section name header

Pronunciation

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 or surgical procedures.
  • Augments the antiemetic effects of dexamethasone and 5-HT3 antagonists in patients receiving chemotherapy.

Pharmacokinetics

Absorption: 60–65% absorbed following oral administration. 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: 9–13 hr.

Time/Action Profile

(antiemetic effect)

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



*Plasma concentration.

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 Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy

Prevention of Postoperative Nausea and Vomiting

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

IV Administration:

Cinvanti

Emend

Aponvie

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Aponvie, Cinvanti, Emend

Code

NDC Code