Anticoagulant Drugs

Front 1

Which pathway of blood coaguloation begins with release of tissue factor and activation of factor VIIa and Ca+?

Back 1

extrinsic cascade

Front 2

What are the three ways drugs affect hemostasis and thrombosis?

Back 2

blood coagulation (fibrin formation),platelet function,fibrin removal (fibrinolysis)

Front 3

What are the indirect thrombin inhibitors?

Back 3

low molecular weight heparin,unfractionated heparin ,fondaparinux

Front 4

Thrombocytopenia is more likely to be caused by low molecular weight or unfractionated heparin?

Back 4

Unfractionated heparin

Front 5

What is the mechanism of action for hirudin?

Back 5

binds substrate recognition and catalytic site of thrombin factor Iia to inhibit the coagulation cascade

Front 6

Lepirudin and argatroban are contrindicated in what comorbid conditions?

Back 6

lepirudin- renal insufficiency,argatroban - hepatic insufficiency

Front 7

What percentage of warfarin is bound to ablumin in the body?

Back 7

99%

Front 8

How do you treat heparin overdose?

Back 8

IV protamine which forms a stable inert complex

Front 9

What discontinued heparinoid drug was a mixture of heparan, dermatan, and chondroitin?

Back 9

danaparoid

Front 10

How can the actions of warfarin be reversed?

Back 10

Vitamin K,Fresh frozen plasma

Front 11

tPA and Urokinase have what effect on fibrinolysis?

Back 11

Activate the conversion of plasminogen to plasmin

Front 12

What receptors on inactive platelets are unable to bind fibrinogen?

Back 12

GP IIb/IIIa

Front 13

ADP has what effect on platelet aggregation?

Back 13

it is one of the most important signalling molecules leading to platelet aggregation

Front 14

Activation of platelets begins with binding of what?

Back 14

Von Willebrand factor

Front 15

How are hereditary clotting defects treated?

Back 15

Fresh frozen plasma,Recombinant factors (more expensive)

Front 16

Unfractionated heparin (Heparin sodium)Mechanism

Back 16

Enhances activity of anti thrombin to form inactive complexes with thrombin IIa, IXa, and Xa

Front 17

Enoxaparin Low molecular weight heparin: Mechanism

Back 17

Faster than UF,Lacks a binding motif for inhibition of thrombin IIa but rapidly inactivates factor Xa

Front 18

Enoxaparin Low molecular weight heparin: Clincal use

Back 18

ACUTE Initial treatment of venous thrombosis and PE (w/oral anticoagulant),Thrombosis on prosthetic heart valves,Thrombosis and embolization in patients with atrial fibrillation,MI with unstable angina

Front 19

Enoxaparin Low molecular weight heparin: Adverse effects

Back 19

Toxicity: Bleeding ,Allergy (animal origin),Osteoporosis,Thrombosis (decreased antithrombin III),,Heparin Induced thrombocytopenia (HIT):,Increased thrombosis due to antibodies to heparin and platelet factor 4,Usually with UF,2-14 days after beginning therapy,Decreased platelet counts

Front 20

Enoxaparin Low molecular weight heparin: Pharmacokinetics

Back 20

Same as unfractionated heparin but Subcutaneous is more predictable than for UFH,Cleared by liver and kidney

Front 21

Enoxaparin Low molecular weight heparin: Contraindications

Back 21

Hypersensitivity to UFH/LMWH, pork products, methylparaban,History of HIT,Active Bleed,Hemophelia,Thrombocytopenia

Front 22

Unfractionated heparin (Heparin sodium):Mechanism?

Back 22

Enhances activity of anti thrombin to form inactive complexes with thrombin IIa, IXa, and Xa

Front 23

Unfractionated heparin (Heparin sodium):Clincal use ?

Back 23

ACUTE Initial treatment of venous thrombosis and PE (w/oral anticoagulant),Thrombosis on prosthetic heart valves,Thrombosis and embolization in patients with atrial fibrillation,MI with unstable angina

Front 24

Unfractionated heparin (Heparin sodium):Adverse effects?

Back 24

Toxicity: Bleeding ,Allergy (animal origin),Osteoporosis,Thrombosis (decreased antithrombin III),,Heparin Induced thrombocytopenia (HIT):,Increased thrombosis due to antibodies to heparin and platelet factor 4,Usually with UF,2-14 days after beginning therapy,Decreased platelet counts

Front 25

Unfractionated heparin (Heparin sodium):Pharmacokinetics ?

Back 25

IV (most rapid/predictable),Subcutaneous (maintenance doses),Avoid IM injection,Dosing based on weight,Cleared by liver and kidney

Front 26

Unfractionated heparin (Heparin sodium):Contraindications ?

Back 26

Hypersensitivity to UFH/LMWH, pork products, methylparaban,History of HIT,Active Bleed,Hemophelia,Thrombocytopenia

Front 27

Fondaparinux Clincal use ?

Back 27

ACUTE Initial treatment of venous thrombosis and PE (w/oral anticoagulant),Thrombosis on prosthetic heart valves,Thrombosis and embolization in patients with atrial fibrillation,MI with unstable angina

Front 28

Lepirudin, Bivalirudin (Hiruden): Mechanism?

Back 28

Irreversibly binds both substrate recognition and catalytic site of thrombin (factor IIa) to inhibit coagulation cycle

Front 29

Lepirudin, Bivalirudin (Hiruden): Clincal use ?

Back 29

Treatment of HIT

Front 30

Lepirudin, Bivalirudin (Hiruden): Adverse effects?

Back 30

Hemorrhage: most serious/most common

Front 31

Lepirudin, Bivalirudin (Hiruden): Contraindications ?

Back 31

Lepirudin:Renal insuficiency

Front 32

ArgatrobanMechanism?

Back 32

Irreversibly binds and blocks the catalytic site of thrombin

Front 33

ArgatrobanClincal use ?

Back 33

Treatment of HIT

Front 34

ArgatrobanAdverse effects?

Back 34

Hemorrhage: most serious/most common

Front 35

ArgatrobanContraindications ?

Back 35

Hepatic Insufficency

Front 36

Warfarin (coumadin)Mechanism?

Back 36

Inhibits Vitamin K reductase which indirectly,Blocks gamma carboxylation of glutamate residues in prothrombin factors VII, IX, and x,No effect on clotting factors made prior to dosing

Front 37

Warfarin (coumadin)Clincal use ?

Back 37

PROLONGED TREATMENT OF:,Venous thrombosis and PE (w/oral anticoagulant),Thrombosis on prosthetic heart valves,Thrombosis and embolization in patients with atrial fibrillation,MI with unstable angina

Front 38

Warfarin (coumadin)Adverse effects?

Back 38

Hemorrhage of bowel or brain stem,Increased risk from:,Certain Drugs,Aspirin,Altered vit K intake,,reversed by VitK/fresh frozen Plasma

Front 39

Warfarin (coumadin)Pharmacokinetics ?

Back 39

100 % bioavailable,99% bound to albumin,Initial effect delayed 12-16 hrs,Full anti-clotting effect delayed 8-16 days,t1/2 is 36 hrs,Requires continual monitoring

Front 40

Warfarin (coumadin)Contraindications ?

Back 40

Pregnancy (teratogenic),Active bleed,Hemophelia,severe liver disease,Inability to monitor treatment

Front 41

Streptokinase Mechanism?

Back 41

Binds to and activated plasminogen to cause conversion to plasmin,Low fibrin specificity

Front 42

Streptokinase Clincal use ?

Back 42

Time is Critical,PE with hemodynamic instability,Severe DVT,Ischemic stroke (tPAs),Acute MI

Front 43

Streptokinase Adverse effects?

Back 43

Hemorrhage,Antibody production

Front 44

Streptokinase A19Contraindications ?

Back 44

Surgery within last 10 days,Serious GI bleed in last 3 months,History of HTN,Active Bleeding or Hemorrhagic disorder,Previous Cerebrovascular accident,Aortic dissection,Acute pericarditis

Front 45

tPA's (Alteplase, Reteplase, Teneteplase Mechanism?

Back 45

Enzymatically convert plasminogen to plasmin,Specific for fibrin-bound plasminogen

Front 46

tPA's (Alteplase, Reteplase, Teneteplase Clincal use ?

Back 46

Time is Critical,PE with hemodynamic instability,Severe DVT,Ischemic stroke (tPAs),Acute MI

Front 47

tPA's (Alteplase, Reteplase, Teneteplase Adverse effects?

Back 47

Hemorrhage

Front 48

tPA's (Alteplase, Reteplase, Teneteplase Contraindications ?

Back 48

Surgery within last 10 days,Serious GI bleed in last 3 months,History of HTN,Active Bleeding or Hemorrhagic disorder,Previous Cerebrovascular accident,Aortic dissection,Acute pericarditis

Front 49

AspirinMechanism?

Back 49

Irreversibly inhibits COX 1,Permanent inhibition of a platelet

Front 50

AspirinClincal use ?

Back 50

Prevention of MI,Transient cerebral ischemia

Front 51

AspirinAdverse effects?

Back 51

Bleeding,Salicylism (large doses)

Front 52

Clopidogrel (Plavix) Mechanism?

Back 52

Irreversibly binds and inhibits P2Y12 receptor (Gi-coupled receptor for ADP release)

Front 53

Clopidogrel (Plavix) Clincal use ?

Back 53

Used alone or with Aspirin,Reduce rate of stroke and MI in recent MI, also in Peripheral Artery Disease or acute coronary syndrome

Front 54

Clopidogrel (Plavix) Adverse effects?

Back 54

Fewer side effects than ticlopidine (less thrombotic thrombocytopenic purpura)

Front 55

Prasugrel (Effient)Mechanism?

Back 55

Irreversibly binds and inhibits P2Y12 receptor (Gi-coupled receptor for ADP release)

Front 56

Prasugrel (Effient)Clincal use ?

Back 56

Used alone or with Aspirin,Reduce risk of heart attack after angioplasty

Front 57

Prasugrel (Effient)Adverse effects?

Back 57

Higher incidence of stroke in those with previous stroke

Front 58

Ticlopidine (Ticlid) Adverse effects?

Back 58

Thrombotic thrombocytopenic purpura

Front 59

Abcixamab (ReoPro), Eptifibadine (IntegrMechanism?

Back 59

Prevent interaction of glycoprotein IIB/IIA to fibrinogen or Von Willebrand factor,Prevents platelet aggregation

Front 60

Abcixamab (ReoPro), Eptifibadine (IntegrClincal use ?

Back 60

Acute coronary syndrome

Front 61

Abcixamab (ReoPro), Eptifibadine (IntegrAdverse effects?

Back 61

Bleeding

Front 62

Dipyridamole Mechanism?

Back 62

Inhibits phosphodiesterase, preventing cAMP breakdown, decreasing platelet activation and aggregation

Front 63

Dipyridamole Clincal use ?

Back 63

Used with Warfarin to prevent formation of emboli originating from prosthetic heart valves