Killing Biological Cascades:<br />An Introduction to blood anticoagulants<br />
Contents<br />Biological Cascades<br />Recap – Blood Clotting Mechanism<br />Vitamin K – How it contributes<br />Anticoagu...
Cascades<br />Consider the chemical reactions below<br />A+ B  X<br />A+ C  D<br />        D + E  F<br />        F + G ...
-Why you don’t bleed to death-<br />When wound occurs:<br />Platelets adhere to collagen fibers and release clotting facto...
2-methyl-1,4-naphthoquinone (ZOMGWTFBBQUBER1337HAX?!)<br />A.K.A Vitamin K.<br />undergoes  reduction to a reduced form of...
Anticoagulants in a nutshell<br />Substance that stops blood from clotting<br />( A.K.A it interferes with the clotting ca...
Warfarin : How it works:<br />Competitive Inhibitor of enzyme EpoxideReductase.<br />Inhibits  enzyme <br /><ul><li>Preven...
Prevents activation of coagulation factors via carboxylation
Coagulation factors cannot bind in a stable manner to wound
Cannot activate clotting to allow formation of a clot
Blood doesn’t clot.</li></ul>Because it is an competitive inhibitor, effects can be undone through providing high concentr...
Heparin : How it works<br />Mucopolysaccharide in nature ( nitrogen groups on carbohydrates)<br />Binds to thrombrin allow...
AT inactivates  thrombin (electrostatic attraction)  and factor Xa (changing active site conformation)
Coagulation pathway jeopardized. </li></li></ul><li>C & C - two of the drugs with same effects? Why?<br />
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Killing biological cascades

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Killing biological cascades

  1. 1. Killing Biological Cascades:<br />An Introduction to blood anticoagulants<br />
  2. 2. Contents<br />Biological Cascades<br />Recap – Blood Clotting Mechanism<br />Vitamin K – How it contributes<br />Anticoagulants?<br />Coumarins – Mechanism<br />Heparin Derivatives – Mechanism<br />So…are they different?<br />
  3. 3. Cascades<br />Consider the chemical reactions below<br />A+ B  X<br />A+ C  D<br /> D + E  F<br /> F + G  H<br /> B + H  X<br />
  4. 4. -Why you don’t bleed to death-<br />When wound occurs:<br />Platelets adhere to collagen fibers and release clotting factors, starting the clotting mechanism.<br />
  5. 5.
  6. 6.
  7. 7. 2-methyl-1,4-naphthoquinone (ZOMGWTFBBQUBER1337HAX?!)<br />A.K.A Vitamin K.<br />undergoes  reduction to a reduced form of vitamin K via enzyme EpoxideReductase. (VKOR)<br />Reduced Vitamin K is then used to carboxylateGlu residues to Gla residues in various coagulation factors to activate them. <br />Associated carboxylation enzyme turns Vitamin K to its oxidised state, which is then reduced by EpoxideReductase.<br />Cycle continues.<br />
  8. 8. Anticoagulants in a nutshell<br />Substance that stops blood from clotting<br />( A.K.A it interferes with the clotting cascade somehow)<br />Used primarily to prevent inappropriate blood clotting ( Eg: Pulmonary Embolism , Stroke, Myocardial Infarctions) <br />We will be looking at 2 types of anticoagulants today, using the examples: <br />Coumarins (Warfarin)<br />Heparin & Derivatives ( Heparin)<br />
  9. 9. Warfarin : How it works:<br />Competitive Inhibitor of enzyme EpoxideReductase.<br />Inhibits enzyme <br /><ul><li>Prevents Vitamin K from being reduced/recycled after caboxylation.
  10. 10. Prevents activation of coagulation factors via carboxylation
  11. 11. Coagulation factors cannot bind in a stable manner to wound
  12. 12. Cannot activate clotting to allow formation of a clot
  13. 13. Blood doesn’t clot.</li></ul>Because it is an competitive inhibitor, effects can be undone through providing high concentrations of Vitamin K.  Vitamin K is an antidote to Warfarin Poisoning.<br />
  14. 14. Heparin : How it works<br />Mucopolysaccharide in nature ( nitrogen groups on carbohydrates)<br />Binds to thrombrin allowing thrombrin inhibition to take place<br />Changes conformation of natural clotting inhibitor Antithrombin III (AT)<br /><ul><li>Strongly increases the efficency of AT
  15. 15. AT inactivates thrombin (electrostatic attraction) and factor Xa (changing active site conformation)
  16. 16. Coagulation pathway jeopardized. </li></li></ul><li>C & C - two of the drugs with same effects? Why?<br />
  17. 17. Conclusion Random Facts<br />Due to the complimentary actions of both drugs, they are often taken together, with heparin stopped after a day or two.<br />Fast action of heparin also means that it is used in various healthcare machines (Dialysis Machines, CPB pumps) to prevent clots forming in the tubes.<br />choice of which anticoagulant to use will depend on the condition being treated as well as how the body reacts to the medication. <br />
  18. 18. Questions?<br />
  19. 19. No Moar Questions?<br />
  20. 20. SO….<br />Try Warfarin today! If it can kill rats, It definitely can kill you!<br />This advertisement is of courtesy to our sponsor - Wilson Pharmaceuticals Pte Ltd<br />
  21. 21. Thank You.<br />-End the d**n thing lar. So boring can?-<br />

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