止吐注射 (antiemetics IV) Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC). Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC).

Fosaprepitant is a prodrug of aprepitant, a substance P/neurokinin 1 (NK1) receptor antagonist. It is rapidly converted to aprepitant which prevents acute and delayed vomiting by inhibiting the substance P/neurokinin 1 (NK1) receptor; augments the antiemetic activity of the 5-HT3 receptor antagonist and corticosteroid activity and inhibits chemotherapy-induced emesis.

Metabolism: Fosaprepitant: Hepatic and extrahepatic; rapidly (within 30 minutes after the end of infusion) converted to aprepitant (nearly complete conversion); Elimination Half-life: Fosaprepitant: ~2 minutes; Aprepitant: ~9-13 hours.

Hypersensitivity to fosaprepitant, aprepitant, polysorbate 80, or any component of the formulation; concurrent use with pimozide, terfenadine, astemizole, or cisapride.

B

Infant risk cannot be ruled out. [MDX]

Fatigue, ALT increased, decreased appetite, hiccups, Injection site reactions (3%; includes erythema, induration, pain, pruritus, or thrombophlebitis).

(Adult)Prevention of chemotherapy-induced nausea/vomiting: IV: Single-dose regimen for highly-emetogenic chemotherapy,150 mg infuse over 20-30 minutes, ~30 minutes prior to chemotherapy on day 1 only (in combination with a 5-HT3 antagonist on day 1 and dexamethasone on days 1 to 4).

Store intact vials at 2°C to 8°C. Solutions diluted to 1 mg/mL for infusion are stable for 24 hours at room temperature or at <25°C.