Anti-Coagulants Flashcards
Aspirin
MOA: irreversible (covalent) COX-2 inhibitor
Effect: 👇🏽TXA2 synthesis = inhibition of platelet aggregation (prolongs bleeding time)
Use: prophylaxis for transient CVA, reduce risk of recurrent MI, decreases mortality in post-MI pt
Clopidogrel
MOA: inhibition of P2Y12 (ADP receptor)
Effect:
Metabolism: prodrug activated by CYP2C19
Use: reduce rate of CVA, MI and death in pt w/ recent MI/CVA
SE: fewer bad things so its preferred
*Omeprazole (inhibits CYP2C19) will reduce plasma levels of the active metabolite
Ticlopidine
P2Y12 inhibitor
SE: more bad things happen with this so you use Clopidogrel instead
Dipyridamole
MOA: phosphodiesterase inhibitor
Effect: 👆🏽cAMP, coronary vasodilator
Use: prophylactically to tx angina pectoris but has little effect alone so used as adjunct w/ Warfarin or Aspirin
Abciximab
Monoclonal Ab directed against GPIIb/IIIa receptor
Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)
Eptifibatide
Cyclic peptide, reversible antagonist of GPIIb/IIIa receptor
Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)
Tirofiban
Nonpeptide reversible antagonist of GPIIb/IIIa receptor
Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)
Unfractionated Heparin (UFH)
Higher molecular weight than LMWH
MOA: inhibits thrombin and factor Xa
Enoxaparin / Dalteparin / Tinzaparin
LMWHs (low molecular weight heparins)
MOA: inhibition of factor Xa (little effect on thrombin)
Compared to UFH: higher bioavailability, longer t1/2, less frequent dosing requirements
Fondaparinux
Synthetic pentasaccharide
MOA: specific inhibitor of Xa
Use: prevention and tx of DVT
Lepirudin
IV Direct thrombin inhibitor
MOA: inactivates fibrin-bound thrombin in a thrombus
Labs: monitored by aPTT
Use: HIT
Bivalirudin
IV DTI (synthetic)
Lab: monitored by aPTT
Use: pt’s undergoing PCI
Argatroban
IV DTI (small)
Labs: monitored by aPTT
Use: pt’s undergoing PCI
Dabigatran Etexilate
Oral DTI
MOA: prodrug is converted to active metabolite
Use: prevent thromboembolic stroke in pt w/ a-fib, prevent and tx of DVT and PE
Apixaban / Rivatoxaban
Oral direct factor Xa inhibitors
Use: prevention and tx of DVT and PE
Warfarin
MOA: inhibits vitamin K epoxide reductase
Effect: decrease of clotting factor 2, 7, 9, 10, anticlotting proteins C and S
Labs: monitor with PT aka INR
Use: prevent/tx DVT and PE following initial heparinization and prevention of thromboembolisms in A-fib pt’s
SE: bleeding, cutaneous necrosis (d/t decreased Protein C activity bc its t1/2 is super short)
CI: Category X (crosses the placenta so never give in pregnancy)
Streptokinase
Fibrinolytic/thrombolytic
Protein produced by group A and B Streptococci
Not used anymore
Urokinase
Fibrinolytic/thrombolytic
Use: lysis of PE
Alteplase
Fibrin-selective thrombolytic
(Recombinant t-Pa)
Use: management of acute MI and acute CVA
Reteplase
Fibrin-selective thrombolytic
(Modified recombinant human t-Pa)
Use: management of acute MI
Tenecteplase
Fibrin-selective thrombolytic
(Mutant form of t-Pa)
Use: management of acute MI
Aminocaproic acid
Inhibits plasminogen activation
Use: adjunct in hemophilia pt and tx bleeding from fibrinolytic therapy
Protamine Sulfate
Heparin antagonist
MOA: high in arginine so it’s cationic and it interacts with anionic heparin to form complex which stops the effect of heparin
Vitamin K
Use: prevention of vitamin K deficiency bleeding in newborns - all babies should receive vitamin K at birth via IM administration
Heparin (UFH and LMWH)
Activates antithrombin III
Effect: rapid inhibition of thrombin, IXa and Xa clotting factors
Use: DVT, PE, MI, DOC during pregnancy
SEs: bleeding, HS rxn, HIT
HIT Type II
Pathogenesis: IgG binds the Fc receptor of the PF4/heparin platelet/complex forming an IC resulting in degranulation and aggregation of platelets
ROS: thrombocytopenia and thrombosis
Tx: d/c heparin and give DTI or Fondaparinux, *give Protamine sulfate if bleeding occurs
