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Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: dizziness, fatigue, weakness.

Derm: STEVENS-JOHNSON SYNDROME.

GI: diarrhea.

Neuro: headache.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), hiccups, infusion reactions (fosaprepitant IV only).

Interactions

Drug-Drug:

Availability

(Generic available)

Route/Dosage

Prevention of Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy

Prevention of Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy

US Brand Names

Emend

Aprepitant (Injection): Cinvanti

fosaprepitant (Injection): Emend

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: antiemetics

Pharmacologic Classification: neurokinin antagonists

Pharmacokinetics

Absorption: 60–65% absorbed following oral administration. Following IV administration, fosaprepitant is rapidly converted to aprepitant, the active component. IV administration results in complete bioavailability.

Distribution: Crosses the blood brain barrier; remainder of distribution unknown.

Protein Binding: 95–99%.

Metabolism/Excretion: Mostly metabolized by the liver (CYP3A4 enzyme system); not renally excreted.

Half-life: Aprepitant — 9–13 hr.

Time/Action Profile

(antiemetic effect)

ROUTEONSETPEAKDURATION
PO1 hr4 hr*24 hr
IVrapidend of infusion*24 hr

*Blood level.

Patient/Family Teaching

Pronunciation

a-PREP-i-tant

Aprepitant (Injection): a-PREP-i-tant

fosaprepitant (Injection): fos-a-PREP-i-tant

Code

NDC Code*