止吐口服 (antiemetics PO) For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly- and moderately emetogenic chemotherapy

Aprepitant is a selective high affinity antagonist at human substance P neurokinin 1 (NK1) receptors. NK1-receptor antagonists have been shown to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Preclinical studies show that aprepitant has a long duration of central activity, inhibits both the acute and delayed phases of cisplatin-induced emesis, and augments the antiemetic activity of 5-HT3 receptor antagonist and dexamethasone.

oral bioavailability: 60 to 65%; time to peak: ∼4 hr; plasma protein binding: ＞95%; crosses the blood brain barrier; extensively hepatic metabolism via CYP3A4 (major), CYP1A2 and CYP2C19 (minor); forms seven metabolites (weakly active); elimination half-life: 9-13 hr.

hypersensitive to any component of the product. EMEND should not be used concurrently with pimozide, terfenadine, astemizole, or cisapride. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions

B

not recommended

hiccups (4.6%), asthenia/fatigue (2.9%), ALT increased (2.8%), constipation (2.2%), headache (2.2%), and anorexia (2.0%).

The recommended dose of EMEND is 125 mg orally 1 hour prior to chemotherapy treatment on Day 1, followed by 80 mg in the morning on Days 2 and 3; totally for 3 days. EMEND could not be used in combination with 5-HT3 receptor antagonist except on Day 1. EMEND may be taken with or without food.