- bile salts emulsify fats

-breakdown of triglycerides by lipase

-formation of micelle and absorption into enterocytes

-lymphatic capillaries, thoracic duct, subclavian veins, inferior vena cava

-primarily involved in transport of dietary lipids from gut to adipose tissue and liver

-emulsified lipids by the bile acids are combined w/ proteins to form chylomicrons in the gut wall

-chylomicrons receive apoprotein C and E from HDL

-deliver TGs to adipose tissue via LPL (lipoprotein lipase) located in vascular endothelial cells

statins

-reduce hepatic cholesterol biosynthesis by competitive inhibitition

-increase number of hepatic LDL receptors and enables more LDL to be delivered to the liver

-reduces LDL in plasma and cholesterol available for formation of VLDL

-rhabdomyolysis is major side effect -> muscle cells are destroyed releasing myoglobulin which can cause acute renal failure

-can increase warfarin levels

-take at night to reduce nocturnal cholesterol biosynthesis

cholestyramine, colesipol, colesevelam

-resins bind to bile acids and then are secreted

-action prevents enterohepatic cycling of bile acids and causes liver to use more cholesterol in production of more bile acids

-the liver increases LDL receptors which reduces LDL in plasma

-have little effect on HDL and TG

-will bind to digoxin, thyroxin, warfarin, and other drugs in the gut -> take 2 hrs apart from these

-colesevelam (newer) does not effect these drugs and can be coadministered with most drugs

-valuable for young patients who will be on longterm therapy -> low side effects

-indicated for diarrhea -> causes constipation

-colestipol given for digoxin OD

ezetemibe

-inhibits absorption of dietary cholesterol by blocking cholesterol/sterol transporter, NPC1L1 at the brush border of the small intestine

-allows for lower statin dose with similar effect

fenofibrate, gemfibrozil

-activate gene trascription factor PPAR-a

-increases expression of LPL (lowers plasma TGs)

-lowers expression of apo C-III

-increases enzymes that oxidize FA

-increases expression of apo A-I and A-II (inc LDL)

-increase expression of cholesterol transport protein

-increases expression of hepatic LDL receptors

-has positive effect on entire lipid panel

-cause blood cell deficiencies

-can cause rhabdo and myopathies

-reduces lipolysis and free fatty acid mobilization from the liver

-high affinity GPCR inhibitor (dec cAMP)

-dec FFA availability reduces hepatic TG synthesis and VLDL secretion from the liver

-may cause vasodilation and flushing

-may elevate transaminase causing hepatitis

-can cause glucose intolerance (consider DM)

-avoid with hepatic disorders, peptic ulcer, or DM

-best agent for increasing HDL

-good for entire lipid panel

fish oil, omega-3 fatty acids

lovaza

-reduce TG in plasma, increase conversion of VLDL to LDL, increase HDL

-decreases thrombogenesis and platelet aggregation

-slows atherosclerosis by reduced expression of endothelial adhesion molecules

-promotes NO-mediated vasodilation

-reduces arrhythmia