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Antiplatelets & Anticoagulants

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DRUGS AFFECTING THE

BLOOD
 Thrombosis – formation of an unwanted clot within the blood
vessel or the heart

 Bleeding – failure of hemostasis which may be due to


hemophilia and Vitamin K deficiency

Dysfuntions of  Anemia – below normal plasma hemoglobin concentration


the blood resulting from a decreased number of circulating red blood
cells or abnormally low total hemoglobin content per unit of
blood volume.
 Puncture / cuts initiate a series of complex interactions
between platelets, endothelial cells and the coagulation
cascade.
Response to
Vascular  Results in the formation of a platelet – fibrin plug.

Trauma
 Unwanted thrombus involves the same step but of a different
stimuli which is of pathologic origin in the vascular system.
 General MOA: Decrease the formation of or the action of
chemical signals that promote platelet aggregation.

Platelet
Aggregation  Indications:
 Treatment and prevention of occlusive CV diseases
Inhibitors  Maintenance of vascular grafts and arterial patency
 Adjuncts to thrombolytic therapy in myocardial infarction
 Drugs:
 Aspirin – blocks thromboxane A2 synthesis from arachidonic acid
in platelets by irreversible acetylation and inhibition of
cyclooxygenase, a key enzyme in prostaglandin and thromboxane
A2 synthesis

Platelet
Aggregation  Ticlopidine – inhibits the ADP pathway involved in the binding of
platelets to fibrinogen and to each other
Inhibitors
 Dipyridamole – increases intracellular levels of cyclic AMP by
inhibiting cyclic nucleotide phosphodiesterase; inhibits
thromboxane A2 synthesis and potentiate the effects of
prostacyclin to antagonize platelet aggregation
 Heparin – binds to antithrombin III (heparin cofactor) to cause
rapid anticoagulant effect by inhibiting serine proteases; limits
the expansion of the thrombi by preventing fibrin formation

Anticoagulants  Indications:
 Treatment of deep vein thrombosis and pulmonary embolism
 Decreases incidence of recurrent thromboembolic episodes
 Prophylactically, prevent postoperative venous thrombosis
 Warfarin / Dicumarol – antagonize the cofactor functions of
Vitamin K, thereby preventing the synthesis of several protein
factors (Factors II, VII, IX and X) in the liver

Anticoagulants  Indications:
 Myocardial infarction
 Hip arthroplasty
 MOA: activate the concersion of plasminogen to plasmin, a
serine protease that hydrolyzes fibrin and thus, dissolves clots

Thrombolytic
Drugs  Indication
 Treatment of myocardial infarction, massive pulmonary embolism
and acute ischemic stroke
 Streptokinase
 Alteplase
Thrombolytic  Anistreplase
Drugs  Urokinase
 Aminocaproic acid / Tranexamic acid – inhibits plasminogen
activation

DRUGS THAT  Protamine sulfate – antagonizes the anticoagulant effects of


TREAT heparin

BLEEDING
 Vitamin K – acts as a cofactor in the synthesis of protein
factors

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