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Home » GATE Study Material » Pharmaceutical Science » Medicinal Chemistry » Anticoagulants


Anticoagulants


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Anticoagulants

Anticoagulants


  • Definition

        Compounds that do not allow blood to clot are called anticoagulants. These include drugs such as heparin and coumarin. Drugs that dissolve pre-formed clot including streptokinase are not referred to as anticoagulants.

        Anticoagulants are usually administered to patients with myocardial infarction, venous thrombosis, peripheral arterial emboli and pulmonary emboli. They have been used to prevent transient ischemic attacks and to reduce the risk of recurrent myocardial infarction.



 

  • Process of clotting

        The circulatory system has to be self-sealing, otherwise continued blood loss from even the smallest injury would be life threatening. Normally, all but the most catastrophic bleeding is rapidly stopped, a process known as hemostasis. This process occurs through a progression of several steps.

        Hemostasis is a combination of events that occur due to physical and chemical forces. The initial steps lead to a reduction in the blood flow due to the formation of a cellular plug. The later steps utilize chemical energy to form a blood clot, medically known as thrombus.

        The Physical Process

 

        The aggregating platelets and the damaged tissue initiate the biochemical process of blood clotting or coagulation, the body's major defense against blood loss.

 

  • Mechanism of clotting

       A blood clot forms as a result of concerted action of some 20 different substances, most of which are plasma glycoproteins (Table).

Coagulation Factors
Factor Name Plasma half-life (h)
     
I Fibrinogen 72 - 96
II Prothrombin 60
III Tissue Factor or thromboplastin --
IV Ca++ --
V Proaccelerin 15
VII Proconvertin 5
VIII Antihemophilic A factor 10
IX Antihemophilic B factor or Christmas factor 25
X Stuart or Stuart-Prower factor 40
XI Plasma thomboplastin antecedent 45-65
XII Hageman factor, contact factor 60
XIII Fibrin stabilizing factor 150
  Prekallikrein factor --
  High-molecular-weight kininogen 156

 

        The phenomenon of blood coagulation is traditionally distinguished into two pathways. These pathways are the intrinsic and the extrinsic pathways (Figure below). The intrinsic pathway is defined as a cascade that utilizes only factors that are soluble in the plasma, whereas the extrinsic pathway consists of some factors that are insoluble in the plasma, e.g., membrane-bound factors (factor VII). However, the boundary differentiating these two is becoming more and more blurred.

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