Drugs Used In Hyperlipidemia

Question 1

The longer and lower the reduction in circulating LDL-C, the lower the incidence of

Answer 1

CHD

Question 2

Cholesterol esters and triglycerides are insoluble in water and circulate in blood as

Answer 2

Lipoprotein particles

Question 3

Low density lipoprotein ApoB is recognized by the

Answer 3

LDL receptor

Question 4

The LDL receptor internalizes circulating

Answer 4

LDL

Question 5

A transcription factor that serves as the master regulator of cholesterol levels in the cell

Answer 5

SREBP (Sterol Regulatory Element Binding Protein)

Question 6

In a low cholesterol diet, SREBP is

Answer 6

Activated

Question 7

Results in increase in cholesterol biosynthesis and increase in receptor-mediated LDL endocytosis from the plasma

Answer 7

SREBP activation

Question 8

In a high-cholesterol diet, SREBP is not activated and thus we see a decrease in

Answer 8

Cholesterol biosynthesis and LDL receptors

Question 9

The most effective and best tolerated agents for treating dyslipidemia

Answer 9

Statins

Question 10

Statins function as

Answer 10

HMG-CoA reductase inhibitors

Question 11

Competitive inhibitors of HMG-CoA reductase

• Inhibits cholesterolgenesis
• Increase expression of LDL receptor

Answer 11

Statins

Question 12

Inactive lactose pro drugs hydrolysis to active drugs

Answer 12

Statins

Question 13

Statin absorption varies from 40% to 75% except for

Answer 13

Fluvastatin (almost completely absorbed)

Question 14

Statins have half-lives of 1-3 hours except for

1. ) Atorvastatin?
2. ) Rosuvastatin?

Answer 14

1. ) 14 hours

2. ) 19 hours

Question 15

Hepatic cholesterol biosynthesis is maximal from midnight-2 AM, so we want to take them in the

Answer 15

Evening (except for the ones w/ the long half-lives)

Question 16

Contraindicated in women who are pregnant, lactating, or likely to become pregnant

Answer 16

Statins

Question 17

Most efficacious agents for severe hypercholesterolemia

-More TG lowering activity compared to other statins

Answer 17

Atorvastatin and Rosuvastatin

Question 18

Two toxic/adverse effects of Statins are

Answer 18

1. ) Hepatotoxicity

2. ) Diabetes Mellitus

Question 19

While statin therapy can reduce occlusive vascular events by 40-50%, many patients discontinue statins due to

Answer 19

Myopathies

Question 20

Monoclonal antibodies (mAbs) against PCSK9 protein

Answer 20

PCSK9 inhibitors

Question 21

Diverts LDLR from recycling pathway towards lysosome for degradation

Answer 21

PCSK9

Question 22

A cholesterol absorption inhibitor

Answer 22

Ezetimibe

Question 23

Ezetimibe’s site of action is at the

Answer 23

NPC1L1 cholesterol transporter

Question 24

Selectively inhibits intestinal cholesterol absorption and also plant sterols

Answer 24

Ezetimibe

Question 25

Increases expression of hepatic LDL receptors, decreases intestinal delivery of cholesterol to the liver, and decreases cholesterol content of atherogenic particles

Answer 25

Ezetimibe

Question 26

The average reduction in LDL-C with drug alone is

Answer 26

18%

Question 27

Ezetimibe is synergistic with -Additional 25% decrease compared to statin alone

Answer 27

Statins

Question 28

Highly positively charged and bind negatively charged bile acids -The bound bile acids are then excreted in stool

Answer 28

Bile acid sequestrants

Question 29

Decline hepatic cholesterol content, increase LDL receptors, increase clearance of LDL from plasma, and lower LDL-C

Answer 29

Bile acid sequestrants

Question 30

However, bile acid sequestrants do upregulate

Answer 30

HMG-CoA reductase

Question 31

Use with extreme caution or avoid completely in patients with severe hypertriglyceridemia

Answer 31

Bile Acid Sequestrants

Question 32

You must take with meals or there is no effect

Answer 32

Bile acid sequestrants

Question 33

Used to treat heterozygous FH

Answer 33

Bile acid sequestrants

Question 34

Can cause constipation, bloating, heart burn, and diarrhea

Answer 34

Bile acid sequestrants

Question 35

These side effects can be relieved by increasing fiber or by mixing bile acid sequestrant with

Answer 35

Psyllium Seed

Question 36

Can interfere with the absorption of many other drugs -Should wait 3-4 hours after taking to take another drug

Answer 36

Bile acid sequestrants

Question 37

What’re soluble vitamin B3

Answer 37

Niacin (nicotinic acid)

Question 38

Has favorable effects on all lipid profiles, but there are a lot of adverse effects

Answer 38

Niacin

Question 39

Has the primary effect of inhibiting VLDL secretion, thereby decreasing production of LDL

Answer 39

Niacin

Question 40

Inhibits lipolysis of TG by hormone-sensitive lipase

Answer 40

Niacin

Question 41

Increased CHD risk associated with TG levels greater than 150 mg/dL

Answer 41

Hypertriglyceridemia

Question 42

Elevated triglycerides (greater than 500 mg/dL) can lead to

Answer 42

Pancreatitis

Question 43

Activated the peroxisome proliferator-activated receptor-alpha

Answer 43

Vibrates

Question 44

A transcription factor regulating genes that control lipid metabolism

Answer 44

Vibrates

Question 45

Primary effect is to reduce plasma TG -Only a modest decrease in LDL

Answer 45

Fibrates