What are the advances in antithrombotic drug therapy

1, antiplatelet drugs: ① aspirin. It is the oldest and most widely used antiplatelet drug, with a history of more than 100 years in the clinic. Its function mainly lies in: irreversibly inhibit platelet cyclooxygenase, block platelet production of thromboxane A2, and inhibit platelet aggregation. ② Clopidogrel. It is a third generation antiplatelet drug. This drug causes an irreversible change in the conformation of the ADP receptor P2Y12 on the platelet membrane, thereby blocking the receptor-mediated activation of ADP by adenylyl cyclase. (iii) Ticlopidine is in the same class of drugs, belonging to the second generation of antiplatelet drugs, and was more widely used in the 1990s. However, in recent years, it is found that ticlopidine can lead to bone marrow suppression, cause neutropenia, and can also be associated with thrombocytopenia, aplastic anemia and thrombotic thrombocytopenic purpura and other diseases.3 Therefore, it is gradually replaced by clopidogrel. 2, anticoagulant drugs: ① Heparin and low molecular heparin are the most widely used anticoagulant drugs. Heparin exerts its anticoagulant effect through antithrombin (AT) and heparin cofactor II (HC-II) in plasma. Although the anticoagulant effect of heparin is well established, heparin application is prone to hematemesis and thrombocytopenia. The three most commonly used low molecular heparins in the domestic market are Farnamycin, Enoxaparin Sodium (Kesai) and Tachykinin. The average molecular weight of fanimin is 6,000, and the half-life is 119~l39 min. enoxaparin sodium has an average molecular weight of 4,200, which is the smallest molecular weight of low molecular weight heparin at present, and the half-life is 129~180 min. quick-avoiding gel has an average molecular weight of 4,500, and the half-life is 111~234 min. ② Fondapariunx (Arixtra. Fondapariunx (Arixtra, Pentosan Sulfated Hepatidyl Sodium) is a synthetic pentose sugar and is the first antithrombotic agent to selectively inhibit factor Xa. ③ The most commonly used oral anticoagulants are vitamin K-dependent antagonists, and warfarin is the most commonly used and representative drug in clinical practice. The antithrombotic effect of warfarin depends on a significant decrease in thrombinogen (coagulation factor II). The half-life of plasminogen is 72h, so it takes at least 3 days for oral warfarin to have a real effect, at which time the original level of coagulation factor II in the body will drop significantly. Increasing the initial dose of warfarin can not quickly achieve effective antithrombotic level, because warfarin can not accelerate the clearance of the original synthesized coagulation factor II, high initial dose will be due to the synthesis of protein C and protein S and rapid clearance, resulting in the initial phase of the drug in a hypercoagulable state, and even thrombotic complications. ④ Rivaroxaban (Xarelto) Rivaroxaban, an orally administered direct thrombin inhibitor, has been shown in studies to not require routine detection of coagulation status compared to warfarin, and to have good compatibility with most drugs. Research on the clinical indications of the drug is currently underway worldwide. 3, thrombolytic drugs: thrombolytic agents, as the name suggests, can ablate the thrombus has formed. Transfected eukaryotic cells (such as Escherichia coli) can be expanded in large numbers to produce recombinant tissue-type fibrinogen activator (rt-PA), which has a stronger thrombolytic effect. Urokinase, streptokinase, and rt-PA are currently the main drugs used in the treatment of thromboembolic disease and thrombosis after revascularization.