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Fosaprepitant

Antiemetic

Also known as EMEND

AntiemeticATC A04AD13
CDSCO approvedSchedule HATC A04AD13
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Nausea in the first trimester of pregnancy is generally mild
FDA category + note
Top interactionssee all 12
  • AcalabrutinibSevereDatabaseDDInter
  • AlfentanilSevereDatabaseDDInter
  • AstemizoleSevereDatabaseDDInter
  • AvanafilSevereDatabaseDDInter

Mechanism

Fosaprepitant is a prodrug that is converted to aprepitant after intravenous administration. Aprepitant is an antagonist of the neurokinin 1 (NK1) receptor. It blocks the binding of Substance P (SP), the preferred ligand for the NK1 receptor, which mediates central and peripheral effects related to emesis.

Indications

Prevention of acute and delayed nausea and vomiting associated with highly emetogenic cisplatin-based chemotherapyPrevention of nausea and vomiting associated with moderately emetogenic chemotherapyPrevention of chemotherapy-induced nausea and vomiting (delayed phase)Prevention of postoperative nausea and vomiting (PONV)antiemetic

Dosing

Adult
▶ BY RECTUM ▶ Antiemetics should be given to prevent motion sickness rather than after nausea or vomiting develop. The most effective drug for the prevention of motion sickness is hyoscine hydrobromide p. 458. The sedating antihistamines are slightly less effective against motion sickness, but are generally better tolerated than hyoscine.…

Pharmacokinetics

Half-life
9-13 hours (as aprepitant)
Protein binding
Extensively bound to plasma proteins (>95%) (as aprepitant)
Metabolism
Metabolized avidly, primarily by hepatic CYP3A4 (as aprepitant)
Excretion
Excreted in the stools (as aprepitant)

Contraindications

  • Concomitant use with cisapride
  • Concomitant use with pimozide
  • Patients receiving cisapride, terfenadine, astemizole, or pimozide

Side effects

Common
FatigueConstipationHiccups
Serious
  • Life-threatening QT prolongation (when co-administered with cisapride or pimozide)

Pregnancy & lactation

Pregnancy

Nausea in the first trimester of pregnancy is generally mild

Drug interactions

Acalabrutinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Alfentanil
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Astemizole
Severe
Database

Drug interaction classified as: metabolism

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

Drug interaction classified as: metabolism

Source: DDInter

Brigatinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Butorphanol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cilostazol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cisapride
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Antiemetic drugs

Ask House about Fosaprepitant

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team