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29 Cards in this Set

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Drugs that inhibit platelet activation act primarily where?
Arteries
Drugs that inhibit thrombin and fibrin act primarily where?
Veins
What is released with platele activation
ADP, Serotoning and TXA2

Leads to conformation change in GP IIb/IIIa to bind fibrinogen (RGD)
Aspirin (ASA)
Irreversible inhibits platelet TXA2 production (which triggers plately aggregation)

SE GI distress, ulcer and bleeding
Dipyridamole
Increase adenosine which increases cAMP levels and inhibits PDE (which breaks down cAMP)

Potentiates aspirin
Acts increase adenosine and inhibit PDE
Dipyridamole
Clopidogrel (Plavix)
Blocks ADP (which aggregates platelets) Takes 4-6 days to take effect. Safe, and more effective than aspirin

CI in active bleeders
ADP inhibitor
Clopidogrel (Plavix)

4-7 days to take effects
Abciximab
mAb that blocks GP IIb/IIIa

adjunct to heparin and aspirin for the usual + PCI
Eptifibatide
Synthetic peptide GP IIb/IIIa inhibitor
Tirofiban
synthetic non-peptide GP IIb/IIIa inhibitor

Reduce MI death 22% when used with heparin and aspirin
Three GP IIb/IIIa inhibitors
Abciximabe
Eptifibatide
Tirofiban
MOA heparin

Measure its effects
binds antithrombin III to block factor Xa and thrombin (IIa)

PTT
UFH vs LMWH
LMWH more specific for Xa, twice daily dosing safely and less incidence of HIT
Tx for HIT
protamine sulfate plus switch to direct thrombin inhibitor
lepirudin
Direct thrombin inhibitor, originially for leeches. May develop antibodies to it which decrease renal clearance
Bivalirudin
VERY expensive direct thrombin inhibitor with short half life (25 mins) for coronary angioplast in pts with prior HIT
Argatroban
Inhibits free and fibirin bound thrombin...excreted via liver
Three direct thrombin inhibitors
Lepirudin
Bilvalirudin
Argatroban
Warfarin MOA
competitive inhibitor of vit K. Vit K needed for carboxylation of factor VII, IX, X, II and protein C. Inhibits synthesis, so it needs days for already synthesized factors to be removed
Risk factors for hemorrhage on warfarin
Prior history
Cigarette smoking
Renal insufficieny
Anemia
HTn
Contraindication for warfarin
Preganacy
Active bleeding
Streptokinase
complexes with plasminogen to convert other plasminogen to plasmin. Not selective, increased risk of bleed
Problems with streptokinase
Not selective for fibrin and resistant to antiplasmin so can cause massive thrombolysis. Also, pt may have preformed Ab's from Strep infection
t-PA - Alteplase
normal t-PA that converts plasminogen and overwhelms plasminogen activator inhibitor causing quick thrombolysis.
t1/2 for t-PA
3 minutes and rapid liver clearance
Reteplase
Lower fibrin affinity and longer half life than t-PA. Can be given in two bolus injections
Tenecteplase
Mutated t-PA for longer half life, high specificity for fibrin bound plasminogen. Given in 1 daily bolus
Fibrinolytics
Streptokinase
t-PA
Reteplase
Tenecteplase