Mechanisms/Drug Class Flashcards
What is the mechanism of action of cholesterol synthesis inhibitors?
Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis; LDL decreases up to 60%, HDL increases 10% and triglycerides decrease up to 40%
lovastatin
Inhibitor of cholesterol synthesis
pravastatin
Inhibitor of cholesterol synthesis
simvastatin
Inhibitor of cholesterol synthesis
fluvastatin
Inhibitor of cholesterol synthesis
atorvastatin
Inhibitor of cholesterol synthesis
rosuvastatin
Inhibitor of cholesterol synthesis
pitvastatin
Inhibitor of cholesterol synthesis
What is the mechanism of action of bile acid absorption inhibitors?
They bind to bile acids, preventing enterohepatic circulation; LDL decreases up to 28%, HDL increases 5%
cholestyramine
Inhibitor of bile acid absorption
colesevelam
Inhibitor of bile acid absorption
colestipol
Inhibitor of bile acid absorption
What is the mechanism of action of inhibitors of cholesterol absorption?
They decrease cholesterol transport from micelles into the enterocyte by inhibiting uptake through brush border protein NCP1L1; LDL decreases up to 20%, HDL increases 3%, triglycerides decrease 8%
ezetimibe
Inhibitor of cholesterol absorption
What is the mechanism of action of fibrates?
They are agonists of peroxisome proliferator-activity receptor α (PPARα); triglycerides decrease up to 50%, HDL increases up to 20%, DLD decreases up to 15%
gemfibrozil
Fibrate
fenofibrate
Fibrate
What is the mechanism of action of niacin?
It reduces free fatty acid release from adipose tissue, increases plasma residence time for apoA1; triglycerides decrease up to 45%, LDL decreases up to 20%, HDL increases up to 30%
What is the mechanism of action of omega-3 fatty acids?
They regulate nuclear transcription factors including SREBP-1c and PPARα to reduce triglyceride biosynthesis and increase fatty acid oxidation; reduces plasma triglycerides by up to 50%
Eicosapenaenoic acid
Omega-3 fatty acid
docosahexaenoic acid
Omega-3 fatty acid
