Sometimes lifestyle changes alone will not bring your cholesterol to healthy levels and medication is required. A decade or so ago, the medications available for reducing cholesterol had only limited effectiveness and often produced unpleasant side effects.

Statins

More recently, however, scientists have developed and successfully tested a class of drugs called statins, which both slow the production of cholesterol and increase the liver’s ability to remove LDL cholesterol already in your bloodstream. They also reduce your triglyceride levels and can often moderately increase your HDL cholesterol levels.

They are extremely effective, are very safe, and people taking them rarely experience side effects at recommended dosages. A number of large clinical trials have shown that when people with heart disease take statins, their cholesterol levels not only go down, but their risk for other heart problems or stroke drops sharply as well.

For example, statins can lower your risk of heart attack by up to 40 percent, lower your chance of needing heart surgery by up to 40 percent, lower your risk of stroke by at least 20 percent (and up to 55 percent), and lower your risk of death by up to 30 percent.

And that’s not all. Another recent clinical study involving more than 20,000 people showed that statins can cut the risk of heart attack and stroke by a third in people with a high risk for heart problems even if they had low or normal cholesterol levels to begin with.

All of this research suggests that statins may have a protective effect on the heart in addition to lowering cholesterol. What’s more, there is evidence that statins may benefit your brain as well as your heart: statins decrease your risk of stroke, of course, but research now suggests that they may also help prevent Alzheimer’s disease.

Consequently, even though the expert guidelines currently recommend drug therapy only after lifestyle modification has failed, statins have proven so effective that many doctors have begun to encourage their use right from the start, in addition to lifestyle management. There are several statin drugs on the market today.

Although simvastatin and pravastatin have been tested the most and other statins have been studied less thoroughly, all appear to have the same benefits for a given reduction in LDL. As with any prescription, you should talk to your doctor about other drugs you are taking before beginning statin treatment.

Some people experience negative reactions when they combine statins with other medications, though most of these reactions are rare. If you have concerns, you should talk with your doctor.

Statins Side Effects

Most people taking statins experience no side effects at all. Of those who do, the most common are mild stomach upset, gas, nausea, diarrhea, constipation, or muscle weakness. More serious reactions, which can include liver damage or muscle breakdown, are possible but rare.

However, the American Heart Association advises that patients have a creatine kinase (or CK) blood test (a test of muscle damage) before starting statins and any time signs of muscle damage appear, suggested by dark urine or severe muscle pain, tenderness, or weakness (though it is possible to have statin-related muscle problems even with a normal CK level).

Two other tests that measure blood levels of two specific liver markers, called AST (short for: aspartate aminotransferase) and ALT (short for: alanine aminotransferase), should be done three months after beginning statin drugs and then at least once a year afterward, or any time a patient shows signs of possible liver disease (excessive fatigue, nausea, and vomiting).

Although these tests for kidney and liver function are recommended for everybody taking a statin, you should know that the overall risk of developing signs of kidney or liver problems while taking a statin is less than 1 percent (that’s less than one in one hundred).

Drinking grapefruit juice can increase the effect of some statins, including simvastatin, atorvastatin, and lovastatin (but not pravastatin). Grapefruit seems to inhibit the enzymes that break down some of the statins. This makes it difficult to be sure how much medication you are getting with each dose.

Nevertheless, for people taking their statin at night, a small glass of grapefruit juice in the morning is unlikely to cause a problem. An issue that is currently under investigation is the impact of statins on behavior and memory. Some researchers are looking into this issue. At this time there is not yet enough evidence to support this concern.

Other Cholesterol Drugs

Statins are the first choice for treating high cholesterol because of the overwhelming evidence supporting their effectiveness. If you cannot take statins, other medications can help you bring your cholesterol under control. In fact, because of their special properties, some of these alternatives are occasionally prescribed with statins.

Bile Acid Resins are not quite as powerful as statins at lowering LDL cholesterol or raising HDL cholesterol, but they can decrease cholesterol levels. Bile acid resins (e.g., cholestyramine [brand names: Cholybar, LoCholest, LoCholest Light, Prevalite, Questran, Questran Light], colestipol [brand name: Colestid], and colesevelam [brand name: Welchol]) are very safe and can be added to statins to help lower LDL cholesterol.

These medications never became very popular—probably because they can cause constipation, bloating, nausea, or gas and need to be taken with a lot of fluid.

Nicotin Acid, commonly known as niacin or vitamin B3, is not as effective at lowering LDL cholesterol as statins, but is better at raising HDL cholesterol and may be better at lowering triglycerides. It is inexpensive and does not require a prescription, but a common side effect is facial flushing or hot flashes that some people find intolerable.

The prescription long-acting forms tend to be better tolerated. As an interesting note, niacin deficiency used to cause a disease called pellagra, which was characterized by problems with the skin, digestive system, and nervous system. With dietary improvements, this disease is no longer a problem in the United States.

Fibrates (e.g., gemfibrozil [brand name: Lopid], fenofibrate [brand name: Tricor], and clofibrate [brand name: Atromid]) are not as effective at lowering LDL cholesterol as statins, but because they are slightly better than statins at raising HDL cholesterol and much better for lowering triglycerides, the two are sometimes combined.

Side effects of fibrates, though uncommon, include nausea, diarrhea, stomach upset, heartburn, and gas. Also, in rare instances, fibrates may cause kidney or muscle problems in people taking statins and may increase the risk of bleeding in people taking blood thinners unless the dose is adjusted.

The interesting thing about fibrates is that studies have found that their modest ability to increase HDL may translate into substantial benefits for patients. In a study of more than 2,500 veterans, gemfibrozil increased HDL levels by 6 percent, reduced total cholesterol by 4 percent, and reduced triglycerides by 31 percent. Over the five years of the study, gemfibrozil was associated with a 22 percent reduction in the risk of heart attacks and death.

Selective Cholective Cholesterol Inhibitor (e.g., ezetimibe [brand name: Zetia]) is a medicine that works in the intestine. It is generally well tolerated and can be helpful for patients who cannot take statins. Also, many doctors are using it in combination with statin drugs.

A recent study suggests that the coadministration of ezetimibe and statin therapy is more effective in reducing LDL cholesterol than statin therapy alone. There is much less information about the long-term effects of this medication. Whether this strategy is better than increasing the dose of the statin is not known. Ezetimibe should not be taken by patients also taking bile acid resins because the bile acid resins may bind to it and make it ineffective.

Cholesterol FAQ

What if my total cholesterol is at target but my LDL is still above target?

It’s a common misunderstanding among patients that total cholesterol is more important than LDL and HDL cholesterol. In fact, it’s just the opposite. Your LDL needs to be below 100 (or 70) for your cholesterol levels to be at target. If your total cholesterol is low despite the fact that your LDL cholesterol is high, it may mean that your HDL cholesterol is too low.

My LDL cholesterol is going down but my HDL cholesterol will not go up. What can I do?

If you have heart disease, it is particularly important that your HDL cholesterol be as high as possible—at least 40 mg/dL. A lower HDL cholesterol level can be a result of your being overweight, physically inactive, or a smoker. Addressing these issues is the first step to raising your HDL.

Beyond this, you and your doctor may decide to use medication (such as fibrates or niacin) to help raise your HDL. In the end, your HDL target may still be hard to reach. Researchers are currently working on products that may specifically target the HDL cholesterol level.

Can eating more fiber, nuts, soy, or gralic lower my cholesterol?

There is not enough evidence to support using any of these foods as first-line approaches to lowering cholesterol. For more information about the effect of certain types of foods on cholesterol, turn to the Managing Your Diet section on pages 109–124.

Does it matter when I take statins?

Doctors generally recommend that patients take statins in a single dose at dinner or at bedtime. By taking the medication at this time you take advantage of the fact that the body manufactures more cholesterol at night than during the day.

How long does it take to see the effects of statins?

Patients usually see the results of statins fairly soon after starting the medication—and the maximum effect is usually seen by four to six weeks. Doctors usually recheck cholesterol levels about six to eight weeks after initiating therapy.