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antithrombotic
UVa med pharmacology block 4
| Question | Answer |
|---|---|
| How is warfarin administered? How is it excreted? What are its side effects / CIs? | oral met by cy p450 bleeding and teratogenic rare skin nerosis OD: tx w/ vit K CI:pregnancy |
| How are clots dissolved naturally? | leukocytes infiltrate and aggregated platelets swell/disintegate, leaving oly fibrin eventually fibrin digested by fibrinolytics released from endothelial cells and leukyes |
| What is virchow's triad? | injury to vessel altered blood flow abnormal coagulability of hte blood |
| What makes up a white thrombus? | platelet aggregates and fibrinogen |
| What drugs are used for arterial disease management? What types are there? | those that inhibit platelet activation and aggregation -antiplatelet -anticoagulant -fibrinolytics |
| What happens in secondary hemostasis? | coagulation cascade occurs over white thrombus, making fibrin network blood cells get trapped in mesh (red thrombus) seen in veins |
| What drugs are used against venous disease? | drugs that inhibit thrombin and fibrin |
| What happens in primary hemostasis? | damage to endothelium exposes basement proteins platelets stick via GPs platelets activated - release ADP and 5HT, synthesize TXA2 Platelet activation = conformation change of GP IIb/IIIa GP IIb/IIIa binds fibrinogen fibrinogen binds other platlets |
| What are the physiologogical regulatory mechanisms against coagulation? | 1 - inhibit platelet aggregation by increasing cAMP (via PGI2) 2 - inhibit clottingenzymes by plasma protesase inhibitors 3 - fibrinolysis or clot busting by plasmin. (mediated by t-PA) |
| What are the general types of treatment against coagulation? | prevention - stop blood from clotting after MI, AF, or angioplasty treatment - dissolve clots replacement - help clotting (for genetic dosrders) |
| What is the mechanism of Eptifibatide? | Anti-platelet - synthetic cyclic heptapeptide wKGD sequence specifically blocks GPIIb/IIIa receptors |
| What is mechanism of Lepirudin? When is it used? | Direct thrombin inhibitor -synthetic of hirudin (from leeches) acts independently of ATIII -can be used in patients with heparin induced thrombocytopenia (HIT) |
| What is mechanism of Bivalirudin? Who gets to use it and why is it restricted? | Direct thrombin inhibitor - 20 aa peptide analog of hirudin -anticoag in patients w/unstable angina undergoing angioplasty -EXPENSIVE - use restricted to px's w/HIT |
| What is mechanism of Argatroban? | Direct thrombin inhibitor - tripeptide directly inhibits free and fibrin bound thrombin -used in PX's with or at risk for HIT |
| What is mechanism of Unfractionated heparin? | Anti-coagulant - binds with ATIII and stimulates its anti-protease activity -used to prevent and treat DVT/PE, prevent thrombosis after MI, for px's w/unstable angina, and as coating for coronary stents |
| When is Unfractionated heparin CI'd? | CI'd in px's who are hypersensitive, actively bleeding, hemophiliacs, thrombocytopenia, severe hypertension, infective endocarditis, active TB, GI ulcers, visceral carcinomas, advanced hepatic/renal disease, or compromised BBB |
| What is mechanism of low molecular weight heparin? | anti-coagulant - inhibits factor Xa - used to prevent DVT/PE |
| What is the difference between unfractionated and low molecular weight heparin? | LMWH is derived by enzymatic or chemical cleavage of UFH - LMWH has less activity than UFH but superior bioavailability, less nonspecific binding, dosing based on weight w/out lab monitoring, and less HIT |
| What is the mechanism of Warfarin? | Anti-coagulant - Blocks Vitamin K cycle preventing gamma-carboxylation of II, VII, IX, and X and protein C -chronic treatment to prevent venous thromboembolism, DVT, systemic arterial embolism in px's w/Afib or prosthetic heart valve, and MI |
| How do you treat Warfarin OD? | If emergency use Fresh frozen plasma Not an emergency hold warfarin and adminster Vit K |
| To what group is Warfarin CI'd? | Pregnant patients - can cross placenta causing hemorrhagic disorder and birth defects |
| What is the mechanism of streptokinase? | Fibrinolytic - complexes with plasminogen causing auto-catalytic conversion to plasmin, drives px into lytic state -px's w/ABs against strep require loading dose |
| What is mechanism of Alteplase? | Fibrinolytic - recombinant tPA - trypsin like serine preotease that cuts plasminogen into plasmin clot buster in DVT, PE, MI, stroke, and for clearing central venous access devices |
| What is mechanism of Retaplase? | Fibrinolytic - recombinant, nonglycosylate, human tPA w/lower fibrin binding affinity than alteplase but longer T1/2 -specific for coronary thrombi |
| What is mechanism of Tenecteplase | Fibrinolytic - mutated recombinant human tPA more resistant to PAI-1 (plasminogen activato inhibitor) than alteplase - prolonged T1/2 and 14 fold greater specificity for fibrin than WT tPA -used for acute MI |
Created by:
sam.mrosenfeld
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