(3) Blood & Inflammation: Anti-coagulants & Thrombolytics (1.1-1.4) Flashcards

1
Q

What enzyme catalyzes the final step of the coagulation cascade?

A

Thrombin

(Factor II, and crosslinking of fibrin occurs via Factor XIII)

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2
Q

What coagulation factor activates thrombin?

A

Factor Xa

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3
Q

ROA: Direct factor Xa inhibitors

A

Oral

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4
Q

What protein mediates Heparin’s effects?

A

Antithrombin III

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5
Q

Which coagulation factors does Heparin inhibit?

A

(1) Factor IIa
(2) Factor Xa

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6
Q

Which clotting time does heparin most affect?

A

PTT

(activated partial thromboplastin time)

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7
Q

Indications (3) : Heparin

A

(1) DVT prophylaxis
(2) Pulmonary embolism prophylaxis
(3) Acute MI

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8
Q

ROA: Heparin

A

IV

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9
Q

What is the antigenic target in Heparin-Induced Thrombocytopenia?

A

Platelet Factor 4

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10
Q

Adverse Effects (4) : Heparin

A

(1) Heparin-induced thrombocytopenia
(2) Hypoaldosteronism
(3) Osteoporosis
(4) Type IV RTA
* (Type 4 renal tubular acidosis)*

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11
Q

What drug reverses the effects of Heparin?

A

Protamine sulfate

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12
Q

What is the difference LMWH and Heparin?

A

LMWH is more specific for Factor Xa

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13
Q

Does LMWH or Heparin have a longer half life?

A

LMWH

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14
Q

How is LMWH eliminated?

A

Renally

(Whereas Heparin is eliminated by the liver)

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15
Q

Which anticoagulant is indicated in pregnancy?

A

Heparin

(or LMWH)

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16
Q

Why doesn’t LMWH require routine monitoring?

A

↓ Risk of HIT

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17
Q

MOA: Fondaparinux

A

≅ LMWH

(Although even more specific for ATIII)

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18
Q

Which indirect thrombin inhibitor has the lowest risk of HIT?

A

Fondaparinux

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19
Q

Suffix: Direct thrombin inhibitors

A

(1) “-rudin”
(2) “-gatro-“

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20
Q

Suffix: Direct factor Xa inhibitor

A

“-xaban”

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21
Q

Other than Warfarin, what class of anticoagulant is used in long term therapy of atrial fibrillation?

A

Direct factor Xa inhibitors

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22
Q

Treatment: Heparin-induced thrombocytopenia

A

Direct thrombin inhibitors

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23
Q

What’s the goal INR value in Warfarin therapy?

A

2-3

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24
Q

Indications (2) : Warfarin

A

(1) Prophylaxis in atrial fibrillation
(2) DVT prophylaxis

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25
Q

Which anticoagulant is a teratogen?

A

Warfarin

26
Q

What causes an initially hypercoagulable state in Warfarin therapy?

A

Early inhibition of Protein C

27
Q

Why do we need to monitor patients early in Warfarin therapy?

A

Warfarin induced skin necrosis

(Common initial presentation of Protein C/S deficiency)

28
Q

What drug should be coadministered early in Warfarin therapy?

A

Heparin

29
Q

How is Warfarin reversed?

A

(1) Delayed: Administer Vitamin K
(2) Immediate: Plasma transfusion

30
Q

How is Warfarin metabolized?

A

CYP-450

31
Q

What does the damaged vascular endothelium expose which activates platelets?

A

(1) vWF
(2) Collagen

32
Q

Which platelet receptor does vWF bind?

A

GP1b

33
Q

Which platelet receptor does ADP bind?

A

P2-Y12

34
Q

What effect does serotonin release from platelets have?

A

(1) ↑ Platelet aggregation
(2) Vasoconstriction

35
Q

Which COX isozyme is responsible for synthesizing TXA2?

A

COX-1

36
Q

Which COX isozyme is only active during inflammation?

A

COX-2

37
Q

MOA: Aspirin

A

Irreversibly inhibits COX-1 and COX-2

38
Q

Suffix: ADP receptor inhibitors

A

“-grel”

39
Q

Which cardiovascular diseases are antiplatelet drugs used in?

A

(1) Peripheral artery disease
(2) MI and Acute coronary syndromes

40
Q

What route of administration should Aspirin be given in the setting of acute MI?

A

Chewable aspirin

41
Q

What is dual antiplatelet therapy used for?

A

Prevent coronary stent thrombosis

42
Q

What ADP receptor inhibitor does NOT have the suffix “-grel”?

A

Ticlopidine

43
Q

Which antiplatelet agent is associated with granulocytopenia?

A

Ticlopidine

44
Q

What platelet receptor does Fibrinogen bind?

A

GP IIb/IIIa

45
Q

Name 3 drugs which block GP IIb/IIIa

A

(1) Abciximab
(2) Eptifibatide
(3) Tirofiban
* (Ab-6-imab = gp2 x gp3)*

46
Q

Adverse Effect: GP IIb/IIIa inhibitors

A

Thrombocytopenia

47
Q

Name 2 PDE inhibitors used as antiplatelet agents

A

(1) Dipyridamole
(2) Cilostazol

48
Q

What effect does Cilostazol have on vasculature?

A

Arterial vasodilation

49
Q

Indication: Cilostazol

A

Claudication symptoms

50
Q

Adverse Effect: Cilostazol

A

Coronary steal

(a phenomenon where an alteration of circulation patterns leads to a reduction in the blood flow directed to the coronary circulation)

51
Q

What are the fibrinolytic agents?

A

(1) tPA
(2) Streptokinase

52
Q

Suffix: Recombinant tPA drugs

A

“-teplase”

53
Q

What effect on clotting time do fibrinolytic agents have?

A

↑ PT and PTT

54
Q

What circulating product is formed as a result of clot degradation?

A

D-dimer

55
Q

When can fibrinolytics be used to treat acute ischemic stroke?

A

Within 3-4.5 hours

56
Q

Indications (4) : Fibrinolytics

A

(1) Acute ischemic stroke

(2) Deep venous thrombosis
(3) Pulmonary embolism

(4) Acute myocardial infarction

57
Q

What is the time frame for percutaneous coronary intervention?

A

Within 2 hrs

58
Q

Adverse Effect: Thrombolytic therapy

A

Hemorrhagic stroke

59
Q

Contraindications (3) : Thrombolytic therapy

A

(1) Recent head trauma
(2) Recent intracranial surgery
(3) Severe hypertension

60
Q

Which thrombolytic can cause anaphylaxis?

A

Streptokinase

(Derived from Streptococcus ∴ foreign protein ∴ immunogenic)

61
Q

What drugs can be used to reverse fibrinolytic therapy?

A

(1) Aminocaproic acid
(2) Tranexamic acid

62
Q

MOA: Aminocaproic Acid

A

Inhibits plasminogen activation