Anti-hyperlipidemics

Question 1

functions of cholesterol

Answer 1

1. essential component of cell membranes
2. precursor to sterols and steroids

Question 2

functions of triglyceride

Answer 2

1. storage form of fuel to support generation of high energy compounds
2. component of structural lipids

Question 3

what do lipoproteins do?

Answer 3

transport cholesterol and triglycerides in the blood

Question 4

rank lipoproteins from largest to smallest

Answer 4

chylomicron (largest)
VLDL
LDL
HDL (smallest)

Question 5

chylomicrons are involved in transport of __________ from the _____ to the ________ & _____________

Answer 5

dietary lipids
gut
liver
adipose tissue

Question 6

VLDL are secreted by the ________ into the blood as a source of ________________

Answer 6

liver
triglycerides

Question 7

LDL are the main form of __________ in the blood

Answer 7

cholesterol

Question 8

HDL are secreted by the ________ and acquire ___________ from ________ ____________ and ______________

Answer 8

liver
cholesterol
peripheral tissues
atheromas

(reverse cholesterol transport)

Question 9

which lipoprotein has the highest concentration of cholesterol?

Answer 9

LDL

Question 10

which lipoprotein has the highest concentration of triglycerides?

Answer 10

chylomicrons

Question 11

which lipoprotein has concentration of protein (and phospholipids lowkey)

Answer 11

HDL

Question 12

which apoproteins are produced in the liver?

Answer 12

ApoA-I (and intestine)
ApoB-100
ApoE (and other tissues)

Question 13

which apoprotein is structural in chylomicrons?

Answer 13

ApoB-48

Question 14

which apoprotein binds to lipoprotein lipase to enhance triglyceride hydrolysis?

Answer 14

ApoCII

Question 15

TC:HDL > _____ is associated with increased risk of CVD

Answer 15

4.5

Question 16

TC:HDL < ________ is desirable

Answer 16

3.5

Question 17

mechanism of action of bile acid resins

Answer 17

inhibit reabsorption of bile acids from intestine by binding bile acids to form insoluble complex excreted in feces

exchange Cl- ioins for bile acids

Question 18

bild acid resin drug interactions (may bind other drugs)

Answer 18

acetaminophen
thiazides
warfarin
fibrates
ezetimibe
oral contraceptives
corticosteroids

Question 19

mechanism of action of ezetimibe

Answer 19

inhibits intestinal absorption of cholesterol from diet and reabsorption of cholesterol in bile

Question 20

mechanism of action of HMG-CoA reductase inhibitors (statins)

Answer 20

competitively inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis

up-regulate LDL receptors enabling more LDL delivered to liver, thus reducing plasma cholesterol

Question 21

which statins are metabolized by CYP3A4?

Answer 21

Lovastatin, simvastatin, atorvastatin

Question 22

which statins are metabolized by CYP2C9?

Answer 22

Fluvastatin, rosuvastatin

Question 23

which statin undergoes sulfation?

Answer 23

pravastatin

Question 24

which statin is mainly excreted unchanged in bile?

Answer 24

pitavastatin

(pravastatin is also mostly excreted unchanged)

Question 25

HMG-CoA reductase inhibitors adverse effects

Answer 25

skeletal muscle effects - monitor serum creatine phosphokinase (protein in skeletal muscle)
-> increased incidence when co-adm. with CYP inhibitors

hepatotoxicity - monitor serum transaminase activity

Question 26

What is homozygous familial hypercholesterolemia?

Answer 26

a mutation where LDLR function is severely reduced

Question 27

three drugs used for homozygous familial hypercholesterolemia

Answer 27

1. Juxtapid (Lomitapide)
2. Mipomersen (Kynamro)
3. Evinacumab-dgnb (Evkeeza)

Question 28

three drugs that primarily reduce serum triglycerides (over LDL)

Answer 28

1. Fibrates
2. Niacin
3. Omega-3 fatty acids

Question 29

what does niacin do in adipose tissue?

Answer 29

decreases fatty acid transport to liver

Question 30

what does niacin do in the liver?

Answer 30

reduces TG export via VLDL, which increases HDL levels and reverse transport