Uses

Aprepitant is indicated in combination with other antiemetics for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy (including high-dose cisplatin) and moderately emetogenic chemotherapy in adults.

Do not use if

Contraindicated in patients hypersensitive to any component of the formulation and in those taking pimozide (due to CYP3A4 inhibition raising pimozide levels and risk of serious cardiac arrhythmias).

Side effects

Common adverse reactions include fatigue, asthenia, nausea, diarrhea, and neutropenia. Hiccups, constipation, and anorexia occur less frequently. Hypersensitivity reactions including anaphylaxis have been reported.

Warnings

Aprepitant is a moderate CYP3A4 inhibitor and inducer; significant drug interactions are possible with CYP3A4 substrates including corticosteroids (dose adjustment required), benzodiazepines, warfarin, and hormonal contraceptives (reduced efficacy). Use is cautious in severe hepatic impairment.

How it works

Aprepitant is a selective, high-affinity antagonist of the substance P/neurokinin-1 (NK1) receptor. It blocks NK1 receptors in the central nervous system, including in the chemoreceptor trigger zone and the nucleus tractus solitarius, preventing the emetogenic effects of substance P released during chemotherapy.

Storage

Store at room temperature, 20°C to 25°C. Keep in original packaging.