Hosam Mohamed-
competitive inhibitors of HMG-CoA reductase; decreases the synthesis of cholesterol & increases the number of LDL-receptors
Statin MOA?
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f; decrease TGs & small increase in HDL
Statins only affect LDL. T/F?
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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?
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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
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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
