Aprepitant is a neurokinin -1 (NK-1) receptor blocker, binding to the NK-1 receptor blocking effect of substance P. It can be used to pass the blood-brain occupied in the NK-1 receptor with high affinity and selectivity, while NK-2 and NK-3 receptor affinity is very low. In the standard method of severe emetic symptoms and serotonin 3 (5-HT) receptor antagonist and dexamethasone combination treatment of chemotherapy-induced, it is possible to improve the acute and delayed nausea and vomiting induced by chemotherapy complete response rate .
This product can be extensively metabolized in the body, mainly through CPY3A4, a small part by CPY1 A2 and CPY2C9 conduct; its metabolites are mainly structural parts of the morpholine ring and side chains. Healthy subjects administered a single dose of 300 mg C-labeled goods after 72 h, the plasma can be detected in 24% of the radioactivity, indicating that the product does exist in plasma metabolites, and at least seven species, but basically no pharmacological effects.
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