Term
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Definition
Anticoagulant - Indirect Thrombin Inhibitor
Binds to antithrombin and inhibits Xa and thrombin (equally); pentasaccharide sequence binds antithrombin, longer polysaccharide sequence binds thrombin
Given IV or SC; short half life
Unpredictable dosing due to binding to virtonectin, platelet factor 4 and histidine-rich GP
Antidote: protamine sulfate (basic peptide)
Monitor effectiveness with PTT
Side Effects: bleeding, HIT, osteoporosis (long term use)
Indication: to maintain patency in dialysis/bypass/venous lines, prevent thrombosis following surgery, treat arterial thrombosis (angina, MI), treat DVT, PE
Ok for pregnancy (doesn't cross placenta) |
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Term
| Low Molecular Weight Heparin |
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Definition
Anticoagulant - Indirect Thrombin Inhibitor
Inhibits Xa more than thrombin due to shorter chain
Fewer side effects and longer half life with more predictable dosing curve vs. unfractionated heparin
Monitor effect with Factor Xa assay
No HIT!
Less effective reversal with protamine sulfate |
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Term
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Definition
Anticoagulant - Indirect Thrombin Inhibitor
Synthetic pentasaccharide that binds to the active site of antithrombin
Inhibits Factor Xa (not thrombin)
Long half life (15hrs)
Can be given in HIT
Activity better than/equal to heparin but CANNOT BE REVERSED WITH AN ANTIDOTE
Side effect: bleeding |
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Term
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Definition
Anticoagulant - Direct Thrombin Inhibitor
Specific and Irreversible Thrombin Inhibitor (isolated from leeches)
Binds to catalytic site and fibrinogen binding site of thrombin - will inactivate both free and fibrinogen-bound thrombin
No antidote
Monitor with PTT
Administer parenterally
Rapid onset (and offset) of action |
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Term
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Definition
Anticoagulant - Direct Thrombin Inhibitor
Inactivates fibrinogen-bound and free thrombin
Given parenterally
No antidote
Rapid onset and offset of action
Monitor with PTT
Recombinant Hirudin (reversible inhibition) |
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Term
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Definition
Anticoagulant - Direct Thrombin Inhibitor
Inactivates both fibrinogen-bound and free thrombin
Give parenterally
Monitor with PTT
No antidote
Rapid onset/offset of action
Synthetic arginine analog
Reversibly inhibits catalytic site of thrombin |
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Term
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Definition
Anticoagulant - Oral
Only anticoagulant taken orally (and only coumarin derivative used)
Fat soluble, vitamin K antagonist: blocks Vit. K-dependent carboxylation of Factors II, VII, IX, X (also Protein C and S)
Absorbed rapidly from gut and extensively bound to plasma proteins (i.e. albumin) = displacement will increase free warfarin, and mineral oil/laxatives will reduce warfarin absorption
Increasing/decreasing vitamin K intake will impact anticoagulant activity
Monitor with PT and INR
Metabolism will be enhanced by induction of hepatic p450 (ex: by barbituates)
Inhibition of Proteins C and S: warfarin-induced skin necrosis and venous thrombosis at onset of use
Teratogen: DO NOT USE IF PREGNANT
Reversal: Cessation of therapy, PO/SC/IV vitamin K, fresh frozen plasma, recombinant factor VII, prothrombin complex concentrate |
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Term
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Definition
Fibrinolytic
Indicated in CVA, MI, DVT, PE
Bacterial protein
Forms active complex when bound to plasminogen
Activates lysis in general circulation and at clot
Risk for fibrinolytic state and bleeding |
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Term
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Definition
Fibrinolytic
Indicated in CVA, MI, DVT, PE
Serine protease
Activates plasminogen in general circulation and at clot
Risk for fibrinolytic state and bleeding |
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Term
| Tissue Plasminogen Activator (t-PA) Reteplase Tenecteplase |
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Definition
| Fibrinolytic Indicated in CVA, MI, DVT, PE Specifically activate fibrin-bound plasminogen at clot site (less systemic activation) |
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Term
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Definition
Antiplatelet
Indicated in treatment and prevention of MI, CVA and in coronary interventions
Irreversibly inhibits cyclooxygenase in platelets to prevent thromboxane A2 formation
Does not decrease PGI2 in endothelial cells at low doses (optimal)
Give low dose baby aspirin (75-100mg daily) |
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Term
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Definition
Antiplatelet
Phosphodiesterase Inhibitor - causes an increase in platelet cAMP which decreases aggregation
Given parenterally (can give with ASA)
A weaker antiplatelet effect |
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Term
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Definition
Antiplatelet
Reduces platetlet aggregation by inhibiting platelet ADP receptor
Dose-dependent antithrombotic effect: inhibits 80% of platelets within 5 hrs
Effective for up to 10 days
Effect may be reversed with a platelet transfusion
Side effects: TTP (rare), bleeding |
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Term
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Definition
Antiplatelet
Inhibits GPIIb-IIIa (fibrinogen receptor on platelets)
Monoclonal antibody
Side effect: may elicit immune response - limits repeated use |
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Term
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Definition
Antiplatelet
Fibrinogen analogs
Compete with endogenous fibrinogen and vWF for binding to GPIIb-IIIa receptor
Given parenterally
Rapid onset, short half life
Eptifibatide comes from rattlesnake venom |
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