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Treatment Options for High Cholesterol

Medicines and More


Updated November 10, 2006

If you have been diagnosed with high cholesterol, there are many treatment options for you. At first, your health care practitioner may want to try lowering your cholesterol through modifying your life style. This would include exercising, eating healthier, smoking cessation, and weight loss. This may or may not work for you. If you are a diabetic or have some form of heart disease, your physician may want to take a more aggressive approach to lowering your cholesterol. If your cholesterol levels are still high after improving your lifestyle, cholesterol medication may be right for you.

There are many prescription drugs on the market that are very effective at lowering your cholesterol levels. Depending on what your lipid profile looks like, you may take either one drug or a combination of drugs.


Also referred to as HMG-CoA reductase inhibitors, these are probably the most commonly prescribed drugs on the market. They work by inhibiting a protein called HMG-CoA reductase, which is an important molecule in making cholesterol. This class of drugs include: pravastatin (Pravachol ®), atorvastatin (Lipitor®), lovastatin (Mevacor®), rosuvastatin (Crestor®), simvastatin (Zocor®), and fluvastatin (Lescol®).

These drugs are used to help every part of your lipid profile: they increase HDL (good cholesterol) up to 15 percent, decrease LDL (bad cholesterol) by 18 to 65 percent, and decrease triglycerides by 7 to 30 percent.

Bile Acid Resins

Also referred to as bile acid sequestrants, these drugs mainly come in a powdered form or pill form. These drugs work by binding bile acid in your intestines. The liver makes bile acids out of cholesterol. Bile acid resins bind bile acids in the gut and cause them to be excreted, therefore forcing the liver to “waste” more cholesterol by manufacturing replacement bile acids. The medications included in this class are cholestyramine (Questran®), colestipol (Colestid®), and colesevelam (WelChol®). Bile acid resins lower LDL between 15 to 30 percent, but only have a modest effect on HDL and do not affect triglyceride levels.


This class of prescription drugs is also referred to as fibric acid derivatives and includes gemfibrozil (Lopid®) and fenofibrate (Tricor®). They function by activating a receptor on cells called PPAR (peroxisome proliferator-activated receptors), which is responsible for regulating the cell’s use of carbohydrates and fats (like cholesterol). Therefore, by activating PPAR receptors, fibrates decrease cholesterol levels. Fibrates are particularly useful in lowering triglyceride levels (by up to 50 percent). Additionally, they can raise HDL levels between 10 to 20 percent. These drugs can also lower LDL levels (by between 5 to 20 percent), but they are not as effective in lowering LDL as they are at lowering triglycerides.

Absorption Inhibitors

Ezetimibe (Zetia®) is the only prescription drug currently in this class. This drug prevents cholesterol from being absorbed from the small intestine and entering the blood, thus lowering your cholesterol levels. Ezetimibe slightly lowers LDL and triglycerides and slightly raises HDL. Therefore, this drug may be taken with another drug (like a statin) to greatly lower cholesterol levels.


This drug is available over-the-counter and as a prescription. On the pharmacy shelf, you may see it listed as vitamin B3 or nicotinic acid. As a prescription, it is marketed under Niaspan®. Niacin works by decreasing the amount of cholesterol made by the liver. It greatly raises HDL levels (up to 35 percent), lowers LDL levels and significantly lowers triglyceride levels (up to 50 percent).

There are also other alternatives you may take to lowering your cholesterol:

Natural Alternatives

There are many spices, amino acids, plant products (like sterols), foods and nutraceuticals (like policosanol and red rice yeast extract) on the market. Some of these treatments may work in lowering cholesterol, and some of these treatments may not. If you decide to take a natural supplement, be sure to notify your health care provider in order to be sure that there are no interactions with any other medications you are taking.

Cholesterol Apheresis

Cholesterol apheresis is a relatively new procedure that is very similar to kidney dialysis. This is reserved for individuals who have tried all of the above treatments, including lifestyle modification, and still have dangerously high cholesterol levels. In this procedure, your blood is passed through a special filter in order to lower your cholesterol. It should be noted that this is a radical approach and is limited to patients who have familial hypercholesterolemia (a genetic syndrome that causes people to have very high cholesterol levels). Additionally, this procedure is usually performed biweekly and can cost up to $2,000 per session.

Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (PDF), July 2004, The National Institutes of Heath: The National Heart, Lung, and Blood Institute.
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