Lipid lowering drugs

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  1. 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%
  2. 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%
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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)
  8. ezetimibe
    • absorbed and glucuronidated
    • excrete into bile and feces
    • impairs intestinal absorption of cholesterol
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319485
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Lipid lowering drugs
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MOHD3 lipid lowering drugs lecture 65
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