Anti-platelet And Anti-coagulant Drugs

Question 1

GPIa/IIa and GPIb are platelet membrane proteins that bind to collagen and

-Cause platelets to adhere to subendothelium of damaged blood vessel

Answer 1

von Willebrand Factor (vWF)

Question 2

Protease activated receptors that respond to thrombin

Answer 2

PAR1 and PAR4

Question 3

ADP receptors that, when stimulated by agonists, these receptors activate the fibrinogen-binding protein and COX-1 to promote platelet aggregation and secretion

Answer 3

P2Y1 and P2Y12

Question 4

The major product of COX-1 involved in platelet activation

Answer 4

Thromboxane A2

Question 5

Highly sulfates mucopolysaccharide

Answer 5

Heparin (antithrombin III activator)

Question 6

Specific pentasaccharide essential for binding and inducing conformational change in antithrombin

Answer 6

Heparin

Question 7

Binds antithrombin III and increases rate of protease inhibition by 1000x

Answer 7

Heparin

Question 8

Catalyzes the antithrombin-protease “suicide substrate” reaction

Answer 8

Heparin

Question 9

The heparin-induced conformational change in antithrombin is sufficient to inactivate

Answer 9

Factor Xa

Question 10

Requires heparin to bridge antithrombin and thrombin

Answer 10

Thrombin inactivation

Question 11

Can rapidly neutralize heparin effects in a life-threatening hemorrhage

Answer 11

Protamine Sulfate

Question 12

A basic peptide that binds to negatively charged heparin forming a stable complex devoid of anticoagulant activity

Answer 12

Protamine

Question 13

Partially effective against LMWH but not against pentasaccharide

Answer 13

Protamine

Question 14

Can lead to major bleeding and osteoporosis

Answer 14

Heparin Therapy

Question 15

Typically caused by antibodies against heparin:platelet factor 4 complex

-Onset is 5-10 days after treatment

Answer 15

Heparin-Induced Thrombocytopenia (HIT)

Question 16

Bind both the catalytic site and expo site I of thrombin to inhibit thrombin

Answer 16

Hirudin and Bivalirudin

Question 17

Inhibits thrombin only by binding the active site

Answer 17

Argtroban

Question 18

A recombinant form of hirudin that functions as the most potent inhibitor of thrombin

Answer 18

Desirudin

Question 19

Can reach and inactivate fibrin-bound thrombin in thrombi

-Found in leeches

Answer 19

Desirudin

Question 20

Desirudin does NOT cause

Answer 20

Thrombocytopenia

Question 21

Approved prevention of DVT and post elective hip replacement

Answer 21

Desirudin

Question 22

Synthetic peptide congeners of hirudin

-used in coronary angioplasty and patients with HIT

Answer 22

Bivalirudin

Question 23

A small synthetic derivative of arginine that blocks catalytic site of soluble and clot-bound thrombin

Answer 23

Argatroban

Question 24

FDA approved for use as an anticoagulant in patients with HIT

Answer 24

Argatroban

Question 25

Monitored by aPTT and also prolongs PT -aPTT returns to normal two hours after discontinuing treatment

Answer 25

Argatroban

Question 26

Inhibits vitamin K epoxied reductase (VKOR) and biosynthesis of vitamin K-dependent zymogens

Answer 26

Warfarin

Question 27

Does not inhibit existing functional clotting factors -Delayed onset of action (4-5 days)

Answer 27

Warfarin

Question 28

Prothrombin and Factors VII, IX, and X are all

Answer 28

Procoagulants

Question 29

Protein C and protein S are both

Answer 29

Anticoagulants

Question 30

Contains 9-13 gamma-carboxylated Glu residues that are required for activity -Binds Ca2+

Answer 30

Gla domains

Question 31

Protein C and Factor VII both have short

Answer 31

Half-lives

Question 32

Cause an increased risk for venous thrombosis

Answer 32

Protein C or S deficiency

Question 33

We can treat adverse bleeding effects caused by warfarin w/

Answer 33

Vitamin K

Question 34

May occur in patients with heterozygous protein C or S deficiency if a high initial dose of warfarin is used

Answer 34

Microvascular thrombosis

Question 35

Warfarin can cause nephrotic syndrome in the form of low plasma

Answer 35

Albumin

Question 36

Can cause decreased cytochrome P450 metabolism

Answer 36

Warfarin

Question 37

Can cause increased target reductase sensitivity (VKORC1)

Answer 37

Warfarin

Question 38

What are the three new/novel direct oral anticoagulants? -Called the Xa inhibitors

Answer 38

Rivaroxaban, Apixaban, and Edoxaban

Question 39

Cause less intracranial bleeding than warfarin (by at least 50%)

Answer 39

Xa inhibitors

Question 40

Cause higher rates of GI bleeding than warfarin

Answer 40

Xa inhibitors

Question 41

The Xa inhibitors have similar uses to warfarin, but are contraindicated in patients with

Answer 41

Mechanical Heart Valves

Question 42

An antidote to da bigot ran

Answer 42

Idarucizumab

Question 43

Recombinant modified human factor Xa decoy protein is an antidote for

Answer 43

Andexanet alfa

Question 44

Process of breaking down fibrin. Particularly urgent when a clot has inappropriately formed or has broken free into the general circulation

Answer 44

Fibrinolysis

Question 45

The central process of fibrinolysis is conversion of inactive plasminogen to plasmin by

Answer 45

Tissue Plasminogen Activator (t-PA)

Question 46

Rapidly lose thrombi by catalyzing the formation of plasmin from plasminogen

Answer 46

Fibrinolytic Drugs

Question 47

A recombinant tissue plasminogen activator

Answer 47

Alteplase (Activase)

Question 48

Physiologically, t-PA activates plasminogen that is bound to fibrin of

Answer 48

Thrombus

Question 49

Has a half-life of 5 minutes and is typically given as an IV bonus and then infusion

Answer 49

Alteplase

Question 50

An anti-platelet drug that functions as a cyclooxygenase (COX) inhibitor

Answer 50

Aspirin

Question 51

Works because platelets have no nucleus and thus can not resynthesize

Answer 51

COX

Question 52

Endothelial cells can regenerate COX and restore antithrombotic effect by producing

Answer 52

PGI2

Question 53

A low dose of aspirin (70-325 mg/day) can selectively inhibit - Spares endothelial COX - sustains antithrombotic effect

Answer 53

Platelet Cox

Question 54

Serves as the primary prophylaxis of MI and as a secondary prevention of vascular events following heart disease

Answer 54

Aspirin

Question 55

Irreversibly inhibits binding of ADP to its receptor on platelets and inhibits platelet aggregation

Answer 55

Clopidogrel and Prasugrel

Question 56

Reversible inhibits the binding of ADP to its receptor on platelets and inhibits platelet aggregation

Answer 56

Ticagrelor (Brilinta)

Question 57

Dual antiplatelet therapy is typically an

Answer 57

ADP inhibitor + Aspirin

Question 58

A platelet membrane receptor which binds to the fibrinogen and vitronectin and also to fibronectin and vWF

Answer 58

GPIIb/IIIa

Question 59

Facilitates formation of the platelet plug

Answer 59

GPIIb/IIIa

Question 60

What are the three platelet GPIIb/IIIa receptor blockers?

Answer 60

Abciximab, eptifibatide, and tirofiban