mechanism of action Names method of delivery therapeutic levels achieved ** Unfractionated Heparin Heparin Delivery: IV 24-48 hours Mechanism of action: Dose: Bolus 80 units/kg followed inactivates thrombin and by infusion of 18 activated factor X (factor Xa) units/kg/hr by binding to antithrombin through a high-affinity pentasaccharide. Low Molecular Weight Lovenox Delivery: 3-5 hours Heparins (enoxaparin) Subcutaneous injections Mechanism of action: binds Fragmin to antithrombin which is Prophylactic dose: Enoxaparin mediated by a unique 30-40 mg q 12-24 (ext release) pentasaccharide hr Innnohep sequence which causes a Therapeutic dose: (tinzaparin change in antithrombin and sodium) 1-1.5 mg/kg q inactivates factor Xa hr Others? Fondaparinux (synthetic Arixtra Delivery: 2-3 hours drug) subcutaneous injections Mechanism of action: Prophylactic Dose provides antithrombotic 2.5 mg/day activity via selectively binding to antithrombin III Therapeutic Dose: (ATIII) which in turn results 5-10 mg/day in inhibition of Factor Xa (based on weight) Vitamin K antagonists Coumadin Delivery: oral Used with (warfarin) LMWH or UFH Mechanism of action: Dosing: inhibiting the synthesis of individualized INR 2-3 vitamin K-dependent clotting based upon factors, especially the C1 individual’s INR subunit of vitamin K epoxide response to drug reductase (VKORC1) enzyme
mechanism of action Names method of delivery therapeutic levels achieved ** Unfractionated Heparin Mechanism of action: inactivates thrombin and activated factor X (factor Xa) by binding to antithrombin through a high-affinity pentasaccharide. Heparin Delivery: IV Dose: Bolus 80 units/kg followed by infusion of 18 units/kg/hr 24-48 hours Low Molecular Weight Heparins Mechanism of action: binds to antithrombin which is mediated by a unique pentasaccharide sequence which causes a change in antithrombin and inactivates factor Xa Lovenox (enoxaparin) Fragmin Enoxaparin (ext release) Innnohep (tinzaparin sodium) Others? Delivery: Subcutaneous injections Prophylactic dose: 30-40 mg q 12-24 hr Therapeutic dose: 1-1.5 mg/kg q hr 3-5 hours Fondaparinux (synthetic drug) Mechanism of action: provides antithrombotic activity via selectively binding to antithrombin III (ATIII) which in turn results in inhibition of Factor Xa Arixtra Delivery: subcutaneous injections Prophylactic Dose 2.5 mg/day Therapeutic Dose: 5-10 mg/day (based on weight) 2-3 hours Vitamin K antagonists Mechanism of action: inhibiting the synthesis of vitamin K-dependent clotting factors, especially the C1 subunit of vitamin K epoxide reductase (VKORC1) enzyme Coumadin (warfarin) Delivery: oral Dosing: individualized based upon individual’s INR response to drug Used with LMWH or UFH INR 2-3