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PMCOL 344 > Other lipid drugs > Flashcards

Other lipid drugs Flashcards

1
Q

what is an example of a fibrate

A

gemfibrozil

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2
Q

what is the mechanism of action of gemfibrozil

A

activates PPAR-α

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3
Q

where is PPAR-α expressed

A

liver, brown fat, kidney, heart, skeletal muscle

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4
Q

what is the effect of activating PPAR-α

A

alter genes that control lipid metabolism

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5
Q

what is a main important thing that PPAR-α activation does

A

increases fatty acid oxidation via increases LPL expression

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6
Q

what happens when you increase LPL expression

A

you enhance removal of TGs from CMs and VLDL

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7
Q

what happens to VLDL production with gemfibrozil

A

decreased

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8
Q

what happens to LDL production with gemfibrozil

A

decreased

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9
Q

what happens to apoA1 production with gemfibrozil

A

increased expression (HDL)

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10
Q

what happens to LDL receptor expression production with gemfibrozil

A

increased in hepatic tissue

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11
Q

how much does gemfibrozil reduce TGs and VLDL

A

by 25-50%

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12
Q

how much does gemfibrozil increase HDL

A

by 10-35%

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13
Q

what does gemfibrozil do to Bile

A

increase excretion

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14
Q

what does gemfibrozil do to inflammation

A

reduce

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15
Q

what does gemfibrozil do to endothelial function

A

improve

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16
Q

what does gemfibrozil do to glucose tolerance

A

improve

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17
Q

can gemfibrozil improve survival rates

A

maybe no

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18
Q

can gemfibrozil cause myositis and rhabdomyolysis

A

yes

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19
Q

what is a bad side effect of gemfibrozil

A

myositis and rhabdomyolysis

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20
Q

which patients do we give gemfibrozil to

A

patients with elevated LDL or VLDL or low HDL

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21
Q

what does gemfibrozil do to VLDL secretion

A

decrease

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22
Q

what does gemfibrozil do to LDL uptake

A

increase

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23
Q

what does gemfibrozil do to lipoprotein lipase

A

enhance

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24
Q

what are the 3 main things gemfibrozil does

A
  • decrease VLDL secretion
  • increase LDL uptake
  • enhance lipoprotein lipase
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25
Q

where do resins act

A

GI tract

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26
Q

what was the first clinical method to lower cholesterol

A

resins

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27
Q

what is another name for resins

A

bile acid sequestrants

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28
Q

what is another name for bile acid sequestrants

A

resins

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29
Q

name an example bile acid sequestrants

A

colesevelam

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30
Q

how do resins work/ mechanism

A

they are +vely charged so they bind -vely charged bile acids to prevent reabsorption, leading to compensatory increase in bile synthesis from cholesterol

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31
Q

do resins work like cation or anion exchange

A

anion

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32
Q

what is a main important thing that resins lead to

A

increased hepatic expression of LDL receptors (wants more cholesterol to turn into bile acids)

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33
Q

what do resins do to cholesterol metabolism

A

increase its conversion into bile acids

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34
Q

what do resins do to plasma LDL + why

A

lower

Liver is looking for more cholesterol to turn into bile acids, so more LDL is taken into liver and is removed from bloodstream

35
Q

what do resins do to LDL receptors

A

increases hepatic expression of them

36
Q

what is one main bad thing that resins cause

A

increases hepatic cholesterol and TG synthesis

37
Q

how to prevent resin induced increases hepatic cholesterol and TG synthesis

A

use statins

38
Q

what are some annoying side effects with resins

A

they cause bloating, need up to 32g a day

39
Q

what can high doses of resins alone do to plasma cholesterol

A

lower by 25%

40
Q

why do we do low doses of resins + statins for plasma cholesterol

A

because statins offset increased hepatic cholesterol synthesis

41
Q

what is the mechanism of action of nicotinic acid / what does it do

A

limit the availability of free fatty acids to reduce hepatic TG synthesis
via orphan receptor HM74A

42
Q

what does nicotinic acid do in adipose tissue

A

inhibits lipolysis of TGs by hormone sensitive lipase

43
Q

what happens once nicotinic acid inhibits lipolysis of TGs in adipose tissue

A

there will be less transport of free fatty acids to liver and so decreases hepatic TG synthesis
-decreased plasma VLDL

44
Q

what does nicotinic acid do in liver tissue

A

reduces TG synthesis by inhibiting synthesis and esterification of fatty acids - decrease plasma VLDL

45
Q

what are 3 ways nicotinic acid decreases VLDL

A
  • inhibit lipolysis of TGs in adipose tissue
  • reduce TG synthesis in liver
  • increase LPL activity
46
Q

what does increases LPL activity cause

A

promotes clearance of CM and VLDL TGs - decreased plasma VLDL

47
Q

what is the main fats that VLDL transport

A

TGs

48
Q

what does nicotinic acid do to apoA-1 + what does this cause

A

decreases hepatic clearance of apoA-1, sp this increases HDL

49
Q

what does nicotinic acid do to ABCA1 + what does this cause

A

increases its expression, so more transfer of free cholesterol from cells to HDL

50
Q

which receptor does nicotinic acid work through

A

maybe the orphan receptor HM74A

51
Q

how does nicotinic acid reduce liver TG synthesis

A

by inhibiting synthesis and esterification of fatty acid

52
Q

what does decreased VLDL lead to

A

reduced plasma LDL

53
Q

what can nicotinic acid do to HDL

A

increase by 30-40%

54
Q

what can nicotinic acid do to VLDL

A

decrease by 35-45% (also also plasma TGs)

55
Q

what can nicotinic acid do to LDL

A

decrease by 20-30%

56
Q

what is special about nicotinic acid

A

it is the only agent to significantly reduce Lp(a)

57
Q

what is the only agent that can significantly reduce Lp(a)

A

nicotinic acid

58
Q

which patients do we use nicotinic acid for

A

with high TGs and high LDL and low HDL

59
Q

does nicotinic acid improve outcome

A

maybe no :( even though it helps lipids

60
Q

what is ezetimibe

A

cholesterol absorption inhibitors

61
Q

what mediates intestinal cholesterol absorption

A

NPC1L1 in epithelium

62
Q

what is the mechanism of ezetimibe

A

selectively block absorption of cholesterol in duodenum by NPC1L1

63
Q

does ezetimibe affect absorption of fat soluble vitamins

A

no

64
Q

does ezetimibe affect absorption of cholesterol

A

yes

65
Q

does ezetimibe affect absorption of TGs

A

no

66
Q

does ezetimibe affect absorption of bile acids

A

no

67
Q

why do we call ezetimibe potent

A

it binds to protein receptor rather than directly interacting with cholesterol

68
Q

how much can ezetimibe reduce cholesterol asborption

A

by 55%

69
Q

what kind of people should take ezetimibe and who shouldnt

A

do it if you have high dietary cholesterol (it wont do much if you have low cholesterol diet or if excessive production of liver disease)

70
Q

what class is ezetimibe

A

inhibition of cholesterol absorption

71
Q

what does ezetimibe do to CM

A

decreases them so decreases CM remnant-mediated delivery of cholesterol to the liver

72
Q

what does ezetimibe do to plasma LDL and how

A

reduction in hepatic cholesterol increases LDL receptors so more uptake and less plasma (20%)

73
Q

what can be a bad thing about ezetimibe

A

increases hepatic cholesterol synthesis

74
Q

how do you counteract ezetimibe induced hepatic cholesterol synthesis

A

give a statin too

75
Q

how clinically useful may ezetimibe be

A

maybe not that much

76
Q

which drug has the biggest decrease in LDL

A

statins

77
Q

which drug has the smallest decrease in LDL

A

fibrates and absorption inhibitors

78
Q

rate the drugs in order of largest to smallest decrease in LDL

A

statins>resins>nicotinic acid>fibrates = absorption inhibitors

79
Q

which drug has the biggest increase in HDL

A

nicotinic acid

80
Q

which drug has the smallest increase in HDL

A

resins and absorption inhibitors

81
Q

rate the drugs in order of largest to smallest increase in HDL

A

nicotinic acid>fibrates>statins>resins>absorption inhibitors

82
Q

which drug has the biggest decrease in TGs

A

nicotinic acid

83
Q

which drug increases TGs

A

resins

84
Q

rate the drugs in order of largest to smallest decrease in TGs

A

nicotinic acid>fibrates>statins> absorption inhibitors» resins(they increase!)

PMCOL 344 (27 decks)

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