Name Aprepitant
Classes Antiemetic Agent
Antivomiting Agent
Diseases

Aprepitant

Aprepitant is a human substance P/neurokinin 1 (NK1) receptor antagonist with a selective high affinity. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, or corticosteroid receptors, which are the targets of current chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) medications (PONV) like ondansetron. palonosteron.

Aprepitant  is indicated for the prevention of-

  • Nausea and vomiting associated with highly emetogenic cancer chemotherapy
  • Nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy
  • Postoperative nausea and/or vomiting
  • Aprepitant can be used alone or in combination with the other anti-emetics. 
  • Aprepitant capsules in adults and pediatric patients 12 years of age and older: 125 mg on Day 1 and 80 mg on Days 2 and 3
  • Aprepitant for oral suspension in pediatric patients 6 months to less than 12 years of age or pediatric and adult patients unable to swallow capsules: 3mg/kg on day 1 with a maximum dose of 125mg. 2mg/kg on day 2 and 3 with a maximum dose of 80mg.
  •  Administer Aprepitant 1 hour prior to chemotherapy on Days 1, 2, and 3. If no chemotherapy is given on Days 2 and 3, administer Aprepitant in morning. 

Common adverse reactions in patients treated for chemotherapy induced vomiting and nausea are-

  • fatigue
  • diarrhea
  • asthenia
  • dyspepsia
  • abdominal pain
  • hiccups
  • Leukopenia
  • dehydration
  • increased alanine aminotransferase 

Clinically Significant CYP3A4 Drug Interactions

  • Aprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4. 
    • Use of Aprepitant with other drugs that are CYP3A4 substrates, may result in increased plasma concentration of the concomitant drug.
  • Use of pimozide with Aprepitant is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide.
  • Use of Aprepitant with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to Aprepitant.
  • Use of Aprepitant with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of Aprepitant. 

Decrease in INR with Concomitant Warfarin

  • Coadministration of Aprepitant with warfarin, a CYP2C9 substrate, may result in a clinically significant decrease in International Normalized Ratio (INR) of prothrombin time.

Risk of Reduced Efficacy of Hormonal Contraceptives

  • Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives may be reduced during administration of and for 28 days following the last dose of Aprepitant 

Contraindication

  • Contraindicated in patients hypersensitive to any component of the formulation.
  • Coadministration with pimozide is contraindicated.

 

There is no known contraindications of the preparation in terms of food and drinks.