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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
``` What are the 4 Aspirin Contraindications: V H H P ```
Vitamin K deficiency Hemophilia Hypoprothrombinemia Pregnancy/Childbirth
26
What Antiplatelet prodrug is used in combination with asprin that has CYP enzyme related drug interactions? (less neutropenia)
Clopidogrel
27
What Antiplatelet prodrug is used in combination with asprin and is potent. It has no CYP related drug interactions
Prasugrel
28
What Antiplatelet drug is potent and has CYP enzyme related drug interactions?
Ticagrelor
29
What Antiplatelet prodrug may cause severe neutropenia in 1% of patients?
Ticlopidine
30
Heparin is a _______ly charged molecule. This causes it to not cross the cell membrane easily.
negatively
31
Heparin is found in what type of cells?
mast cells
32
______________ 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
Antithrombin III
33
Heparin toxicity leads to ________. this can be treated using _____________.
Hemorrhage | Protamine sulfate
34
HIT = ______________
heparin-induced thrombocytopenia.
35
___________ is when there is more than 50% decrease in platelet count due to antigen antibody reaction.
Thrombocytopenia
36
HIT incidence can be lowered by the use of what 2 alternative anticoagulants?
Thrombin | factor Xa Inhibitors
37
``` What are the 4 main Therapeutic uses for Heparin? V P H P ```
Venous thrombosis pulmonary embolism Any Heart surgery DRUG OF CHOICE - during pregnancy (does not cross placenta)
38
LMWH have no space to bind _________. But can still inactivate _________.
thrombin IIA | factor Xa
39
What are the 3 major advantages of LMWHs? A O T & H
Better absorbed (higher bioavailability) Given subcutaneously without lab monitoring (outpatients) Lower risk of thrombocytopenia and bleeding (hemorrhage)
40
What are the 2 disadvantages of LMWHs?
more expensive | cleared unchanged by kidney (DO NOT USE IN KIDNEY FAILURE)
41
Which parenteral anticogulant drug promotes inhibition of Xa by antithrombin, is a nonheparin glycosaminoglycan, and is used in patients with heparin-induced thrombocytopenia?
Danaparoid
42
What parenteral Anticoagulant drug is a direct thrombin (IIa) inhibitor- a derivative of hiruden(in leech). ?
Lepirudin
43
What oral anticoagulant inhibits vitamin K epoxide reductase in the liver where clotting factors are synthesized?
Coumarins (Warfarin)
44
How long does it take for Coumarins to become effective?
4-5 days. (active carboxylated factors must be cleared before inactive factors in the liver predominate)
45
Coumarins have a _______ (steep or shallow) D-R curve, and a ______ (large/small) Vd
Steep small can easily become toxic with a small increase in dose.
46
Warfarin is Teratogenic. This means what?
it crosses the placenta and causes birth defects and abortion.
47
What is the use of Warfarin?
treats thrombo-embolic conditions
48
Coumarins (warfarin) are metabolized by _____ and _____ enzymes.
CYP1A & CYP2C9
49
What two main drug interactions should be watched for when taking Warfarin ?
- Reduced effect in case of induction of enzymes | - Increased effect (hemorrhage) in case of reduced metabolism and/or displacement from protein binding.
50
In the case of Warfarin overdose, what can be used as an antidote?
Excess Vitamin K uses the enzyme Diaphorase (not inhibited by warfarin) but cannot reduce vit K epoxide.
51
Warfarin acts by blocking what enzyme?
Vitamin K epoxide reductase
52
Direct Thrombin (IIa) inhibitors (Dabigatran) are useful in patients with ____________.
HIT - heparin-induced thrombocytopenia
53
Comparison of Warfarin and newer Oral Anticoagulants: Which has a slow onset and offset of action?
Warfarin
54
Comparison of Warfarin and newer Oral Anticoagulants: what has a predictable anticoagulant effect?
Newer oral anticoagulants
55
Comparison of Warfarin and newer Oral Anticoagulants: | What has a narrow therapeutic index?
Warfarin
56
Comparison of Warfarin and newer Oral Anticoagulants: | What has a specific coagulation enzyme target so there is a low risk of other side effects?
Newer oral anticoagulants
57
Comparison of Warfarin and newer Oral Anticoagulants: Which has higher food and drug interactions? (lab tests needed)
warfarin
58
Comparison of Warfarin and newer Oral Anticoagulants: | Which reduce synthesis of ALL vitamin K dependent proteins? (many side effects)
Warfarin
59
Comparison of Warfarin and newer Oral Anticoagulants: Which varies more in dose requirements and anticoagulant effect?
Warfarin
60
What fibrinolytic drug dissolves clots after myocardial infarction, thrombosis, and pulmonary emboli?
Streptokinase
61
Streptokinase may cause increased bleeding as a side effect because its believed to cause __________ (not just at sites of clot formation)
systemic plasmin formation
62
``` Streptokinase side effects include : B A Hypo F ```
Bleeding Allergic Reactions Hypotension Fever
63
Streptokinase Contraindications:
Any type of tissue or brain damage.
64
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.
fibrin bound plasminogen. (less systemic plasmin formation)
65
Tissue plasminogen activator is used in which 3 situations?
Myocardial infarction, thrombosis, pulmonary emboli

Phpy 305 (5 decks)

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