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Cardiovascular agents

Cardiovascular agents. anticoagulants. Platelet aggregation is affected by two factors: (1) In platelets; thromboxan A2 is synthesized to induce platelet aggregation, while (2) In blood vessels; prostacyclin PGI2 is synthesized to inhibit platelet aggregation.

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Cardiovascular agents

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  1. Cardiovascular agents anticoagulants

  2. Platelet aggregation is affected by two factors: (1) In platelets; thromboxan A2 is synthesized to induce platelet aggregation, while (2) In blood vessels; prostacyclin PGI2 is synthesized to inhibit platelet aggregation. VIT.K is required in the liver biosynthesis of prothrombin (factor II), thromboplastin (factor III) is released from the injured cells and tissues. Thromboplastin in presence of Ca2+ (factor IV) convert Prothrombin to Thrombin which consequently convert Fibrinogen (factor I) to fibrin The main uses of anti coagulants is to prevent blood coagulation in myocardial infarction, venous thrombosis, peripheral arterial emboli, pulmonary emboli and atrial fibrillation. .

  3. Heparin is a mucopolysaccharide, acidic in nature ( Heparinic ) and used as sodium salt. Heparin combines with coagulant factor ( antithrombin III ) forming Heparin-antithrombin III complex which inactivate factor Xa and consequently inhibit the generation of Thrombin. The antidote of Heparin is protamine sulfate Heparin is the best anticoagulant during pregnancy, so it doesn't cross the placental membrane. Heparin is also used with the patients suffering from renal failure and used only during the hemodialysis on artificial kidney units.

  4. Classes of oral anticoagulants 4-Hydroxycoumarin derivatives : Warfarin sodium, Dicumarol and Ethylbiscoumacetate. 1,3-Indandiones: phenindione and ansindione competitive inhibitors of vit.k in the biosynthesis of prothrombin in the liver and produce abnormal prothrombin. This attributed to the structural similarity between the hemiketal form of vit.k and the cyclic hemiketal of 4-hydroxycoumarin e.g. Warfarin.

  5. Warfarin sodium : 3-( acetonylbenzyl)-4-hydroxycoumarin sodium salt. Warfarin contains chiral benzylic carbon, and the more potent isomer is the S isomer ,but it is marketed as sodium salt of racemic mixture.

  6. Dicumarol : 3,3”-Methylene bis (4-hydroxycoumarin)

  7. Ethylbiscoumacetate Ethyl bis (4-hydroxy-2-oxo-1(2H)-benzopyran-3-yl)acetate

  8. 1,3-indandione This group of anticoagulants includes Phenindione and Anisidione which are appears of the same potency, substitution of methoxy group of Anisindion with bromine increase the activity, while nitro-group decrease the activity.

  9. Phenindione 2-Phenyl-1,3-indandione Ansindione 2-(p-Methoxyphenyl)-1,3-indandione

  10. synthesis of phenindione

  11. The enol-form of 1,3-indandione is a highly conjugated compound and may be responsible for the red colour of urine with patients who take this drugs, this color is removed by urine acidification to be distinguished from hematuria. 1,3-indandione inhibits the synthesis of prothrombin and other coagulating factors.

  12. assay of indandione derivatives:

  13. Antiplatelet agents This group includes Aspirin, Dipyridamole,Sulfinpyrazone and Ticlopidine.

  14. Sulfinpyrazone is related to phenylbutazone, but is used as uricosuric and antiplatelet. It is a cyclooxygenase inhibitor. 1,2-diphenyl-4-(2-(phenylsulphinyl)ethyl)-3,5-pyrazolidindione

  15. Ticlopidine is a newer oral antiplatelet drug that is not a NSAID. It works by inhibiting the aggregation effect of ADP on the platelets.

  16. Clot Busting Drugs Blood clots are designed to be temporary. After the vessel is healed and the blood clot is no longer needed, the clot is removed by the following way: the clot itself stimulates the secretion of tissue plasminogen activator (TPA), which catalizes the activation of plasminogen to plasmin which is an enzyme that dissolves clots.

  17. Drugs used clinically to remove clots include: Tissue plasminogen activator (TPA), it was recently cloned and is now produced as Alteplase or Reteplase. It is used clinically to dissolve clots in coronary arteries following a heart attack. It is also used to dissolve clots in the brain following stroke. Streptokinase, it is an enzyme that directly dissolves blood clots. It is produced by streptococcus bacteria. The bacteria use streptokinase to dissolve clots that negatively affects their growth in the human host. However, streptokinase is not a human enzyme and might initiate immune response.

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