Exam 3; Agents used to treat Hyperlipidemias

Question 1

What causes hyperlipidemia

Answer 1

a defect in the lipid transport system which provides cholesterol and triglycerides to the cell

Question 2

There is an increased risk of these three things with an increase in blood lipids

Answer 2

coronary artery disease; due to increased plaque formation
pranceatitis
xanthoma; deposition of fat in the skin

Question 3

This form on lipoprotein when in high levels, causes more potential problems

Answer 3

LDL; low density lipoproteins

Question 4

What is the desirable level of LDL

Answer 4

< 100mg/DL

Question 5

What converts chylomicrons ti free fatty acids

Answer 5

lipoprotein lipase

Question 6

The chylomicron remnants (cholesterol) travel to which organ

Answer 6

the liver

Question 7

These two things combine to form vLDL

Answer 7

apolipoprotein and cholesterol

Question 8

What is the intermediate step in the formation of LDL from vLDL

Answer 8

vLDL → IDL → LDL

steps all catalyzed by lipoprotein lipase

Question 9

If LDL becomes oxidized, what occurs

Answer 9

it is taken up by macrophage and deposited on arterial linings

Question 10

What is a major carrier of cholesterol

Answer 10

LDL

Question 11

LDL binds to what on the cell

Answer 11

LDL receptor

Question 12

This enzyme in the cells can make cholesterol

Answer 12

HMG CoA reductase

Question 13

Cholesterol can make these oh which can go into the gut

Answer 13

bile acids

Question 14

What is considered the “good cholesterol”

Answer 14

HDL

high density lipoproteins

Question 15

What four things cause secondary hyperlipoproteinemias

Answer 15

cirrhosis
alcoholism
nephrosis
diabetes

Question 16

What are four things that cause primary hyperlipoproteinemias

Answer 16

decreased lipoprotein lipase
abnormal LDL receptors
over production of vLDL
decreased HDL synthesis

Question 17

What are two non-pharmacologic treatments of hyperlipoproteinemias

Answer 17

diet/exercise

stop smoking

Question 18

What are three mechanisms behind pharmacologic effects of drugs treating hyperlipoproteinemia

Answer 18

decrease production of lipoproteins
increase removal of lipoproteins/cholesterol
decrease absorption of lipoproteins

Question 19

Can agents that treat hyperlipoproteinemias affect the fetus

Answer 19

Yes

Question 20

What will happen to the effects of hyperlipoproteinemia drugs upon stoppage of taking them

Answer 20

the effects will stop as well

Question 21

Which family of drugs are the HMG CoA reductase inhibitors

Answer 21

“-statin’s”

Question 22

True or False

the HMG CoA reductase inhibitors (-statins) are the most effective LDL lowering agents

Answer 22

True

Question 23

What is the mechanism of action behind the statin drugs

Answer 23

inhibits HMG CoA reductase; the rate limiting step in the cell synthesis of cholesterol

Question 24

When the cells cannot make their own cholesterol, how do they compensate

Answer 24

they increase the LDL receptors on the cell

Question 25

What is a major side effect of the statin drugs

Answer 25

myositis; muscle pain | especially true since many are metabolized by P450

Question 26

What are three side effects of statin drugs

Answer 26

liver toxicity teratogenis; pregnancy category X some memory loss

Question 27

What is the main difference between all the statin drugs

Answer 27

pharmacokinestics

Question 28

What is the mechanism of action behind niacin

Answer 28

it inhibits an enzyme essential for vLDL synthesis and may also bind to a receptor that decreases vLDL synthesis

Question 29

What is the result of using niacin

Answer 29

decrease in vLDL | increase in HDL; strongest increaser of HDL

Question 30

What are four side effects of Niacin

Answer 30

cutaneous flushing (red face) itching increased uric acid; gout increase incidence of diabetes

Question 31

What are the three bile acid binding resins

Answer 31

cholestyramine colestipol coleselevam "coles"

Question 32

What is the mechanism of action behind the "coles"

Answer 32

irreversibly bind to bile acids in the gut; are excreted along with their cholesterol

Question 33

What two things do the "cole" drugs cause

Answer 33

decrease in circulating cholesterol | increase in LDL receptors

Question 34

What are the side effects of the "cole" drugs

Answer 34

no side effects because they are not absorbed; but can cause nausea or GI irritants

Question 35

This family of drugs are the best triglyceride lowering agents

Answer 35

the fibrates

Question 36

What is the mechanism behind the fibrates

Answer 36

binds to PPAR; perixosome proliferator activating receptor | increasing the activity of LPL

Question 37

What are the fibrates

Answer 37

gemfibrozil fenofibrate (both have fibr)

Question 38

What are two side effects of gemfibrozil and fenofibrate

Answer 38

GI upset | can displace warfarin from plasma binding sites

Question 39

These two things decrease triglyceride synthesis via inhibition of an enzyme

Answer 39

omega 3 fatty acids | icosapent ethyl

Question 40

This essentially inhibits assembly of vLDL in the liver; both an enzyme and a transporter

Answer 40

imoitapide

Question 41

This is an anti-sense oligonucleotide

Answer 41

mipomersen

Question 42

What is the mechanism of mipomersen

Answer 42

binds to the mRNA for apoloprotein-B; preventing it from being synthesized

Question 43

This drug blocks cholesterol transport

Answer 43

ezetimibe

Question 44

This drug looks like cholesterol and blocks its uptake

Answer 44

sitostanl

Question 45

This inhibits GI and pancreatic lipase, decreasing fat absorption from the gut and causes loose stools

Answer 45

orlistat

Question 46

This is an non-absorbable oil used for frying/cooking but causes anal leakage → gross.

Answer 46

olestra