Term
| Heparin ( site of action and effect) |
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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 |
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Term
| Heparin (clinical application) |
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Definition
| Used in prevention of DVT’s & Pulmonary Embolism; Acute MI, Prevention of stroke in A-fib patients; Prevents initial formation of thrombi/recurrence |
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Term
| Heparin ( side effects and otehr jazz) |
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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 |
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Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin
(site of action and effect) |
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Definition
Selectively inhibits Factor 10a
Inhibits Factor 10a, which normally converts prothrombin to thrombin (2a), so no clot can be formed |
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Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin
(clinical application) |
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Definition
| Used in prevention of DVT’s & Pulmonary Embolism; Acute MI, Prevention of stroke in A-fib patients; Prevents initial formation of thrombi/recurrence |
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Term
Low Molecular Weight (LMW) Heparin: Enoxaparin, Dalteparin, Tinzaparin
(side effects extra jazz) |
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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 |
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Term
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Definition
Heparin Antagonist
Strongly basic, so will neutralize Heparin (acidic); Less effectively neutralizes LMW Heparin
Used to counteract Heparin or in a Heparin overdose |
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Term
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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 |
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Term
| Lepirudin*, Argatroban*, Hirudin,Bivalirudin |
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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 |
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Term
| Vitamin K Antagonists (in general) |
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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 |
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Term
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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 |
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Term
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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 |
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Term
| Streptokinase, Anistreplase |
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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 |
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Term
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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) |
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Term
| (t-PA): Alteplase**, Reteplase, Tenecteplase |
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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) |
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Term
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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) |
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Term
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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 |
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Term
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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 |
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Term
| Abciximab, Eptifibatide, Tirofiban |
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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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