Pharmacology of Lipid-Modifying Agents

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mstengs
ID:
188831
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Pharmacology of Lipid-Modifying Agents
Updated:
2012-12-11 21:09:27
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Pharmacology Lipid Modifying Agents
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Pharmacology of Lipid-Modifying Agents
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  1. Statins
    • - First-line therapy for lowering LDL
    • - HMG-CoA reductase inhibitors
    • - Reduce production of VLDL/IDL/LDL
    • - Increase expression of LDL-R
    • - Contraindicated in liver disease, pregnancy/nursing
    • - Muscle-toxicity (esp. high doses, interacting meds)
  2. Lovastatin
    • - Low potency
    • - CYP3A4 metabolism
  3. Simvastatin
    • - Low potency
    • - CYP3A4 metabolism
  4. Pravastatin
    • - Low potency
    • - Not metabolized by CYP450 enzymes
  5. Fluvastatin
    • - Low potency
    • - CYP2C9 metabolism
  6. Atorvastatin
    • - High potency
    • - CYP3A4 metabolism
  7. Rosuvastatin
    • - High potency
    • - CYP2C9 metabolism
  8. Pitavastatin
    • - Medium potency
    • - CYP2C9, CYP2C8 metabolism
  9. Bile Acid Sequestrants (aka Resins)
    • - Add-on therapy to statins or Monotherapy for pt's who can't tolerate statins
    • - Bind to/promote excretion of bile acids in intestinal lumen
    • - Increase bile acid production
    • - Increase expression of LDL-R
    • - Contraindicated in elevated TG > 400
    • - Constipation + drug interactions
  10. Cholestyramine
    - Bile acid sequestrant
  11. Cholestipol
    - Bile acid sequestrant
  12. Colesevelam
    - Bile acid sequestrant
  13. Niacin
    • - Add-on therapy to statins
    • - Decrease TG synthesis in liver
    • - Decreases FFA --> liver, decreased TG & VLDL/IDL/LDL
    • - Increases HDL
    • - Facial flushing
    • - IR, SR, ER formulations
  14. Fibrates
    • - First-line therapy for lowering TG
    • - PPARα agonist
    • - Upregulate LPL, which breaks down TG's to FFA's
    • - Contraindicated in severe liver disease
    • - Myopathy (esp. Gemfibrozil + statin)
    • - Increase effects of Warfarin
    • - Dose-adjusted for renal function
  15. Gemfibrozil
    • - Fibrate
    • - Increased risk of myopathy + statins
  16. Fenofibrate
    • - Fibrate
    • - No increased risk of myopathy + statin
  17. Cholesterol Absorption Inhibitor
    • - Add-on therapy to statins for lowering LDL (~18%)
    • - Impacts NPC1L1 sterol transporter
    • - Reduces absorption of cholesterol at small intestine brush border
    • - Upregulation of LDL-R
    • - Contraindicated in severe liver disease
  18. Ezetimibe
    - Cholesterol absorption inhibitor (only one)
  19. Fish oils (Omega-3 FA's)
    • - EPA & DHA
    • - Decrease TG's (4g/day)
    • - Decrease risk of sudden cardiac death (~1 g/day)
    • - Smelling of fish
    • - Better absorbed with food
    • - Read the label to acheive needed dose
  20. Plant Sterols
    • - Competitively block cholesterol aborption in small intestines
    • - Naturally occurring in plants + margarine/chews
    • - TLC diet recommends 2 g/day
    • - Difficult to acheive this dose

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