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FIBRINOLYTICS AND
ANTI-COAGULANTS
FRIBRINOLYTIC SYSTEM
• The process of dissolution of clot is called fibrinolysis.
FRIBRINOLYTICS
• Used to lyse the thrombi/clot to recanalize the occluded blood vessel ( mainly
coronary artery)
• Works by activating the fibrinolytic system/
• Streptokinase
• Urokinase
• Reteplase
• Alteplase(t-PA)
• Tenecteplase
STREPTOKINASE
• Ontained from Beta-hemolytic streptococci
• Binds with circukating plasminogen to form complex that activates plasminogen
to plasmin
• T1/2 is 30-80mins
• Anitgeinc, pyrogenic
• Destroyed by circulating antistreptococcal antibodies
• Hypotension and arrhythmia can occur.
STREPTOKINASE
• Uses
• Acute Myocardial infarction
• 7.5 to 15 lac IU; IV over 1 hour
• Deep vein thrombosis, Pulmonary embolism
• Adverse effects
• Bleeding, Hypotension, allergic reactions, fever, arrhythmias
• Contra-indictaions
• Recent trauma, surgery, abortion, stroke, severe hypertension, peptic ulcer, bleeding
disorders.
UROKINASE
• Enzyme islolated from human urine, now prepared from cultured human kidney
cells,
• Direct plasminogen activator.
• T ½ of 10-15mins.
• Non- antigenic, non-allergenic.
• Fever can occur but hypotension is rare.
• Indicated in patients in whom streptokinase had a allergic response earlier.
ALTEPLASE
• Recombinant tissue plasminogen activator rt-TA.
• Selectively activates plasminogen bound to fibrin
• Non-antigenic, not destroyed by anti-bodies.
• Rapid acting, more potent.
• Superior in dissolving old clots
• Short half life of 4-8mins
• Nausea, mild hypotension, fever may occur.
• expensive
NEWER RECOMBINANT TISSUE PLASMINOGEN
ACTIVATORS
• Reteplase
• Modified rt-PA.
• Longer half life ot 15-20mins, but less specific for fibrin bound plasminogen
• Tenecteplase
• Genetically engineered mutant form of alteplase
• Higher fibrin selectivity and longer half life- 2hours.
• Singl bolus dose 0.5mg/kg suffiecient
• Very expensive
USES OF FIBRINOLYTICS
• Acute myocardial infarction
• Deep vein thrombosis
• Pulmonary embolism
• Peripheral arterial occlusion
• Ischemic stroke

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edit 12.pptx

  • 2. FRIBRINOLYTIC SYSTEM • The process of dissolution of clot is called fibrinolysis.
  • 3.
  • 4. FRIBRINOLYTICS • Used to lyse the thrombi/clot to recanalize the occluded blood vessel ( mainly coronary artery) • Works by activating the fibrinolytic system/ • Streptokinase • Urokinase • Reteplase • Alteplase(t-PA) • Tenecteplase
  • 5. STREPTOKINASE • Ontained from Beta-hemolytic streptococci • Binds with circukating plasminogen to form complex that activates plasminogen to plasmin • T1/2 is 30-80mins • Anitgeinc, pyrogenic • Destroyed by circulating antistreptococcal antibodies • Hypotension and arrhythmia can occur.
  • 6. STREPTOKINASE • Uses • Acute Myocardial infarction • 7.5 to 15 lac IU; IV over 1 hour • Deep vein thrombosis, Pulmonary embolism • Adverse effects • Bleeding, Hypotension, allergic reactions, fever, arrhythmias • Contra-indictaions • Recent trauma, surgery, abortion, stroke, severe hypertension, peptic ulcer, bleeding disorders.
  • 7. UROKINASE • Enzyme islolated from human urine, now prepared from cultured human kidney cells, • Direct plasminogen activator. • T ½ of 10-15mins. • Non- antigenic, non-allergenic. • Fever can occur but hypotension is rare. • Indicated in patients in whom streptokinase had a allergic response earlier.
  • 8. ALTEPLASE • Recombinant tissue plasminogen activator rt-TA. • Selectively activates plasminogen bound to fibrin • Non-antigenic, not destroyed by anti-bodies. • Rapid acting, more potent. • Superior in dissolving old clots • Short half life of 4-8mins • Nausea, mild hypotension, fever may occur. • expensive
  • 9. NEWER RECOMBINANT TISSUE PLASMINOGEN ACTIVATORS • Reteplase • Modified rt-PA. • Longer half life ot 15-20mins, but less specific for fibrin bound plasminogen • Tenecteplase • Genetically engineered mutant form of alteplase • Higher fibrin selectivity and longer half life- 2hours. • Singl bolus dose 0.5mg/kg suffiecient • Very expensive
  • 10. USES OF FIBRINOLYTICS • Acute myocardial infarction • Deep vein thrombosis • Pulmonary embolism • Peripheral arterial occlusion • Ischemic stroke