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21 Cards in this Set

  • Front
  • Back
What are the HMG-COA reductase inhibitor drugs?
- Lovastatin
- mevacor
- these are the most effective agents currently available
Where is the major effect of HMG-COA drugs?
- in the liver
- marked first pass hepatic extraction
Major effect of HMG-CoA?
- reduce cholesterol synthesis in the liver by competitively inhibiting HMG-CoA reductase
- this is the rate limiting enzyme in cholesterol synthesis
- induce an increase synthesis of LDL reseptors
- this results in an increase in liver's extraction of LDL and reducing LDL in the plasma
When used?
Adverse effects?
- used in hypercholesterolemia and mixed hyperlipidemia
- increase in hepatic enzymes (hepatitis) and myalgia (myositis)
- should be discontinued if levels of creatine is found to be elevated
drug of Nicotinic acid?
- Niacin
Mechanism of Niacin?
- reduces VLDL secretion and increases VLDL clearance in plasma
- inhibits lipolysis in adipose tissue***
- decreases supply of FFA to the liver and hepatic synthesis of VLDL
When is Niacin useful?
- mixed hyperlipidemia because of it's favorable influence on serum levels of VLDL, LDL, and HDL
- can be combined with other drugs
Adverse effects
- marked vasodilation and flushing of the skin ... may see pruritis
- treat above with aspirin
- elevation of serum transaminase
- gastric distress
- glucose intolerance
Niacin should be avoided by..
- pts with liver disease, peptic ulcer, or hyperuricemia and diabetes
What drugs are Fibric Acid derivatives?
- Gemfibrozil
- Lopid
Fibric acid derivative mechanisms
- decrease VLDL and tri's by increasing the activity of lipoprotein lipase and hydrolysis of VLDL
- promote delivery of tri's to adipose tissue
When are fibric acid derivatives used?
- primarily in hypertriglyceridemia
- also in mixed and HDL deficiency
Fibric acid adverse effects
- allergic reactions
- blood deficiencies
- myalgia
- increase myopathy when given with HMG-COA
what drugs are the bile acid binding agents?
- Colestipol
- Colestid
Bile acid binding mechanism
- bind bile acids and prevent their absorptions
- this leads to the synthesis of replacement bile acids from cholesterol in the liver
- liver then increases the number of LDL receptors and removes LDL from plasma!
Bile acid binders have no effect on
- HDL or triglycerides
Bile acid binders used with pts that
- cannot tolerate other drugs
- or these are used in comb with other drug
bile acid binder effects
- GI effects:
nausea, bloating, constipation
- interfere with absorption of fat-soluble vitamins such as DIG, hydrochlorothiazide adn warfarin
what are the inhibitor of intestinal cholesterol absortion drugs?
- ezetimibe
- zetia
Mechanism of inhibitors of intestinal cholesterol absorption drugs?
- inhibits intestinal absoption of cholesterol adn phytosterols
- effective even in absense of dietary cholesterol because inhibits absorption of cholesterol excreted in bile