Agents used to treat hyperlipedemias Flashcards

1
Q

what is hyperlipidemia?

A

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

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2
Q

what does hyperlipidemia increase the risk of?

A

inc risk of coronary artery disease with increase in blood lipids
inc risk of plaque formation
inc risk of pancreatitis
inc risk of xanthoma

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3
Q

what do different levels of LDL cause?

A

160- 4x inc in coronary artery disease

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4
Q

what causes secondary hyperlipoproteinemias?

A

cirrhosis, nephrosis- alcohol and diabetes

drugs

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5
Q

what causes primary hyperlipoproteinemias?

A
genetic abnormalities- 
decrease lipoprotein lipase
abnormal LDL receptors
overproduction of VLDL
decrease HDL synthesis
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6
Q

non-pharmacologic treatment of hyperlipidemias

A

weight loss
diet- decrease fat and cholesterol
stop smoking
aerobic exercise

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7
Q

pharmacologic treatment of hyperlipdemias

A

decrease production of lipoproteins
increase removal of lipoproteins
decrease absorption of lipoproteins
some of these agents may affect the fetus

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8
Q

what are the hypolipidemic agents?

A
HMG coA reductase inhibitors
niacin
bile acid binding resin
fibrates
omega 3 fatty acids and icosapent
lomitapide
mipomersen
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9
Q

what are the agents that decrease cholesterol absorption by the intestine?

A

ezetimibe
sitostanol
orlistat
olestra

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10
Q

what is the most effective LDL lowering agent?

A

HMG CoA reductase inhibitors

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11
Q

what causes the strongest increase of HDL?

A

Niacin

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12
Q

what is the best triglyceride lowering agents?

A

fibrates

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13
Q

what can bind to acidic drugs? acidic drug example?

A

bile acid binding resins

digoxin

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14
Q

what can displace warfarin from plasma binding sites?

A

the fibrates

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15
Q

what are the HMG CoA reductase inhibitors?

A

statins

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16
Q

what is the mechanism of the statins?

A

prodrug that inhibit HMG coA reductase which is the rate limiting step in cell synthesis of cholesterol
when cells cannot make cholesterol- increase LDL receptor on cell- increase LDL uptake
LDL decrease is from 25-60%
also decrease VLDL synthesis

17
Q

what are the side effects of statins?

A
myositis (muscle pain)
at worst- rhabdomyolysis
liver toxicity
teratogenic- pregnancy category x
some of them associated with memory loss
18
Q

differences in the different statins?

A

pharmacokinetics

19
Q

what is the mechanism of action of niacin?

A

inhibits an enzyme essential for VLDL synthesis
may also bind to a receptor that decreases VLDL synthesis
decrease VLDL
increase HDL (strongest increase of HDL)

20
Q

side effects of niacin

A

cutaneous flushing, itching- prevented by aspirin
increased uric acid, increased gout
increased incidence of diabetes

21
Q

what are the bile acid binding resins

A

cholestyramine
colestipol
coleselevam
highly charged cationic resins

22
Q

bile acid mechanism of action

A

irreversibly bind to bile acids in the gut- cholesterol is excreted
decrease circulating cholesterol
increase LDL receptors

23
Q

what are the side effects of bile acids?

A

no systemic side effect- not absorbed
can bind to acidic drug like digoxin
decrease absorption of fat soluble vitamins
nausea

24
Q

what are the fibrates?

A

gemfibrozil and fenofibrate

best triglyceride lowering agents

25
Q

what are the fibrates mechanism of action?

A

bind to PPAR (peroxisome proliferator activating receptor)
increase transcription of lipoprotein lipase
decrease triglycerides
decrease VLDL

26
Q

what are the side effects of fibrates?

A

GI upset- nausea, vomiting

can displace warfarin from plasma binding sites

27
Q

mechanisms of omega 3 fatty acids and icosapent?

A

decrease triglyceride synthesis

inhibit an enzyme

28
Q

mechanism of lomitapide?

A

inhibits assembly of VLDL in the liver

both an enzyme and transporter

29
Q

side effects of lomitapide?

A

hepatotoxicity

30
Q

mechanism of mipomersen?

A

antisense oligonucleotide
binds to mRNA for apo B
prevents apo B from being synthesized
MUST BE GIVEN VIA INJECTION

31
Q

mechanism of ezetimibe?

A

blocks cholesterol transporter in intestine

inhibit reuptake/absorption of cholesterol from gut

32
Q

side effect of ezetimibe

A

flatulence

33
Q

mechanism of sitostanol?

A

looks like cholesterol

blocks uptake

34
Q

mechanism of orlistat?

A

inhibits GI and pancreatic lipases (enzyme)
decrease fat absorption from gut
loose stools

35
Q

mechanism of olestra?

A

blocks oil from being abosrbed

wow chips