Exam 3; Agents used to treat Hyperlipidemias Flashcards
What causes hyperlipidemia
a defect in the lipid transport system which provides cholesterol and triglycerides to the cell
There is an increased risk of these three things with an increase in blood lipids
coronary artery disease; due to increased plaque formation
pranceatitis
xanthoma; deposition of fat in the skin
This form on lipoprotein when in high levels, causes more potential problems
LDL; low density lipoproteins
What is the desirable level of LDL
< 100mg/DL
What converts chylomicrons ti free fatty acids
lipoprotein lipase
The chylomicron remnants (cholesterol) travel to which organ
the liver
These two things combine to form vLDL
apolipoprotein and cholesterol
What is the intermediate step in the formation of LDL from vLDL
vLDL → IDL → LDL
steps all catalyzed by lipoprotein lipase
If LDL becomes oxidized, what occurs
it is taken up by macrophage and deposited on arterial linings
What is a major carrier of cholesterol
LDL
LDL binds to what on the cell
LDL receptor
This enzyme in the cells can make cholesterol
HMG CoA reductase
Cholesterol can make these oh which can go into the gut
bile acids
What is considered the “good cholesterol”
HDL
high density lipoproteins
What four things cause secondary hyperlipoproteinemias
cirrhosis
alcoholism
nephrosis
diabetes
What are four things that cause primary hyperlipoproteinemias
decreased lipoprotein lipase
abnormal LDL receptors
over production of vLDL
decreased HDL synthesis
What are two non-pharmacologic treatments of hyperlipoproteinemias
diet/exercise
stop smoking
What are three mechanisms behind pharmacologic effects of drugs treating hyperlipoproteinemia
decrease production of lipoproteins
increase removal of lipoproteins/cholesterol
decrease absorption of lipoproteins
Can agents that treat hyperlipoproteinemias affect the fetus
Yes
What will happen to the effects of hyperlipoproteinemia drugs upon stoppage of taking them
the effects will stop as well
Which family of drugs are the HMG CoA reductase inhibitors
“-statin’s”
True or False
the HMG CoA reductase inhibitors (-statins) are the most effective LDL lowering agents
True
What is the mechanism of action behind the statin drugs
inhibits HMG CoA reductase; the rate limiting step in the cell synthesis of cholesterol
When the cells cannot make their own cholesterol, how do they compensate
they increase the LDL receptors on the cell
What is a major side effect of the statin drugs
myositis; muscle pain
especially true since many are metabolized by P450
What are three side effects of statin drugs
liver toxicity
teratogenis; pregnancy category X
some memory loss
What is the main difference between all the statin drugs
pharmacokinestics
What is the mechanism of action behind niacin
it inhibits an enzyme essential for vLDL synthesis and may also bind to a receptor that decreases vLDL synthesis
What is the result of using niacin
decrease in vLDL
increase in HDL; strongest increaser of HDL
What are four side effects of Niacin
cutaneous flushing (red face)
itching
increased uric acid; gout
increase incidence of diabetes
What are the three bile acid binding resins
cholestyramine
colestipol
coleselevam
“coles”
What is the mechanism of action behind the “coles”
irreversibly bind to bile acids in the gut; are excreted along with their cholesterol
What two things do the “cole” drugs cause
decrease in circulating cholesterol
increase in LDL receptors
What are the side effects of the “cole” drugs
no side effects because they are not absorbed; but can cause nausea or GI irritants
This family of drugs are the best triglyceride lowering agents
the fibrates
What is the mechanism behind the fibrates
binds to PPAR; perixosome proliferator activating receptor
increasing the activity of LPL
What are the fibrates
gemfibrozil
fenofibrate
(both have fibr)
What are two side effects of gemfibrozil and fenofibrate
GI upset
can displace warfarin from plasma binding sites
These two things decrease triglyceride synthesis via inhibition of an enzyme
omega 3 fatty acids
icosapent ethyl
This essentially inhibits assembly of vLDL in the liver; both an enzyme and a transporter
imoitapide
This is an anti-sense oligonucleotide
mipomersen
What is the mechanism of mipomersen
binds to the mRNA for apoloprotein-B; preventing it from being synthesized
This drug blocks cholesterol transport
ezetimibe
This drug looks like cholesterol and blocks its uptake
sitostanl
This inhibits GI and pancreatic lipase, decreasing fat absorption from the gut and causes loose stools
orlistat
This is an non-absorbable oil used for frying/cooking but causes anal leakage → gross.
olestra
