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9 Cards in this Set
- Front
- Back
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Cholestyramine (Questran)
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"Bile Acid Binding Resins"-LDL
stop bile acids from re-entering the gut via entero-hepatic circulation- body senses low LDL- upregulates LDLR, endogenous cholesterol is used to form bile acids and therefore blood LDL falls Limited effect |
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Atorvastatin (Lipitor)
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"Statin"-LDL first line Tx
act by reversibly inhibiting HMG CoA Reductase (rate-limiting step in cholesterol synthesis)- decrease production on endogenous Cholesterol and increases LDLR expression which lowers serum LDL 25-50% reduction * does NOT work in familial hypercholesterolemia (mutations of the LDLR gene) or Familial Defective Apoplipoprotein B (defect in the ApoB ligand for LDL, which prevents binding of LDL to the LDLR) |
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Ezetimibe (Zetia)
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Newest-LDL
selectively inhibiting uptake of cholesterol from the intestinal lumen (unknown mechanism-inhibits the active transport mechanism in the enterocytes?) |
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Nicotinic Acid (Niacin)
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acts in the liver to inhibit triglyceride synthesis
reduces VLDL production and secretion, also increases the activity of lipoprotein lipase (LPL) *Additionally it increases HDL |
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Gemfibrozil (Lopid)
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Fibrate derivatives- "PPAR agonists"- TG
increase the synthesis of lipoprotein lipase (LPL)- act by activating PPAR_ nuclear receptor |
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Omega-3 fatty acids (Omacor)
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found in oily fish- or use a combination of eicosaphentaenoic (EPA) acid and docosahexanenoic (DHA) acids- TG
activates the PPAR_ recpetor |
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“Normal” Lipoprotein Levels
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Total Cholesterol: < 200 mg/dL
LDL: < 100 mg/dL HDL: > 40-45 mg/dL TG: < 150 mg/dL. |
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Theropeudic options for HYPERLIPOPROTEINEMIA
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1) Diet: eat less fat and cholesterol.
2) Exercise – via activation of LPL (unknown mech) 3) Control diseases that derange lipid metabolism (thyroid disorders / diabetes mellitus). 4) Discontinue drugs that negatively affect lipid metabolism 5) Drug therapy - currently blocking LDL or TG, future is to increase HDL |
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Vytorin
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combination drug of ezetimibe and a statin- LDL
acts via both pathways to further decrease serum cholesterol |
