Antiplatelet, Anticoagulant, Thrombolytics Flashcards
aspirin
acetylsalicylate
Irreversibly binds COX
Anti-platelet
Clopidogrel
Ticlopidine
Prasugrel
Irreversible ADP receptor antagonist
Anti-platelet
*ADP released from ACTIVATED platelet
Abciximab
Eptifibatide
Tirofiban
Inhibits GPIIb-IIIa receptor for fibrinogen and vWF
Anti-platelet
*GPIIb-IIIa expressed on ACTIVATED platelets
Dipryridamole
Anti-platelet
Inhibits phosphodiesterase, increases cAMP, inhibits platelet activation
Unfractionated heparin
LMW heparin
Fondaparinux
Parenteral anti-coagulant
Indirect thrombin inhibitors
Inhibits thrombin and Xa
Fondaparinux
Xa inhibitor
Indirect thrombin inhibitors
Bivalirudin
Argatroban
Dabigatran etexilate
Direct thrombin inhibitor
Protamine
Reverses heparin effect
Warfarin
Oral
Anti-coagulant
Inhibits VKOR
Vitamin K
Oral: Phytonadione
Reverses warfarin effect (overcomes VKOR deficiency)
Rivaroxaban
Apixaban
Edoxaban
Oral
Xa Inhibitors
Phytonadione
Vitamin K
Coagulants
Streptokinase
Urokinase
tPAs
Fibrinolytic
Make plasmin to bust clot
alteplase
reteplase
tenecteplase
tPAs
activate fibrin-bound plasminogen to plasmin
STROKE TX
fibrinogen –> fibrin via…
thrombin (IIa)
prothrombin (II) –> thrombin (IIa) via…
Xa
X –> Xa via…
Intrinsic and extrinsic pathways
Size fibrinogen and fibrin
fibrinogen: small
fibrin: big
Antithrombin inactivates…
thrombin and factor Xa
==> can’t make fibrin
Antidote effect on heparin vs. fondaparinux
heparin: complete
fondaparinux: none
aPTT measures which coagulation pathway?
intrinsic
PT measures which coagulation pathway?
extrinsic
= INR
measures fibrinogen, prothrombin, V, VII, and X
Direct thrombin inhibitors, think…
leeches
lepirudin: binds DIRECTLY to thrombin and inhibits the enzyme
Dabigatran etexylate
ORAL
new
binds DIRECTLY to thrombin
Vitamin K dependent clotting factors
II, VII, IX, X, protein C
VKOR
vitamin K dependent epoxide reductase
Warfarin pharmacokinetics
delayed hypothrombic effect
narrow therapeutic index
Which enantiomer more active in warfarin
S enantiomer
pharmacodynamics vs. pharmacokinetics
dynamics: VKORC1 polymorphisms
kinetics: ADME (CYP2C9 affects metabolism, 30% slow metabolizers)
tPAs specific to clot because…
bind to fibrin-bound plasminogen
= dissolve EXISTING life-threatening thrombi
used in strokes
