14 hypercholesterol& Dyslipidemia

Question 1

Many clinical trials demonstrate that increase of LDL levels induce formation of what?

Answer 1

Atherosclerosis plaques

Question 2

What are the lipid lowering drugs?

Answer 2

Statins

Nicotinic Acid (Niacin)

Resins

Fibric Acid derivatives

Inhibitors of cholesterol absorption

PCSK9 Inhibitors

Question 3

What are the 6 statins that are FDA approved?

Answer 3

Lovastatin

Simvastatin

Pravastatin

Atorvastatin

Rosuvastatin

Fuvastatin

Question 4

Effects on LDL-C, HDL-C, triglycerides are dose related, meaning?

Answer 4

Dose should be set to achieve target LDL-C levels

Question 5

What is Statin MOA?

Answer 5

Competitive inhibitors of HMG-CoA reductase

• > prevents mevalonte synthesis
• > dec in endogenous cholesterol synthesis by liver
• > up regulation of LDL receptors in liver
• > reduction in blood LDL levels

Question 6

What is HMG-CoA?

Answer 6

Precursor for cholesterol synthesis

Integral ptn. of ER membranes

Question 7

What is the major adverse effect of statin?

Answer 7

Myopathies

Question 8

What is myopathy?

Answer 8

Intense myalgia

Serum creatinine levels elevated 10x

Question 9

When taking a Statin, what drugs greatly increase myopathic symptoms?

Answer 9

Use with other lipid lowering drugs (fibrates)
= Gemfibrozil

drugs that inhibit P450 isoenzymes

Question 10

Avoid administering statins with what drugs?

Answer 10

Fibrates

Antibiotics

Antifungals

HIV protease inhibitors

Question 11

What are statin contraindications?

Answer 11

Active liver disease

Grapefruit juice

Pregnancy

Question 12

What happens when a statin is taken with oral contraceptives, such as estrogens? What about progestins?

Answer 12

Estrogens:
Inc HDL
Dec LDL

Progestins:
opposite

Question 13

What statin can be given to children 8 and older? 11 and older?

Answer 13

8: prova
11: atora, lova

Question 14

What does Niacin refer to?

Answer 14

Nicotinic acid
&
Nicotinamide (B3)

Question 15

What does a deficiency in vit B3 cause?

Answer 15

(along with def in tryptophan)

pellagra

Question 16

What is considered the best agent to increase HDL levels?

Answer 16

Nicotinic acid

= Niacin

Question 17

What does Nicotinic acid do?

Answer 17

Inc HDL
Dec triglyceride
Dec LDL

Question 18

What are adverse effects of Niacin (nicotinic acid)?

Answer 18

Dyspesia accentuated by coffee, tea, alcohol

Flushing
Pruritus

Question 19

What drug should you limit for pt with diabetes? Why?

Answer 19

Niacin

Inc uric acid = gout

Question 20

What are bile-acid sequestrates?

Answer 20

Resins

Question 21

What is the safest lipid lowering agents?

Answer 21

Resins

Question 22

What is Bile-acid sequestrates (resins) MOA?

Answer 22

High (+) charged resins bind (-) charged bile acids

Resins are not absorbed & arrest bile acids

deplete cholesterol content
up regulate LDL
Inc triglyceride

Question 23

What are the 3 bile acid resins drugs?

Answer 23

Cholestyramine

Colestipol

Colesevelam

Question 24

What are resins drug interactions?

Answer 24

Interfere with absorption of Statins

Give statins 1 hr prior or 3-4 hr after

Question 25

What is fibric acid derivatives MOA?

Answer 25

Bind to PPAR activated receptors & stimulate beta oxidation of fatty acids

Question 26

What is the best way to decrease triglyceride levels?

Answer 26

Fibric Acid Derivatives

Question 27

What drug is given to pt with severe hypertriglyceridemia?

Answer 27

Genfibrozil

Question 28

What drug is given to pt with high triglycerides & high cholesterol?

Answer 28

Fenofibrate

Question 29

What are beneficial effects do fibric acids have independent of lipid lowering activity?

Answer 29

Antithrombotic Immunomodluation Antiinflammatory

Question 30

What drug does inhibition of dietary cholesterol uptake?

Answer 30

Ezetimibe

Question 31

What is Ezetimibe MOA?

Answer 31

Blocks NPC1L1, which facilitates cholesterol absorption

Question 32

What drug is used to prevent the compensatory increase in endogenous cholesterol synthesis when taking Ezetimbe?

Answer 32

Statins

Question 33

What should not be combined with Ezetimibe? Why?

Answer 33

Bile Acid Sequestrants They inhibit absorption

Question 34

What are side effects of Ezetimibe?

Answer 34

Myopathy Rhabdomyolysis Myalgia Hepatitis Eczema Fatigue Headache

Question 35

What is PCSK9 inhibitors MOA?

Answer 35

dec LDL receptor degradation inc recirculation of the receptor to the hepatocytes -> lowers LDL in blood

Question 36

What drug do PCSK9 inhibitors work with?

Answer 36

Statins that inc LDL receptor expression