Aprepitant(ah pre’ pit ant)
Emend
Fosaprepitant
Emend for Injection
PREGNANCY CATEGORY B
Drug Classes
Antiemetic
Substance P and neurokinin 1 receptor antagonist
Therapeutic Actions
Selectively blocks human substance P and neurokinin 1 (NK1) receptors in the CNS, blocking the nausea and vomiting caused by highly emetogenic chemotherapeutic agents. Does not affect serotonin, dopamine, or corticosteroid receptors.
Indications
In combination with other antiemetics for prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately or highly emetogenic cancer chemotherapy, including high-dose cisplatin
Prevention of postoperative nausea and vomiting (oral only)
Contraindications and Cautions
Contraindicated with hypersensitivity to any component of aprepitant, concurrent use of pimozide, lactation.
Use cautiously with concomitant use of any CYP3A4 inhibitors (docetaxel, vinblastine, vincristine, ifosfamide, irinotecen, imatinib, vinorelbine, paclitaxel, etoposide), warfarin and with pregnancy, severe hepatic impairment.
Available Forms
Capsules—40, 80, 125 mg; powder for injection—150 mg (fosaprepitant)
Dosages
Adults
Highly emetogenic cancer chemotherapy: 150 mg IV (fosaprepitant) over 20–30 min, starting 30 min prior to chemotherapy or 125 mg PO 1 hr prior to chemotherapy (day 1) and 80 mg PO once daily in the morning on days 2 and 3; given in combination with 12 mg dexamethasone PO 30 min before chemotherapy on day 1 and 8 mg dexamethasone PO days 2 to 4 and 32 mg ondansetron IV on day 1 only.
Moderately emetogenic cancer chemotherapy: 115 mg IV (fosaprepitant) over 15 min, starting 30 min prior to chemotherapy or 125 mg PO 1 hr before chemotherapy on day 1 with 12 mg dexamethasone PO and two 8-mg doses ondansetron PO (the first given 1 hr before, the second 8 hr after chemotherapy); 80 mg PO on days 2 and 3 in the morning.
Postoperative nausea and vomiting: 40 mg PO within 3 hr before induction of anesthesia.
Pediatric patients
Safety and efficacy not established.
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