What Are Statins?

Posted: June 1, 2004

To reach a low-density lipoprotein cholesterol (LDL or “bad” cholesterol) goal of less than 100 mg/dL, you may need to take cholesterol-lowering medicine, such as statins, in addition to making life habit changes.

Heart disease patients and those at high risk for developing heart disease need to lower their LDL more than other people. As a result, medications are more often used by patients with heart disease and those at high risk than by those who do not have heart disease or who have a lower risk of developing it.

If your doctor prescribes medicine, you also will need to:

• Follow your cholesterol-lowering diet.
• Be more physically active.
• Lose weight if overweight.
• Control all of your other heart disease risk factors, including smoking, high blood pressure, and diabetes.

Taking all these steps together may lessen the amount of medicine you need or make the medicine work better – and that reduces your risk for a heart attack.

How statin drugs work
There are currently five statin drugs on the market in the United States: lovastatin, simvastatin, pravastatin, fluvastatin, and atorvastatin (cerivastatin was withdrawn from the market by the manufacturer in August 2001).

The major effect of the statins is to lower LDL-cholesterol levels, and they lower LDL-cholesterol more than other types of drugs. Statins inhibit an enzyme, HMG- CoA reductase, that controls the rate of cholesterol production in the body.

These drugs lower cholesterol by slowing down the production of cholesterol and by increasing the liver's ability to remove the LDL-cholesterol already in the blood.

Statins were used to lower cholesterol levels in several studies. The large reductions in total and LDL-cholesterol produced by these drugs resulted in large reductions in heart attacks and heart disease deaths. Thanks to their track record in these studies and their ability to lower LDL-cholesterol, statins have become the drugs most often prescribed when a person with heart disease needs a cholesterol-lowering medicine.

Studies using statins have reported 20 to 60 percent lower LDL-cholesterol levels in patients on these drugs. Statins also reduce elevated triglyceride levels and produce a modest increase in HDL-cholesterol.

Taking statins
The statins are usually given in a single dose at the evening meal or at bedtime. It is important that these medications be given in the evening to take advantage of the fact that the body makes more cholesterol at night than during the day.

You should begin to see results from the statins after several weeks, with a maximum effect in 4 to 6 weeks. After about 6 to 8 weeks, your doctor can do the first check of your LDL-cholesterol while on the medication. A second measurement of your LDL-cholesterol level will have to be averaged with the first for your doctor to decide whether your dose of medicine should be changed to help you meet your goal.

The statins are well tolerated by most patients, and serious side effects are rare. A few patients will experience an upset stomach, gas, constipation, and abdominal pain or cramps. These symptoms usually are mild to moderate in severity and generally go away as your body adjusts.

Rarely a patient will develop abnormalities in blood tests of the liver. Also rare is the side effect of muscle problems. The symptoms are muscle soreness, pain, and weakness. If this happens, or you have brown urine, contact your doctor right away to get blood tests for possible muscle problems.

Source: National Heart, Lung and Blood Institute

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