Pharm/Thrombolytics

Question 1

Anticoagulants are useful for what?

Answer 1

prevent both arterial and venous thromboses

Question 2

Antiplatelet drugs are useful for what?

Answer 2

Prevent arterial venous thrombosis only, not as good at preventing venous thrombi (bc platelets have a bigger role in arteries)

Question 3

Aspirin MOA

Answer 3

irreversible COX1 and COX2 inhibitor that prevents prostacyclin (ups cAMP) and platelet thromboxane synthesis

acetyl group is transferred to COX and permanently inactivates them

Question 4

Aspirin is also known as

Answer 4

Acetylsalicylic acid (ASA)

Question 5

What are the major side effects of aspirin?

Answer 5

GI bleeding
hemorrhagic stroke
asthma (leukotrienes)

Question 6

Contraindications for aspirin?

Answer 6

Hx of peptic ulcers, asthma (bc aspirin inc leukotrienes in asthmatics); coumarin anticoags (bc inc risk of bleeding)

Question 7

What happens if you take ibuprofen and aspirin together?

Answer 7

Ibuprofen outcompetes for platelets; meanwhile aspirin is excreted; then when ibuprofen is excreted soon thereafter you have no antiplatelet effect

Question 8

Who should take aspirin?

Answer 8

Males over 45 and females over 55 who have at least one risk factor for CHD

Question 9

Dipyridamole MOA

Answer 9

PDE inhibitor

Inc cAMP which dec platelet Ca2+, therefore inhibiting platelets

Question 10

How does dipyridamole monotherapy compare to + aspirin?

Answer 10

Alone it reduces risk of stroke OK but the reduction is better with aspirin combination

General idea is that there are so many ways to activate/block platelets that going for multiple targets will give an increased effect

Question 11

What is the dipyridamole + aspirin combination called?

Answer 11

Aggranox

Question 12

DTIs

Answer 12

block thrombin receptor on platelets

Question 13

Clopidogrel MOA

Answer 13

prodrug metabolized by CYP2C19; P2Y12 receptor blocker

ADP antagonist

Question 14

Prasugrel MOA

Answer 14

ADP antagonist

Question 15

What does ADP do to platelets?

Answer 15

Binds surface receptor and causes fibrinogen receptor activation and TXA2 generation

Question 16

Clopidogrel - why would you choose it over prasugrel?

Answer 16

Clopidogrel has a lower incidence of bleeding

Question 17

What is a significant contraindication for clopidogrel?

Answer 17

Want to know CYP2C19 genotype since it is required to convert the prodrug into active drug

Question 18

Clopidogrel outperforms aspirin for what indication?

Answer 18

Peripheral artery disease risk reduction (CAPRIE study)

Question 19

Clopidogrel and CABG

Answer 19

discontinue 5 days beforehand

Question 20

Eptifibidate MOA

Answer 20

peptide that binds fibrinogen receptor site of GpIIb/IIIa to block formation of primary hemostatic plug

Question 21

Abciximab MOA

Answer 21

Antibody fragment to GpIIb/IIIa receptor

Question 22

Which drugs are great to use before coronary artery angioplasty?

Answer 22

Abciximab and Eptifibidate

Question 23

What drugs are always used simultaneously with thrombolytic agents

Answer 23

aspirin and heparin

Question 24

What is the most serious side effect of thrombolytics?

Answer 24

Intracranial hemorrhage

Question 25

Major contraindications of thrombolytics?

Answer 25

Situations where you would have uncontrollable bleeding (i.e., noncompressible vessel, uncontrolled HT) Being old, recent surgery, GI bleeding, etc.

Question 26

What are the thrombolytics we learned about?

Answer 26

Streptokinase and urokinase

Question 27

Streptokinase MOA

Answer 27

Forms activator complex with plasminogen (no intrinsic protease activity)

Question 28

What is a major streptokinase side effect?

Answer 28

Immunogenic Generate antibodies to streptococci May induce serum sickness second time around, so you can only give it ONCE

Question 29

Urokinase MOA

Answer 29

Naturally occurring serine protease that cleaves plasminogen to plasmin

Question 30

What is an advantage of urokinase over streptokinase?

Answer 30

Non-immunogenic

Question 31

t-PA MOA

Answer 31

Serine protease that complexes with fibrin and plasminogen to localize plasminogen activation

Question 32

Downside of t-PA

Answer 32

Rapidly metabolized

Question 33

Reteplase MOA

Answer 33

variant of t-PA that is smaller and is metabolized more slowly

Question 34

Compare t-PA vs Reteplase ROA

Answer 34

t-PA metabolized quickly so it must be continuous infusion whereas reteplase is recombinant smaller version that is metabolized more slowly so given IV bolus

Question 35

How do fibrinolysis and angioplasty compare

Answer 35

Angioplasty is preferred for acute MI

Question 36

Aminocaproic Acid MOA

Answer 36

lysine analog that inhibits plasmin

Question 37

If a hemophiliac is about to go to the dentist what should they do

Answer 37

Take aminocaproic acid

Question 38

What is the most effective drug for preventing MI/stroke in patients with atrial fibrillation?

Answer 38

Warfarin

Question 39

What's the best treatment for post-MI and for stent placement

Answer 39

aspirin + clopidogrel

Question 40

Warfarin inhibits proper synthesis of these factors

Answer 40

prothrombin, 7, 9, 10, S, C

Question 41

Leperidin MOA

Answer 41

Direct thrombin inhibitor

Question 42

How is leperidin cleared?

Answer 42

kidneys

Question 43

Argatroban

Answer 43

Small direct thrombin inhibitor

Question 44

How is argatroban cleared?

Answer 44

Liver

Question 45

Bivalirudin MOA

Answer 45

thrombin direct inhibitor

Question 46

HIT treatment

Answer 46

bivalirudin

Question 47

RIvaroxaban MOA

Answer 47

direct anti-Xa inhibitor

Question 48

Dabigatran MOA

Answer 48

direct thrombin inhibitor

Question 49

Apixaban MOA

Answer 49

direct anti-Xa inhibitor