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31 Cards in this Set
- Front
- Back
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What are the 4 classes of lipid lowering drugs?
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1. HMG CoA Reductase Inhibitors (statins)
2. Bile acid sequestrants 3. Nicotinic acid 4. Fibric Acids |
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What are the 4 major steps of lipoprotein metabolism?
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1. Cholesterol transport and chylomicron formation
2. Transport from intestine to liver 3. Transport from liver to periphery 4. Transport from periphery to liver (formation of HDL) |
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What do chylomicrons do?
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Transport exogenous dietary lipids
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What does lecithin-cholesterol acyltransferase (LCAT) do?
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converts cholesterol to cholesteryl ester (more hydrophobic), allowing a mature HDL lipoprotein to form
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What are major risk factors that modify LDL goals?
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cigarette smoking, HTN, Low HDL, FHx of premature CHD, Age, DM
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What is the first line therapy for high cholesterol?
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therapeutic lifestyle change
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What is Lovaza?
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first clinically approved concentration of EPA, DHA, and fish oils
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What is the first line drug therapy for reduction of LDL-C?
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HMG CoA reductase inhibitors (statins)
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What is the mechanism of the statins?
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inhibit RLS in cholesterol biosynthesis (HMG CoA reductase). This causes upregulation of HMG CoA reductase and LDL receptors. you get near normal levels of cholesterol synthesis, but increased LDLr --> clear more LDL and VLDL from blood (20-50%).
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Are statins indicated for increasing HDL or lowering Triglycerides?
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No
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What are the most common side effect of statins?
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hepatotoxicity (1% of pts), rhabdomyolysis
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What is the only statin that is water soluble and not metabolized by a CYP mechanism?
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Pravastatin
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When are stains contraindicated?
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during pregnancy (linked to birth defects)
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What is the 2nd line drug therapy for lowering LDL?
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Bile acid sequestrants
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What is the mechanism of the bile acid sequestrants?
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They bind neg charged bile acids in the intestine which then cannot be absorbed and excreted in stool. Liver then converts more cholesterol to bile acids --> lower serum Chol levels. They also cause an upregulation of LDLr on the liver --> more taken out of circulation
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What is a downside to bile acid sequestrants? Why are they 2nd line to the statins?
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There is a compensatory upregulation of HMG CoA reductase which enhances cholesterol synthesis --> negates the drug
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When are bile acid sequestratns indicated?
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1. If statins are ineffective (i.e., in pts w/ acetyl CoA reductase mutations)
2. Used w/ statins for familial hyperlipidemia 3. Used in pregnant women instead of statin |
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What are some common bile acid sequestrants?
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Cholestyramine, Colestipol, Colesevelam
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What are the main side effects of the bile acid sequestrants?
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similar to cholecystectomy --> constipation, abd pain, wt loss, diarrhea, etc.
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What is nicotinic acid (niacin) used for?
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2nd/3rd line therapy for lowering LDL
1st line therapy for increasing HDL and decreasing triglycerides |
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What are the mechanisms of niacin?
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prevents FFA dispersal from adipose to liver --> reduces triglycerides --> reduces VLDL amounts --> can't make LDL
Also prevents uptake of ApoAI --> more formation of HDL |
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What is the most effective drug on the market to raise HDL?
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niacin
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What is the main side effect of niacin?
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hot flushes
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What is Niaspan?
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time released formulation of niacin
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What is the first line therapy for lowering TGs?
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Fibric acid derivatives
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What is the mechanism of fibrates?
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activate PPARa --> activates LL --> increase synthesis of ApoAI --> increase HDL
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What drugs interfere w/ the fibrates?
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Statins. Joint use can cause rhabdomyolysis
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What are some side effects of fibrates?
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GI disorders, skin rxns
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What is the mechanism of Ezetimibe?
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blocks Nieman-Pick C1-like 1 protein --> blocks dietary cholesterol absorption in intestine
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What are the CETP inhibitors used for?
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Raising HDL (primarily). Also lower LDL
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What do PCSK9 Inhibitors do?
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Decreases expression of LDLr
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