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Antithrombotic Pharm
pharmacology
| Question | Answer |
|---|---|
| primary hemostasis | platelet plug formation |
| secondary hemostasis | fibrin formation |
| drugs that infere with thrombus formation | antithrombotics |
| drugs that promote degradatio of existing thrombi | thrombolytics/fibrinolytics |
| thrombi that form in arteries | white thrombi |
| thrombi w/more platelets and less fibrin | white thrombi |
| thrombi that form in veins | red thrombi |
| thrombi w/more fibrin and less platelets | red thrombi |
| types of antithrombotic drugs | antiplatelets and anticoagulants |
| drugs that interfere w/platelet plug formation | antiplatelets |
| test(s) used to measure antiplatelet effectiveness | bleeding time |
| drugs that interfere w/fibrin formation | anticoagulants |
| test(s) used to measure anticoagulant effectiveness | PT, INR, and PTT |
| site of von Willebrand factor binding | glycoprotein Ib receptors |
| 1st step of platelet plug formation | platelet adhesion |
| 2nd step of platelet plug formation | platelet activation/secretion |
| 3rd step of platelet plug formation | platelet aggregation |
| needed to anchor platelets to BV wall | von Willebrand factor |
| 5HT, ADP, and PDGR are secreted via | platelet cytoplasmic granules |
| TXA2 is secreted via | de novo synthesis/secretion |
| undergoes conformation change during platelet activation | glycoprotein IIb/IIIa receptors |
| platelet activation allows this to bind | fibrinogen molecules |
| instrinc and extrinsic pathways converge here | factor X |
| measures integrity of extrinsic and common pathways | PT |
| measures integrity of intrinsic and common pathways | PTT |
| usually ordered w/PT | INR |
| test(s) ordered to check warfarin's efficacy | PT & INR |
| test(s) ordered to check unfractionated heparin's efficacy | PTT |
| test(s) ordered to check LMW heparin's efficacy | factor Xa inhibition assay |
| MOA = irreversibly acetylates COOX, inhibiting production of TXA2 | ASA |
| cardioprotective dose of ASA | 75-325 mg/day |
| avoid in pts w/asthma and nasal polyps | ASA |
| tinnitus may indicate | ASA toxicity |
| AE = GI sx, hemorrhagic strokes | ASA |
| MOA = inhibit ADP-mediated platelet activation by irreversibly binding to ADP receptors | thienopyridines |
| ticlopidine | thienopyridines |
| clopidogrel | thienopyridines |
| prasugrel | thienopyridines |
| AE = dyspepsia, diarrhea, neutropenia | thienopyridines |
| AE = thombotic thrombocytopenic purpura, severe neutropenia | ticlopidine |
| dosing = twice daily | ticlopidine, ticagrelor |
| used w/ASA following coronary stenting and for acute corony syndromes | clopidogrel |
| dosing = once daily | clopidogrel |
| metabolized by CYP-2C19 | clopidogrel |
| 30% are "poor responders" | clopidogrel |
| used w/ASA following PCI | prasugrel |
| CI= elderly, TIA/CVA hx, small frame | prasugrel |
| MOA = reversibly binds to platelet ADP receptors | ticagrelor |
| used w/ASA for acute coronary syndromes | ticagrelor |
| most effective antiplatelet drugs | GP IIb/IIIa inhibitors |
| MOA = prevent fibrinogen-mediated platelet aggregation | GP IIb/IIIa inhibitors |
| MOA = monoclonal AB against GPIIb/IIIa receptors | abciximab |
| MOA = peptide antagonist | eptifibatide |
| MOA = nonpeptide antagonist | tirofiban |
| MOA = inc cAMP in platelets, decreasing cystolic Ca++ and inhibiting platelet aggregation | dipyridamole |
| AE = thrombocytopenia | abciximab |
| not usually given alone, but may enhance effect of other antithrombotics | dipyridamole |
| needs at least 18 saccharide residues to produce effect | heparin |
| selectively inhibits factor Xa | LMW heparin |
| has equal inhibitory activity against factor Xa and thrombin | UF heparin |
| AE = bleeding, thrombocytopenia, osteoporosis, skin necrosis, alopecia, hypoaldosteronism | heparin |
| lower incidence of heparin-induced thrombocytopenia | LMW heparin |
| given when severe bleeding complications occur w/heparin | protamine sulfate |
| most common type of HIT | non-immune mediated |
| life-and-limb threatening thrombosis can occur with this | immune-mediated HIT |
| IgG + heparin + PF4 = | platelet activation/aggregation |
| given when immune-mediated HIT occurs | direct thrombin inhibitors |
| MOA= inhibit thrombin activity independent of antithrombin III | direct thrombin inhibitors |
| lepirudin | direct thrombin inhibitors |
| bivalirudin | direct thrombin inhibitors |
| argatroban | direct thrombin inhibitors |
| AE = BLEEDING | direct thrombin inhibitors |
| MOA = synthetic heparin analog, bind to antithrombin III | fondaparinux |
| inhibits factor Xa without causing HIT | fondaparinux |
| dosing = subQ injection once daily | fondaparinux |
| used for DVT prophylaxis in ortho surgery, and to treat DVT/PE | fondaparinux |
| MOA = inhibits formation of reduced Vit K | warfarin |
| necessary for activation of coagulation factors II, VII, IX, and X | Vit K |
| delayed onset of anticoagulation | warfarin |
| Vit K protein w/shortest half life | Protein C |
| avoid large loading doses | warfarin |
| given to avoid transient paradoxical hypercoagulable state | warfarin and heparin together |
| AE = bleeding, teratogenic, skin necrosis | warfarin |
| associated w/protein C or S deficiency & warfarin use | skin necrosis |
| given when bleeding complications occur with warfarin | vit K or fresh frozen plasma transfusion |
| used for DVT, atrial fib, mechanical heart valve, and STEMI | warfarin |
| used for unstable angina/NSTEMI, STEMI, DVT, and PCI | UF heparin |
| used for unstable angina/NSTEMI, STEMI, and DVT | LMW heparin |
| used for PIC and HIT | direct thrombin inhibitors |
| used for chronic angina, unstable angina/NSTEMI, STEMI, and PCI | ASA |
| used for unstable angina/NSTEMI and STEMI | thienopyridines |
| used for PCI and unstable angina/NSTEMI | GP IIb/IIIa inhibitors |
| given if pt is unable to take warfarin for mechanical heart valve or a fib | UF heparin |