Anticoagulants Flashcards
HEPARIN
Idirectly Inibits: Factor IX, X, XI, and XII, and thrombin (II) via Antithrombin III
Only dad can trap the Thrombeaver
Monitor PTT
Toxicity:
Heparin Induced Thrombocytopenia (HIT) — antibodies directed against Platelet Factor 4 (PF4)
Hypoaldosteronism - Potassium retention (Think same as spironolactone)
LMWH
Inhibitor of Factor IX & X only
End with -parin
Longer half life
Can still cause HIT, but less likely
PROTAMINE SULFATE
Low molecular weight positively charged protein that can directly inhibit Heparin.
Less effective for LMWH and Fondaparinux
FONDAPARINUX
Antithrombin III activator — synthetic, very low molecular weight heparin derivative
Only inhibits Factor X
Will not cause HIT
Not sensitive to Protamine Sulfate
HIRUDIN and LEPIRUDIN
HIRUDIN — naturally occurring (salivary gland of leech)
LEPIRUDIN — recombinant derivative of hirudin
Both bind and directly inhibit thrombin
Treat HIT
BIVALIRUDIN
Synthetic, derived form of hirudin
Also binds and directly inhibits thrombin
Coronary angioplasty - as a substitute for heparin
ARGATROBAN
Synthetic L-arginine analogue
Competitively inhibits thrombin
Treat HIT
RIVAROXABAN (Xarelto)
Xa Inhibitor
APIXABAN (Elaquis)
Xa Inhibitor
Treat Venous Thrombosis
Fixed oral doses with no need for monitoring
Long term anticogulant prophylaxis —> Such as in A. Fib
STREPTOKINASE
Nonenzymatic protein derived from Streptococci, binds to plasminogen and induces conformation changes that expose the active site.
Promote clot lysis
Can cause allergic reaction
UROKINASE
Serine protease enzyme that activates plasminogen directly
Derived from human fetal kidney cells via recombinant technology
ALTAPLASE
RETEPLASE
TENECTEPLASE
Tissue-type Plasminogen Activator (t-PA) - endogenous, with a high binding affinity for fibrin; can produce clot-selective plasminogen activation.
Reteplase and Tenectplase have longer half-lives
Alteplase - catheter coagulation
AMINOCAPROIC ACID
Inhibits plasmin-fibrin interaction
Will reverse fibrinolysis drugs - tPA, Streptokinase, Urokinase
TRANSEXAMIC ACID
Reverses tPA
WARFARIN
Blocks action of EPOXIDE REDUCTASE (VKOR) trapping Vitamin K in its inactive form
No gamma carboxylation
Affects 2, 9, 7, 10, C/S
Monitor PT
LONG Half Life
8-12 hour delay - must start with a more acute anticoagulant then switch to Warfarin
Metabolized by CYP450
Teratogenic - use heparin instead
High Dose Vitamin K
Reverse Warfarin therapy
Protein C Deficiency
Warfarin Skin Induced Necrosis — from early hypercoagulable state
Heparin must be used in addition to prevent this
DIPYRAMIDOL, CILOSTAZOL
PDE Inhibitors
Increase cAMP
Dipyridamole + Warfarin
Prosthetic Heart Valves
Dipyridamole + Aspirin
Prior Stroke
ABCIXIMAB
GpIIb-IIIa Inhibitor
Monoclonal antibody used in angioplasty, often with aspirin and heparin
EPTIFIBATIDE
GpIIb-IIIa Inhibitor
Cyclic peptide inhibitor that binds to RGD motifs on alpha2beta3 integrins
Also used for angioplasty
TIROFIBAN
GpIIb-IIIa Inhibitor
Non-peptide small molecule inhibitor of alpha2beta3 integrin
TICLOPIDINE
Block ADP receptor P2Y12
Increased cAMP blocks expression of GPIIb-IIIa on cell surface
Can cause Neutropenia and Graulocytopenia
CLOPIDOGREL (Plavix)
Block ADP receptor P2Y12
Increased cAMP blocks expression of GPIIb-IIIa on cell surface
PLASOGREL
Block ADP receptor P2Y12
Increased cAMP blocks expression of GPIIb-IIIa on cell surface
Clopidogrel + Aspirin
Angioplasty
ASPIRIN
Irreversible COX Inhibitor
Decreases levels of TXA2 and PGI2
TXA2 - normally causes vasoconstriction
PGI2 - levels will recover on endothelial cells
Allergic Symptoms — From synthesis of leukotrienes. Use an ADP Blocker instead
