Drugs - Cholesterol

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Author:
GaryW
ID:
136211
Filename:
Drugs - Cholesterol
Updated:
2012-02-18 23:02:01
Tags:
Cholesterol
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Description:
Lipids Test
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  1. What can elevated triglycerides (>500 mg/dL) cause?
    Life-threatening pancreatitis
  2. Lovastatin
    Mevinolin
  3. Simvastatin
    Zocor
  4. Pravastatin
    Pravachol
  5. Fluvastatin
    Lescol
  6. Atorvastatin
    Lipitor
  7. Rosuvastatin
    Crestor
  8. Niacin: Side Effects
    “Hot Flashes” or “Pruritus” due to prostaglandin-mediated & histamine release o May be able to give aspirin (81mg – 325mg) daily or NSAID 30 minutes b4 o Could try extended release · Hepatic effects: ↑ amino transaminase · Hyperglycemia · GI disturbances & peptic ulcer · Renal effects - ↑ plasma uric acid & contraindicated w/ gout
  9. Niacin (Nicotinic Acid)
    MOA?
    Reduces VLDL synthesis and esterfication of Fatty Acids in Liver

    ↓ VLDL / ↓ LDL (@ FULL DOSE) / ↑ HDL (decrease HDL catabolism)
  10. Which cholesterol drug is cardioprotective?
    Niacin (Nicotinic Acid)
  11. Which nicotinic acid drug is not used for the tx. of cholesterol?
    Nicotinamide (used for pellagra)
  12. Which cholesterol drugs require monitoring of liver enzymes?
    Statins and Niacin
  13. What are the contraindications for Niacin?
    • 1. Gout
    • 2. Peptic Ulcer Dz
    • 3. Macula edema
  14. Niacin - what are the side effects?
    • 1. Hot flash via prostaglandin release
    • 2. Elevated LFT and CPK
    • 3. GI upset
    • 4. Renal - increase in plasma uric acid
    • 5. increase in amino transferases
  15. What can be given 30 minutes prior to the admin of niacin to prevent the "hot flashes"?
    Aspirin
  16. Cholestyramine
    (Questran)
  17. Colesevelam
    (Welchol)
  18. Colestipol
    (Colestid)
  19. What are the contraindications for bile acid binding resins?
    · Triglycerides above 500 mg/dL · Family defect in genes for LDL receptors (needs functional receptors)
  20. What drug may help the GI side effects of Bile Acid Binding Resins?
    Psyllium
  21. Which bile acid binding resin is the best w/ the least side effects?
    Welchol (Colesevelam)
  22. What are the side effects for Bile Acid Binding Resins?
    · GI: constipation and gas, including absorption of fat soluble vitamins o Affects warfarin & digitalis (affects anionic drug absorption) o Psyllium may prevent GI symptoms o Best one is Welchol – less effects
  23. Which cholesterol drug may reduce MI in older middle-aged men both w/ RF and not?
    Statins
  24. When shoulds Statins be taken?
    At night - highest syn at that time by the liver.
  25. Which of the statins is know to lower total cholesterol by 30-50% and LDL up to 60%?
    (rosuvastatin)
  26. Statins - Mech of Action?
    MOA [↓ LDL & Tri / ↑ HDL]

    Inhibit the rate-limiting enzyme [3-hydroxy-3-methylglutaryl coenzyme A reductase] in the formation of cholesterol biosynthesis (HMGA to mevalonic acid)

    ↓ syn. Of cholesterol in Liver / ↑ LDL receptors allow for liver to pull from blood
  27. Contraindications for Statins?
    Utilizes CYP3A4: drug levels will increase w/ protease inhibitors, imidazole antifungals, grapefruit juice, cyclosporine & erythromycin à ↑ levels = ↑ chance of myositis
  28. Which drug may affect osteoclasts and therefore preventing osteoporosis?
    Statins
  29. Side effects of Statins?
    Myositis (↑ incidence w/ concurrent use of fibrates or niacin)

    Monitor liver and muscle enzymes q 3 mo then q 6mo – hepatotoxicity and ↑ aminotransferases

    • Affects level of Warfarin
    • CPK – muscle elevation may be harmless

    Erythromycin, cyclosporine and azole antifungals reduce drug effectiveness
  30. What is the first step in treating hypertriglyceridemia?
    Diet modification - as TRIG reflects what is eaten.
  31. What risk is posed when triglycerides are higher than 500 mg/dL
    Pancreatitis
  32. Fibrinic Acid (Fibrates) MOA?
    • Peroxisome proliferative-activated receptor-alpha (PPAR-alpha), a class of nuclear receptor agonists – alters gene transcription in triglyceride metabolism including lipoprotein lipase (LPL) & apolipoprotein CIII
    • o ↑ peripheral catabolism of VLDL and chylmicrons
    • o ↓ liver production of triglycerides
    • o ↓ triglycerides / ↑ HDL
  33. Which cholesterol drug in the Helsinki study - lowered cholesterol in middle aged men free of CAD?
  34. Gemfibrozil (Lopid)
  35. Which fibrate has an increased chance of neoplasm?
    Clofibrate
  36. Side effects of Fibrates?
  37. SIDE EFFECTS
    • · Cholelithiasis (gall stones) & cholecysitis
    • · GI intolerance: N/V/mild D
    • · Hepatitis
    • · Myositis
    • · Gynecomastia
    • · Weight gain
  38. Fibrates: Contraindications?
    Displaces other albumin bound drugs – sulfonylureas & warfarin

    ↓ Renal or hepatic function
  39. Ezetimibe: MOA?
    • Lipid lowering by blocking intestinal absorption of dietary & biliary cholesterol à inhibits cholesterol transporter (@ brush border cells), so it won’t cross intestinal wall
    • · ↓ LDL by 10-15% alone
    • · w/ statin – total cholesterol reduction of ~72%
  40. Ezetimibe: Side Effects?
    Fatigue, abdominal pain and diarrhea – all are rare!

    USUALLY well tolerated
  41. Ezetimibe: Contraindications?
    Warfarin & thyroxin – time meds so it doesn’t interfere
  42. Ezetimibe: Brand Name?
    Zetia

    Cholesterol Absorption Inhibitors
  43. Gemfibrozil - brand name?



    [Fibrates]
    Lopid
  44. Fenofibrates - brand names?
    • 1. Antara
    • 2. Triglide
    • 3. Lofibra
  45. Clofibrate
    Atromid
  46. Atorvastatin
    Liptor
  47. Simvastatin
    Zocor
  48. Rosuvastatin
    Crestor
  49. Pravastatin
    Pravacol
  50. Lovastatin
    Mevacor
  51. Fluvastatin
    Lescol
  52. Colesevelam
    Welchol


    [bile acid binding resin]
  53. Colestipol
    Colestid

    [bile acid binding resin]
  54. Cholestyramine
    Questran

    [bile acid binding resin]
  55. Niacin (Nictonic Acid)
    • 1. Nicobid
    • 2. Nicolar
    • 3. Nicotinamide (not used for cholesterol) – in small dose these can be used for tx of pellagra

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