-
cholestyramine
- insoluble in water (polymeric cationic exchange resin)
- safe/effective but not appetizing (4-5g, 3-4x/day)
- side effects: dyspepsia, constipation, decreased absorption of other drugs (digoxin, thyroxine, coumadin)
- binds bile acids and prevents reabsorption
- up regulates LDL receptors = increase uptake of LDL
- increase hepatic production of VLDL = increase triglycerides by 15-20%
-
colestipol
- insoluble in water (polymeric cationic exchange resin)
- safe/effective but not appetizing (4-5g, 3-4x/day)
- side effects: dyspepsia, constipation, decreased absorption of other drugs (digoxin, thyroxine, coumadin)
- binds bile acids and prevents reabsorption
- up regulates LDL receptors = increase uptake of LDL
- increase hepatic production of VLDL = increase triglycerides by 15-20%
-
nicotinic aid (Niacin)
- regular or timed release
- water soluble vitamin incorporated into NAD
- inhibits VLDL secretion = decreases production of LDL
- decreases triglycerides more than cholesterol
- no effect on bile production
- decreases circulating fibrinogen
- prostaglandin mediated cutaneous vasodilation
- glucose intolerance, hyperuricemia, worsens peptic ulcer disease
- sustained release and hepatic dysfunction
-
mevastatin and lovastatin
- competitive HMG CoA reductase inhibitor
- some prodrugs, some active drugs
- decreases cholesterol synthesis, up-regulates LDL receptors, and decreases LDL
- marked first pass metabolism
- mild hepatotoxicity
- rhabdomyolysis (worse if concurrent cyclosporin, clofibrate, niacin, erythromycin)
- lovastatin metabolized by CYP3A4
-
simvastatin, pravastatin, fluvastatin, and atorvastatin
- competitive HMG CoA reductase inhibitor
- some prodrugs, some active drugs
- decreases cholesterol synthesis, up-regulates LDL receptors, and decreases LDL
- marked first pass metabolism
- mild hepatotoxicity
- rhabdomyolysis (worse if concurrent cyclosporin, clofibrate, niacin, erythromycin)
- fluvastatin metabolized by CYP2C9
- simvastatin and atorvastatin metabolized by CYP3A4
-
alirocumab and evolocumab
- monoclonal antibody, PCSK9 inhibitor = increased LDL receptor expression at surface of liver
- injection
- useful alternative to patients who don't respond to statins
- current known side effects: irritation at site of injection, rash, limb pain, and fatigue
-
gemfibrozil, clofibrate, and fenofibrate
- fibric acid - ligand for PPARĪ±
- upregulates lipoprotein lipase, apo-A1 and A2 (major components of HDL)
- clears chylomicrons and VLDL quickly
- lowers VLDL and raises HDL
- increase side effects: GI (nausea, hepatic, myositis - worse with gemfibrozil and lovastatin)
-
ezetimibe
- absorbed and glucuronidated
- excrete into bile and feces
- impairs intestinal absorption of cholesterol
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