Pharm block 2 (hyperlipoproteinemia #2)

• 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.

• Fenofibrate
• Gemfibrozil

They are PPAR-alpha agonists, which is involved in regulation of carbohydrates and lipid metabolism

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

• -—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.

• -—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

• 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

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.

• -Elevated LDL (Can be used in pregnancy and children)
• -↓ LDL(20%) ↑ TGs (~5%)
• -GI problems

-Elevated LDL, Low HDL and Elevated TG

-↓ TG (40%), ↓ LDL (15%), ↑ HDL (25%)

-Flushing of face & Pruritus and Hepatotoxicity

-Elevated TG

• -↓ TG (50%), ↓ LDL (10%), ↑ HDL (15%)
• - GULL STONES

- Elevated LDL

-↓ LDL (30%),↑ HDL (8%), ↓ TG (20%)

- Hepatotoxicity

• Weight reduction--- 5-20%
• Physical Activity--- 5-30%
• Smoking cessation---5%
• Moderate alcohol consumption---8%
• Mediteranean diet---2%

It is an anti-obesity drug

- it reduces intestinal fat absorption by inhibiting pancreatic lipase.

It is an anti-obesity drug.

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

- Because it increase MI and strokes

It is an anti obesity drug

- it is an inverse agonist for the CB1 receptor. Main effect is reduction of appotite