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21 Cards in this Set
- Front
- Back
What are the HMG-COA reductase inhibitor drugs?
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- Lovastatin
- mevacor - these are the most effective agents currently available |
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Where is the major effect of HMG-COA drugs?
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- in the liver
- marked first pass hepatic extraction |
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Major effect of HMG-CoA?
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- reduce cholesterol synthesis in the liver by competitively inhibiting HMG-CoA reductase
- this is the rate limiting enzyme in cholesterol synthesis |
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HMG-CoA
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- induce an increase synthesis of LDL reseptors
- this results in an increase in liver's extraction of LDL and reducing LDL in the plasma |
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HMG-CoA
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 |
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drug of Nicotinic acid?
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- Niacin
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Mechanism of Niacin?
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- 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 |
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When is Niacin useful?
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- mixed hyperlipidemia because of it's favorable influence on serum levels of VLDL, LDL, and HDL
- can be combined with other drugs |
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Niacin
Adverse effects |
- marked vasodilation and flushing of the skin ... may see pruritis
- treat above with aspirin - elevation of serum transaminase - gastric distress - glucose intolerance |
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Niacin should be avoided by..
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- pts with liver disease, peptic ulcer, or hyperuricemia and diabetes
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What drugs are Fibric Acid derivatives?
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- Gemfibrozil
- Lopid |
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Fibric acid derivative mechanisms
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- decrease VLDL and tri's by increasing the activity of lipoprotein lipase and hydrolysis of VLDL
- promote delivery of tri's to adipose tissue |
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When are fibric acid derivatives used?
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- primarily in hypertriglyceridemia
- also in mixed and HDL deficiency |
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Fibric acid adverse effects
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- allergic reactions
- blood deficiencies - myalgia - POTENTIATES THE EFFECTS OF WARFARIN - increase myopathy when given with HMG-COA |
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what drugs are the bile acid binding agents?
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- Colestipol
- Colestid |
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Bile acid binding mechanism
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- 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! - COLESTIPOL DOES THIS |
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Bile acid binders have no effect on
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- HDL or triglycerides
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Bile acid binders used with pts that
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- cannot tolerate other drugs
- or these are used in comb with other drug |
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bile acid binder effects
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- NO SYSTEMIC EFFECTS
- GI effects: nausea, bloating, constipation - interfere with absorption of fat-soluble vitamins such as DIG, hydrochlorothiazide adn warfarin |
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what are the inhibitor of intestinal cholesterol absortion drugs?
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- ezetimibe
- zetia |
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Mechanism of inhibitors of intestinal cholesterol absorption drugs?
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- inhibits intestinal absoption of cholesterol adn phytosterols
- effective even in absense of dietary cholesterol because inhibits absorption of cholesterol excreted in bile |