anti dyslipid Flashcards
hats the goal of anti dyslipidemia therapy?
lower LDL and VLDL and increase HDL
not all the available drugs are effective in all lipoprotein
what are the hypolipidemic agents?
1- statins
2- bile acid sequestrants
3- fibrates
4-nicotinic acid
5-plant sterols
6- agents reducing cholesterol absorption from intestine ( ezetimibe )
what are the most effective and most widely prescribed and best tolerated group?
statins
what are the bile acid sequestrants? or RESINS
cholestyramine and colestipol
whats their mechanism of action?
bind to bile acid and stops cholesterol and triglyceride absorption
will it make bile get secreted outside so the liver has to make new bile–> and bile is made via cholesterol and then the new bile come and same thing again it gets excreted and again
cholesterol is decreased and wasted in bile and is excerted
work mainly on cholesterol
what are the adverse effects of cholestyramine?
- Constipation ( heart burn, abdominal pain , bloating, nausea )
- Impaired absorption of any fat soluble compound : vitamines and anticoagulat , digoxin, thyroid
- bind weak acidic drugs
what are the inhibitors of intestinal sterol absorption?
ezetimibe
whats the mechanism of action of ezetimibe ?
binds directily to the cholesterol and impair its absorption
work only on cholesterol
what drugs do you usually combine ezetimibe with to reduce cholesterol?
statins
what are common adverse effects of ezetimibe?
fatigue , abdominal pain, diarrhea
reversible hepatic dysfunction
what are statins?
HMG coa- reductase inhibitor?
whats the mechanism of action of statins?
inhibit HMG COA- reductase and INHIBIT CHOLESTEROL SYNTHESIS IN THE LIVER.
Increased LDL receptors ( decreasing ldl in circulation)
WORK MAINLY ON CHOLESTEROL
what are the uses of statins?
familial and non familial hypercholesterolmias
reduce osteoporosis
reduce incidence of some cancers
imrpove endothelial function
what are the adverse effects of statins?
H –> hepatic dysfunction and elevation of transaminases
M–> myopathies, myositis,rhabdomyolysis , myoglobinuria and increased creatine kinase in blood due to heart muscle damage
G–> GIT upset –> nausea , epigastirc fullnes, vomitting
COA –? cataract ( lenticular opacity )
REDUCTASE –> renal dysfunction ( could lead to hypotension )
other side notes,
given in night
contraindicated in pregnancy
dont give with drugs that inhibit cyp450
whats drugs could lead to increased statin levels?
eryhtromycin
cyclosporin
gemfibrozil
niacin
cuz these drugs inhibit cyp450?
what are the fibrates agents?
colfibrate, fenofibrate,bezafibrate anything that ends with fibrate
whats the mechanism of action of fibrates?
they increase the activity of lipoprotein lipase ( which apo protein activate lipoprotein lipase)
SO mainly works on triglycerides not cholesterol
what are the uses of fenofibrate?
- used treat hyperlipidemia of several causes
has some uricosuric effect ( decreases uric acid )
when is fenofibrate is useleess?
in primary chylomicronemia where theres a deficiency in lipoprotein lipase
why cuz the enzyme itself its not there so theres nothing to work
what are the side effects of fenofibrates?
-cholelithiasis and cholecystitis
- GI upsets –> nausea and vomiting like statins and bile sequetrates
- Hepatic dysfunction ( elevate enzyme levels ) like statins
- myopathies like statins
what are nicotinic acids?
vitamin b3 ( NIACIN )
whats the mechanism of action of niacin?
Reduce VLDL production in liver by inhibiting lipolysis of adipose tissue ( inhibit adipose tissue lipase enzyme )
work on both cholesterol and triglycerides
what are other uses of niacin?
in low doses can be used as vitamin supplement in treatment of pellagra
which type of vitamin is niacin
its vitamin B so water soluble
what are the side effects of niacin?
Skin flushing and tingling and headache cuz it increases PGI and histamine ( countered by aspirin )
- GI irration, nausea and vomitting
- Peptic ulcer
-Hyperglycemia ( contraindicated in diabetic patients )
- Hyperuricemia ( contraindicated in gout )
-hepatotoxicity
whats the function of Evolocumab , alirocumab
they are PCSK9 inhibitors
whats the function of PCSK9?
downregulate the LDL receptors
statins work mainly on reducing what?
Cholesterol and LDL ( decrease by 20-50)
fibrates work mainly on reducing what?
triglycerides ( decrease by 20-50 )
niacin works mainly reducing what?
triglycerides (20-50%)
increase HDL ( 15-35%)
