Anti-platelet And Anti-coagulant Drugs Flashcards

1
Q

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

-Cause platelets to adhere to subendothelium of damaged blood vessel

A

von Willebrand Factor (vWF)

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2
Q

Protease activated receptors that respond to thrombin

A

PAR1 and PAR4

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3
Q

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

A

P2Y1 and P2Y12

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4
Q

The major product of COX-1 involved in platelet activation

A

Thromboxane A2

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5
Q

Highly sulfates mucopolysaccharide

A

Heparin (antithrombin III activator)

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6
Q

Specific pentasaccharide essential for binding and inducing conformational change in antithrombin

A

Heparin

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7
Q

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

A

Heparin

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8
Q

Catalyzes the antithrombin-protease “suicide substrate” reaction

A

Heparin

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9
Q

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

A

Factor Xa

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10
Q

Requires heparin to bridge antithrombin and thrombin

A

Thrombin inactivation

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11
Q

Can rapidly neutralize heparin effects in a life-threatening hemorrhage

A

Protamine Sulfate

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12
Q

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

A

Protamine

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13
Q

Partially effective against LMWH but not against pentasaccharide

A

Protamine

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14
Q

Can lead to major bleeding and osteoporosis

A

Heparin Therapy

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15
Q

Typically caused by antibodies against heparin:platelet factor 4 complex

-Onset is 5-10 days after treatment

A

Heparin-Induced Thrombocytopenia (HIT)

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16
Q

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

A

Hirudin and Bivalirudin

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17
Q

Inhibits thrombin only by binding the active site

A

Argtroban

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18
Q

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

A

Desirudin

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19
Q

Can reach and inactivate fibrin-bound thrombin in thrombi

-Found in leeches

A

Desirudin

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20
Q

Desirudin does NOT cause

A

Thrombocytopenia

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21
Q

Approved prevention of DVT and post elective hip replacement

A

Desirudin

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22
Q

Synthetic peptide congeners of hirudin

-used in coronary angioplasty and patients with HIT

A

Bivalirudin

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23
Q

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

A

Argatroban

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24
Q

FDA approved for use as an anticoagulant in patients with HIT

A

Argatroban

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25
Q

Monitored by aPTT and also prolongs PT

-aPTT returns to normal two hours after discontinuing treatment

A

Argatroban

26
Q

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

A

Warfarin

27
Q

Does not inhibit existing functional clotting factors

-Delayed onset of action (4-5 days)

A

Warfarin

28
Q

Prothrombin and Factors VII, IX, and X are all

A

Procoagulants

29
Q

Protein C and protein S are both

A

Anticoagulants

30
Q

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

-Binds Ca2+

A

Gla domains

31
Q

Protein C and Factor VII both have short

A

Half-lives

32
Q

Cause an increased risk for venous thrombosis

A

Protein C or S deficiency

33
Q

We can treat adverse bleeding effects caused by warfarin w/

A

Vitamin K

34
Q

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

A

Microvascular thrombosis

35
Q

Warfarin can cause nephrotic syndrome in the form of low plasma

A

Albumin

36
Q

Can cause decreased cytochrome P450 metabolism

A

Warfarin

37
Q

Can cause increased target reductase sensitivity (VKORC1)

A

Warfarin

38
Q

What are the three new/novel direct oral anticoagulants?

-Called the Xa inhibitors

A

Rivaroxaban, Apixaban, and Edoxaban

39
Q

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

A

Xa inhibitors

40
Q

Cause higher rates of GI bleeding than warfarin

A

Xa inhibitors

41
Q

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

A

Mechanical Heart Valves

42
Q

An antidote to da bigot ran

A

Idarucizumab

43
Q

Recombinant modified human factor Xa decoy protein is an antidote for

A

Andexanet alfa

44
Q

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

A

Fibrinolysis

45
Q

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

A

Tissue Plasminogen Activator (t-PA)

46
Q

Rapidly lose thrombi by catalyzing the formation of plasmin from plasminogen

A

Fibrinolytic Drugs

47
Q

A recombinant tissue plasminogen activator

A

Alteplase (Activase)

48
Q

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

A

Thrombus

49
Q

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

A

Alteplase

50
Q

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

A

Aspirin

51
Q

Works because platelets have no nucleus and thus can not resynthesize

A

COX

52
Q

Endothelial cells can regenerate COX and restore antithrombotic effect by producing

A

PGI2

53
Q

A low dose of aspirin (70-325 mg/day) can selectively inhibit

  • Spares endothelial COX
  • sustains antithrombotic effect
A

Platelet Cox

54
Q

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

A

Aspirin

55
Q

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

A

Clopidogrel and Prasugrel

56
Q

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

A

Ticagrelor (Brilinta)

57
Q

Dual antiplatelet therapy is typically an

A

ADP inhibitor + Aspirin

58
Q

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

A

GPIIb/IIIa

59
Q

Facilitates formation of the platelet plug

A

GPIIb/IIIa

60
Q

What are the three platelet GPIIb/IIIa receptor blockers?

A

Abciximab, eptifibatide, and tirofiban