All have "statin" at the end

Lowers LDL

Competitively inhibits HMG-CoA reductase (which is the rate limiting step of cholesterol synthesis that converts HMG-CoA to mevalonate)

Increases LDL receptors (to remove LDL from circulation)

Improve in efficacy over time

New Drugs (PITA AT ROSie's); Synthetic; active and more potent metabolites, longer t1/2, pleiotropy (improve other stuff too-platelet function, blood viscosity, leukocyte adhesiveness), $$

Highly protein bound, except pravastatin (50%)

CYP3A4 incteractions except pravastatin (none) and fluvastatin (2C9)

"PRavastatin=Private"-No interactoins with protein or CYP3A4's

Low compliance (patients don't feel better)

SE: Increased liver transaminases, Myopathy (CK<10x normal), Rhabdomyolysis->toxic components into blood and cardiac arrest (CK>10x normal)

Colesevelam, Cholestyramine, Cholestipol ("Cole Cho Cho")

Bind bile acids->can't be reabsorbed via portal vein and get excreted instead

Lower LDL (not as much as statins)

Increase HDL

Increase TG's (Contra: TG>200)

2nd line: For pregnancy or statin intolerance

Unpalatable pills/powders 1 hour before meal or 4 hours after

SE: GI distress, impair ADEK absorption

All have "fibr" in the middle

Lower TG's (High TG common in type II DM, contribute to heart disease, associated with pancreatitis-levels >500mg/dL!)

Activates transcription factor PPARalpha->increased VLDL/TG clearance

Increases FA oxidation

Decreases Apolipoprotein CIII->knocking it out allows increased liver uptake of TG's (Apo CIII normally works as a component of VLDL to inhibit TG uptake)

2-4x/day before meals

Fenofibrate: Once a day w/o regard to meals ("Fenofibrate is fine to take 1x/day")

SE: Myopathy, GI stuff (SE's more common when taken with statins)

Contra: Liver or kidney disease (cleared hepatically and renally)

Vitamin B3 (Niacin)

Increases HDL (1pt increase->2-3% decrease in MI/stroke risk)

Lowers TG

Lowers LDL/reduces ApoB expression

Can be combined with statins for greater effect

Large dose (200mg) required

Immediate release, extended release (niaspan), and OTC counter sustained release

Niaspan: High stroke rate, no CV benefit->currently unavailable

SE: Flushing (20-60 minutes after taking, worse w/ missed doses; reduced w/ food or NSAID); itching (pruritis), headaches, peptic ulcer

Conra: Liver disease or Gout

Raise HDL

Lower TG

Possible LDL elevation

Fish oil supplements are a good source

Lovaza ("LOVes fish"): Most concentrated

Contra: Bleeding disorders, thrombocytopenia

SE: GI distrubance, bleeding, fishy burps

Increase HDL

Switch cholesterol transport from transport by LDL to transport by HDL

Torcetrapib (CET in the middle=cholesterol ester transfer)

SE: Death

Inhibits cholesterol absorption across gut->increases fecal excretion

Lowers LDL

Taken w/o respect to meals, low adverse effects...except cancer

Combined ezetimibe+statins->No significant intimal thickness reducing effects