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Mechanism and pharmacological action of enoxaparin sodium

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

  1. Anti-xa activity

  Most of the Mr Of low-molecular heparin sodium is between 4~6*103 in one gas, and the molecular chain is less than 18 sugar units. Therefore, it can only bind to ATIII, thus inhibiting FXa, but not to ATIII and FIIa, forming a triad to inhibit FIIa. According to different production processes, the anti-FXA activity of LMWH is 80-120IU/mg, which is 2 times higher than that of FIIa. Therefore, it has a stronger inhibitory effect on FIIa, that is, it enhances the formation of FIIa and prevents 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 effect. Oligosaccharides and even pentosan have antithrombotic effect in large doses. In plasma, antithrombotic effects last longer than anticoagulants.

  2. Anti-fiia activity

  Low molecular weight heparin molecules still contain a third of heparin, or more than 18 sugar units of heparin, which can fight both FIIa and FXa. The anti-FIIA activity is designed to be 35-45IU/mg, which is necessary for anticoagulant therapy, primarily to inactivate the FIIa that has been generated. The combination of the high affinity heparin component and the 30% low affinity heparin component had a higher antithrombotic effect than either of the two alone.

Mechanism and pharmacological action of enoxaparin sodium

  3. The TFPI release

  TFPI is a physiological inhibitor of exogenous coagulation pathway. In recent years, it has been found that its molecular structure has multiple functional binding points and functions, which can inhibit FVIIa, Xa leukocyte prothrombin and monocyte procoagulant factors, and inhibit tissue factors released at thrombosis sites. After 12h of subcutaneous injection, no anti-xa activity was detected in the blood circulation, but the patient was still in the anti-thrombotic state, indicating that the work was still functioning.

  4. Enhance fibrinolytic activity

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

  5. Effects on platelets

  The results of platelet aggregation inducer showed that the effect of low molecular weight heparin on platelet aggregation and enhancement was lower than that of heparin. In platelet activating factor and adenosine diphosphate induced platelet aggregation, the ability to induce platelet aggregation was significantly lower than that of heparin. The inhibition of prostacyclin and antiplatelet aggregation activity was also lower than that of heparin. Therefore, low molecular weight heparin preparation caused by thrombocytopenia 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.