Aprepitant is indicated for:

• Prevention of postoperative nausea and vomiting (PONV)
• Prevention of chemotherapy-induced nausea and vomiting (CINV)

Aproxi EZY is a convenient combi-pack developed by Beacon Pharmaceuticals PLC, containing one 125 mg capsule and two 80 mg capsules in a single strip. This packaging is designed to simplify chemotherapy treatment and improve patient convenience.

Aprepitant is a selective, high-affinity antagonist of substance P neurokinin-1 (NK1) receptors. Substance P plays a key role in triggering nausea and vomiting by binding to NK1 receptors in the brain. Aprepitant blocks this binding, thereby preventing nausea and vomiting associated with chemotherapy and surgical procedures.

Post Operative Nausea and Vomiting: The recommended oral dosage of Aprepitant is 40 mg within 3 hours prior to induction of anesthesia.

Chemotherapy-Induced Nausea and Vomiting: The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy

• Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
• Day 2: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
• Day 3: Aprepitant 80 mg orally, Dexamethasone 8 mg orally
• Day 4: Dexamethasone 8 mg orally

Aprepitant is administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3. Dexamethasone is administered 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4. The dose of dexamethasone accounts for drug interactions.

The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:

• Day 1: Aprepitant 125 mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
• Day 2: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
• Day 3: Aprepitant 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day.

Aprepitant is administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3. Dexamethasone is administered 30 minutes prior to chemotherapy treatment on Day 1. The dose of dexamethasone accounts for drug interactions.

Aprepitant may be taken with or without food. No dosage adjustment is necessary for the elderly patients

Aprepitant acts as a substrate, moderate inhibitor, and inducer of CYP3A4, and also induces CYP2C9. Caution is required when co-administered with drugs metabolized by these enzymes, such as warfarin, tolbutamide, phenytoin, ketoconazole, itraconazole, clarithromycin, ritonavir, diltiazem, rifampin, and carbamazepine.

Additionally, Aprepitant may reduce the effectiveness of hormonal contraceptives during treatment and for up to 28 days after the last dose; therefore, alternative or backup contraceptive methods should be used during this period.

Aprepitant is contraindicated in patients with known hypersensitivity to any component of the formulation. It should not be used together with drugs such as pimozide, terfenadine, astemizole, or cisapride due to the risk of serious adverse effects.

Reported side effects include constipation, low blood pressure, itching, and fever.

Pregnancy Category B. Aprepitant should be used during pregnancy only if clearly necessary. It is not known whether the drug is excreted in human breast milk. A decision should be made to either discontinue breastfeeding or the medication, depending on its importance to the patient.

• Renal impairment: No dose adjustment is required, including in patients undergoing hemodialysis
• Hepatic impairment: No adjustment is needed in mild to moderate cases; however, there is limited data in severe hepatic impairment

There is no specific antidote for Aprepitant overdose. Doses up to 600 mg have been generally well tolerated. Overdose may cause drowsiness and headache. Management includes discontinuation of the drug and supportive care. Hemodialysis is not effective in removing the drug.

Antiemetic agent.

Store below 30°C, protected from light and moisture. Keep out of reach of children.