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31 Cards in this Set
- Front
- Back
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What are the 3 major drugs that prevent blood coagulation?
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1. Anticoagulants
2. Platelet inhibitors 3. Thrombolytic agents |
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What are anticoagulants?
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-any drug that affects coagulation cascade
-fibrin soluble--> fibrin insoluble -must have Ca++ present/available for the coagulation cascade to work |
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What are 4 various drug targets of platelet inhibitors?
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1. cAMP
2. Thromboxane A2 3. ADP 4. GpIIb/IIIa |
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What is the difference between thrombin and plasmin?
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1. Thrombin--> makes the clot (converts fibrinogen to fibrin)
2. Plasmin breaks the clot (activated from plasminogen by tPa) |
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What is Prothrombin Time?
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-Tests the Extrinsic + Common path (Factors II, V, VII* + I, II, V, X)
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What is INR?
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-International Normalized Ratio
-Pt's PT: normal PT -warfarin levels measured using this |
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Partial Thromboplastin Time (PTT)
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-Tests the Intrinsic + Common Path (Factors VIII, IX, XI, XIII + I, II, V, X)
-Heparin levels measured using this |
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****Why is antithrombin III so important?
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-need antithrombin III to neutralize activated coagulation factors to their inactive forms
-Factors II, IX, X, XI, XII |
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Heparin
Type of drug and MOA* |
-anticoagulant
-glycosaminoglycan (GAG) -large w/ high molecular weight, looks like starch *Activates antithrombin III (1000 fold) |
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Heparin
General information |
-injected (not absorbed in GI tract)
-safe in pregos -Heparin toxicity: bleeding, thrombocytopenia, abnormal LFTs, unpredictable coagulation |
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What is used in the reversal of heparin action?
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-IV Protamine Sulfate (+ charged)
-forms complex w/ (-) charged heparin -Protamine is also used w/ insulin to increase the action of insulin, comes from salmon sperm |
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Lepirudin (Refludan)
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-anticoag from leeches which secrete Hirudin
-blocks thrombogenic activity of thrombin -1st drug approved for anticoag in pts w/ HIT (Heparin Induced Thrombocytopenia) |
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Argatroban (Acova)
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-Anticoagulant, thrombin inhibitor
-used in patients w/ HIT -substitute for heparin esp in pts w/ renal disease b/c liver eliminates it |
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Bivalirudin (Angiomax)
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-anticoagulant ( Hirudin analog)
-thrombin inhibitor -also used in unstable angina and to prevent myocardial infarction or in pts w/ history of HIT |
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What are the 4 drugs that are classified as Low Molecular Wt Heparin (LMWH)?
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1. Enoxaparin (Lovenox)
2. Dalteparin (Fragmin) 3. Tinzaparin (innohep) 4. Fondaparinux (Arixtra) |
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What is the MOA of LMWHs and general information?
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-Inhibit factor X but much less effect on antithrombin III
-prevent DVT -more predictable coagulation that high molecular weight heparin -given paraenterally |
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Antithrombin III (thrombate III, Atnativ)
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-anticoagulant, protease inhibitor, cofactor for heparin
-inhibits thrombin and factors IXa, Xa, Xia, XIIa and plasmin -for pts w/ antithrombin III deficiency |
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Dabigatran (Pradaxa)
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-platelet inhibitor, direct thrombin inhibitor
-***only available in Europe but may become the future replacement of heparin -given orally |
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Warfarin (Coumadin)
Type of Drug and MOA |
-anticoagulant
-inhibits Vit K Epoxide Reductase (blocks the Ca++ dependent oxidation/reduction coupling) thereby inhibiting Vit K dependent factors (II,VII, IX, X) |
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Warfarin (Coumadin)
General information |
-given orally
-takes time to achieve desired anticoagulation -measure levels using PTT -has specific drug interactions (not on test) |
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***How do your reverse Warfarin action?
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1. Vit K (slow)
2. Fresh Frozen Plasma (Rapid) *Drug is absolutely contraindicated in pregos (teratogen) |
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Aspirin
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-platelet inhib, irreversibly inhibits COX so no TxA2 produced
-81 mg most common anticoag -SEs: hem stroke (if BP not controlled) -Cinchonism (tinnitus, blurred vision, dizziness) |
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Ticlopidine (Ticlid)
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-platelet inhibitor
-ADP inhib (blocks binding of platelets to fibrinogen and binding of platelets to each other -can cause neutropenia |
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Clopidogrel (Plavix)
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-platelet inhibitor
-ADP inhibitor -2nd MC anticoag and has GI SEs -for Acute Coronary Syndrome, pts who have had strokes, MI, etc |
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Prasugrel (Effient)
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-Platelet inhitor
-ADP inhibitor -reduces thrombotic CV events -newer than Clopidogrel and works faster, but has higher SE of bleeding |
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Dipyridamole
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-Platelet inhib
-increases cAMP in platelets thus inhibiting TXA2 synthesis -used in angina (coronary vasodilation) and prevents embolization from prosthetic heart valves |
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Abciximab (Reopro)
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-platelet inhib, chimmonoclonal Ab
-MOA: monoclonal Ab against GpIIb/IIIa receptor which inhibs fibrin binding to the receptors -angioplasty/artherectomy to decrease risk of MI |
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Cilostazol (Pletal)
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-platelet inhib
-inhibits platelet aggregation |
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Streptokinas (Kabikinase, Streptase)
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-thrombolytic agent for B-hemolytic streptococci
-indirectly activates plasminogen (but NOT AN ENZYME* and doesn't have phosphorylation activity) -MIs, pulm embolism, and stroke |
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Anistreplase (APSAC, Eminase)
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-Thrombolytic agent that is streptokinase + recombinatn human plasminogen
-used in MIs, PEs, strokes |
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Tenecteplase (TNK-tPA, TNKase)
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-Thrombolytic agent, modified human tPa
-binds fibrin and converts plasminogen to plasmin -use as IV bolus to treat acute MI |
