Aprepitant Cas:170729-80-3
Aprepitant received marketing authorization in the United States and the European Union in 2003 for use in combination with other anti-vomiting agents to prevent acute or delayed nausea and vomiting during initial or repeated chemotherapy for highly or moderately emetic tumors. It is currently approved in more than 75 countries. The drug blocks the action of substance P by binding to NK-1 receptors (mainly found in the central nervous system and its periphery), and can cross the blood-brain barrier, occupying the NK-1 receptor in the brain, with selectivity and high affinity, and very low affinity for NK-2 and NK-3 receptors. At the same time, the affinity of other drugs used to treat chemotherapy-induced nausea and vomiting symptoms (such as dopamine receptors, 5-HT receptors) is also low, and its effect on reducing nausea and vomiting is better than other drugs.
Aprepitant received marketing authorization in the United States and the European Union in 2003 for use in combination with other anti-vomiting agents to prevent acute or delayed nausea and vomiting during initial or repeated chemotherapy for highly or moderately emetic tumors. It is currently approved in more than 75 countries. The drug blocks the action of substance P by binding to NK-1 receptors (mainly found in the central nervous system and its periphery), and can cross the blood-brain barrier, occupying the NK-1 receptor in the brain, with selectivity and high affinity, and very low affinity for NK-2 and NK-3 receptors. At the same time, the affinity of other drugs used to treat chemotherapy-induced nausea and vomiting symptoms (such as dopamine receptors, 5-HT receptors) is also low, and its effect on reducing nausea and vomiting is better than other drugs.
Dose administration
Aprepitant is often used in combination with ondansetron (first day only) and dexamethasone for chemotherapy-induced nausea and vomiting. Specific usage is as follows: 30min before chemotherapy, 32mg ondansetron, 12mg dexamethasone, 2 ~ 4 days, in the morning, 8mg dexamethasone. For chemotherapy-induced nausea and vomiting, the initial dose is 125mg on the first day, 1h before chemotherapy; 2 ~ 3 days, 80mg daily. Take one hour before chemotherapy for major depression (with anxiety) 300mg each time, qd. But the efficacy is not clear, and there is no need to adjust the dose by gender or race. No dose adjustment is required for patients with renal insufficiency. Dose adjustment is also not required in patients with mild to moderate hepatic insufficiency, and pharmacokinetic data for severe hepatic impairment are lacking. The elderly also do not need to adjust their dose. Patients with end-stage renal disease undergoing hemodialysis also do not need to adjust the dose.
