Aprepitant

Aprepitant is a prescription medicine used to prevent nausea and vomiting caused by chemotherapy. It is also used in the prevention of postoperative nausea and vomiting in adults.

Aprepitant works by blocking the action of substance P at the neurokinin 1 (NK1) receptors in the brain. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to NK1 receptors, preventing nausea and vomiting.

Common side effects include headache, hiccups, loss of appetite, fatigue, and constipation.

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

Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors.

Aprepitant also enhances the antiemetic activity of 5HT3 antagonists and corticosteroids.

Aprepitant blocks NK1 receptors in the chemoreceptor trigger zone of the brain. Substance P (a neurotransmitter) normally binds to these receptors and triggers nausea and vomiting signals. Aprepitant prevents this binding, thereby preventing nausea and vomiting.

Postoperative Nausea and Vomiting (PONV):

• 40 mg orally within 3 hours prior to induction of anesthesia

Chemotherapy-Induced Nausea and Vomiting (CINV):

Highly Emetogenic Chemotherapy:

Moderately Emetogenic Chemotherapy:

Special Populations: No dose adjustment needed in renal impairment. No dose adjustment needed in mild-moderate hepatic impairment. No dose adjustment needed in elderly patients.

Your doctor or nurse will give you this medicine. Do not self-administer. May be taken with or without food.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.

• Headache
• Dizziness
• Hiccup
• Loss of appetite
• Fatigue
• Constipation
• Hypotension
• Pruritus
• Pyrexia

Serious Precautions:

• Will not help if you already have nausea and vomiting
• Do not use continuously for a long time
• May damage sperms and may harm the baby if used during pregnancy or breastfeeding
• May cause dizziness and sleepiness - do not drive if affected
• May cause diarrhea - drink plenty of fluids
• Consult your doctor if pregnant, planning pregnancy or breastfeeding
• Inform your doctor if you have kidney or liver diseases

• Coadministration with astemizole, cisapride, pimozide, or terfenadine
• Hypersensitivity to any component of the product

• CYP3A4 Inhibitors (e.g., clarithromycin, troleandomycin, diltiazem, verapamil, itraconazole, ketoconazole, nefazodone, ritonavir, nelfinavir): May increase aprepitant plasma levels
• CYP3A4 Inducers (e.g., carbamazepine, phenytoin, rifampicin, primidone, phenobarbital): May reduce aprepitant efficacy
• CYP2C9 Substrates (e.g., phenytoin, tolbutamide, warfarin): May decrease concentrations
• Dexamethasone & Methylprednisolone: May increase plasma levels
• Benzodiazepines (e.g., midazolam, diazepam, alprazolam): May increase plasma levels
• Colchicine: Serum concentrations may increase
• Chemotherapy drugs metabolized by CYP3A4 (e.g., docetaxel, etoposide, ifosfamide, imatinib, paclitaxel, vincristine, vinblastine): May increase toxicity
• Ergot derivatives: May increase levels → ergotism risk
• Oral contraceptives: May reduce efficacy → use additional contraception during treatment and for 1 month after last dose
• Potentially Fatal: Astemizole, cisapride, pimozide, and terfenadine may cause life-threatening torsade de pointes arrhythmias

[CONSULT YOUR DOCTOR] It is not known whether it is safe to consume alcohol with Aprepitant. Please consult your doctor.

[CONSULT YOUR DOCTOR] Aprepitant may be unsafe to use during pregnancy (Pregnancy Category B). Animal studies have shown harmful effects on the developing baby. Your doctor will weigh the benefits and potential risks before prescribing. Use only if clearly needed.

[CONSULT YOUR DOCTOR] It is not known whether aprepitant is excreted in human milk. Caution should be exercised during breastfeeding.

Safety and efficacy in children aged <12 years and weight <30 kg have not been established.

No dosage adjustment is necessary for elderly patients.

[SAFE IF PRESCRIBED] Safe to use in patients with kidney disease. No dose adjustment recommended. No dose adjustment needed for ESRD patients undergoing hemodialysis.

[SAFE IF PRESCRIBED] No dose adjustment needed for mild-to-moderate hepatic impairment. No clinical data available for severe hepatic impairment.

Single doses up to 600 mg of aprepitant were generally well tolerated. Overdose may cause drowsiness and headache. In the event of overdose, discontinue aprepitant and provide general supportive treatment. Aprepitant cannot be removed by hemodialysis.

Store below 30°C, away from light & moisture. Keep out of reach of children.