Hematological Agents Flashcards
What does serotonin do in the blood vessels?
vasoconstriction
What is the stimulus to secrete endothelin-1?
thrombin
Upon activation, the platelets secrete what three coagulation mediators?
ADP
Serotonin
TXA2
What are the two receptors for ADP on platelets?
P2Y1 and P2Y12
P2Y12 activation increases the concentration of what intracellular ion? Decreases the concentraion of what intracellular signaling molecule?
calcium
cAMP
What is the function of factor XIII?
stabilize fibrin clots
What two molecules does thrombomodulin bind?
thrombin and Protein C
What protein binds to and activates Activated Protein C?
Protein S
The association of which two coagulation factors are inhibited by TFPI?
three and seven
What clotting factors are inhibited by Antithrombin III? Which two coagulation factors promarily?
two, seven, nine, ten, eleven, twelve
two and ten
What molecule inhibits tPA?
Plasminogen Activator Inhibitor
What does α2 anti-plasmin inhibit?
plasmin not yet bound to fibrin
What is the broad definition of acute coronary syndrome?
any disease process that limits blood flow through the coronary arteries
What does Dipyridamole do to cAMP levels? What does increased cAMP do to calcium levels?
increase
decrease Ca2+
Would dipyradimole be a vasoconstrictor or vasodilator?
vasodilator
What receptor do Clopidogrel antagonize?
P2Y12
What specific CYP enzyme activates Dipyradimole?
CYP 2C19
What is the MOA of Prasugrel?
irreversibly inhibits P2Y12
Is the activity of Prasugrel affected by CYP2C19 polymorphisms?
no
What is the MOA of Ticagrelor?
reversibly inhibits P2Y12
Which P2Y12 inhibitor is not a prodrug?
Ticagrelor
What is the MOA of Cangrelor?
reversible inhibitor of P2Y12
What is the MOA of Abciximab?
GPIIb/IIIa inhibitor
What is the MOA of Eptifibatide?
peptide that prevents fibrinogen from binding GPIIb/IIIa
What is the MOA of Tirofiban?
non-peptide inhibitor of GPIIb/IIIa
What is the inhibitor of the Protease Activated Receptor (PAR)?
Vorapaxar
What type of severe hemorrhage can too much anti-coagulation medication produce?
Cerebral hemorrhage
In what cell type of heparin normally found?
mast cells
What is the inhibitor of heparin?
Protamine sulfate
What is the name for LMW Heparin?
Enoxaparin
What clotting factor does LMWH heparin inhibit the most?
factor X
Which has better bioavailability after a subQ injection, LMWH or Heparin?
LMWH
Which has better half-life after a subQ injection, LMWH or Heparin?
LMWH
What binds to plasma proteins and endothelial cells less, LMWH or Heparin? What does this mean?
LWMH
more predictable response
What is notable about the clearance of LMWH?
clearance = dose dependent
Would a patient with low renal function be put on LWMH or heparin? Why?
unfractioned
LWMH heparin is cleared almost exclusively by the kidneys
What is the effect of protamine sulfate on LMWH?
partial reversal
What drug does Fondaparinux funtion similarly to?
LMWH
What clotting factor does fondaparinux primarily inhibit?
Factor ten
What are the effects of protamine sulfate on Fondaparinux?
no effects
What is the MOA of hirudin?
direct thrombin inhibitor
What is the MOA of lepirudin?
direct thrombin inhibitor
What is the MOA of bivalirudin?
- inhibits thrombin
2. blocks thrombin binding site of fibrin
What is the MOA of argatroban?
direct thrombin inhibitor
What is the MOA of dabigatran?
direct thrombin inhibitor
How long does it take for the full anti-coagulant effects of warfarin to be reached?
3-5 days
Which cytochrome metabolizes warfarin?
CYP 2C9