Heparin, warfarin, direct oral anticoagulants, and antiplatelet drugs with mechanism of action, distinct from the monitoring and antidote focus of the Nursing Pharmacology anticoagulants deck.
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- What plasma protein does unfractionated heparin activate to exert its anticoagulant effect?
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Antithrombin III (antithrombin)
- Which two clotting factors does heparin-activated antithrombin III primarily inactivate?
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Thrombin (factor IIa) and factor Xa
- What is the route of administration for unfractionated heparin?
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IV or subcutaneous injection, not oral
- Heparin binds antithrombin through a unique ____ sequence, greatly accelerating antithrombin's activity.
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pentasaccharide
- Name two low molecular weight heparins.
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Enoxaparin and dalteparin
- Compared to unfractionated heparin, low molecular weight heparin preferentially inhibits which factor?
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Factor Xa, with much less effect on thrombin
- Why does LMWH have less effect on thrombin than UFH does?
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Its shorter chains are too short to bridge antithrombin to thrombin at the same time
- What is fondaparinux?
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A synthetic pentasaccharide that selectively inhibits factor Xa through antithrombin
- Does fondaparinux have any direct effect on thrombin?
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No, it is selective for factor Xa
- Warfarin's mechanism of action
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Inhibits vitamin K epoxide reductase (VKORC1)
- Warfarin's inhibition of vitamin K epoxide reductase prevents ____ of vitamin K-dependent clotting factors.
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gamma-carboxylation
- Which four clotting factors have reduced synthesis due to warfarin?
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Factors II, VII, IX, and X
- Besides clotting factors, which two natural anticoagulant proteins does warfarin also reduce?
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Protein C and protein S
- Why does warfarin have a delayed onset of anticoagulant effect after starting therapy?
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Already-circulating clotting factors must degrade according to their own half-lives first
- Why can warfarin cause a transient hypercoagulable state early in therapy?
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Protein C has a short half-life and falls before the procoagulant factors do