Aprepitant
Antiemetic & Gastroprokinetic · Neurokinin-receptor antagonist
Indications
As combination therapy for prevention of acute and delayed nausea and vomiting associated with cisplatin-based chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic chemotherapy.
Dosage
Adults: To be used in combination with a 5HT3-antagonist and corticosteroid. 125 mg cap 1 hr prior to chemotherapy on Day 1, then 80 mg 1 cap in the morning on Day 2 and Day 3. Children: Not recommended.
Adverse Effects
Hiccups, asthaenia, fatigue, GI upset, headache, dizziness, anorexia, increased ALT and AST levels.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Ensure effective non-hormonal contraception during and for 2 months after treatment. Precautions: Moderate or severe hepatic impairment.
Interactions
Pimozide, immunosuppressants, ergot alkaloids, fentanyl, alfentanil, etoposide, vinorelbine, antifungals, macrolides, protease inhibitors, rifampicin, phenytoin, carbamazepine, phenobarbital, oral anticoagulants, tolbutamide; any other substrate, inhibitor or inducer of CYP3A4 or substrate of CYP2C9. Irinotecan, hormonal contraceptives, St John's wort, corticosteroids, benzodiazepines.
Advice to Patient
Take with or without meals. Avoid grapefruit juice and St John's Wort during therapy. Patients taking warfarin should have clotting status monitored closely for 2 weeks after first aprepitant dose, especially every 7 to 10 days during each chemotherapy cycle.
Pharmacokinetics
Metabolism: Extensively hepatic. Bioavailability: Approx. 60%-65%. Half-life elimination: Terminal: IV, Oral: Approx. 9-13 hrs. Time to peak, plasma: Paed: Cap: Approx. 4 hrs. Susp: Approx. 6 hrs. Adults: 40 mg: Approx. 3 hrs, 125 mg followed by 80 mg for 2 days: Approx. 4 hrs. Excretion: Primarily through metabolism.
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
Always consult a pharmacist or doctor.