Anticoagulants, Antiplatelets, and Fibrinolytic Drugs Flashcards
what is the MOA of clopidogrel
ADP/P2Y12 inhibitors (antiplatelets)
inactivation of p2y12 receptors increases cAMP
what is the MOA of prasugrel
ADP/P2Y12 inhibitors (antiplatelet)
what is the MOA of ticagrelor
ADP/P2Y12 inhibitor
what is the MOA of abciximab
GP IIb/IIIa inhibitor (antiplatelet)
what is the MOA of eptifibatide
GP IIb/IIIa inhibitor (antiplatelet)
what is the MOA of tirofiban
GP IIb/IIIa inhibitor (antiplatelet)
what is the MOA of dipyridamole
phosphodiesterase inhibitor (PDE3)
when PDE3 is inhibited, the breakdown of cAMP is reduced
what is the MOA of Cilostazol
PDE3 inhibitor
what is the MOA of vorapaxar
protease-activated receptor-1 inhibitor (antiplatelet)
what is the MOA of Aspirin
Thromboxane A2 inhibitor via irreversible acetylation of COX1 receptors in platelets (antiplatelet)
what are the clinical uses of aspirin
prophylaxis in MI and stroke
what are the adverse effects of aspirin
GI upset and bleeding
which P2Y12 inhibitor is not used in the states due to life-threatening aplastic anemia
ticlopidine
does the inactivation of P2Y12 increase or decrease cAMP levels
increase, causing inhibition of platelet aggregation
what are the clinical uses of ADP/P2Y12 inhibitors
Treatment of ACS, prevention of stroke, DAPT (dual antiplatelet therapy) for drug eluted stent (usually combined with aspirin)
how does glycoprotein IIb/IIIa inhibition contribute to antiplatelet formation
it inhibits fibrinogen from binding to IIb/IIIa receptors
what is the MOA of Dipyridamole
inhibition of phosphodiesterase
what is the MOA of cilostazol
inhibition of PDE3 (phosphodiesterase 3)
what are the clinical uses of dipyridamole
thromboembolism prophylaxis, cardiac stress test for patients who can’t use the treadmill
what is the clinical use of cilostazol
treatment of intermittent claudication (PVD)
what is the clinical use of vorapaxar
thrombotic event prevention
what are some adverse effects of vorapaxar besides bleeding
depression and rash
what is the MOA of warfarin
Vit K antagonist (inhibits hepatic synthesis of vit k factors II, VII, IX, and X)
what are the adverse effects of warfarin besides bleeding
skin necrosis, purple toe syndrome, teratogenic (bone defects)
what is the anticoagulant that is teratogenic
warfarin
why is warfarin an ambulatory anticoagulant
bc it takes 2-3 days to work)
what is the MOA of skin necrosis with warfarin therapy
since protein c depends on gamma carboxylation and that’s the MOA of warfarin, it can cause a protein C deficiency ultimately leading to hypercoagulability
what is the MOA of unfractionated heparin
potentiator of antithrombin: activates the plasma antithrombin III by enhancing the serine protease activity. In turn, the antithrombin III will inactivate factors IIa, IXa, Xa, XIa, and XIIa
what is an adverse effect of heparin
heparin induced thrombocytopenia, osteoporosis
why is heparin safe during pregnancy
it doesn’t cross the placenta, unlike warfarin
What is the MOA of LMWHs: enoxaparin and dalteparin
potentiator of antithrombin via activity against factor X
what is the MOA of synthetic heparinoid, fondaparinux
selective antithrombin III Xa inhibition
why is enoxaparin contraindicated in prosthetic valves
high risk of thromboembolism
of the LMWH, which one is safer in heparin induced thrombocytopenia
fonaparinux
what is the MOA of the hirudin family of drugs
direct thrombin inhibitor
what are the clinical uses of lepirudin and bivlirudin (direct thrombin inhibitors)
prevention of thrombosis in pts with unstable angina and acute MI
what is the MOA of argatroban
synthetic direct thrombin inhibitor
what is the clinical use of argatroban
treatment of thrombosis in pts with HIT
what is the MOA of dabigatran (pradaxa)
(oral) direct thrombin inhibitor
what are the clinical uses of dabigatran
reduce the risk of stroke in prs with afib; prevent thrombotic complications of hip and knee replacement surgery
what is a unique side effect of dabigatran
gastritis like symptoms
why is dabigatran contraindicated with Pgp inducers (rifampin) and pgp inhibitors (verapamil, amiodarone and clarithromycin)
because its a substrate for P-glycoprotein (Pgp)
what is the MOA of apixaban (eliquis)
oral direct factor Xa inhibitor
what are the clinical uses of apixaban
Afib to reduce risk of stroke, prevention and treatment of venous thromboembolism
what is the MOA of rivaroxaban (xarelto)
oral direct factor Xa inhibitor
what are the clinical uses of rivaroxaban (xarelto)
DVT, blood clots and pulmonary embolism after knee replacement
what are the overarching clinical uses of anticoagulants
- thromboembolic disorders: DVT, PE, and Afib
- Unstable angina undergoing PCI
what is the antidote for heparin
protamine sulfate
what is the antidote for warfarin
Vit K1 (phytonadione)
Heparin affects PT/PTT while warfarin affects PT/PTT?
heparin: PTT (intrinsic pathway)
warfarin: PT (extrinsic pathway)
what test do you need to run every 2 weeks for patients on warfarin
INR (normal is 1.0 and warfarin patients should be around 2.0)
what is the normal PTT that you would expect to see in pts on heparin
normal is 21-35 sec, heparin pts expect 50-55
what are the overarching clinical uses of fibrinolytics (thrombolytics)
Acute MI, Acute PE, DVT, Thromboembolic stroke
what is the MOA of fibrinolytics
activate the conversion of plasminogen to plasmin –> causes lysis fibrin clot
what is the antidote or alteplase/fibrinolytics
aminocaproic acid
what are the most common 3 tPA drugs
alteplase, reteplase and tenecteplase
what antifibrinolytic drug is used to treat heavy menstrual bleeding
tranexamic acid
what are the adverse effects of tranexamic acid
thrombotic events (increased in pregnant women and obese pts)
