(3) Blood & Inflammation: Dyslipidemia (2.1-2.3)

Question 1

How is dietary cholesterol sent to the liver?

Answer 1

(1) Converted to cholesterol esters
(2) Packaged in chylomicrons

Question 2

Which apoliproteins do chylomicrons have?

Answer 2

A-E

(A, B, C, E)

Question 3

What enzyme releases FFAs from chylomicrons and VLDLs?

Answer 3

LPL

(Lipoprotein Lipase)

Question 4

What is the receptor and ligand for receptor-mediated endocytosis of chylomicrons?

Answer 4

Receptor: LDL receptor

Ligand: ApoE

Question 5

What is the product of HMG-CoA reductase?

Answer 5

Mevalonate

Question 6

What apolipoprotein is found on “bad cholesterol”?

Answer 6

ApoB100

Question 7

What is the receptor and ligand for receptor-mediated endocytosis of LDL?

Answer 7

Receptor: LDL receptor

Ligand: ApoB100

(Also scavenger receptor)

Question 8

What enzyme converts free cholesterol to cholesterol esters for transport by HDL?

Answer 8

LCAT

(Lecithin cholesterol acyltransferase)

Question 9

What are two mechanisms HDLs transfer cholesterol to the liver?

Answer 9

(1) Deliver to LDLs via CETP
(2) Receptor-mediated endocytosis via SR-1

Question 10

MOA: Statins

Answer 10

Inhibits HMG-CoA reductase

(↓ Intracellular Cholesterol ⇒ Upregulation of LDL receptors ⇒ ↑ Rate of peripheral cholesterol removal)

Question 11

What part of the lipid fraction do statins reduce?

Answer 11

(1) ↓↓↓ LDL
(2) ↓ TGs
(3) ↑ HDL

Question 12

What is the first-line treatment for hypercholesterolemia?

Answer 12

Lifestyle modification + statins

Question 13

What is the most effective lipid-lowering drug to prevent future cardiovascular events?

Answer 13

Statins

Question 14

Adverse Effects (3) : Statins

Answer 14

(1) Myopathy
(2) ↑ LFTs
(3) Teratogen

Question 15

What is the only statin drug not metabolized by the CYP-450 system?

Answer 15

Pravastatin

(Primadonna-statin = Too good for CYP-450 system)

Question 16

MOA: Bile acid resins

Answer 16

Inhibits bile acid reabsorption

(∴ ⇒ Stimulate HMG-CoA reductase & Upregulate LDL receptors)

Question 17

What are two examples of bile acid resins?

Answer 17

(1) Cholestyramine
(2) Cholestipol

Question 18

What effect do bile acid resins have on lipid fraction?

Answer 18

(1) ↓↓↓ LDL
(2) ↑ TGs

Question 19

Why might bile acid resins cause colicky pain?

Answer 19

↑ Risk of gallstones

Question 20

What type of vitamin deficiency can result from using bile acid resins?

Answer 20

Fat-soluble vitamin deficiency

(A, D, E, K)

Question 21

What is the treatment protocol for administering bile acid resins with statins?

Answer 21

Administer > 4 hrs apart

Question 22

MOA: Ezetimibe

Answer 22

Inhibits intestinal absorption of cholesterol

Question 23

Adverse Effects (2) : Ezetimibe

Answer 23

(1) ↑ LFTs
(2) Diarrhea

Question 24

MOA: Evolocamab

Answer 24

Inhibits PCSK9

(∴ Inhibits degradation of LDL receptors)

Question 25

What are the possible fates of FFAs released by LPL?

Answer 25

(1) Used by muscle (2) Coverted back to TG in adipose tissue

Question 26

What are two examples of fibrate drugs?

Answer 26

(1) Gemfibrozil (2) Fenofibrate

Question 27

**MOA**: Fibrate drugs

Answer 27

Activate PPAR-**α** *(⇒ ↑ LPL ⇒ ↓ TG levels)*

Question 28

What effect do fibrates on the lipid fraction?

Answer 28

(1) ↓↓↓ TGs (2) ↓ LDL (3) ↑ HDL * (↑ HDL by increasing ApoA1 and ApoA2)*

Question 29

**Adverse Effects** (2) : Fibrates

Answer 29

(1) Myopathy (2) Gallstones

Question 30

**Contraindication**: Fibrates

Answer 30

Gallbladder disease *(↑ Risk of gallstones)*

Question 31

What is the most effective drug for increasing HDL levels?

Answer 31

Niacin

Question 32

What effect does Niacin have on the lipid fraction?

Answer 32

(1) ↓ TGs (2) ↓ LDL (3) ↑↑↑ HDL

Question 33

**Adverse Effect**: Niacin

Answer 33

Cutaneous flushing

Question 34

What drug should be given prior to taking Niacin?

Answer 34

NSAID

Question 35

**Contraindications** (3) : Niacin

Answer 35

(1) Liver disease (2) Diabetics (3) Gout

Question 36

Fish oil is rich in what type of fatty acid?

Answer 36

ω-3 fatty acids

Question 37

How does fish oil lower serum triglycerides?

Answer 37

(1) ↓ VLDL (2) ↓ ApoB