Pharmacology - ACS (Acute Coronary Syndrome) Part 2 Flashcards
true or false
brilinta (ticagrelor) has a greater and more predictable inhibition of platelet aggregation than clopidogrel
true
which drug is similar to brilinta (ticagrelor), but is mainly only different in that it is given IV and not PO?
cangrelor
true or false
cangrelor is a reversible inhibitor and has the same MOA as ticagrelor
true
true or false
the risk for bleeding is greater with cangrelor than with clopidogrel
true
***recap from lipid:
if an OATP INHIBITOR is coadministered with atorvastatin, what will happen
increased risk of myopathy and liver toxicity
**which GpIIb/IIIa receptor blockers ARE SPECIFIC for GpIIb/IIa
eptifibatide and tirofiban
NOT abciximab
**which GpIIb/IIIa receptor blocker is a nonpeptide RGD-mimetic
tirofiban
**which GpIIb/IIIa receptor blocker is a cyclical KGD-containing hexapeptide?
eptifibatide
**which GpIIb/IIIa receptor blocker is a Fab fragment of humanized mouse monoclonal antibody
abciximab
**which Gp IIb/IIIa receptor blockers have a SHORT PLASMA half life (minutes) and which have a LONG half life (~2 hours)
short - abciximab
long - eptifibatide and tirofiban
**Whic Gp IIb/IIIa receptor blockers have a short PLATELET-BOUND half life and which have a LONG (DAYS) platelet-bound half life?
long (days) - abciximab
short (seconds) - eptifibatide and tirofiban (seconds)
**which Gp IIb/IIIa receptor blockers are renally cleared and which are hepatically cleared?
abciximab is cleared by LIVER (all monoclonals cleared by liver)
eptifibatide and tirofiban are renally cleared
name 4 things that cannot bind to Gp IIb/IIIa receptor in the presence of an inhibitor like abciximab
fibrinogen
fibronectin
von willebrand factor
vibronectin
**important peptide sequence of tirofiban
RGD (arginine/glycine/aspartate)
**important peptide sequence of eptifibatide
KGD (lysine/glycine/aspartate)
true or false
abciximab has a short plasma half life but long platelet-bound half life
TRUE
platelet bound for days, only in plasma for 30 minst
true or false
abciximab is given SUBQ
FALSE - IV
AE abciximab
injection site rxns, bleeding, hypotension, bradycardia
true or false
eptifibatide is a cyclic peptide derived from rattlesnake venom, and the critcal AA sequence is RGD
FALSE - everything true except the critical aa sequence is KGD
actual GpIIb/IIIa receptor is RGD residue, but KGD is close enough
route administration eptifibatide
IV
true or false
tirofiban is given IV
true
true or false
tirofiban can be used for non STEMI
true
dipyridamole MOA
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
true or false
dipyridamole has both vasodilator and antithrombotic effects
true
explain what dipyridamole is approved for
secondary prevention of stroke when combined with low dose aspirin
how is dipyridamole administered? is it highly protein bound? onset?
orally, fast onset (minutes)
highly protein bound - DDI concern
is the metabolite of dipyridamole active?
NO - no impact on bleeding time or platelet aggregation
true or false
dipyridamole does not improve mortality in patients with CAD, MI, DVT, or embolism
true - not shown to have mortality benefit. not really used
cilostazol MOA
PDE3 inhibitor
promotes vasodilation and inhibits platelet aggregation
like dipyridamole - increased cGMP……etc
cilostazol is primarily used to treat ___ ___
intermitten claudication
3 AE of cilostazol
headache (30% of people!)
diarrhea
irregular heart beat
true or false
cilostazol is a PDE5 inhibitor
FALSE - PDE3
dipyridamole was PDE5
