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Pharmacological action and mechanism of enoxaparin sodium

  Enoxaparin sodium is a kind of low molecular weight heparin sodium, which has the following pharmacological activities:

  1. Anti-xa activity

  Low molecular weight heparin sodium Mr Is mostly in a gas 4~6*103, molecular chain less than 18 sugar units, can only combine with ATIII, so as to inhibit FXa, but can not combine with ATIII and FIIa, to form a triad to inhibit FIIa. According to the production process, the anti-fxa activity of low molecular weight heparin sodium preparation is 80-120 iu /mg, which is 2 times higher than the anti-fiia activity. Therefore, it has a stronger inhibitory effect on FIIa, that is, it can enhance the inhibition of the formation of industrial FIIa and prevent thrombosis. It also inactivates FXa, which binds to platelets. Animal experiments showed that at low doses, the minimum Mr Required 3.6*103, equivalent to 14 sugar units, to produce antithrombotic effects. In large doses, oligosaccharide and even pentosan have antithrombotic effects. In plasma, the antithrombotic effect lasted longer than the anticoagulant effect.

  2. Anti-fiia activity

  Low molecular weight heparin molecules still contain a third of heparin, that is, more than 18 sugar units of heparin molecules, which can fight both FIIa and FXa. The anti-fiia activity design is 35-45iu /mg, which is necessary for anticoagulant therapy, mainly to inactivate the generated FIIa. The antithrombotic effect of high affinity heparin and 30% low affinity heparin in combination was higher than that of either of them alone.

  3. The TFPI release

  TFPI is a physiological inhibitor of the exogenous coagulation pathway. In recent years, it has been found that its molecular structure has multiple functional junctions and functions, which can inhibit FVIIa, Xa, leukocyte thrombin and monocyte thrombin, as well as the tissue factor released from the thrombus formation site. After 12h of subcutaneous injection, the antixa activity was not detected in the blood circulation, but the patient was still in the antithrombotic state, indicating that the work was still playing its role.

  4. Enhance fibrinolytic vitality

  Subcutaneous injection can promote the release of plasminogen and shorten the time of euglobulin dissolution. In animal experiments, antifibrinolytic drugs, which can resist the enhanced fibrinolytic activity, can enhance the thrombolytic effect of recombinant tissue plasminogen activator or single-chain urokinase plasminogen activator.

  Effect on platelets

  Experiments with platelet aggregation inducers showed that the platelet aggregation and enhancement inducers of low molecular weight heparin were lower than those of heparin. The ability to induce platelet aggregation with platelet activator and adenosine diphosphate was significantly lower than that with heparin. The inhibition of prostacyclin and antiplatelet aggregation activity was also lower than that of heparin. Therefore, thrombocytopenia caused by low molecular weight heparin was significantly reduced.

  6. Anti-tumor effect

  Antitumor mechanism has not fully elucidated, and the research evidence that is related to the following factors: (1) inhibition of thrombin/fibrin formation, (2) adjust the immune system, (3) the resistance of tumor cells and host cell adhesion (endothelial cells, platelets, white blood cells), (4) inhibition of new blood vessels to form, (5) inhibit endothelial cell proliferation, and inducing apoptosis, 7 inhibit tumor cells to produce ethyl phthalein enzyme activity, heparin was interference sugar glycosaminoglycans of tumor cells.