Pharm block 2 (hyperlipoproteinemia #2)

  1. While a patient is On Simvistatin, what should be avoided? Why?
    • 1. Potent inhibitors of Cytochrome p450
    • - stop of Statin theropy
    • 2. Fibrates or Niacin
    • - do not exceed 10mg of Statins
    • 3. Amiodarone or verapamil
    • - do not exceed 20mg of statins

    These need to be avoided because Cytochrome p450 inhibitors block the metabolism of Statin drugs, prolonging their actions.
  2. What are the Firic acid derivatives?

    What is their mechanism of action?
    • Fenofibrate
    • Gemfibrozil

    They are PPAR-alpha agonists, which is involved in regulation of carbohydrates and lipid metabolism
  3. Gemfibrozil. What is it?

    What are its effects?
    It is a Fibric Acid Derivative

    • —These act by activating the lipoprotein lipase – key enzyme in the degradation of VLDL -- resulting in lowering of TG
    • —-Most effective for reducing TG
    • —-Reduce VLDL secretion also
    • —-Increase HDL synthesis
    • —-Modest decrease in LDL level
  4. What are some Adverse effects of Gemfibrozil?
    • -—Gall stones- there is an increased amount of Cholesterol trying to be brocken down.
    • —-Myopathy (when statins are combined with gemfibrozil)
    • —-Fenofibrates is less associated with myopathy than any other fibric acid
    • derivates.
  5. What does Nicotinic acid do?

    How does it do this?

    What is Nicotinic acid?
    • -—It reduces VLDL and TG production
    • -—It increase HDL
    • -—Effective drug in reducing LDL.

    - It inhibits adenylyl cyclase and HSL (heat sensative lipase)--> less FFA released into the plasma going to the liver--> less VLDL and TG being made and released from the Liver

    - like Vitamin B3
  6. Nicotinic acid, What is it the most effective treatment for?

    What are some of its adverse side effects?
    • It is the most effective medication to raise HDL cholesterol and it reduce the incidence of death and myocardial infarction among those with history of MI.
    • -—Cutaneous dilator– flushing, itching
    • -—Liver dysfunction
    • —-Hyperglycemia
    • -—Gout
    • -Concurrent use of niacin and statins can cause myopathy
  7. What does Ezetimibe do?
    Decrease cholesterol absorption by the small intestine. Decreased cholesterol absorption leads to an increase in LDL-cholesterol uptake into cells, thus decreasing levels in the plasma.
  8. Cholestyramine and Colistipol
    Main indication?
    Effects ?
    Main adverse effects?
    • -Elevated LDL (Can be used in pregnancy and children)
    • -↓ LDL(20%) ↑ TGs (~5%)
    • -GI problems
  9. Niacin
    Main indication?
    Main Adverse effects?
    -Elevated LDL, Low HDL and Elevated TG

    -↓ TG (40%), ↓ LDL (15%), ↑ HDL (25%)

    -Flushing of face & Pruritus and Hepatotoxicity
  10. Gemfibrozil
    Main Indication?
    Main Adverse effects?
    -Elevated TG

    • -↓ TG (50%), ↓ LDL (10%), ↑ HDL (15%)
  11. HMG-CoA Reductase Inhibitors (statins)
    Main Indication ?
    Main Adverse effects?
    - Elevated LDL

    -↓ LDL (30%),↑ HDL (8%), ↓ TG (20%)

    - Hepatotoxicity
  12. Name some things that increase HDL?
    • Weight reduction--- 5-20%
    • Physical Activity--- 5-30%
    • Smoking cessation---5%
    • Moderate alcohol consumption---8%
    • Mediteranean diet---2%
  13. What is Orlistat?
    what is its mechanism?
    It is an anti-obesity drug

    - it reduces intestinal fat absorption by inhibiting pancreatic lipase.
  14. What is Sibutramine?
    What is its Mechanism of action?
    Why isnt it used anymore?
    It is an anti-obesity drug.

    - It is a centrally acting serotonin norepinephrine re-uptake inhibitor (SNRI)

    - Because it increase MI and strokes
  15. what is Rimonabant?
    what is its mechanism of action?
    It is an anti obesity drug

    - it is an inverse agonist for the CB1 receptor. Main effect is reduction of appotite
Card Set
Pharm block 2 (hyperlipoproteinemia #2)
Pharm block 2 (hyperlipoproteinemia #2)