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Aprepitant
- indication:For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).
- pharmacologypharmacology:
- mechanism: Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT<sub>3</sub>-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.
- toxicity:
- absorprion: The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.
- halflife: 9-13 hours
- roouteelimination: Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted. Aprepitant is excreted in the milk of rats. It is not known whether this drug is excreted in human milk.
- volumedistribution: * 70 L
- clearance: * Apparent plasma cl=62-90 mL/min