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Updated: Dec 10 2021

Thrombolytics

  • Overview
    • Thrombolytics catalyze the formation of endogenous plasmin from plasminogen precursor
      • plasmin is a serine protease that degrades clots (thrombi)
    • Drugs
      • tPA (alteplase)
      • streptokinase
      • urokinase
      • APSAC (anistreplase)
    • Mechanism
      • catalyze conversion of plasminogen to plasmin
        • cleaves fibrin clots
        • cleaves thrombin
      • clot-specificity
        • tPA is clot-specific
          • acts only on fibrin-bound plasminogen
        • streptokinase is not clot specific
          • depletes circulating plasminogen, factor V, factor VIII
      • ↑ PT, ↑ PTT, no change in platelet count
    • Clinical use
      • administer as early as possible following
        • ischemic stroke (tPA)
        • MI
        • DVT
        • pulmonary embolism
    • Toxicity
      • bleeding and intracerebral hemorrhage
        • contraindicated in patients with history of bleeding, surgery, hypertension
      • streptokinase may cause hypersensitivity
        • derived from β-hemolytic streptococci
    • Antagonist
      • aminocaproic acid and tranexamic acid
        • lysine analog that prevents conversion of plasminogen to plasmin
        • inhibitor of fibrinolysis
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