprepitant capsules 1 hour prior to chemotherapy treatment on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant capsules in the morning. † Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4. A 50% dosage reduction of dexamethasone is recommended to account for a drug interaction with aprepitant [see Clinical Pharmacology ( 12.3 )] . Table 2: Recommended Dosing for the Prevention of Nausea and Vomiting Associated with MEC Population Day 1 Day 2 Day 3 Aprepitant capsules * Adults and Pediatric Patients 12 Years and Older 125 mg orally 80 mg orally 80 mg orally Dexamethasone Adults 12 mg orally none none Pediatric Patients 12 Years and Older If a corticosteroid, such as dexamethasone, is co-administered, administer 50% of the recommended corticosteroid dose on Days 1 through 4 [see Clinical Studies (14.3)].† 5-HT 3 antagonist Adults and Pediatric Patients 12 Years and Older See the selected 5-HT 3 antagonist prescribing information for recommended dosage none none * Administer aprepitant capsules 1 hour prior to chemotherapy treatment on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant capsules in the morning. † Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1. A 50% dosage reduction of dexamethasone is recommended to account for a drug interaction with aprepitant [see Clinical Pharmacology ( 12.3 )]. 2.2 Recommended Dosage For Postoperative Nausea and Vomiting (PONV) The recommended oral dosage of aprepitant capsules in adults is 40 mg within 3 hours prior to induction of anesthesia. 2.4 Administration Instructions Aprepitant capsules can be administered with or without food. Aprepitant capsules Swallow capsules whole.

Max Dose

See official label

Primary Use

1 INDICATIONS AND USAGE Aprepitant is a substance P/neurokinin 1 (NK 1 ) receptor antagonist.

Summary

Indications and usage 1 INDICATIONS AND USAGE Aprepitant is a substance P/neurokinin 1 (NK 1 ) receptor antagonist.

Aprepitant capsules are indicated in combination with other antiemetic agents, in patients 12 years of age and older 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 ) Aprepitant has not been studied for treatment of established nausea and vomiting.

Structured Monograph

Clinical summary

Indications and usage 1 INDICATIONS AND USAGE Aprepitant is a substance P/neurokinin 1 (NK 1 ) receptor antagonist. Aprepitant capsules are indicated in combination with other antiemetic agents, in patients 12 years of age and older 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 ) Aprepitant has not been studied for treatment of established nausea and vomiting. Chronic continuous administration of aprepitant is not recommended. 1.1 Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) Aprepitant capsules, in combination with other antiemetic agents, are indicated in patients 12 years of age and older 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. nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). 1.2 Prevention of Postoperative Nausea and Vomiting (PONV) Aprepitant capsules are indicated in adults for the prevention of postoperative nausea and vomiting. 1.3 Limitations of Use Aprepitant has not been studied for the treatment of established nausea and vomiting. Chronic continuous administration of aprepitant is not recommended because it has not been studied, and because the drug interaction profile may change during chronic continuous use. Dosage and administration 2 DOSAGE AND ADMINISTRATION Recommended Dosage for Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) ( 2.1 ) Aprepitant capsules in adults and pediatric patients 12 years of age and older: is 125 mg on Day 1 and 80 mg on Days 2 and 3. Administer aprepitant 1 hour prior to chemotherapy on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant in morning. See Full Prescribing Information for recommended dosages of concomitant dexamethasone and 5-HT 3 antagonist for HEC and MEC. Recommended Dosage for PONV ( 2.2 ) Adults: 40 mg aprepitant capsules within 3 hours prior to induction of anesthesia. Administration ( 2.4 ) Aprepitant capsules can be administered with or without food. Swallow aprepitant capsules whole. 2.1 Recommended Dosage For Chemotherapy Induced Nausea and Vomiting (CINV) Adults and Pediatric Patients 12 Years of Age and Older The recommended oral dosage of aprepitant capsules, dexamethasone, and a 5-HT 3 antagonist in adults and pediatric patients 12 years of age and older 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. Table 1: Recommended Dosing for the Prevention of Nausea and Vomiting Associated with HEC Population Day 1 Day 2 Day 3 Day 4 Aprepitant capsules * Adults and Pediatric Patients 12 Years and Older 125 mg orally 80 mg orally 80 mg orally none Dexamethasone Adults 12 mg orally 8 mg orally 8 mg orally 8 mg orally Pediatric Patients 12 Years and Older If a corticosteroid, such as dexamethasone, is co-administered, administer 50% of the recommended corticosteroid dose on Days 1 through 4 [see Clinical Studies (14.3) ] . 5-HT 3 antagonist Adults and Pediatric Patients 12 Years and Older See selected 5-HT 3 antagonist prescribing information for the recommended dosage none none none * Administer aprepitant capsules 1 hour prior to chemotherapy treatment on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant capsules in the morning. † Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4. A 50% dosage reduction of dexamethasone is recommended to account for a drug interaction with aprepitant [see Clinical Pharmacology ( 12.3 )] . Table 2: Recommended Dosing for the Prevention of Nausea and Vomiting Associated with MEC Population Day 1 Day 2 Day 3 Aprepitant capsules * Adults and Pediatric Patients 12 Years and Older 125 mg orally 80 mg orally 80 mg orally Dexamethasone Adults 12 mg orally none none Pediatric Patients 12 Years and Older If a corticosteroid, such as dexamethasone, is co-administered, administer 50% of the recommended corticosteroid dose on Days 1 through 4 [see Clinical Studies (14.3)].† 5-HT 3 antagonist Adults and Pediatric Patients 12 Years and Older See the selected 5-HT 3 antagonist prescribing information for recommended dosage none none * Administer aprepitant capsules 1 hour prior to chemotherapy treatment on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer aprepitant capsules in the morning. † Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1.

Monitoring

• 5 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 aprepitant 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 aprepitant.
• ( 5.2 , 7.1 ) Hormonal Contraceptives : Efficacy of contraceptives may be reduced during administration of and for 28 days following the last dose of aprepitant.
• Use effective alternative or back-up methods of contraception.

Interaction Notes

• 7 DRUG INTERACTIONS See Full Prescribing Information for a list of clinically significant drug interactions.
• ( 4 , 5.1 , 5.2 , 5.3 , 7.1 , 7.2 ) 7.1 Effect of Aprepitant on the Pharmacokinetics of Other Drugs Aprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4.
• Aprepitant is also an inducer of CYP2C9 [see Clinical Pharmacology ( 12.3 )] .
• Aprepitant acts as a moderate inhibitor of CYP3A4 when administered as a 3-day regimen (125 mg/80 mg/80 mg) and can increase plasma concentrations of concomitant drugs that are substrates for CYP3A4.