EMEND® (aprepitant) Dosage Information

Dosage

For patients receiving highly emetogenic chemotherapy,

Flexible dosing with I.V. or P.O.

EMEND for Injection 150 mg:

EMEND for Injection 150 mg is administered intravenously on Day 1 only as an infusion over 20 to 30 minutes initiated approximately 30 minutes before chemotherapy.
No capsules of EMEND are administered on Days 2 and 3.
On Days 3 and 4, the recommended dosage of dexamethasone with EMEND for Injection 150 mg differs from the recommended dosage of dexamethasone with the 3-day regimen of EMEND.

— Or —

Oral EMEND 125 mg/80 mg:

EMEND is given for 3 days as part of a regimen that includes a corticosteroid and a 5-HT₃ antagonist.
The recommended dosage includes EMEND 125 mg 1 hour prior to chemotherapy treatment on Day 1 followed by EMEND 80 mg once daily on Days 2 and 3.

EMEND for injection is given as part of a regimen
that includes a 5-HT₃ antagonist and a corticosteroid

Administered on Day 1 of chemotherapy; no capsules of EMEND are administered on Days 2 and 3.

	Day 1 (Prechemotherapy)	Day 2	Day 3	Day 4
Injection For highly emetogenic chemotherapy	EMEND for Injection 150 mg I.V. and Dexamethasone^g 12 mg P.O. and Ondansetron^h 32 mg I.V.	Dexamethasone 8 mg P.O. qd	Dexamethasone 8 mg P.O. bid	Dexamethasone 8 mg P.O. bid
Orally For highly emetogenic chemotherapy	EMEND 125 mg P.O. and Dexamethasone^g 12 mg P.O. and Ondansetron^h 32 mg I.V.	EMEND 80 mg P.O. and Dexamethasone 8 mg P.O. qd	EMEND 80 mg P.O. and Dexamethasone 8 mg P.O. qd	Dexamethasone 8 mg P.O. qd

Capsules may not be shown at actual size.
qd=once daily; bid=twice daily.
^aDexamethasone should be administered 30 minutes before chemotherapy on Day 1 and in the morning on Days 2 through 4. The dose of dexamethasone is modified for drug interactions.
^bOndanseteron should be administered 30 minutes before chemotherapy on Day 1.

Important Safety Information

EMEND and EMEND for Injection, in combination with other antiemetic agents, are indicated in adults for prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy, including high-dose cisplatin.

EMEND and EMEND for Injection have not been studied for treatment of established nausea and vomiting. Chronic continuous administration of EMEND or EMEND for Injection is not recommended.

Selected Important Safety Information

EMEND for Injection is contraindicated in patients who are hypersensitive to EMEND for Injection, aprepitant, polysorbate 80, or any other components of the product. Known hypersensitivity reactions include flushing, erythema, dyspnea, and anaphylactic reactions.

Aprepitant, when administered orally, is a moderate cytochrome P450 isoenzyme 3A4 (CYP3A4) inhibitor. Because fosaprepitant is rapidly converted to aprepitant, neither drug should be used concurrently with pimozide or cisapride. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions.

EMEND is contraindicated in patients who are hypersensitive to any component of the product.

EMEND is a dose-dependent inhibitor of cytochrome P450 isoenzyme 3A4 (CYP3A4). EMEND should not be used concurrently with pimozide, terfenadine, astemizole, or cisapride. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions.

EMEND and EMEND for Injection should be used with caution in patients receiving concomitant medications, including chemotherapy agents, that are primarily metabolized through CYP3A4. Inhibition of CYP3A4 by EMEND could result in elevated plasma concentrations of these concomitant medications. Conversely, when EMEND or EMEND for Injection is used concomitantly with another CYP3A4 inhibitor, aprepitant plasma concentrations could be elevated. When EMEND or EMEND for Injection is used concomitantly with medications that induce CYP3A4 activity, aprepitant plasma concentrations could be reduced, and this may result in decreased efficacy of aprepitant.

Chemotherapy agents that are known to be metabolized by CYP3A4 include docetaxel, paclitaxel, etoposide, irinotecan, ifosfamide, imatinib, vinorelbine, vinblastine, and vincristine. In clinical studies, EMEND was administered commonly with etoposide, vinorelbine, or paclitaxel. The doses of these agents were not adjusted to account for potential drug interactions. In separate pharmacokinetic studies, EMEND did not influence the pharmacokinetics of docetaxel or vinorelbine.

Because a small number of patients in clinical studies received the CYP3A4 substrates vinblastine, vincristine, or ifosfamide, particular caution and careful monitoring are advised in patients receiving these agents or other chemotherapy agents metabolized primarily by CYP3A4 that were not studied.

In clinical trials, EMEND and EMEND for Injection increased the AUC of dexamethasone, a CYP3A4 substrate, by approximately 2-fold; therefore, the oral dose of dexamethasone administered in the regimen with EMEND [or EMEND for Injection] should be reduced by approximately 50% to achieve exposures of dexamethasone similar to those obtained without EMEND [or EMEND for Injection]. See PRECAUTIONS, Drug Interactions, in the Prescribing Information for EMEND [or EMEND for Injection] for additional information on dosage adjustment for methylprednisolone when coadministered with EMEND or EMEND for Injection.

Before prescribing EMEND or EMEND for Injection, please read the Prescribing Information. The Patient Information also is available.