Antilipidemics (4)

Question 1

t/f thyroid hormones can have hypocholesterimic effects

Answer 1

true

Question 2

what does dextrothyroxine require?

Answer 2

99% + pure optical isomer

Question 3

dextrothyroxine overall effect

Answer 3

increase LDL receptors (enhance removal of LDL)

Question 4

Dextrothyroxine stimulates the ______ of cholesterol in liver through increase of _______

Answer 4

oxidative catabolism

7a-cholesterol-hydroxylase

Question 5

Adverse effects of dextrothyroxine

Answer 5

• increase frequency and severity of anginal attacks
• cause cardiac arrhythmias
• potentiates action of anticoagulants

Question 6

Diabetics and dextrothyroxine

Answer 6

requires increased dose of insulin or hypoglycemic agents

Question 7

What is a vitamin used as hypocholesteremic?

Answer 7

niacin

Question 8

Niacin is effective for all types of hyperlipidemica except _____ at doses given as vitamin supplement

Answer 8

type I

Question 9

niacin overall effect

Answer 9

• decrease VLDL synthesis (decrease IDL, LDL)
• inhibit lipolysis

Question 10

What is the drug of choice for all type II hyperlipoproteinemias?

Answer 10

Niacin

Question 11

Why is niacin have limited use?

Answer 11

vasodilation side effects

Question 12

What is an extended release preparation of niacin?

Answer 12

Nispan

Question 13

Probucol overall effect

Answer 13

decrease level of cholesterol by increasing rate of LDL catabolism

• may also inhibit cholesterol synthesis and delay cholesterol absorption

Question 14

How does probucol decrease levels of cholesterol?

Answer 14

increasing rate of LDL catabolism

Question 15

What is probucol believed to act on?

Answer 15

ABCA1

Question 16

Why was probucol withdrawn from market?

Answer 16

cause QTc prolongation

Question 17

Cholestyramine is a ______ that binds _____ in GI tract and prevents reabsorption

Answer 17

bile acid sequestrant

bile

Question 18

Cholestyramine is a ____ resion with what type of group?

Answer 18

strong ion exchange resin

quaternary ammonium group

Question 19

With cholestyramine, due to loss of bile acids, more ____ is converted to bild acids in liver to normalize levels

Answer 19

plasma cholesterol

Question 20

cholestyramine overall effect

Answer 20

decrease plasma cholesterol levels

Question 21

What does ACAT do?

Answer 21

catalyze cholesterol esterification and cholesterol absorption

maintain cholesterol homeostasis in blood

Question 22

What is a new attractive target for hyperlipidemia?

Answer 22

ACAT inhibitors

Question 23

ACAT1 regulates cholesterol homeostasis where?

Answer 23

brain

macrophages

adrenal glands

Question 24

ACAT2 ____ cholesterol where?

Answer 24

esterfies

intestine and liver

Question 25

What regulates cholesterol homeostasis in brain, macrophages and adrenal glands?

Answer 25

ACAT1

Question 26

What esterfies cholesterol in small intestine and liver?

Answer 26

ACAT2

Question 27

what is CIMT?

Answer 27

carotid intima media thickness

Question 28

What does CETP do?

Answer 28

facilitates transport of cholesteryl esters and TGs between lipoproteins

Question 29

What are CETP designed to do?

Answer 29

raise HDL (thought to be protective)

Question 30

What can reverse transport of cholesterol out of macrophages?

Answer 30

CETP: so cholesterol can be metabolized

Question 31

How does CETP work?

Answer 31

collects TGs from VLDL or LDL and exchange for cholesteryl esters from HDL

Question 32

What CETP inhibitor does not have cardiovascular problems?

Answer 32

dalcetrapib

Question 33

What CETP inhibitor is on the market?

Answer 33

NONE!

Question 34

CETP inhibitors may produce a form of ____ that does not enhance reverse cholesterol transport

Answer 34

HDL

Question 35

What is an adipose tissue derived adipokine?

Answer 35

resistein

Question 36

resistin AKA

Answer 36

- ADSF or XCP1

Question 37

resistin is a small, _____ protein secreted from \_\_\_\_

Answer 37

cysteine rich macrophages and adipose tissue

Question 38

resistin overall effect

Answer 38

increase LDL in human liver cells degrae LDL receptors in liver

Question 39

What is thought to be an important link between obesity and insulin resistance and diabetes?

Answer 39

resistin

Question 40

serum levels of ____ are increased in human obesity and + correlated with \_\_\_\_

Answer 40

resistin atherosclerotic CVD

Question 41

At physiological levels observed in human obesity, resistin reduces human hepatocyte expression of \_\_\_\_

Answer 41

LDLRs

Question 42

Statins are ineffective in 40% of patients due to ____ secretion in adipose tissue

Answer 42

resistin

Question 43

\_\_\_\_ may be new therapeutic target because statins may be ineffective in some

Answer 43

resistin

Question 44

What is a key regulator of LDL-C metabolism?

Answer 44

PCSK9

Question 45

PCSK9 has been shown to be stimulated by ____ and leads to what?

Answer 45

resistin downregulation of LDLR

Question 46

Resistin and PCSK9 have notable structural similarity where?

Answer 46

cysteine rich C terminal domain

Question 47

Atherosclerosis is buildup of what lipoproteins?

Answer 47

LDL-C

Question 48

PCSK9 inhibitors in transgenic mice lower \_\_\_\_

Answer 48

LDL

Question 49

ODYSSEY long term study

Answer 49

65 weeks alirocumab reduced risk of major events compared to those with placebo and max tolerated statin

Question 50

ODYSSEY results

Answer 50

decrease LDL 61% 79% achieved target LDL \<70 after treatment with alirocumab

Question 51

Why were CETP inhibitor trials stopped?

Answer 51

lack of clinically meaningful efficacy

Question 52

What are CETP inhibitors thought to do?

Answer 52

Increase HDL

Question 53

What do PCSK9 inhibitors supposed to do?

Answer 53

decrease LDL