Using Medication for Cholesterol

Sometimes for an individual, lifestyle changes such as eating healthy and exercising isn't enough. If this is the case, your doctor may start you on some form of drug therapy to help fight your high cholesterol and prevention of heart disease.
Statins (also known as HMG CoA reductase inhibitors)
This class of drugs works in the liver to prevent the formation of cholesterol. Statins are most effective at lowering the LDL (bad) cholesterol, but also have modest effects on lowering triglycerides (blood fats) and raising HDL (good) cholesterol.

Most of statins' side effects are mild and generally go away as your body adjusts. Muscle problems and liver abnormalities are rare, but your doctor may order regular liver function tests. Patients who are pregnant or who have active or chronic liver disease should not take statins.

Selective cholesterol absorption inhibitors
This relatively new class of cholesterol-lowering medications works by preventing the absorption of cholesterol from the intestine. Selective cholesterol absorption inhibitors are most effective at lowering the LDL (bad) cholesterol, but may also have modest effects on lowering triglycerides (blood fats) and raising HDL (good) cholesterol.

The first medication of this class, ezetimibe (Zetia®)**, was approved in 2002 for the treatment of high cholesterol and certain inherited lipid abnormalities.

Resins (also known as bile acid sequestrant or bile acid-binding drugs)
This class of LDL-lowering drugs works in the intestines by promoting increased disposal of cholesterol. Your body uses cholesterol to make bile, an acid used in the digestive process. These medicines bind to bile, so it can't be used during digestion. Your liver responds by making more bile. The more bile your liver makes, the more cholesterol it uses. That means less cholesterol is left to circulate through your bloodstream.

Fibrates (fibric acid derivatives)
Fibrates are best at lowering triglycerides and in some cases increasing HDL (good cholesterol) levels. These drugs are not very effective in lowering LDL (bad) cholesterol. That's why fibrates are generally used in people whose triglycerides are high or whose HDL is low, after reaching LDL goal. Fibrates are most effective at lowering triglycerides (blood fats). Additionally, they act to raise the levels of HDL (good) cholesterol. Fibrates may be used in combination therapy with the statins.

Niacin (nicotinic acid)
This drug works in the liver by affecting the production of blood fats. Niacin is prescribed to lower triglycerides and LDL cholesterol and raise HDL ("good") cholesterol.

Niacin side effects may include flushing, itching and stomach upset. Your liver functions may be closely monitored, as niacin can cause toxicity. Nonprescription immediate release forms of niacin usually have the most side effects, especially at higher doses. Niacin is used cautiously in diabetic patients as it can raise blood sugar levels.

Niacin comes in prescription form and as “dietary supplements.” Dietary supplement niacin must not be used as a substitute for prescription niacin. It should not be used for lowering cholesterol because of potential serious side effects. Dietary supplement niacin is not regulated by the U.S. Food and Drug Administration (FDA) the same way that prescription niacin is. It may contain widely variable amounts of niacin — from none to much more than the label states. The amount of niacin may even vary from lot to lot of the same brand. Consult your doctor before starting any niacin therapy.

For more information on drug therapy Read the latest FDA Drug Safety Newsletter

Taking medicine may be new to you, and there may be a lot to remember. For example, why are you taking it? What time should you take it? How often do you take it and how many pills do you take? It's important to take medicine the right way — just as prescribed. For quick tips on how you should manage your medicines click here.