Pharmacology - ACS (Acute Coronary Syndrome) Part 2

Question 1

true or false

brilinta (ticagrelor) has a greater and more predictable inhibition of platelet aggregation than clopidogrel

Answer 1

true

Question 2

which drug is similar to brilinta (ticagrelor), but is mainly only different in that it is given IV and not PO?

Answer 2

cangrelor

Question 3

true or false

cangrelor is a reversible inhibitor and has the same MOA as ticagrelor

Answer 3

true

Question 4

true or false

the risk for bleeding is greater with cangrelor than with clopidogrel

Answer 4

true

Question 5

***recap from lipid:

if an OATP INHIBITOR is coadministered with atorvastatin, what will happen

Answer 5

increased risk of myopathy and liver toxicity

Question 6

**which GpIIb/IIIa receptor blockers ARE SPECIFIC for GpIIb/IIa

Answer 6

eptifibatide and tirofiban

NOT abciximab

Question 7

**which GpIIb/IIIa receptor blocker is a nonpeptide RGD-mimetic

Answer 7

tirofiban

Question 8

**which GpIIb/IIIa receptor blocker is a cyclical KGD-containing hexapeptide?

Answer 8

eptifibatide

Question 9

**which GpIIb/IIIa receptor blocker is a Fab fragment of humanized mouse monoclonal antibody

Answer 9

abciximab

Question 10

**which Gp IIb/IIIa receptor blockers have a SHORT PLASMA half life (minutes) and which have a LONG half life (~2 hours)

Answer 10

short - abciximab

long - eptifibatide and tirofiban

Question 11

**Whic Gp IIb/IIIa receptor blockers have a short PLATELET-BOUND half life and which have a LONG (DAYS) platelet-bound half life?

Answer 11

long (days) - abciximab

short (seconds) - eptifibatide and tirofiban (seconds)

Question 12

**which Gp IIb/IIIa receptor blockers are renally cleared and which are hepatically cleared?

Answer 12

abciximab is cleared by LIVER (all monoclonals cleared by liver)

eptifibatide and tirofiban are renally cleared

Question 13

name 4 things that cannot bind to Gp IIb/IIIa receptor in the presence of an inhibitor like abciximab

Answer 13

fibrinogen
fibronectin
von willebrand factor
vibronectin

Question 14

**important peptide sequence of tirofiban

Answer 14

RGD (arginine/glycine/aspartate)

Question 15

**important peptide sequence of eptifibatide

Answer 15

KGD (lysine/glycine/aspartate)

Question 16

true or false

abciximab has a short plasma half life but long platelet-bound half life

Answer 16

TRUE

platelet bound for days, only in plasma for 30 minst

Question 17

true or false

abciximab is given SUBQ

Answer 17

FALSE - IV

Question 18

AE abciximab

Answer 18

injection site rxns, bleeding, hypotension, bradycardia

Question 19

true or false

eptifibatide is a cyclic peptide derived from rattlesnake venom, and the critcal AA sequence is RGD

Answer 19

FALSE - everything true except the critical aa sequence is KGD

actual GpIIb/IIIa receptor is RGD residue, but KGD is close enough

Question 20

route administration eptifibatide

Answer 20

IV

Question 21

true or false

tirofiban is given IV

Answer 21

true

Question 22

true or false

tirofiban can be used for non STEMI

Answer 22

true

Question 23

dipyridamole MOA

Answer 23

inhibits PDE (mainly PDE5 specifically) (phosphodiesterase)

this is the enzyme that breaks down cAMP into AMP

therefore, dipyridamole will ultimately INCREASE cAMP levels – inhibits platelet aggregation

it is also a vasodilator, bc increased cGMP increases myosin light chain phosphatase. myosin light chain WITHOUT PHOSPHATE causes vasodilation

Question 24

true or false

dipyridamole has both vasodilator and antithrombotic effects

Answer 24

true

Question 25

explain what dipyridamole is approved for

Answer 25

secondary prevention of stroke when combined with low dose aspirin

Question 26

how is dipyridamole administered? is it highly protein bound? onset?

Answer 26

orally, fast onset (minutes) highly protein bound - DDI concern

Question 27

is the metabolite of dipyridamole active?

Answer 27

NO - no impact on bleeding time or platelet aggregation

Question 28

true or false dipyridamole does not improve mortality in patients with CAD, MI, DVT, or embolism

Answer 28

true - not shown to have mortality benefit. not really used

Question 29

cilostazol MOA

Answer 29

PDE3 inhibitor promotes vasodilation and inhibits platelet aggregation like dipyridamole - increased cGMP......etc

Question 30

cilostazol is primarily used to treat ___ ___

Answer 30

intermitten claudication

Question 31

3 AE of cilostazol

Answer 31

headache (30% of people!) diarrhea irregular heart beat

Question 32

true or false cilostazol is a PDE5 inhibitor

Answer 32

FALSE - PDE3 dipyridamole was PDE5