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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 |