Aprepitant
EMEND
What it isNK1-receptor antagonist; chemotherapy-induced nausea, particularly the delayed phase.
Why this oneIts NK1 blockade is especially valuable for delayed chemotherapy nausea, which setrons cover poorly.
What limits itIt inhibits CYP3A4, requiring adjustment of dexamethasone and some chemotherapy; it also reduces oral-contraceptive efficacy.
FDA-approved for
- chemo nausea (2003)
FDA label
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prevention of CINV (highly/moderately emetogenic chemo), with corticosteroid + 5-HT3 antagonist | adults — Day 1 | 125 mg 1 h before chemo | 125 mg (Day 1) | 125 mg |
| Prevention of CINV — Days 2-3 | adults | 80 mg QD (morning) | 80 mg QD | 80 mg QD |
| Prevention of postoperative nausea/vomiting (PONV) | adults | 40 mg within 3 h before anesthesia induction | 40 mg once | 40 mg |
Renal No adjustment needed
Hepatic Mild-moderate (Child-Pugh 5-9): no adjustment; severe (>9): no clinical data, use with caution.
Instructions
- May take with or without food.
- CINV: give as 3-day regimen with a corticosteroid and a 5-HT3 antagonist.
- IV fosaprepitant (115 mg) may substitute for oral 125 mg on Day 1 only.
Contraindications
- Concurrent use with pimozide, terfenadine, astemizole, or cisapride (CYP3A4 inhibition → serious/life-threatening reactions)
Cautions
- Dose-dependent CYP3A4 inhibitor — caution with CYP3A4-metabolized drugs
- Decreased INR with warfarin (CYP2C9 substrate)
- Reduced efficacy of hormonal contraceptives during and 28 days after last dose — use backup
- Caution in severe hepatic impairment
Adverse reactions
- CINV: alopecia, anorexia, asthenia/fatigue, constipation, diarrhea, headache, hiccups, nausea
- PONV: constipation, hypotension, nausea, pruritus, pyrexia
Pregnancy Pregnancy Category B; no evidence of fetal harm in animals; use during pregnancy only if clearly needed.
Lactation Excreted in rat milk; unknown in human milk; decide to discontinue nursing or the drug.
NO BOXED WARNINGS
Principal riskIt reduces oral contraceptive efficacy
Cost, est. cash$10–$300/month
Generic entry2012
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySedation, QT prolongation, extrapyramidal symptoms or anticholinergic toxicity vary by receptor target.
Mechanism of action: Aprepitant ballicule
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