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Pronunciation

fos-a-PREP-i-tant

Classifications

Therapeutic Classification: antiemetics

Pharmacologic Classification: neurokinin antagonists

Indications

REMS


Action

  • Acts as a selective antagonist at substance P/neurokinin 1 (NK1) receptors in the brain.
Therapeutic effects:
  • Decreased nausea and vomiting associated with chemotherapy.

Pharmacokinetics

Absorption: 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 by the CYP3A4 isoenzyme; not renally excreted.

Half-Life: Aprepitant: 9–13 hr.

Time/Action Profile

(antiemetic effect)

ROUTEONSETPEAKDURATION
IVrapidend of infusion*24 hr



*Plasma concentrations.

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Interactions

Drug-drug:

Route/Dosage

Prevention of Acute and Delayed Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy

Prevention of Delayed Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

IV Administration:

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Emend, Focinvez

Code

NDC Code