pharmacology: antihyperlipidemics Flashcards
what are the HMG-CoA reductase inhibitors? what does inhibition result in?
-statins
causes decreased liver cholesterol, increased LDL receptor expression, decreased plasma LDL and also decreased VLDL synthesis
statins (HMG-CoA reductase inhibitors) side effects
myalgia, myopathy, rabdomyolysis, hepatotoxicity (can’t get rid of fats - cause free radical damage)
how does increased LDL cause disease?
too much cholesterol in liver = no need to take up LDLs = if LDL not taken up, then releases cholesterol in fatty streaks = atherosclerosis
what are the bile acid sequestrants? mechanism?
cholestyramine and colestipol
mechanism: complexation of bile salts in the gut resulting in
decreased enterohepatic recirculation of bile salts
increased synthesis of new bile salts by the liver
decreased liver cholesterol
increased LDL-receptor expression
decreased blood LDL
cholestyramine and colestipol side effects
increased VLDL and triglycerides
GI disturbances
malabsorption of lipi-soluble vitamine (ADKE)
drug interactions with orally administered drugs
contraindication of bile acid sequestrants (cholestyramine and colestipol)
hypertriglyceridemia
nicotinic acid (niacin) mechanism and side effects
mechanism: inhibition of VLDL synthesis resulting in
decreased plasma VLDL
decreased plasma LDL
increased plasma HDL
side effects: flushing, pruritus, buring pain (aspirin), hepatotoxicty
what is the burning pain in nicotinic acid (niacin vit b3) due to?
prostaglandins (NOT HISTAMINE) - why it can be treated with aspirin!
gemfibrozil and fenofibrate mechanism
bind to the PPARalpha and increase induction of lipoprotein lipases resulting in
decreased VLDL and IDL
modest decrease LDL
increased HDL
what is gemfibrozil and fenofibrate used in?
hypertriglyceridemia
gemfibrozil and fenofibrate side effects
gallstones and myositis
ezetimibe mechanism and side effect
prevents intestinal absorption of cholesterol, results in decreased LDL
SE: GI distress (POO!)
what does ezetimibe need to be used with
STATIN!
what should be used in increased cholesterol?
cholestyramine, colestipol, ezetimibe
what should be used in increased triglycerides?
gemfibrozil and fenofibrate
