HMG CoA reductase inhibitors

Lovastatin & other -statins:

MOA: inhibits the rate limiting enzyme in cholesterol synthesis (dec. liver cholesterol & plasma LDL but inc. LDL receptor expression)

Decrease in VLDL synthesis resuls in dec. TG's too

SE: myalgia, myopathy, rhabdomyolysis, hepatotoxicity (check LFT's)

 DI: Gemfibrozil (increases rhabdomyolysis)

P450 inhibitors enhance toxicity

Bile Acid Sequestrants

Cholestyramine & colestipol

MOA: prevent recycling of bile salts in the gut which dec. liver's recirculation of bile salts so the liver has to make new each time (overall dec. liver cholesterol and blood cholesterol but inc. LDL receptor expression)

SE: increases VLDL and TG's, GI disturbances, malabsorption of lipid-soluble vitamins

DI: w/ orally administered warfarin, thiazides, dig

Contraindication: w/ hypertriglyceridemia

Nicotinic Acid

Niacin & Vitamin B3

MOA: inhibition of VLDL synthesis so decreases plasma VLDL/LDL and increases HDL

SE: flushing, pruritits (pretreat w/ ASA)

hepatotoxicity

Gemfibrozil (fenofibrate)

MOA: activation of lipoprotein lipases (dec. VLDL/IDL w/ modest decrease in LDL but increases HDL) used in pts w/ hypertriglyceridemia

SE: May actually increases LDL in some

Gallstones, myositis

Ezetimibe

MOA: prevents intestinal absorption of cholesterol results in dec. LDL

SE: GI distress

Pts w/ only high cholesterol (meds to use)

Pts w/ high TG's

Pts w/ high cholesterol and high TG's