Anticoagulants Flashcards

1
Q

The _____________ is non-thrombogenic.

A

Endothelial lining

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2
Q
Name the 5 Procoagulants:
T
T
T
A
S
A
Thrombin
Tissue factor
Thromboxane
ADP
5-HT
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3
Q
Name the 5 Anticoagulants:
H
P
N
A
P
A
Heparan sulfate
Prostacyclin
Nitric Oxide
Antithrombin
Proteins C and S
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4
Q

What is found on the surface of endothelial cells and in the extracellular matrix, that interacts with circulating antithrombin to provide a natural antithrombotic mechanism?

A

Heparan Sulfate

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5
Q

What drugs target Platelet clumps (initial clot) ?

A

antiplatelet drugs

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6
Q

What drugs target Fibrin mesh formation around platelet clot?

A

Anticoagulant drugs (block single or multiple steps in coagulation cascade)

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7
Q

What drugs dissolve formed clots ?

A

fibrinolytic drugs

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8
Q
What are the Anticoagulant Drug classes?
A
H
O
F
A

Antiplatelet agents
Heparin & derivatives
Oral anticoagulants
Fibrinolytic agents

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9
Q

Streptokinase & Tissue plasminogen activator belong to which drug class?

A

Fibrinolytic agents

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10
Q

Warfarin belongs to which drug class?

A

Oral anticoagulants

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11
Q

Antithrombin belongs to which drug class?

A

heparin & derivatives

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12
Q

Asprin and Clopidogrel belong to which drug class?

A

Antiplatelet agents

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13
Q

Hypercholesterolemia, diabetes, hypertension can all cause _____________, platelet ___________, and plaque formation, which can rupture and activate coagulation.

A

endothelial dysfunction
platelet activation
plaque formation

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14
Q
4 Steps of Coagulation
V
P
F
R
A

Vasospasm
Platelet plug
Fibrin plug
Recanalization

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15
Q

__________ initiates the coagulation cascade.

A

Tissue Factor

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16
Q

What platelet function takes place following Disruption of endothelium?

A

Platelet adhesion

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17
Q

What platelet function takes place following platelet activation?

A

Platelet release

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18
Q
During the platelet release function , what Proaggregator mediators are released?
S
A
T
VWF
P4
A
Serotonin
ADP
Thromboxane
Von Willebrand Factor
Platelet Factor 4
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19
Q

Which Proaggregatory mediator activates platelets?

A

Thrombin (from prothrombin)

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20
Q

Which drug inhibits platelet COX and prevents formation of thromboxane and Arachidonic acid?

A

Asprin

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21
Q

Which drugs block platelet purinergic P2Y receptors for ADP and increase cyclic AMP ?

A

Clopidogrel and ticlopidine

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22
Q

Which drug inhibits platelet phosphodiesterase and prevents breakdown of cAMP?

A

Dipyridamole

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23
Q

What 3 drugs block the GPIIb-IIIa receptor for fibrinogen on platelets and prevent platelet aggregation?

A

Eptifbatide
Abciximab
tirofiban

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24
Q

Aspirin is therapeutically used for what 2 things?

A

Prophylaxis for Myocardial infaction (MI)

Prophylaxis for Ischemic attacks (TIA)

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25
Q
What are the 4 Aspirin Contraindications:
V
H
H
P
A

Vitamin K deficiency
Hemophilia
Hypoprothrombinemia
Pregnancy/Childbirth

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26
Q

What Antiplatelet prodrug is used in combination with asprin that has CYP enzyme related drug interactions? (less neutropenia)

A

Clopidogrel

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27
Q

What Antiplatelet prodrug is used in combination with asprin and is potent. It has no CYP related drug interactions

A

Prasugrel

28
Q

What Antiplatelet drug is potent and has CYP enzyme related drug interactions?

A

Ticagrelor

29
Q

What Antiplatelet prodrug may cause severe neutropenia in 1% of patients?

A

Ticlopidine

30
Q

Heparin is a _______ly charged molecule. This causes it to not cross the cell membrane easily.

A

negatively

31
Q

Heparin is found in what type of cells?

A

mast cells

32
Q

______________ circulates in the plasma and rapidly inhibits activated clotting factors: IIa (thrombin), Xa, IXa, XIa, and XIIa. Heparin acts as a catalyst to increase the rate of the reaction

A

Antithrombin III

33
Q

Heparin toxicity leads to ________. this can be treated using _____________.

A

Hemorrhage

Protamine sulfate

34
Q

HIT = ______________

A

heparin-induced thrombocytopenia.

35
Q

___________ is when there is more than 50% decrease in platelet count due to antigen antibody reaction.

A

Thrombocytopenia

36
Q

HIT incidence can be lowered by the use of what 2 alternative anticoagulants?

A

Thrombin

factor Xa Inhibitors

37
Q
What are the 4 main Therapeutic uses for Heparin?
V
P
H
P
A

Venous thrombosis
pulmonary embolism
Any Heart surgery
DRUG OF CHOICE - during pregnancy (does not cross placenta)

38
Q

LMWH have no space to bind _________. But can still inactivate _________.

A

thrombin IIA

factor Xa

39
Q

What are the 3 major advantages of LMWHs?
A
O
T & H

A

Better absorbed (higher bioavailability)
Given subcutaneously without lab monitoring (outpatients)
Lower risk of thrombocytopenia and bleeding (hemorrhage)

40
Q

What are the 2 disadvantages of LMWHs?

A

more expensive

cleared unchanged by kidney (DO NOT USE IN KIDNEY FAILURE)

41
Q

Which parenteral anticogulant drug promotes inhibition of Xa by antithrombin, is a nonheparin glycosaminoglycan, and is used in patients with heparin-induced thrombocytopenia?

A

Danaparoid

42
Q

What parenteral Anticoagulant drug is a direct thrombin (IIa) inhibitor- a derivative of hiruden(in leech). ?

A

Lepirudin

43
Q

What oral anticoagulant inhibits vitamin K epoxide reductase in the liver where clotting factors are synthesized?

A

Coumarins (Warfarin)

44
Q

How long does it take for Coumarins to become effective?

A

4-5 days. (active carboxylated factors must be cleared before inactive factors in the liver predominate)

45
Q

Coumarins have a _______ (steep or shallow) D-R curve, and a ______ (large/small) Vd

A

Steep
small
can easily become toxic with a small increase in dose.

46
Q

Warfarin is Teratogenic. This means what?

A

it crosses the placenta and causes birth defects and abortion.

47
Q

What is the use of Warfarin?

A

treats thrombo-embolic conditions

48
Q

Coumarins (warfarin) are metabolized by _____ and _____ enzymes.

A

CYP1A & CYP2C9

49
Q

What two main drug interactions should be watched for when taking Warfarin ?

A
  • Reduced effect in case of induction of enzymes

- Increased effect (hemorrhage) in case of reduced metabolism and/or displacement from protein binding.

50
Q

In the case of Warfarin overdose, what can be used as an antidote?

A

Excess Vitamin K uses the enzyme Diaphorase (not inhibited by warfarin) but cannot reduce vit K epoxide.

51
Q

Warfarin acts by blocking what enzyme?

A

Vitamin K epoxide reductase

52
Q

Direct Thrombin (IIa) inhibitors (Dabigatran) are useful in patients with ____________.

A

HIT - heparin-induced thrombocytopenia

53
Q

Comparison of Warfarin and newer Oral Anticoagulants:

Which has a slow onset and offset of action?

A

Warfarin

54
Q

Comparison of Warfarin and newer Oral Anticoagulants: what has a predictable anticoagulant effect?

A

Newer oral anticoagulants

55
Q

Comparison of Warfarin and newer Oral Anticoagulants:

What has a narrow therapeutic index?

A

Warfarin

56
Q

Comparison of Warfarin and newer Oral Anticoagulants:

What has a specific coagulation enzyme target so there is a low risk of other side effects?

A

Newer oral anticoagulants

57
Q

Comparison of Warfarin and newer Oral Anticoagulants:

Which has higher food and drug interactions? (lab tests needed)

A

warfarin

58
Q

Comparison of Warfarin and newer Oral Anticoagulants:

Which reduce synthesis of ALL vitamin K dependent proteins? (many side effects)

A

Warfarin

59
Q

Comparison of Warfarin and newer Oral Anticoagulants:

Which varies more in dose requirements and anticoagulant effect?

A

Warfarin

60
Q

What fibrinolytic drug dissolves clots after myocardial infarction, thrombosis, and pulmonary emboli?

A

Streptokinase

61
Q

Streptokinase may cause increased bleeding as a side effect because its believed to cause __________ (not just at sites of clot formation)

A

systemic plasmin formation

62
Q
Streptokinase side effects include :
B
A
Hypo
F
A

Bleeding
Allergic Reactions
Hypotension
Fever

63
Q

Streptokinase Contraindications:

A

Any type of tissue or brain damage.

64
Q

Tissue plasminogen activator (t-PA) activates ________________ and therefore theoretically is believed to act only at sites of clot formations but clinically does not turn out to be more specific than streptokinase. More expensive than streptokinase.

A

fibrin bound plasminogen. (less systemic plasmin formation)

65
Q

Tissue plasminogen activator is used in which 3 situations?

A

Myocardial infarction, thrombosis, pulmonary emboli