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Aprepitant

Antiemetic

Also known as Emend

AntiemeticATC A04AD12
CDSCO approvedSchedule HATC A04AD12
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
not curated
Top interactionssee all 12
  • CilostazoleContraindicatedTextbookKDT 7e · p555
  • EbastineSevereTextbookKDT 7e
  • AcalabrutinibSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter

Mechanism

Aprepitant is a neurokinin 1-receptor antagonist. It prevents nausea and vomiting by blocking the substance P neurokinin 1 (NK1) receptor.

Indications

Prevention of nausea and vomiting associated with highly emetogenic chemotherapyPrevention of nausea and vomiting associated with moderately emetogenic chemotherapyAdjunct to dexamethasone and a 5HT3-receptor antagonist in preventing nausea and vomiting associated with moderately and highly emetogenic chemotherapyantiemeticPrevention of chemotherapy-induced nausea and vomiting (delayed phase, typically with a 5HT3 antagonist and dexamethasone)Prevention of postoperative nausea and vomiting (PONV)chemotherapy induced nausea and vomiting (CINV) (acute and delayed phases, especially with cisplatin and cyclophosphamide-based chemotherapy)postoperative nausea and vomiting (PONV)Prevention of chemotherapy-induced nausea and vomiting (severely emetogenic and moderately emetogenic regimens)

Dosing

Adult
Initially 125 mg orally, taken 1 hour before chemotherapy, then 80 mg orally once daily for 2 days. Consult product literature for dose of concomitant dexamethasone and 5HT3-antagonist.

Pharmacokinetics

Half-life
9 to 13 h
Protein binding
Extensively bound to plasma proteins (>95%)
Metabolism
Primarily by hepatic CYP3A4
Excretion
In the stools

Contraindications

  • Acute porphyrias
  • Patients receiving cisapride, terfenadine, astemizole, or pimozide (due to life-threatening QT prolongation)
  • concomitant use with Q-T interval prolonging drugs like cisapride

Side effects

Common
Appetite decreasedastheniaconstipationgastrointestinal discomfortheadachehiccupsFatigueweaknessflatulence
Serious
  • Anaemia
  • febrile neutropenia
  • anxiety
  • dizziness
  • drowsiness
  • malaise
  • palpitations
  • skin reactions
  • urinary disorders
  • vomiting
  • Bradycardia
  • cardiovascular disorder
  • chest discomfort
  • cognitive disorder
  • conjunctivitis
  • cough
  • disorientation
  • euphoric mood
  • gait abnormal
  • hyperhidrosis
  • increased risk of infection
  • muscle spasms
  • muscle weakness
  • oedema
  • oropharyngeal pain
  • photosensitivity reaction
  • polydipsia
  • seborrhoea
  • severe cutaneous adverse reactions (SCARs)
  • sneezing
  • stomatitis
  • taste altered
  • throat irritation
  • Life-threatening QT prolongation (with contraindicated drugs)
  • rarely rise in liver enzymes

Drug interactions

Cilostazole
Contraindicated
Textbook

Increased plasma levels and toxicity of cilostazole.

Should not be administered along with inhibitors of CYP3A4.

Source: KDT 7e · p555

Ebastine
Severe
Textbook

Increased risk of arrhythmogenic potential.

Exercise caution with coadministration.

Source: KDT 7e

Acalabrutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Astemizole
Severe
Database

Life-threatening QT prolongation.

Aprepitant is contraindicated in patients receiving astemizole.

Source: DDInter

Avanafil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Avapritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bosutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Brexpiprazole
Severe
Database

Increased AUC by 2-fold.

Reduce brexpiprazole dose by 50%.

Source: DDInter

Brigatinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Butorphanol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Antiemetic drugs

Ask House about Aprepitant

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-10 · House clinical team