Agents used to treat hyperlipedemias Flashcards
what is hyperlipidemia?
defect in lipid transport system that provides cholesterol and triglycerides to the cell
what does hyperlipidemia increase the risk of?
inc risk of coronary artery disease with increase in blood lipids
inc risk of plaque formation
inc risk of pancreatitis
inc risk of xanthoma
what do different levels of LDL cause?
160- 4x inc in coronary artery disease
what causes secondary hyperlipoproteinemias?
cirrhosis, nephrosis- alcohol and diabetes
drugs
what causes primary hyperlipoproteinemias?
genetic abnormalities- decrease lipoprotein lipase abnormal LDL receptors overproduction of VLDL decrease HDL synthesis
non-pharmacologic treatment of hyperlipidemias
weight loss
diet- decrease fat and cholesterol
stop smoking
aerobic exercise
pharmacologic treatment of hyperlipdemias
decrease production of lipoproteins
increase removal of lipoproteins
decrease absorption of lipoproteins
some of these agents may affect the fetus
what are the hypolipidemic agents?
HMG coA reductase inhibitors niacin bile acid binding resin fibrates omega 3 fatty acids and icosapent lomitapide mipomersen
what are the agents that decrease cholesterol absorption by the intestine?
ezetimibe
sitostanol
orlistat
olestra
what is the most effective LDL lowering agent?
HMG CoA reductase inhibitors
what causes the strongest increase of HDL?
Niacin
what is the best triglyceride lowering agents?
fibrates
what can bind to acidic drugs? acidic drug example?
bile acid binding resins
digoxin
what can displace warfarin from plasma binding sites?
the fibrates
what are the HMG CoA reductase inhibitors?
statins
what is the mechanism of the statins?
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
what are the side effects of statins?
myositis (muscle pain) at worst- rhabdomyolysis liver toxicity teratogenic- pregnancy category x some of them associated with memory loss
differences in the different statins?
pharmacokinetics
what is the mechanism of action of niacin?
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)
side effects of niacin
cutaneous flushing, itching- prevented by aspirin
increased uric acid, increased gout
increased incidence of diabetes
what are the bile acid binding resins
cholestyramine
colestipol
coleselevam
highly charged cationic resins
bile acid mechanism of action
irreversibly bind to bile acids in the gut- cholesterol is excreted
decrease circulating cholesterol
increase LDL receptors
what are the side effects of bile acids?
no systemic side effect- not absorbed
can bind to acidic drug like digoxin
decrease absorption of fat soluble vitamins
nausea
what are the fibrates?
gemfibrozil and fenofibrate
best triglyceride lowering agents
