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64 Cards in this Set
- Front
- Back
drugs that inhibit the synthesis of coagulation factors
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1) warfarin
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drugs that indirectly inactivate coagulation factors
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1) unfractionated and low molecular weight heparin
--UFH --Fondaparinux --Enoxaparin --dalteparin |
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drugs that directly inactivate coagulation factors
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1) Bivalirudin
2) Hirudin 3) Kepirudin |
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antiplatelet drugs
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1) Aspirin
2) NSAID's 3) clopidogrel 4) ticlopidine 5) abciximab 6) tirofiban 7) eptifibitide |
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Fibrinolytic drugs
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1) Alteplase
2) reteplase 3) tenecteplase 4) streptokinase 5) urokinase |
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____________inhibits plasminogen activation
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aminocaproic acid
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___________antagonizes heparin
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protamine sulfate
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normal hemostasis
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Injury to blood vessel --> vasospasm --> platelet aggregation --> coagulation --> fibrin clot formation --> healing --> fibrinolysis
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thrombin converts ___________--> __________
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fibrinogen --> fibrin
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fibrinolysis
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plasminogen --> plasmin
---plasmin converts fibrin --> split products --plasmin also converts fibrinogen --> degredation products |
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3 major factors released by platelets
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1) TXA2
2) ADP 3) 5-HT |
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____is the GP that connects plalets tgether in platelet aggregation
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GP IIb/IIIa
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Xa converts _________-->_________
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prothrombin --> thrombin
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major thrombotic disorders
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1) acute coronary syndrome
----unstable angina ----MI 2) stroke 3) DVT |
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warfarin blocks _________
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Vit K reductase
--therefore prevents carboxylation of clotting factors |
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adverse effects of warfarin
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1) hemorage
2) fetal abnormalities --fetal warfarin syndrome --chondrodysplasia punctata |
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Drug interactions of warfarin
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1) anything that inhibits or induces p450
2) anything that has a direct effect on coagulation |
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what drugs interact with warfarin by increasing PT (longer to clot)
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1) cimetidine (histimine Rc antagonist ; ulcers)
2) Aspirin (High doses) 3) cephalosporins (antibacterial, pneumonia) 4) Heparin 5) Hepatic disease |
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what drugs interact with warfarin by decreasing PT
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1) barbituates (CNS depressant)
2) Rifampin (antibiotics, Tb, Meningitis) 3) Diuretics 4) Vit K 5) Hereditary resistance |
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clinical uses of warfarin
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1) DVT
2) A-fib 3) artificial heart valves 4) stroke prevention 5) MI prevention |
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tx of bleeding caused by warfarin
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1) reduce dosage of warfarin
2) administer vit K1 (phytonadione) to accelerate the recovery of clotting factors 3) give FFP or Factor IC concentrate |
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ROA for warfarin
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Oral
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onset of action of warfarin
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delayed onset
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warfarin inhibits _________
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Vit K reductase
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warfarin inhibits synthesis of which factors
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1) vit K dependant factors
--II --VII --IX --X |
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warfarin is monitored with______
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PT
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is warfarin used in pregnancy?
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No
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the Heparin family are _______thrombin inhibitors
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indirect
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Unfractionated heparin (UFH)
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1) contains high and low molecular weight fractions
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Low molecular weight heparins (LMWH)
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less effective than the HMW of the UFH but more bioavalability
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2 LMH
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Enoxaparin
Dalteparin |
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__________is a synthetic pentasaccaride for heparin
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fondaparinux
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heparin is a naturally occurring mixture of sulfated mucopolysaccarides that binds to _________when administered?
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Antithrombin III
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MOA of heparin
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1) heparin binds and activates antithrombin III
2) antithrombin III inactivates clotting factors (thrombin, Xa, and others) 3) this has a more imediate anticoagulatn effect than warfarin |
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antithrombin III is a
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endogenous protease anticoagulant
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heparin site of action
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intrinsic pathway and common pathway (Xa)
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Factors inhibited by warfarin
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VII
IX X Prothrombin |
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most important factors inhibited by warfarin
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X
prothrombin |
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factors inhibited by heparin
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XIIa
Xa IXa VIIa Xa Thrombin |
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Most important factors inhibited by heparin
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Xa
thrombin |
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3 key characteristics of heparin
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1) it is a sulfated polysaccaride
2) it potentiates antithrombin III 3) it inactivates activated clotting factors |
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Heparin Pharmicokinetics
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1) it is not absorbed from the gut
2) administered as an IV infusion or subcutaneous injection |
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clinical use of heparin
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acute thromboembolism
--venous thrombosis --pulmonary and other emboli --DIC 2) cardiovascular surgery 3) a-fib 4) renal dialysis 5) blood transfusion 6) blood sampling |
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adverse effectsof heparin
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1) hemorrage (elderly woman with renal failure)
2) thrombocytopenia (25% mild, ?5% severe) 3) hyperkalemia (decrease aldosterone) 4) osteoporosis (chronic administration) |
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tx of bleeding caused by heparin
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1) discontinue heparin
2) give protamine sulfate 3) give FFP for severe bleeding |
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clinical uses of the direct thrombin inhibitars
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1) acute coronary syndrome
2) heparin nduced thrombocytopenia (particularly lepirudin) |
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process of platelet hemostasis
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adhesion of platelets to collagen and endothelium --> platelet activation (synthesis and release of mediators) --> platelet agregation (fibrinogen forms between GPIIb/IIIa sites on the platelets --> formation of platelet plug
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drugs that inhibit thromboxane synthesis
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Aspirin
NSAID's |
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antiplatelet Drugs that block ADP receptors
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clopidogrel
ticlopidine |
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antiplatelet drugs that block GPIIa/IIIb Rc
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1) abiximab
2) Tirofiban 3) Eptifibitide |
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MOA of aspirin
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inhibits COX --> decrease in TXA2 synthesis --> prevents platelet agregation
--has less of an effect on prostoglandin synthesis |
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clinical indications for aspirin
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1) unstable angina
2) TIA and stroke prevention 3) AMI |
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ticlopidine and clopidogrel
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1) block ADP Rc --> reduces expression of GP receptor --> inhibits platelet aggregation
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MOA of abciximab
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MAB to the GP receptor (blocking it)
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MOA of tirofiban
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it has an analog sequence within fibrinogen (occupying the GP receptor)
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MOA of eptifibatide
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it has an analog sequence within fibrinogen (occupying the GP receptor)
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fibrinolytic drugs catalyze the formation of _________
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plasmin
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which fibrinolytic drugs are tissue fibrinogen activators?
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alteplase
reteplase tenecteplase |
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2 fibrinolytic drugs that are not tissue plasminogen activators
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streptokinase
urokinase |
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clinical uses of fibrinolytic drugs
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1) AMI
2) ischemic (thrombotic) stroke) 3) PE |
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contraindications to fibrinolytic drugs
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1) active bleeding
2) hemoragic stroke 3) severe HTN 4) intracranial surgery / trauma, anurysm, tumor |
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drugs used to tx bleeding caused by fibrinolytic drugs
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1) aminocaproic acid (inhibits plasminogen activation)
2) protamine sulfate (antagonizes heparin) 3) Vit K |
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warfarin has a simular structure to_______
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vit K
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warfarin prevents _________
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1) carboxylation of clotting factors...therefore preventing the formation of prothrombin
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