Thrombolytics, Anticoagulants, Anti-platelet drugs

Question 0

High doses of Aspirin can see this neurologic side effect:

Answer 0

Tinnitus

Question 1

Mechanism of action of Aspirin

Answer 1

Irreversible COX inhibitor, prevents thromboxane release

Question 2

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

Answer 2

Platelets, endothelial cells

Question 3

What are the three ADP receptor antagonists?

Answer 3

Clopidogrel
Prasugrel
Ticlopidine

Question 4

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

Answer 4

Ticlopidine

Question 5

Clopidogrel requires activation by _______

Answer 5

CYP2C19

Question 6

What is a very serious side effect of Ticlopidine use?

Answer 6

Thrombotic thrombocytopenic purpura

Question 7

What is the mechanism of action of Dipyridamol?

Answer 7

Inhibits phosphodiesterase, results in increased cAMP, decrease platelet activation

Question 8

What is another effect of dipyridamol for vessels?

Answer 8

vasodilation

Question 9

What is the mechanism of action of Abciximab?

Answer 9

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

Question 10

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

Answer 10

Antagonists of GPIIa/IIIb

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

Question 11

What is a major drawback to GPIIa/IIIb inhibitors?

Answer 11

Given IV

Question 12

What are the four direct heparin inhibitors?

Answer 12

Lepirudin
Bivalirudin
Argatroban
Dabigatran etexylate

Question 13

What are the three indirect thrombin inhibitors?

Answer 13

Heparin
LMW heparin
Fondaparinux

Question 14

What do direct thrombin inhibitors do?

Answer 14

…directly inhibit the thrombin enzyme.

Question 15

What do indirect thrombin inhibitors do?

Answer 15

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

Question 16

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

Answer 16

Heparin takes out both factor Xa and thrombin

Fondaparinux only takes out Xa

Question 17

What are some side effects for heparin?

Answer 17

Bleeding

Heparin induced thrombocytopenia

Question 18

What drug is used to reverse activity of heparin?

Answer 18

Protamine

Question 19

What is the mechanism of action of warfarin?

Answer 19

Blocks synthesis of vitamin K dependent clotting factors

Question 20

What conversion of vitamin K does warfarin affect?

Answer 20

vitamin K epoxide to vitamin K hydroquinone

Question 21

What factors are affected by warfarin use?

Answer 21

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

Question 22

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

Answer 22

Its effects initially cause a hyper-coagulable state

Question 23

What do you give along with warfarin at first administration?

Answer 23

heparin

Question 24

What are the side effects of Warfarin?

Answer 24

Bleeding Flatulence and diarrhea cutaneous necrosis chondrodysplasia punctata

Question 25

What is the more active enantiomer of warfarin?

Answer 25

S

Question 26

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

Answer 26

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

Question 27

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

Answer 27

Warfarin

Question 28

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

Answer 28

Enzyme induction Enzyme inhibition Reduced plasma protein binding

Question 29

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

Answer 29

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

Question 30

What drug should be given to antidote overdose of warfarin?

Answer 30

Phytonadione (Vitamin K from plants)

Question 31

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

Answer 31

Tissue plasminogen activators. Alteplase Reteplase Tenecteplase

Question 32

What drawback does the tPA drug have?

Answer 32

Given IV, Cost

Question 33

What are the tPA's particularly good for treating?

Answer 33

stroke