prasugrel intermediate | prasugrel is a thienopyridine antiplatelet drug developed by Eli Lilly and Japanese drugmaker First Pharmaceutical Sankyo (Daiichi Sankyo). It is a prodrug that forms active molecules after being metabolized by cytochrome P450 in the liver, which binds to platelet P2Y12 receptors to exert anti-platelet aggregation activity. Clinical studies have proved that the 60 mg dose has a better anticoagulant effect than the 300 mg standard dose of clopidogrel and the 600 mg increased dose, which can reduce the overall risk of heart attack, stroke, and death due to heart disease by 20%, and It has quick effect, good curative effect, good drug resistance and bioavailability, and low toxicity. Prasugrel also has stronger performance than clopidogrel in interventional surgery for stable angina and acute coronary syndrome, but the stronger the antiplatelet effect, the more likely it is to cause bleeding. The key question now is how to identify patients at high risk of thrombosis in clinical practice and how to identify people at high risk of bleeding, so that prasugrel and clopidogrel can be used differently in the two high-risk groups, which can reduce coronary thrombosis and avoid major bleeding. On December 18, 2008, prasugrel received its first important international recognition, and the European Medical Products Committee (CHMP) of the European Medicines Agency recommended the approval of the drug. The permission of the European Commission was passed in late February 2009. In Europe, it is sold under the trade name Efient for the treatment of acute coronary syndrome. The working principle of prasugrel is to inhibit platelet activation and concurrent aggregation by blocking P2Y12 adenosine diphosphate receptors on the platelet surface. Antiplatelet drugs are used to prevent platelets from gathering or sticking together. If platelets accumulate, they can cause artery blockage and may cause heart disease or stroke. On July 10, 2009, the U.S. Food and Drug Administration approved prasugrel tablets for patients undergoing angioplasty to reduce the risk of thrombosis. In April 2010, it was approved in Canada for the treatment of acute coronary syndrome. Prasugrel's label contains framed warnings to remind doctors that the drug may cause obvious and sometimes fatal bleeding. This product should not be used for the following patients: current pathological bleeding; a history of transient ischemic attack or stroke; or emergency surgery, including coronary artery bypass surgery. |