Anti-Coagulant Drugs

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Anti-Coagulant Drugs

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Heparin/Enoxaparin
Lepirudin
Warfarin/Coumadin
Drotrecogin Alpha
Dabigatran Etexilate

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Fibrinolytics

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Streptokinase
Alteplase/Tenecteplase/Reteplase

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Anti-Platelet Drugs

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Aspirin
Clopidogrel
Abciximab

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Heparin/Enoxaparin

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Heparin MoA: binds to antithrombin and stimulates it to inhibit Factor IXa;
Enoxaparin MoA: selective inhibitor of Factor Xa;
Clinical Uses: venous thromboses, pulmonary embolism, unstable angina, acute MI, coronary balloon angioplasty;
Toxicity: bleeding, thrombocytopenia, osteoporosis with long treatment

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Lepirudin

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Recombinant form of leech saliva protein hirudin;
MoA: inhibits soluble thrombin and bound thrombin;
Clinical Uses: alternative to heparin in patients with heparin induced thrombocytopenia;
Toxicity: bleeding, antibody formation

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Warfarin/Coumadin

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MoA: inhibits Vit.K epoxide reductase (VKOR) which converts Vit.K epoxide into reduced Vit.K which is needed for the synthesis of Factors II, VII, IX, and X; also inhibits protein C;
RoA: oral, however does not reach CSS until 5 days!
AE: bleeding, fetal toxicity, inhibition of protein C can lead to skin and tissue necrosis

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Drotrecogin Alpha

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Recombinant form of human activated protein C (APC);
MoA: inactivates Factors Va and VIIIa, also interrupts the amplification cycle of inflammation and suppresses TNF-alpha, IL-6, and IL-1B production;
Clinical Uses: anti-coagulant, anti-inflammatory effects, septic shock;
AE: bleeding

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Dabigatran Etexilate

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MoA: competitive direct inhibitor of thrombin, preventing the thrombin-mediated conversion of fibrinogen to fibrin;
RoA: oral; fast OoA = 2 hours vs. Warfarin (OoA = 5 days!!);
Clinical Uses: prevention of stroke in patients with atrial fibrillation;
AE: bleeding

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Alteplase

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aka: Tenecteplase, Reteplase;
Human recombinant tissue plasminogen activators;
MoA: converts plasminogen into plasmin, preferentially activates plasminogen bound to fibrin;
RoA: IV;
Clinical Uses: MI (w/in 3 hours of onset), pulmonary thromboembolism, ischemic stroke;
AE: hemorrhage;
CI: any active internal bleeding or hemorrhagic crisis, cerebral vascular lesions, closed head trauma or facial trauma within 3 months, acute pericarditis, recent surgery

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Clopidogrel

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MoA: irreversibly blocks ADP receptors downregulating GP2b/3a receptors so fibrinogen cannot bind them on the platelet surface;
Clinical Uses: prevention of TIAs and ischemic strokes, used in patients with coronary artery stents;
AE: rash, diarrhea, low frequency of GI upsets or bleeding

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Abciximab

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Humanized monoclonal antibody;
MoA: non-competitively binds to GP2b/3a, inhibiting fibrinogen from binding to them;
Clinical uses: coronary stenting procedures, unstable angina