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Anti-thrombotics
learn this jazz
19
Medical
Professional
08/13/2010

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Term
Heparin ( site of action and effect)
Definition
Acts via Heparin-Antithrombin III Complex

Enhance the activity of the endogenous anticoagulant Antithrombin III(ATIII-made in endothelial cells) by increasing its affinity for thrombin (F2); Also inhibits Intrinsic Factors 9,10 & 11
Term
Heparin (clinical application)
Definition
Used in prevention of DVT’s & Pulmonary Embolism; Acute MI, Prevention of stroke in A-fib patients; Prevents initial formation of thrombi/recurrence
Term
Heparin ( side effects and otehr jazz)
Definition
SE: Bleeding, Thrombocytopenia, Osteoporosis, Alopecia

NB: Has lots of Sulfate molecules making it very acidic; Highly Ionized & NOT orally absorbed; Dose-dependent kinetics; MUST monitor w/ aPTT levels (Will be 1-2 times prolonged)
NB: Safest anti-coagulant to give in pregnancy b/c does not cross the placenta; Rapid onset, so can be used for immediate situations
Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin

(site of action and effect)
Definition
Selectively inhibits Factor 10a


Inhibits Factor 10a, which normally converts prothrombin to thrombin (2a), so no clot can be formed
Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin

(clinical application)
Definition
Used in prevention of DVT’s & Pulmonary Embolism; Acute MI, Prevention of stroke in A-fib patients; Prevents initial formation of thrombi/recurrence
Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin

(side effects extra jazz)
Definition
NB: Longer acting, Lab monitoring is NOT required b/c not as effective at inactivating Factor 2a, so lower risk of bleeding

SE: Lower risk of thrombocytopenia & osteoporosis
Term
Protamine Sulfate
Definition
Heparin Antagonist

Strongly basic, so will neutralize Heparin (acidic); Less effectively neutralizes LMW Heparin

Used to counteract Heparin or in a Heparin overdose
Term
Fondaparinus (Arixtra)
Definition
Direct factor Xa inhibitor

Inhibits Factor 10a and has little effect on inhibiting Factor 2a

Similar action to LMW Heparin

SE: Low risk for HIT
Term
Lepirudin*, Argatroban*, Hirudin,Bivalirudin
Definition
Direct Thrombin Inhibitor

Binds to the catalytic site of Thrombin & directly inhibits thrombin w/out involving anti-thrombin & Vitamin K

Used as an anti-coagulant in patients who developed HIT
Term
Vitamin K Antagonists (in general)
Definition
Inhibition of the synthesis of Vitamin K dependent functional clotting factors 2,7,9,10 and anticoagulant protein C

ORAL!!!

can result in paradoxical blood coagulation initially
Term
Warfarin
Definition
Competitive Vitamin K Antagonist & ↓ the functional level of clotting factors 2,7,9,10 & Anticoagulant Protein C in the liver

Tx: Patients w/clotting disorders, Atrial fibrillation (prevention of stroke), patients with a mechanical heart valve

SE: Bleeding (must monitor using PT OR INR); Skin Necrosis, Purple Toes, Alopecia, Fetal Warfarin Syndrome (Can cross the Placenta)

NB: Broad spectrum antibiotics decrease Vitamin-K synthesis & can exaggerate the anti-coagulant effects

NB: Anticoagulant effect is delayed for 3days, so may need to start on Heparin as well initially
Term
Warfarin Antidote
Definition
Vitamin K*, Mephyton, Konakion

NB: Effect takes a few hours, so Serious Hemorrhage may be stopped by fresh frozen plasma or concentrates of factors 2,7,9,10
Term
Streptokinase, Anistreplase
Definition
Converts plasminogen into plasmin so that it can catalyze the degradation of fibrin; Used for lysis of ALREADY FORMED clots to recanalize the vessel

Tx: Pulmonary Embolism, Myocardial Infarction

NB: Antigenic (could produce an allergic reaction) & Non-Fibrin Specific (so could result in bleeding
Term
Urokinase
Definition
Converts plasminogen into plasmin so that it can catalyze the degradation of fibrin (can do this directly); Used for lysis of ALREADY FORMED clots to recanalize the vessel

Tx: Pulmonary Embolism, Myocardial Infarction

NB: Non-antigenic (No allergic reaction); Non-Fibrin specific (Could result in bleeding)
Term
(t-PA): Alteplase**, Reteplase, Tenecteplase
Definition
Converts plasminogen into plasmin so that it can catalyze the degradation of fibrin; Used for lysis of ALREADY FORMED clots to recanalize the vessel

Tx: Pulmonary Embolism, Myocardial Infarction, Non-hemorrhagic stroke

NB: Non-antigenic (No allergic rxn); Fibrin Specific (Less bleeding b/c only activates Plasminogen bound to fibrin clots)
Term
Aprotinin
Definition
Inhibits plasmin & kallikrein

Tx: Fibrinolytic Overdose (Use when have excessive bleeding)

SE: The inactivation of kallikrein could result in bleeding tendencies (at higher doses)
Term
Aspirin
Definition
Irreversibly inhibits TXA2(critical for vasoconstriction & platelet aggregation) by blocking COX enzymes

Prophylactically prevents clot formation especially in patients who has had TIA’s or MI’s

SE: Gastric Bleeding
NE: Low dose spares endothelial synthesis of PGI-2 (Promotes vasodilation & inhibits platelet aggregation) & thus better anti-platelet activity
Term
Clopidogrel (Plavix)
Definition
ADP Pathway Inhibitor

Irreversibly binds to purigenic ADP receptors on platelets thus preventing platelet cross-linking

Tx: Reduces the risk of thrombotic stroke; (Use for patients with peptic ulcers & cannot take Aspirin)

NB: Does NOT cause Neutropenia & Thrombocytopenia, so it has largely replaced Ticlopidine
Term
Abciximab, Eptifibatide, Tirofiban
Definition
Bind to IIb/IIIa receptors on platelets & block the binding of fibrinogen & thus inhibit aggregation of platelets

Used in acute coronary syndrome & coronary angioplasty

SE: Bleeding
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