Drugs For Thromboembolic Disorders (Konorev) Flashcards

1
Q

What pathologic conditions are associated with white thrombi?

A

Local ischemia d/t arterial occlusion (in coronary arteries: MI/unstable angina)

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2
Q

This type of thrombus forms in low-prssure veins and in the heart; result of platelet bidning and aggregation followed by formation of bulky fibrin tails in which RBCs become enmeshed.

A

Red thrombus (fibrin-rich with trapped RBCs)

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3
Q

What are pathologic conditions associated with red thrombi?

A

Pain and severe swelling, embolism and distal pathology (embolic stroke)

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4
Q

This type of drug regulates the function and synthesis of clotting factors and is primarily used to prevent clots from forming in the venous system and heart (RED THROMBI)

A

Anticoagulants

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5
Q

This type of drug inhibits platelet function and is primarily used to prevent clots from forming in the arteries (white thrombi)

A

Antiplatelet drugs

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6
Q

This type of drug destroys blood clots after they are formed. These re-establish blood flow through vessels once clots have formed

A

Thrombolytic

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7
Q

Heparin sodium is this type of anticoagulant

A

Parenteral –> Indirect thrombin and FXa inhibitor –> HMW or UFH

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8
Q

Enoxaprin, Tinzaparin, and Dalteparin are this type of anticoagulant:

A

Parenteral –> Indirect thrombin and FXa inhibitor –> LMW

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9
Q

Fondaparinux is this type of anticoagulant:

A

Parenteral –> Indirect thrombin and FXa inhibitor –> Synthetic pentasaccharide

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10
Q

Lepirudin, Bivalirudin, and Argatroban are this type of anticoagulant:

A

Parenteral –> Direct thrombin inhibitors

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11
Q

What is the MOA of indirect thrombin and FXa inhibitors?

A

Bind plasma serine protease inhibitor ANTITHROMBIN III

Antithrombin III inhibits several clotting factor proteases, esp Thrombin (IIa), IXa, and Xa. Heparin increases antithrombin III activity 1000fold

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12
Q

This anticoagulant inhibits the activity of both thrombin and FXa

A

HMW heparin

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13
Q

This anticoagulant inhibits FXa with little effect on thrombin

A

LMW heparin

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14
Q

This anticoagulant inhibits FXa activity with no effect on thrombin

A

Fondaparinux

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15
Q

What is the MOA of DIRECT thrombin inhibitors (Parenteral)?

A

Direct inhibition of the protease activity of thrombin

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16
Q

The MOA of these anticoagulants is bivalent direct thrombin inhibitors (bind at both active site and substrate recognition site)

A

Lepirudin and Bivalirudin

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17
Q

The MOA of this anticoagulant is an inhibitor binding only at the thrombin active site

A

Argatroban

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18
Q

Warfarin (coumadin) is this type of anticoagulant:

A

Oral –> Coumarin anticoagulant

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19
Q

Rivaroxaban, Apixaban, Edoxaban are these types of anticoagulant:

A

Oral –> Novel oral anticoagulants (NOAC) –> Factor Xa inhibitors

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20
Q

Dabigatran is this type of anticoagulant:

A

Oral –> NOAC –> Direct thrombin inhibitor

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21
Q

What is the MOA of warfarin?

A

Inhibits reactivation of Vit K by inhibiting Vit K epoxide reductase. Inhibits carboxylation of GGCX in prothrombin and factors VII,IX, and X, making them inactive

22
Q

What makes warfarin dosing so difficult?

A

Narrow therapeutic window of the drug and high individual variability, i.e., genetics, disease states, drug-drug interactions, diet

23
Q

What is the INR for pts on warfarin?

A

2.0-3.0

24
Q

Rivaroxaban, Apixaban, and Edoxaban inhibit ___

A

Xa

25
Q

Dabigatran inhibits ___

A

IIa (thrombin)

26
Q

Who gets parenteral anticoagulants?

A

Pts with DVT, atrial arrhythmias and other conditions that predispose towards RED THROMBI
Tx/prevention of embolic stroke, PE
Prevent emboli during surgery or in hospitalized pts
Heparin locks

27
Q

Who gets oral anticoagulants?

A

Used to prevent thrombosis or prevent/treat thromboembolism
A Fib
Prosthetic heart valves

28
Q

What is the antidote for HMW and LMW heparin?

A

Protamine sulfate

29
Q

What is the antidote for warfarin?

A

Vit K, prothrombin complex concentrate

30
Q

What is the antidote for NOAC-DTI?

A

Idarucizumab

31
Q

Which coagulation test is specific for heparin?

A

PTT, anti-Xa –> the intrinsic pathway

32
Q

Which coagulation test is specific for warfarin?

A

PT-based (INR) –> Extrinsic pathway

33
Q

What blood coagulation test is specific for NOAC-FXa inhibitors?

A

Anti-Xa

34
Q

What blood coagulation test is specific for NOAC-DTI?

A

Diluted thrombin time (TT)

35
Q

What type of antiplatelet drug is aspirin?

A

Inhibitor of TxAs synthesis

36
Q

What type of antiplatelet drug is Clopidogrel, Prasugrel, Ticlopidine, and Ticagrelor?

A

ADP receptor blocker

37
Q

What type of antiplatelet drug is Abciximab, Eptifibatide, and Tirofiban?

A

Platelet glycoprotein receptor blocker

38
Q

What type of antiplatelet drug is Dipyridamole and Cilostazol?

A

Phosphodiesterase inhibitor

39
Q

What is the MOA of aspirin?

A

Inhibit COX

Decreased TxA2 production

40
Q

What is the MOA of ADP receptor blockers?

A

Inhibition of AC by ai is relieved
Increased production of cAMP

Clopidogrel, ticlopidine, and prasugrel

41
Q

What is the MOA of phosphodiesterase inhibitors?

A

Inhibit cAMP degradation
Levels of cAMP in platelets are increased

Dipyramidole and cilostazol

42
Q

Platelet GP receptor antagonists target this sequence to prevent binding of ligands to the GP IIb/IIIa receptor to inhibit platelet aggregation

A

RGD

Abciximab, Tirofiban, Eptifibatide

43
Q

What are clinical uses of antiplatelet drugs?

A

Prevent thrombosis in unstable angina and other acute coronary syndromes
Prevent ischemic stroke and arterial thrombosis in peripheral vascular disease
Pts undergoing percutaneous coronary angioplasty and stunting

44
Q

This combo can be used to prevent cerebrovascular ischemia:

A

Dipyridamole (PDE inhibitor) with aspirin

45
Q

This combo can be used to tx pts with prosthetic heart valves

A

Dipyridamole (PDE inhibitor) with warfarin

46
Q

This drug can be used to tx intermittent claudication

A

Cilostazol

47
Q

What is the MOA of thrombolytic drugs?

A

Activate endogenous fibrinolytic system by converting plasminogen into plasmin

48
Q

Alteplase, Reteplase, and Tenecteplase are these types of thrombolytics:

A

tPA drugs

49
Q

Urokinase is this type of thrombolytic drug:

A

uPA activator

50
Q

Streptokinase is this type of thrombolytic drug:

A

Streptokinase preparation purified from bacteria

51
Q

What are clinical uses of thrombolytic drugs?

A
Acute embolic/thrombotic stroke (within 3 hr)
Acute MI (within 3-6 hr)
PE
DVT
Ascending thrombophlebitis
52
Q

This type of thrombus forms in high-pressure arteries and is the result of platelet binding to the damaged endothelium and aggregation with little involvement of fibrin.

A

White (platelet-rich) thrombus