Flashcards in hypolipidemic drugs Deck (52)
Cholestin and Evolve
dietary supplements that inhibit HMGCoA reductase
almost as effective as lovastatin
HMG coa reductase
enzyme that controls the rate of cholesterol production
effects of omega 3 FA?
like fish oil
decrease LDL and TG
effects of omega 6 FA?
like veg oil
BUT increases TG and decreases HDL
how does diet increase VLDL synthesis and secretion
excess caloric intake and not necessarily fat
risk factors for CHD
history of CHD/sudden death
when should dietary aid be passed and go right to drugs?
if patient has 2 or more risk factors OR history of CHD death OR just diabetes
three bile acid binding resins
and what do they do?
--> lower cholesterol(especially LDL)
which bile acid binding resin is best to lower LDL/cholesterol?
colesevelam (less GI side effects and less interference with other drugs)
bile acid binding resins are used to treat:
-heterozygous familial hypercholesterolemia
mechanism of cholesyramine/colestipol/colesevelam
bile acid binding resin
-> binds bile acids in intestines and inhibits its reabsorption
-cholesterol is the precursor to bile acid so more cholesterol is channeled to bile
-decrease in serum cholesterol, increase in LDL receptors, clearance of lipoproteins
adverse effects of bile acid binding resins
reduced intrahepatic cholesterol can cause secondary cholesterol production --> constipation and bloating(fix with fiber)
--resins can bind other drugs(warfarin/anticoagulants, vitamin K, B blockers)
when should bile acid resins be taken?
with or just before meals
--any other drugs should be taken 2 hrs before the resins or 4 hrs after to prevent resin binding
are resins safe to use in pregnancy?
what type of drug are bileacidbinding resins usually combined with?
HMGcoareductase (like lovastatin)
HMGcoa reductase inhibitors
any drugs that ends in -statin
what to use HMGcoareductase inhibitors for?
use statins for familial hypercholersterolemia, and combined hyperlipidemia
what do statins do?
they competitively inhibit HMGcoa reductase, decreasing cholesterol synthesis
causing upregulation(more ) of LDL receptors --> clearance of apoB and apoE lipoproteins (IDL, LDL, VLDL)
which statins reduce TG up to 40%?
simvastatin and atorvastatin
why are statins/reductase inhibitors usually given at night?
due to the diurnal pattern of cholesterol biosynthesis
side effects of statins
-high doses plus fibric acid derivative = rhabdomyolysis and renal failure
can pregnant women use statins?
statins and normal levels of blood cholesterol...
can reduce risk of heart attack and stroke
statins are excreted...
by CYP3A in the liver
statins drug interactions
grapefruit juice and verapamil increase serum statin  because they inhibit CYP3A (which breaks statins down)
what two statins are not broken down by CYP3A (use different paths)
pravastatin and fluvastatin
which statin is least potent (only 3% reaches circulation as active drug) - begins as inactive drug
active drug AS GIVEN
2nd MOST EFFECTIVE STATIN at reducing LDL cholesterol and TG
which statin is most effective at reducing LDL cholesterol and TG? 2nd?