PMC EXAM 4 QUESTIONS AND ANSWERS
Aspirin MOA - Answers :inhibits the synthesis of thromboxane A2 (TXA2) by irreversible
acetylation of COX-1
-inhibits platelet activation and aggregation
Aspirin Drug Interactions - Answers :NSAIDs compete for binding sites
-use APAP or narcotic analgesics
Aspirin Toxicities - Answers :-bleeding
-hemorrhagic stroke
-can cause asthma and hypersensitivity in aspirin-intolerant pts
What are the thienopyridines? - Answers :Clopidogrel, Prasugrel, Ticlopidine
Thienopyridine MOA - Answers :Reduce platelet aggregation by inhibiting the ADP
pathway
-bind and irreversibly block the P24(12)ADP receptor
Do thienopyridines affect prostaglandin metabolism? - Answers :No
How do genetic variations affect clopidogrel therapy? - Answers :-Prodrug activated by
CYP2C19
-Patients with genetic polymorphisms of CYP2C19 have reduced enzyme activity
-may experience more cardiovascular events
Thienopyridine drug interactions - Answers :-PPIs inhibit CYP2C19
-use a H2-blocker
What is unique about eptifibatide and tirofiban? - Answers :-bind reversibly to the
GPIIb/IIIa receptor complex of activated platelets
-specifically inhibit the binding of fibrinogen to the receptor complex
GPIIb/IIIa receptor antagonist toxicities - Answers :bleeding and thrombocytopenia
What is the PAR-1 antagonist? - Answers :Vorapaxar
How do you use vorapaxar? - Answers :with aspirin and/or clopidogrel to reduce the risk
of thrombotic cardiovascular events in patients with peripheral arterial disease or hx of
MI
Vorapaxar MOA - Answers :-blocks protease-activated receptor-01 (PAR-1), the major
thrombin receptor on platelets and inhibits thrombin-induced platelet aggregation
Vorapaxar toxicities - Answers :-bleeding, anemia, depression, rash
, Vorapaxar contraindications - Answers :hx of stroke, transient ischemic attack, or
intracranial hemorrhage
-pts with pathological bleeding
Can you use vorapaxar with CYP3A4 inhibitors? - Answers :No-it is a substrate of
CYP3A4
What is the dipyridamole? - Answers :Persantin
Persantin MOA - Answers :inhibits platelet aggregation by inhibiting platelet uptake of
adenosine and blocking ADP-induced platelet aggregation
How do you use Persantin? - Answers :with aspirin or warfarin
Persantin toxicites - Answers :severe headache and diarrhea
Which class of drugs is the most effective at reducing LDL levels? - Answers :HMG-CoA
reductase inhibitors (the statins)
HMG-CoA reductase Inhibitors MOA - Answers :-structural analogs of the HMG-CoA
intermediate formed during the reductive conversion of HMG-CoA to mevalonate
-competitive inhibitors of HMG-CoA
-also increase high-affinity LDL receptors (increases extraction of ILDLs, reducing
plasma LDL)
HMG-CoA reductase inhibitor toxicities - Answers :-elevation of serum aminotransferase
activity
-elevation of serum creatine kinase activity
-elevated A1c and fasting glucose levels
-myopathy (rhabdomyolysis)--> rare
-cognitive impairment (rare)
Niacin MOA - Answers :1. inhibits VLDL secretion from hepatocytes (decreased LDL
production)
2. inhibits intracellular lipase of adipose tissue (reduces VLDL production)
3. induces clearance of VLDL via the LPL pathway (decrease in triglyceride levels)
4. inhibits intracellular lipase (fewer FFAs, less VLDL production)
Niacin toxicities - Answers :skin flushing, pruritus, glucose intolerance, hyperuricemia,
and heptatoxicity
What is the cyclopenyltriazolopyridine? - Answers :Ticagrelor (Brilinta)
How is ticagrelor used? - Answers :with low-dose aspirin to reduce the rate of
thrombotic cardiovascular events
Aspirin MOA - Answers :inhibits the synthesis of thromboxane A2 (TXA2) by irreversible
acetylation of COX-1
-inhibits platelet activation and aggregation
Aspirin Drug Interactions - Answers :NSAIDs compete for binding sites
-use APAP or narcotic analgesics
Aspirin Toxicities - Answers :-bleeding
-hemorrhagic stroke
-can cause asthma and hypersensitivity in aspirin-intolerant pts
What are the thienopyridines? - Answers :Clopidogrel, Prasugrel, Ticlopidine
Thienopyridine MOA - Answers :Reduce platelet aggregation by inhibiting the ADP
pathway
-bind and irreversibly block the P24(12)ADP receptor
Do thienopyridines affect prostaglandin metabolism? - Answers :No
How do genetic variations affect clopidogrel therapy? - Answers :-Prodrug activated by
CYP2C19
-Patients with genetic polymorphisms of CYP2C19 have reduced enzyme activity
-may experience more cardiovascular events
Thienopyridine drug interactions - Answers :-PPIs inhibit CYP2C19
-use a H2-blocker
What is unique about eptifibatide and tirofiban? - Answers :-bind reversibly to the
GPIIb/IIIa receptor complex of activated platelets
-specifically inhibit the binding of fibrinogen to the receptor complex
GPIIb/IIIa receptor antagonist toxicities - Answers :bleeding and thrombocytopenia
What is the PAR-1 antagonist? - Answers :Vorapaxar
How do you use vorapaxar? - Answers :with aspirin and/or clopidogrel to reduce the risk
of thrombotic cardiovascular events in patients with peripheral arterial disease or hx of
MI
Vorapaxar MOA - Answers :-blocks protease-activated receptor-01 (PAR-1), the major
thrombin receptor on platelets and inhibits thrombin-induced platelet aggregation
Vorapaxar toxicities - Answers :-bleeding, anemia, depression, rash
, Vorapaxar contraindications - Answers :hx of stroke, transient ischemic attack, or
intracranial hemorrhage
-pts with pathological bleeding
Can you use vorapaxar with CYP3A4 inhibitors? - Answers :No-it is a substrate of
CYP3A4
What is the dipyridamole? - Answers :Persantin
Persantin MOA - Answers :inhibits platelet aggregation by inhibiting platelet uptake of
adenosine and blocking ADP-induced platelet aggregation
How do you use Persantin? - Answers :with aspirin or warfarin
Persantin toxicites - Answers :severe headache and diarrhea
Which class of drugs is the most effective at reducing LDL levels? - Answers :HMG-CoA
reductase inhibitors (the statins)
HMG-CoA reductase Inhibitors MOA - Answers :-structural analogs of the HMG-CoA
intermediate formed during the reductive conversion of HMG-CoA to mevalonate
-competitive inhibitors of HMG-CoA
-also increase high-affinity LDL receptors (increases extraction of ILDLs, reducing
plasma LDL)
HMG-CoA reductase inhibitor toxicities - Answers :-elevation of serum aminotransferase
activity
-elevation of serum creatine kinase activity
-elevated A1c and fasting glucose levels
-myopathy (rhabdomyolysis)--> rare
-cognitive impairment (rare)
Niacin MOA - Answers :1. inhibits VLDL secretion from hepatocytes (decreased LDL
production)
2. inhibits intracellular lipase of adipose tissue (reduces VLDL production)
3. induces clearance of VLDL via the LPL pathway (decrease in triglyceride levels)
4. inhibits intracellular lipase (fewer FFAs, less VLDL production)
Niacin toxicities - Answers :skin flushing, pruritus, glucose intolerance, hyperuricemia,
and heptatoxicity
What is the cyclopenyltriazolopyridine? - Answers :Ticagrelor (Brilinta)
How is ticagrelor used? - Answers :with low-dose aspirin to reduce the rate of
thrombotic cardiovascular events
