Medications
Aprepitant - Emend-oral
EMEND is a substance P/neurokinin 1 (NK1) receptor antagonist.
Most common adverse reactions are:
Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
• Adults (≥3%): fatigue, diarrhea, asthenia, dyspepsia, abdominal pain, hiccups, white blood cell count decreased, dehydration, and alanine aminotransferase increased.
• Pediatrics (≥3%): neutropenia, headache, diarrhea, decreased appetite, cough, fatigue, hemoglobin decreased, dizziness, and hiccups.
PONV
• Adults (≥3%): constipation and hypotension.
- Effect of Aprepitant on the Pharmacokinetics of Other Drugs
Aprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of
CYP3A4 and CYP2C9 [see Clinical Pharmacology. Aprepitant acts as a moderate inhibitor of CYP3A4 when administered as a 3-day regimen (125 mg/80-mg/80-mg) and can increase plasma concentrations of concomitant drugs that are substrates for CYP3A4. Aprepitant acts as a weak inhibitor when administered as a single 40-mg dose and has not been shown to alter the plasma concentrations of concomitant drugs that are primarily metabolized through CYP3A4. Some substrates of CYP3A4 are contraindicated with EMEND
• CYP3A4 Interactions: Aprepitant is a substrate, weak-to-moderate inhibitor and inducer of CYP3A4; See Full Prescribing Information for recommendations regarding contraindications, risk of adverse reactions, and dosage adjustments of EMEND and concomitant drugs.
• Warfarin (a CYP2C9 substrate): Risk of decreased INR of prothrombin time; monitor INR in 2-week period, particularly at 7 to 10 days, following initiation of EMEND.
• Hormonal Contraceptives: Efficacy of contraceptives may be reduced during administration of and for 28 days following the last dose of EMEND. Use effective alternative or back-up methods of contraception.
