Pharm Test 3

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  1. Activates LCAT, ligand for ABC (ATP binding cassette), involved in reverse cholesterol transport
  2. Ligands for HDL receptor
    A-1, A-II
  3. Ligands for LDL receptor
  4. Cofactor for activation of LCAT;  modulates remnant binding to receptors
  5. Cofactor for activation of LPL
  6. Inhibits C-II activation of LPL; modulates remnant binding to receptors
  7. Mediates remnant uptake through the LDL recpetor and the LDL receptor-related protein
  8. Statins
    HMG-CoA Reductase Inhibitors (Inhibit enzyme from making cholesterol out of HMG-CoA)
  9. Bile Acid Binding Resins
    • Inhibit bile uptake from gut.  Include:
    • Cholestyramine
    • Colestipol
    • Colesevelam
  10. Inhibitor of Cholesterold Absorption from gut
  11. Ezetimibe
    Inhibitor of cholesterol absorption from gut
  12. Fibrates
    • Gemfibrozil
    • Fenofibrate
    • Clofibrate
  13. Resins and Ezetimibe work where?
    Small intestine
  14. Fibrates work in
    Endothelium, liver
  15. Statins work in
    liver only
  16. Only thing that works in adipose tissue and muscle
  17. 3 things that work in liver
    Statin, Niacin, Fibrates
  18. 3 indications for HMG-CoA reductase inhibitors
    • Hypercholesterolemia
    • Hypertriglycerdemia
    • Mixed dyslipidemias
  19. Only two HMG-CoA Reductase Inhibitors that have inactive metabolites
    Fluvastatin, pravastatin
  20. Causes myopathy (myalgia)
  21. Mechanism of action:  HMG-CoA Reductase Inhibitors
    • Primary:  Competitive, reversible inhibition of HMG-CoA Reductase
    • Secondary Actions: Induction of LDL receptor w/ increased LDL, IDL, and VLDL clearance
    • Inhibition of VLDL synthesis
  22. HMG-CoA effects
    • LDL:  Decreased
    • TG:  Decreased
    • HDL: Increased
  23. What decreases statin-induced myopathy
    Vitamin D
  24. Can't give statins w/ two things
    • 1)  Fibrate --> myopathy
    • 2)  Niacin --> cardiomyopathy
  25. Can causes hepatotoxicity
  26. Absolute contraindication of statins
    Liver Disease
  27. MoA:  Ezetimibe and Resins (E&R)
    • Primary actions (gut):  inhibit reabsorption of bile acids (resins) or cholesterol (ezetimibe)
    • Secondary actions (liver):  Increased expression of LDL receptors and clearance of LDL from plasma
    • Resins:  increased TG and bile acid synthesis
  28. Hypercholesterolemia in pregnant children
    Resins (pregnant children like raisins)
  29. Benefits
    • Reduced major coronary events:  Statins, Resins, Niacin, FAD
    • Reduced CHD mortality:  Statins, Resins
    • Reduced incidence of stroke:  Statins
    • Reduced overall CVS mortality:  Statins, Niacin
    • Slow progression of coronary lesions:  FAD
  30. Causes exacerbation of hemorrhoids or interference w/ absorption of other drugs
  31. 2 contraindications for resins
    • Dysbetalipoproteinemia
    • Hypertriglyceridemia
  32. Indications for ezetimibe
  33. Enterohepatic recycling
  34. Ezetimibe MoA
    Inhibits NPC1L1 transporer in jejunal and duodenal enterocytes
  35. Most efficacious of hypolipidemic drugs at increasing HDL-cholesterol
  36. B vitamin
  37. Niacin indications
    All hyperlipidemias except those w/ lipoprotein lipase deficiency (type 1)
  38. Niacin:
    Lipoprotein lipase activity
    Hormone sensitive lipase activity
    Triglyceride and FA synthesis
    • Increases
    • Inhibits
    • Inhibits
  39. Impaired glucose tolerance, liver function, increased urate formation and peptic ulceration, cardiac arrhythmia, blurred vision
  40. 5 contraindications of Niacin
    • Pregnancy
    • PUD (NSAIDs)
    • Liver disease
    • Severe gout
    • Statins
  41. All defivatives of niacin are associated w/
  42. Ester of niacin and clofibrate
  43. Derivative of niacin that reduces LDL and is also hypoglycemic
  44. 2 Fibric Acid Derivatives
  45. Fenofibrate is a prodrug that is activated?
    in the gut
  46. Drug of first choice if TG >500 mg/dL (hypertriglyceridemia)
    Fibric Acid Derivatives (gemfibrozil, fenofibrate)
  47. Like Niacin, Fibric acid derivatives inhibit
    • Hormone sensitive lipase
    • (they also inhibit expression of ApoC-III)
  48. Fibri Acid derivatives are a ligand for
    PPAR-a (Peroxisome proliferator-activated receptor)
  49. Drugs that are ligands for PPAR-a
    Fibric acid derivatives
  50. Fibric Acid derivatives have increased expression of
    • FA oxidation
    • LPL
    • ApoA-1, A-II
  51. 3 Contraindications of FAD
    • Renal failure
    • Pregnancy
    • Childhood
  52. Adverse effects of FAD
    • Myopathy (particularly w/ statin)
    • Cholecystitis
Card Set:
Pharm Test 3
2012-12-19 07:02:07

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