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November 22, 2009
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Cholesterol (cont.)

What are fibric acid derivatives (fibrates)?

Fibric acid derivatives (fibrates) are effective medications in lowering blood triglyceride levels. Fibrates lower blood triglyceride levels by inhibiting the liver production of VLDL (the triglyceride-rich lip-protein fraction), and by speeding up the removal of triglycerides from the blood. Fibrates are also modestly effective in increasing blood HDL cholesterol levels. However, fibrates are not effective in lowering LDL cholesterol. Examples of fibrates available in the United Sates include Gemfibrozil (Lopid) and fenofibrate (Tricor).

Very high triglyceride levels (usually > 1000 mg/dl) can cause pancreatitis (inflammation of the pancreas that can result in a serious an illness with severe abdominal pain). By lowering the blood triglycerides, fibrates are used to prevent pancreatitis.

Fibrates are not effective in lowering LDL cholesterol and cannot be used alone in lowering LDL cholesterol levels. However, when a high risk patient (see NCEP recommendations above) also has high blood triglyceride or low HDL cholesterol levels, doctors may consider combining a fibrate, such as fenofibrate (Tricor), with a statin. Such a combination will not only lower the LDL cholesterol, but will also lower blood triglycerides and increase HDL cholesterol levels.

Fibrates have also been used alone to prevent heart attacks especially in patients with elevated blood triglycerides and low HDL cholesterol levels. In one large study, gemfibrozil decreased the risk of heart attacks but did not affect the overall survival of persons with high cholesterol levels. For more, please read our article on Fibrates.

What are bile acid sequestrants?

Bile acid sequestrants such as Cholestyramine (Questran), colestipol (Colestid), and colesevelam (Welchol) are medications for lowering LDL cholesterol. Bile acid sequestrants bind bile acids in the intestine and cause more of the bile acids to be excreted in the stool. This reduces the amount of bile acids returning to the liver and forces the liver to produce more bile acids to replace the bile acids lost in the stool. In order to produce more bile acids, the liver converts more cholesterol into bile acids, which lowers the level of cholesterol in the blood.

Bile acid sequestrants have modest LDL cholesterol-lowering effects. Low doses (for example 8 gram/day of Cholestyramine) can lower LDL cholesterol by 10%-15 %. But even high doses (24 gram/day of cholestyramine) can only lower LDL cholesterol by approximately 25%. Therefore, bile acid sequestrants used alone are not as effective as statins in lowering LDL cholesterol.

However, bile acid sequestrants are most useful in combining with a statin or niacin to aggressively lower LDL cholesterol levels. The statin-bile acid sequestrant combination can lower LDL cholesterol levels by approximately 50%, lower than a statin alone. A statin-niacin combination can substantially reduce LDL cholesterol and elevate HDL cholesterol. For more, please read our article on Bile Acid Sequestrants.



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