agents used to treat hyperlipidemias

Question 1

hyperlipidemia

Answer 1

defect in lipid transport system that provides cholesterol and triglycerides to the cell.

Question 2

hyperlipidemia leads to what

Answer 2

increase risk for coronary artery disease
increase risk of plaque formation in vascular
increase risk of pancreatits
increase risk of xanthoma

Question 3

LDL stands for what

Answer 3

low density lipoprotein

Question 4

how much LDL should you have

Answer 4

<100 mg/DL

Question 5

secondary hyperlipoproteinemias

Answer 5

environmental causes
alcholoism- cirrhosis
diabetes- nephrosis

Question 6

primary hyperlipoproteinemias.

Answer 6

genetic abnormalities 
decrease in lipoprotein lipase
abnormal LDL receptors
overproduction of VLDL 
decrease in HDL synthesis

Question 7

treatment of hyperlipidemias

Answer 7

non-pharmacologic- diet, weight loss, aerobic exercise, stop smoking
also pharmacologic

Question 8

decreasing fats in diet = decrease in what

Answer 8

cholesterol

Question 9

pharmacologic treatment of hyperlipidemias

Answer 9

decrease production of lipoproteins
decrease absorption
increase removal of lipoproteins
(all effective with oral admin)

Question 10

what is the most effective LDL lowering agent?

Answer 10

HMG CoA reductase inhibitors- lovastatin, “statin”s

Question 11

lovastatin mech of action

Answer 11

prodrug

HMG CoA reductase- rate limiting step in cell synthesis of cholesterol

Question 12

if cells can’t make any of their own cholesterol what happens?

Answer 12

find another way to get more LDL- increase LDL receptors of the cell = increase in LDL uptake (25%- 60%).

Question 13

SE of lovastatin

Answer 13

• myositis (muscle pain) -> rhabdomyolysis (total breakdown of muscle)
• liver toxicity
• teratogenic pregnancy category X
• some memory loss

Question 14

fats go into the gut and come out as _____ containing _____ and _____

Answer 14

chylomicrons, triglycerides, cholesterol

Question 15

fate of chylomicrons

Answer 15

• lipoprotein lipase convert to free fatty acids that go to the cell
• remnants go to liver

Question 16

chylomicrons remnants in the liver and do 2 things

Answer 16

1. bind with apolipoprotein B and make VLDL

2. relased from liver as bile acids into the gut

Question 17

liver also produces _____ that is ultimately reabsorbed by it

Answer 17

HDL

Question 18

fate of VLDL

Answer 18

lipoprotein lipase takes of triglycerides = IDL,

Lplipase takes off more stuff = LDL

Question 19

LDL is major carrier of what

Answer 19

cholesterol

Question 20

fate of LDL

Answer 20

1. oxidized and taken up by macrophages and deposited on arterial lining
2. bind to LDL receptors on cell membrane where its converted to cholesterol

Question 21

another way to make cholesterol in the cell

Answer 21

HMG CoA reductase

Question 22

what is niacin?

Answer 22

vitamin B3

Question 23

mechanism of action of niacin

Answer 23

1. inhibits an enzyme essential for VLDL synthesis

2. bind to receptor that decreases VLDL synthesis

Question 24

T/F niacin is best increaser of HDL

Answer 24

True

Question 25

ultimately niacin increases what and decreases what

Answer 25

increases HDL, decrease VLDL

Question 26

SE of niacin

Answer 26

cutaneous flushing "red face" itching increase uric acid-gout increase incidence of diabetes

Question 27

drugs that bing to bile acid

Answer 27

cholestyramine colestipol coleselevam

Question 28

mech of action of bile acid binding resins

Answer 28

irreversibly bind to bile acids in gut causing them to be excreted with their cholesterol

Question 29

outcome of taking bile acid binding agents

Answer 29

decreases circulating cholesterol | increases LDL receptors

Question 30

do you have to take a lot of this drug to be effective?

Answer 30

yes 5-30g a day

Question 31

SE of bile acid binding resins

Answer 31

no systemic cuz too big to be absorbed can bind to acidic drugs like oral anticoagulants and digoxin decrease absorption of fat soluble vitamins nausea

Question 32

agents that decrease cholesterol absorption by the intestines

Answer 32

``` SOOE Sitostanol orlistat olestra ezetimibe ```

Question 33

ezetimibe

Answer 33

blocks cholesterol transporter

Question 34

sitostanol

Answer 34

looks like cholesterol, blocks uptake

Question 35

orlistat

Answer 35

inhibits GI, pancreatic lipase, decreases fat absorption in gut, major problem is loose stools

Question 36

fibrates

Answer 36

best triglyceride lowering agents, bind to PPAR

Question 37

fibrate drugs

Answer 37

gemfibrozil, fenofibrate

Question 38

mech. of action of fibrates

Answer 38

increase transcription of lipoprotein lipase- decrease in triglycerides and VLDL

Question 39

what can you not take with fibrates

Answer 39

warfarin- displaces it.

Question 40

omega 3 fatty acids

Answer 40

decrease triglyercide synthesis, by inhibiting enzymes

Question 41

omega 3 FA drug

Answer 41

icosapent

Question 42

lomitapide

Answer 42

inhibits assembly of VLDL in liver | both enzyme and a transporter

Question 43

SE of lomitapride

Answer 43

hepatoxicity

Question 44

other hyperlipidemias

Answer 44

lomitapide | mipomersen

Question 45

mipomersen

Answer 45

amhistase oligonucleotide | binds to RNA for APOb and prevents synthesis of APO