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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 (SJS)

GI: diarrhea

Neuro: headache

Misc: hiccups, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Availability ⬆ ⬇

(Generic available)

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

US Brand Names ⬆ ⬇

Aponvie, Cinvanti, Emend

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.

Classifications ⬆ ⬇

Therapeutic Classification: antiemetics

Pharmacologic Classification: neurokinin antagonists

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 via the CYP3A4 isoenzyme.

Half-Life: 9–13 hr.

Time/Action Profile ⬆ ⬇

( antiemetic effect)

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

* Plasma concentration.

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

a-PREP-i-tant

Code ⬆

NDC Code