Statins: Cholesterol-Lowering Drugs

What are statins?

If you have high cholesterol that you can’t lower through diet and exercise, doctors will likely recommend statins as a treatment option. Some of these medications which include atorvastatin (Lipitor), rosuvastatin (Crestor), lovastatin (Mevacor, Altoprev), pravastatin (Pravachol), simvastatin (Zocor), and fluvastatin (Lescol) can lower your LDL (“bad”) cholesterol by as much as 60 percent, depending on the dosage and your particular cholesterol problem.

Who should take statins?

Ideally, everyone should have an LDL level of less than 100 milligrams per deciliter and an HDL (or “good” cholesterol) level of 40 or above (women should aim for an HDL of 50 or above). However, many people fall short. If you have at least two other risk factors for heart disease — if you smoke, have high blood pressure, have a family history of heart disease, or you’re a man over 45 or a woman over 55 — you should make sure your levels of LDL and HDL are optimal. In fact, if you have multiple risk factors, diabetes, or have already been diagnosed with coronary heart disease, your LDL cholesterol level should definitely be under 100 mg/dL.

Some people can reach these goals simply by sticking to a low-fat diet and getting regular exercise, but others will require medications to bring their cholesterol down.

According to the latest guidelines from the National Cholesterol Education Program, the first line of defense against high cholesterol is still a change in lifestyle — getting regular exercise, eating a low-fat, high-fiber diet, and if necessary, losing weight. But for people who are at high risk for heart attacks, or for those whose LDL levels don’t budge after a program of prescribed lifestyle changes, the NCEP recommends more aggressive action.

In 2004, the NCEP updated its guidelines and now suggests drug therapy be considered for high-risk individuals with LDL levels of 100 mg/dL or higher. People with at least two other risk factors who are deemed to be at “moderately high-risk” for a heart attack may be advised to take a statin or similar drug if their LDL is between 100 to 129 mg/dL, despite a healthy diet. The organization also recommends cholesterol-lowering drugs for people with coronary heart disease and for those whose HDL cholesterol level is at 40 or below. Drug therapy to reduce LDL cholesterol to below 70 mg/dL should be considered for those at “very high” risk for heart attacks, such as people who already have heart disease plus multiple risk factors such as diabetes, smoking, or high blood pressure.

New heart and stroke guidelines adopted in 2013 also suggest statin treatment for anyone 21 and older whose “bad” LDL cholesterol is 190 mg/dL or more.

Even though statins have been used widely to lower cholesterol levels, however, they don’t appear to reduce the chances of death in people who are merely at risk for heart disease but who don’t have it, a recent large-scale British analysis of previous studies found.

How safe are statins?

Compared with other cholesterol-lowering drugs, statins have a good safety record and are easy to take. In several studies, patients taking sugar pills (placebos) reported as many side effects as patients taking statins.

Still, no drug is risk-free, and there are some things to watch out for. All statins have been associated with a potential risk of rhabdomyolysis, or severe muscle damage. One drug, cerivastatin (Baycol), was pulled off the market in 2001 because of reports of rhabdomyolysis linked to 31 deaths in the United States.

The risk of rhabdomyolysis may be greater with some statins when they are combined with other drugs, including macrolide antibiotics like erythromycin and clarithromycin, the transplant drug cyclosporine, and cholesterol drugs like gemfibrozil (for example, Lopid) and niacin (for example, Niaspan). Be sure to tell your doctor or pharmacist if you’re taking these or any other medications, and ask for a list of drugs that may interact adversely with your medications. Some statins can also interact in dangerous ways with the anticoagulant warfarin (Coumadin).

In addition, ethnic or genetic differences may play a role in adverse reactions to statins. In 2005, the FDA asked the makers of Crestor to change its label, which now suggests that Asian patients should be started on a lower dose (5 mg once a day. You should always get medical help immediately if you experience unusual pain, weakness, or tenderness in your muscles, particularly in your back or calves. Other early signs of rhabdomyolysis may include general weakness, fever, nausea, vomiting, and dark urine.

About one out of 100 patients develops high liver enzymes — a sign of liver inflammation — while taking a statin. Your doctor will check your enzymes before prescribing a statin and from time to time afterwards to make sure your liver isn’t inflamed. To further protect your liver, you should go easy on alcohol or avoid it completely while taking a statin. If your liver enzymes are very elevated, you may need to discontinue use of the statin, which usually will reverse the problem.

As with many other medications, you may want to avoid grapefruit juice while taking some statins, as it may cause side effects. Always check the label and ask your doctor to be sure.

Are some statins better than others?

All of the statins can provide powerful protection for your heart, but some may be better choices than others, depending on your particular situation. If your LDL is extremely high, your doctor may choose to prescribe one of the more potent single agent statins, such as Crestor or Lipitor. Your level of cholesterol, other medical conditions you may have, and medications you are taking will all dictate which statin or other cholesterol-lowering agent your doctor may prescribe.

What about other cholesterol lowering drugs?

Statins aren’t the only medications that can improve your cholesterol levels. If your HDL (“good”) cholesterol is too low, your doctor may prescribe niacin instead of — or in addition to — a statin. While statins can slightly increase your HDL, niacin will give it a much bigger boost. Likewise, you may need a fibrate drug such as Tricor if your triglycerides (another type of fat in the blood) are too high. Both niacin and fibrates tend to cause more side effects than statins. Ask your doctor which side effects you can expect. In addition, since combining certain statins with niacin or fibrates can increase your risk of rhabdomyolysis, contact your doctor immediately if you develop a change in gait or muscle weakness, tenderness, or pain.

There are some combination drugs that combine statins with a second medicine. Your doctor is the best judge of whether these are appropriate choices for your particular situation.

How long will I have to keep taking this medication?

You may have to keep taking a statin for the rest of your life. At the very least, you should take the drug until your doctor says it’s okay to quit.

Unfortunately, many patients set aside their prescription bottles without telling their doctor. It’s easy to “forget” to take a pill when it doesn’t make you feel any better. But remember: Heart disease can work silently, too. No matter how good you feel, sticking to your prescription just might save your life.

References

Ray K., Kausik et al. Statins and All-Cause Mortality in High-Risk Primary Prevention: A Meta-Analysis of 11 Randomized Controlled Trials Involving 65,229 Participants. Archives of Internal Medicine, June 28, 2010.

Crouch MA. Effective use of statins to prevent coronary heart disease. American Family Physician. January 15, 2000. 63(2):309-319.

National Institutes of Health. “Update on Cholesterol Guidelines: More-Intensive Treatment Options for Higher Risk Patients.” July 12, 2004. Safeer RS and CL Lacivita. Choosing drug therapy for patients with hyperlipidemia. American Family Physician. June 1, 2000. 61 (11):3371-3382.

Bayer Voluntarily Removes Baycol, FDA Talk Paper, U.S. Food and Drug Administration, T01-34 Aug. 8, 2001

New guidelines take a personal approach to preventing cardiovascular disease in women. American Heart Association. Feb. 4, 2004.

American Heart Association. What Your Cholesterol Levels Mean.
http://www.americanheart.org/presenter.jhtml?identifier=183

Mann D, Reynolds K, Smith D, Muntner P. Trends in statin Use and low-density lipoprotein levels among US adults: Impact of the 2001 National Cholesterol Education Program guidelines. The Annals of Pharmacotherapy. September 2008; 42(9): 1208-1215.

2013 Heart and Stroke Guidelines. Guidelines Resource Center. American Heart Association, 2016. http://news.heart.org/aha-guidelines-resource-center/

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