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64 Cards in this Set

  • Front
  • Back
drugs that inhibit the synthesis of coagulation factors
1) warfarin
drugs that indirectly inactivate coagulation factors
1) unfractionated and low molecular weight heparin
--UFH
--Fondaparinux
--Enoxaparin
--dalteparin
drugs that directly inactivate coagulation factors
1) Bivalirudin
2) Hirudin
3) Kepirudin
antiplatelet drugs
1) Aspirin
2) NSAID's
3) clopidogrel
4) ticlopidine
5) abciximab
6) tirofiban
7) eptifibitide
Fibrinolytic drugs
1) Alteplase
2) reteplase
3) tenecteplase
4) streptokinase
5) urokinase
____________inhibits plasminogen activation
aminocaproic acid
___________antagonizes heparin
protamine sulfate
normal hemostasis
Injury to blood vessel --> vasospasm --> platelet aggregation --> coagulation --> fibrin clot formation --> healing --> fibrinolysis
thrombin converts ___________--> __________
fibrinogen --> fibrin
fibrinolysis
plasminogen --> plasmin
---plasmin converts fibrin --> split products
--plasmin also converts fibrinogen --> degredation products
3 major factors released by platelets
1) TXA2
2) ADP
3) 5-HT
____is the GP that connects plalets tgether in platelet aggregation
GP IIb/IIIa
Xa converts _________-->_________
prothrombin --> thrombin
major thrombotic disorders
1) acute coronary syndrome
----unstable angina
----MI
2) stroke
3) DVT
warfarin blocks _________
Vit K reductase
--therefore prevents carboxylation of clotting factors
adverse effects of warfarin
1) hemorage
2) fetal abnormalities
--fetal warfarin syndrome
--chondrodysplasia punctata
Drug interactions of warfarin
1) anything that inhibits or induces p450
2) anything that has a direct effect on coagulation
what drugs interact with warfarin by increasing PT (longer to clot)
1) cimetidine (histimine Rc antagonist ; ulcers)
2) Aspirin (High doses)
3) cephalosporins (antibacterial, pneumonia)
4) Heparin
5) Hepatic disease
what drugs interact with warfarin by decreasing PT
1) barbituates (CNS depressant)
2) Rifampin (antibiotics, Tb, Meningitis)
3) Diuretics
4) Vit K
5) Hereditary resistance
clinical uses of warfarin
1) DVT
2) A-fib
3) artificial heart valves
4) stroke prevention
5) MI prevention
tx of bleeding caused by warfarin
1) reduce dosage of warfarin
2) administer vit K1 (phytonadione) to accelerate the recovery of clotting factors
3) give FFP or Factor IC concentrate
ROA for warfarin
Oral
onset of action of warfarin
delayed onset
warfarin inhibits _________
Vit K reductase
warfarin inhibits synthesis of which factors
1) vit K dependant factors
--II
--VII
--IX
--X
warfarin is monitored with______
PT
is warfarin used in pregnancy?
No
the Heparin family are _______thrombin inhibitors
indirect
Unfractionated heparin (UFH)
1) contains high and low molecular weight fractions
Low molecular weight heparins (LMWH)
less effective than the HMW of the UFH but more bioavalability
2 LMH
Enoxaparin
Dalteparin
__________is a synthetic pentasaccaride for heparin
fondaparinux
heparin is a naturally occurring mixture of sulfated mucopolysaccarides that binds to _________when administered?
Antithrombin III
MOA of heparin
1) heparin binds and activates antithrombin III
2) antithrombin III inactivates clotting factors (thrombin, Xa, and others)
3) this has a more imediate anticoagulatn effect than warfarin
antithrombin III is a
endogenous protease anticoagulant
heparin site of action
intrinsic pathway and common pathway (Xa)
Factors inhibited by warfarin
VII
IX
X
Prothrombin
most important factors inhibited by warfarin
X
prothrombin
factors inhibited by heparin
XIIa
Xa
IXa
VIIa
Xa
Thrombin
Most important factors inhibited by heparin
Xa
thrombin
3 key characteristics of heparin
1) it is a sulfated polysaccaride
2) it potentiates antithrombin III
3) it inactivates activated clotting factors
Heparin Pharmicokinetics
1) it is not absorbed from the gut
2) administered as an IV infusion or subcutaneous injection
clinical use of heparin
acute thromboembolism
--venous thrombosis
--pulmonary and other emboli
--DIC
2) cardiovascular surgery
3) a-fib
4) renal dialysis
5) blood transfusion
6) blood sampling
adverse effectsof heparin
1) hemorrage (elderly woman with renal failure)
2) thrombocytopenia (25% mild, ?5% severe)
3) hyperkalemia (decrease aldosterone)
4) osteoporosis (chronic administration)
tx of bleeding caused by heparin
1) discontinue heparin
2) give protamine sulfate
3) give FFP for severe bleeding
clinical uses of the direct thrombin inhibitars
1) acute coronary syndrome
2) heparin nduced thrombocytopenia (particularly lepirudin)
process of platelet hemostasis
adhesion of platelets to collagen and endothelium --> platelet activation (synthesis and release of mediators) --> platelet agregation (fibrinogen forms between GPIIb/IIIa sites on the platelets --> formation of platelet plug
drugs that inhibit thromboxane synthesis
Aspirin
NSAID's
antiplatelet Drugs that block ADP receptors
clopidogrel
ticlopidine
antiplatelet drugs that block GPIIa/IIIb Rc
1) abiximab
2) Tirofiban
3) Eptifibitide
MOA of aspirin
inhibits COX --> decrease in TXA2 synthesis --> prevents platelet agregation

--has less of an effect on prostoglandin synthesis
clinical indications for aspirin
1) unstable angina
2) TIA and stroke prevention
3) AMI
ticlopidine and clopidogrel
1) block ADP Rc --> reduces expression of GP receptor --> inhibits platelet aggregation
MOA of abciximab
MAB to the GP receptor (blocking it)
MOA of tirofiban
it has an analog sequence within fibrinogen (occupying the GP receptor)
MOA of eptifibatide
it has an analog sequence within fibrinogen (occupying the GP receptor)
fibrinolytic drugs catalyze the formation of _________
plasmin
which fibrinolytic drugs are tissue fibrinogen activators?
alteplase
reteplase
tenecteplase
2 fibrinolytic drugs that are not tissue plasminogen activators
streptokinase
urokinase
clinical uses of fibrinolytic drugs
1) AMI
2) ischemic (thrombotic) stroke)
3) PE
contraindications to fibrinolytic drugs
1) active bleeding
2) hemoragic stroke
3) severe HTN
4) intracranial surgery / trauma, anurysm, tumor
drugs used to tx bleeding caused by fibrinolytic drugs
1) aminocaproic acid (inhibits plasminogen activation)
2) protamine sulfate (antagonizes heparin)
3) Vit K
warfarin has a simular structure to_______
vit K
warfarin prevents _________
1) carboxylation of clotting factors...therefore preventing the formation of prothrombin