competitive inhibitors of HMG-CoA reductase; decreases the synthesis of cholesterol & increases the number of LDL-receptors
Statin MOA?
f; decrease TGs & small increase in HDL
Statins only affect LDL. T/F?
at night; cholesterol synthesis occurs mostly at night
When should we advise patients to take statins? Why?
OATP1B1
located on the basolateral surface of hepatocytes and facilitates uptake of drugs into the liver.
a, e, f
Which statin(s) are metabolized by CYP3A4?
a) lovastatin
b) pravastatin
c) fluvastatin
d) rosuvastatin
e) atorvastatin
f) simvastatin
g) pitavastatin
fluvastatin
Which statin(s) are metabolized by CYP2C9?
g
Which statin(s) are metabolized by UGT1A3/UGT2B7?
a) lovastatin
b) pravastatin
c) fluvastatin
d) rosuvastatin
e) atorvastatin
f) simvastatin
g) pitavastatin
rosuvastatin
Which statin(s) is metabolized by BOTH CYP2C9 & CYP2C19?
a, f
Which statin(s) are prodrugs?
a) lovastatin
b) pravastatin
c) fluvastatin
d) rosuvastatin
e) atorvastatin
f) simvastatin
rosuvastatin, pitavastatin, atorvastatin
Which statin(s) have long half-lives? (3)
SLCO1B1
the gene responsible for encoding the hepatic transporter protein
b
Who is more likely to experience AE's when taking Statins?
a) Normal function
b) poor metabolizer (increased function)
c) rapid metabolizer (increased function)
inhibits ACL enzyme; decreases cholesterol synthesis, cholesterol in the liver, and plasma LDL ; increases LDL receptors
Bempedoic Acid MOA?
d
What is the enzyme responsible for activating Bempedoic Acid?
a) CYP3A4
b) CYP2C9
c) OATP1B1
d) ACSVL1
T
Bempedoic acid is a prodrug. T/F?
alirocumab, evolocumab,
What are the PCSK9 inhibitors?
block the binding of PCSK9 to LDL-R complex; prevent degradation of LDL receptors, increase LDL-R recycling; increased LDL clearance
PCSK9 inhibitors MOA?
statins increase PCSK9 levels; this protects LDL-Rs from degradation
Why is it beneficial to add a PCSK9 inhibitor to a statin?
siRNA molecule that cleaves PCSK9 mRNA
Inclisiran MOA?
chylomicrons, VLDL
Which lipids transport Triglycerides?
Gemfibrozil, fenofibrate
What are the fibrates?
activate the transcription factor of PPAR-a; increasing clearance of VLDL & decreasing synthesis of fatty acids
Fibrates MOA?
inhibits TG synthesis, increases VLDL clearance by lipoprotein lipase, decreases HDL catabolism
Niacin MOA?
activates PPAR; increasing lipoprotein lipase activity & fatty acid b oxidation; inhibits DGAT; decreasing biosynthesis/secretion
Omega-3 Fatty acids MOA?
a,b
Which drugs inhibit cholesterol synthesis?
a) statins
b) bempedoic acid
c) ezetimibe
d) bile acid-binding resins
e) PCSK9 inhibitors
f) Inclisiran
g) fibrates
h) niacin
i) icosapent ethyl
c
Which drugs inhibit sterol absorption?
a) statins
b) bempedoic acid
c) ezetimibe
d) bile acid-binding resins
e) PCSK9 inhibitors
f) Inclisiran
g) fibrates
h) niacin
i) icosapent ethyl
d
Which drugs inhibit enterohepatic recirculation of bile salts?
a) statins
b) bempedoic acid
c) ezetimibe
d) bile acid-binding resins
e) PCSK9 inhibitors
f) Inclisiran
g) fibrates
h) niacin
i) icosapent ethyl
e, f
Which drugs inhibit degradation of LDL-R?
a) statins
b) bempedoic acid
c) ezetimibe
d) bile acid-binding resins
e) PCSK9 inhibitors
f) Inclisiran
g) fibrates
h) niacin
i) icosapent ethyl
a
Which Omega-3 Fatty acid contains both EPA & DHA?
a) Lovaza
b) Vascepa
statins, bempedoic acid, ezetimibe, BAB resins, PCSK9 inhibitors, Inclisiran
Which drugs lower LDL? (6)
fibrates, statins, niacin, vascepa
Which drugs decrease VLDL? (4)
statins, fibrates, niacin
Which drugs increase HDL? (3)
statins, fibrates, niacin
Which drugs decrease Triglycerides? (3)
fibrates, lovaza
Which drugs can actually increase LDL? (2)
h
Which agent is the most effective for increasing HDL?
a) statins
b) bempedoic acid
c) ezetimibe
d) bile acid-binding resins
e) PCSK9 inhibitors
f) Inclisiran
g) fibrates
h) Niacin
i) icosapent ethyl
c
Which drug has DDI with warfarin & sulfonlyureas?
a) statins
b) ezetimibe
c) fibrates
d) niacin
e) omega-3 FA
Bile Acid- Resin
-large polymeric cationic exchange resin that blocks the production of bile acid formation.
- causes LDL receptors to increase and absorb more cholesterol to convert into bile.
Ezetimibe
-selective inhibitor of intestinal absorption through blockage of sterol transporter NPC1L1