Thrombolytics, Anticoagulants, Anti-platelet drugs Flashcards

0
Q

High doses of Aspirin can see this neurologic side effect:

A

Tinnitus

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1
Q

Mechanism of action of Aspirin

A

Irreversible COX inhibitor, prevents thromboxane release

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2
Q

If given at a low dose, aspirin affects _____, if given at a high dose, aspirin affects ______.

A

Platelets, endothelial cells

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3
Q

What are the three ADP receptor antagonists?

A

Clopidogrel
Prasugrel
Ticlopidine

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4
Q

Which of the three ADP receptor antagonists has the most side effects?

A

Ticlopidine

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5
Q

Clopidogrel requires activation by _______

A

CYP2C19

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6
Q

What is a very serious side effect of Ticlopidine use?

A

Thrombotic thrombocytopenic purpura

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7
Q

What is the mechanism of action of Dipyridamol?

A

Inhibits phosphodiesterase, results in increased cAMP, decrease platelet activation

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8
Q

What is another effect of dipyridamol for vessels?

A

vasodilation

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9
Q

What is the mechanism of action of Abciximab?

A

Antibody that blocks GPIIb/IIIa, prevents binding of fibrinogen and vW factor to platelets

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10
Q

What is the mechanism of action of Eptifibatide and Tirofiban? What’s different about them?

A

Antagonists of GPIIa/IIIb

Eptifibatide is an analogue of fibrinogen, tirofiban is not a peptide

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11
Q

What is a major drawback to GPIIa/IIIb inhibitors?

A

Given IV

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12
Q

What are the four direct heparin inhibitors?

A

Lepirudin
Bivalirudin
Argatroban
Dabigatran etexylate

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13
Q

What are the three indirect thrombin inhibitors?

A

Heparin
LMW heparin
Fondaparinux

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14
Q

What do direct thrombin inhibitors do?

A

…directly inhibit the thrombin enzyme.

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15
Q

What do indirect thrombin inhibitors do?

A

Interact with antithrombin in its inactivation of factor Xa (which activates thrombin)
Also accelerate antithrombin’s deactivation of thrombin

16
Q

How does the mechanism of action of Heparin and fondaparinux differ?

A

Heparin takes out both factor Xa and thrombin

Fondaparinux only takes out Xa

17
Q

What are some side effects for heparin?

A

Bleeding

Heparin induced thrombocytopenia

18
Q

What drug is used to reverse activity of heparin?

A

Protamine

19
Q

What is the mechanism of action of warfarin?

A

Blocks synthesis of vitamin K dependent clotting factors

20
Q

What conversion of vitamin K does warfarin affect?

A

vitamin K epoxide to vitamin K hydroquinone

21
Q

What factors are affected by warfarin use?

A

factors II, VII, IX, X, and protein C

22
Q

What is unique about warfarin’s effects on protein C?

A

Its effects initially cause a hyper-coagulable state

23
Q

What do you give along with warfarin at first administration?

A

heparin

24
Q

What are the side effects of Warfarin?

A

Bleeding
Flatulence and diarrhea
cutaneous necrosis
chondrodysplasia punctata

25
Q

What is the more active enantiomer of warfarin?

A

S

26
Q

What are the S and R enantiomers of warfarin metabolized by in the liver?

A

R: CYP 1A1, 1A2, 3A4
S: CYP 2C39

27
Q

Which drug that we’ve been learning about has a crazy long list of drug/drug interactions?

A

Warfarin

28
Q

Pharmacokinetic drug interactions of oral anticoagulants are primarily due to the following three things:

A

Enzyme induction
Enzyme inhibition
Reduced plasma protein binding

29
Q

Pharmacodynamic drug/drug interactions for oral anticoagulants are primarily due to these three things:

A

Reduced clotting factor synthesis
Competitive antagonism with Vitamin K
Hereditary resistance to oral anticoag

30
Q

What drug should be given to antidote overdose of warfarin?

A

Phytonadione (Vitamin K from plants)

31
Q

What does tPA stand for and what three are we supposed to know?

A

Tissue plasminogen activators.
Alteplase
Reteplase
Tenecteplase

32
Q

What drawback does the tPA drug have?

A

Given IV, Cost

33
Q

What are the tPA’s particularly good for treating?

A

stroke