Statins are a type of cholesterol-reducing drug that lower the levels of fats (lipids) in the blood, including cholesterol and triglycerides. Statins work by blocking the production of a specific enzyme used by the body to make cholesterol. They are effective in lowering blood fat levels in patients with high cholesterol (hypercholesterolemia) and are therefore helpful in the prevention of coronary, cerebrovascular and peripheral vascular disease.
Other types of cholesterol reducing drugs include fibrates, bile acid resins, nicotinic acid and ezetimibe. All are commonly used to treat high cholesterol, but statins are considered the first line of treatment for patients with this condition.
While all cholesterol-lowering drugs are effective to some degree in lowering blood fat levels, statins are particularly effective at lowering levels of LDL “bad” cholesterol and – to a lesser degree – triglycerides. Statins have been shown to decrease LDL levels between 30 and 60 percent, depending on the kind of statin and the dosage. While statins do increase levels of HDL “good” cholesterol, they do not seem to increase those levels as well as nicotinic acid.
Recent studies suggest that statins have a mild anti-inflammatory action and may reduce blood levels of C-reactive protein, an indicator of inflammation in the body. C-reactive protein is proving to be a useful “marker” for predicting heart disease and stroke, which are associated with inflammation of the blood vessel walls.
There are currently six statins approved for sale in the United States. They are:
Generic name Brand name
Although the statins are used interchangeably to reduce LDL cholesterol, studies have shown differences in the degree of effectiveness and the possible side effects associated with various statins. In particular, rosuvastatin has shown the greatest ability to reduce LDL cholesterol, while low-dose fluvastatin is the least potent statin. Because side effects tend to occur at higher dosages, the goal of therapy to find the lowest dose of the least potent statin that yields acceptable results.
To reduce the risk of stroke and heart attack, statins may be prescribed for individuals who have multiple risk factors for heart-related problems, including:
- Family history of heart disease
- High blood pressure
- Low HDL ("good") cholesterol
Conditions of concern
Patients should discuss with their physician the benefits and risks of taking statins if they have any of the following:
- Alcohol abuse, or history of alcohol abuse
- Liver disease (history of disease or persistently high liver enzymes)
- Electrolyte imbalance or metabolic enzyme deficiencies
- Thyroid problems
- Severe infection
- Low blood pressure (hypotension)
- Organ transplant (e.g. heart transplant)
- Recent major surgery (e.g. open-heart surgery) or trauma
- Side effects
Potential side effects of statins
There are a number of side effects that could occur as a result of taking statins. Some side effects are more serious than others and require patients to immediately contact their physician. These side effects include muscle pain or tenderness and dark urine. Statins also may result in the development of abnormal liver function, which is diagnosed by a liver enzyme test. A very rare, but potentially fatal, side effect of statins is rhabdomyolysis, a severe muscle reaction.
Physicians monitor for this condition by measuring the blood level of the muscle enzyme called creatine phosphokinase (CPK). Risk of this severe complication appears to be higher in elderly patients, those taking high doses of statins and those taking statins in conjunction with other cholesterol-reducing drug called fibrates. In August 2001, one type of statin, called cerivastatin (brand name “Baycol”), was voluntarily withdrawn from the market by its manufacturer due to reports that fatal cases of rhabdomyolysis had been significantly more common with cerivastatin than with other approved statin drugs.
Other less serious side effects that may be seen in some patients taking stations include the following:
- Allergic reaction (new onset of wheezing, respiratory congestion, itching or skin rashes)
- Decreased sexual interest or ability
- Difficulty sleeping
- Dizziness or lightheadedness
- Excessive gas or belching
- Heartburn or indigestion
- Nausea or vomiting or abdominal pain
- Skin rash
Drug or other interactions
Patients should consult their physician before taking any other medication (either prescription or over-the-counter) or nutritional supplements. Of particular concern to patients taking statins are:
- Other cholesterol-reducing drugs.
- Inotropes (e.g., digoxin). Medications that strengthen the heart’s contractions so that it can pump more blood per minute. Use with atorvastatin, fluvastatin or simvastatin may increase blood levels of inotropes, increasing the potential for side effects.
- Birth control pills. Use with atorvastatin may increase the blood levels of the hormones used in birth control pills, increasing the risk of side effects.
- Calcium channel blockers. Medications that block the movement of calcium ions into heart cells and blood vessels. This increases the supply of oxygen-rich blood to the heart, lowers blood pressure and reduces the heart's workload. Use with simvastatin may increase the risk of muscle problems.
- Protease inhibitors. Medications used in the treatment of human immunodeficiency virus (HIV). Use with simvastatin may increase the risk of developing kidney failure or muscle problems.
- Azole antifungals (systemic antifungals). Medications used to treat serious fungal infections in the body. They may be taken orally in pill form or may be injected. Using some statins and azole antifungals in combination may increase an individual’s risk of developing muscle problems (rhabdomyolysis) that can lead to kidney failure.
- Erythromycins. A type of antibiotic used in the treatment of infections. Using some statins in combination with erythromycins may increase an individual’s risk of developing rhabdomyolysis.
- Grapefruit juice.
Ongoing research regarding statins
Statins are the first line of medical treatment for cholesterol reduction. Research into their use has produced numerous results, related to coronary artery disease, heart attacks, strokes and other conditions.
Overall, research continues to show that statins lower the risk of heart attack, stroke and heart-related death in patients with heart disease and some other conditions such as peripheral vascular disease. Research has also suggested that statins may slow the progression of heart valve disease.
Some of benefits appear when statins are used with nicotinic acid. The benefits may also occur when high doses of statins are administered after a heart attack or episode of unstable angina. Statins also significantly reduce the rates of death and coronary events in elderly patients. Recent studies have indicated that patients with heart failure who used statins for the first time had a reduced risk of death of nearly 25 percent when compared to individuals who did not use statins. Research is continuing as to the benefit of statin use in individuals with heart failure.
Statins also may reduce the risk of death and coronary events for people with diabetes, even when these patients have normal cholesterol levels. As a result, the American Diabetes Association recommends statins for individuals with diabetes bwho are over the age of 40 with a total cholesterol greater than 135. In addition, pravastatin has been shown to reduce the risk of developing type 2 diabetes.
Although diet is effective in lowering blood cholesterol levels, research has shown that fewer cardiac events occur in patients treated with statins compared to those treated with diet alone. This demonstrates statins can benefit both lipid levels and other factors in the cardiovascular system.
New research has also suggested that taking atorvastatin prior to heart surgery may reduce the risk of atrial fibrillation (AF) in patients. AF is an irregular heartbeat that is usually triggered by certain heart surgeries. These procedures included heart bypass surgery and surgical repair of a faulty heart valve. The statin was given for a week before surgery and reduced AF by 61 percent in the statin patients. Additional research is necessary to test other statins and obtain conclusive results of the benefits.
Statins have been shown to benefit areas not specifically related to lipid levels. These include the following:
- Statins may reduce blood levels of C-reactive protein (CRP). CRP is a substance produced by the liver in response to any inflammation (an inflammatory marker). CRP is the only inflammatory marker that has been found to be an indicator of heart health. Very high levels of CRP are found in the blood of patients who are having a heart attack or unstable angina symptoms. Mildly elevated CRP levels have been found in people with diabetes, glucose intolerance and high blood pressure (hypertension), all of which are independent risk factors for heart disease.
- Statins are thought to have mild anticoagulant properties, with an ability to help prevent blood clots.
- Statins have been found to improve symptoms of claudication associated with peripheral vascular disease.
- In addition to lowering LDL levels, statins have been shown to slow the process of calcification, the hard buildup of calcium deposits on the walls of an artery. Calcification is one of the factors involved in hardening and narrowing of arteries (atherosclerosis) and, if severe enough, may be associated with blockages.
Some drug manufacturers have proposed that certain statins be approved for over-the-counter use. However, the United States Food and Drug Administration (FDA) has yet to approve of their proposals. All statins in the U.S. are available only through prescription.
Some cholesterol reducers can cause liver inflammation, which tends to resolve on its own after patients stop taking the medication. To monitor this and other complications, patients should undergo regular blood tests and liver function tests.
Some statins (e.g., lovastatin) work better when taken with food. Patients should carefully follow the directions for taking their medication provided by their physician and pharmacy. Those who miss a dose of this medication should take it as soon as possible, unless it is nearly time for the next dose. In that case, the missed dose should be skipped. Double doses of this medication should NOT be taken.
Patients should not abruptly stop or the change the dosage and timing of their medications without first consulting their physicians. Studies have shown that many patients on statins do not take their medication as prescribed or stop taking the medications on their own. Individuals who do not take statins as prescribed by their physicians are at higher risk for preventable heart attacks. It is also important that patients notify all physicians (including dentists) that they are taking statins before undergoing any surgical procedure.
The American Heart Association (AHA) recommends the following for patients who have been prescribed statins:
- Patients taking statins should continue to take their medications as prescribed and contact their physician if they have concerns about the type of drug, dosage or side effects.
- Be aware of the side effects and risks that are associated with the prescribed statin, especially those that indicate the need for immediate attention. (e.g. muscle pain, dark urine).
- Do not discontinue the drug without consulting a physician. If the drug is discontinued by a physician, the patient should be aware of risks and side effects that can occur.
- How to use
Pregnancy use issues
Pregnant women or women planning to become pregnant in the near future are advised not to take statins. These medications block the formation of cholesterol, which is needed for the fetus to properly develop. If a woman becomes pregnant or thinks she might be pregnant while taking a statin, she should immediately contact her physician. Statin use during pregnancy could lead to birth defects. Statins are also not recommended for women who are breastfeeding as the drug may pass into the breast milk and harm the baby.
Child use issues
It has been reported that approximately 50 million children in the United States have high cholesterol levels. However, the United States Preventative Services Task Force does not encourage the routine screening of all young children because coronary heart disease tends to begin later in life. The majority of clinical trials on the use and effectiveness of statins have been conducted on adults. A limited number of studies conducted have shown that these medications may be safe and effective for use in children under 18. However the long-term effects of such use have not been determined. In addition, appropriate doses have not been determined for use by children and the effectiveness of statins has not been compared to other lipid tools and medications in children. Recent findings have suggested that a prescribed regimen of vitamins C and E can help reduce the risk of atherosclerosis in children with abnormally high cholesterol levels.
Elderly use issues
Statin use has been tested to determine safety and effectiveness in a limited number of older adults (age 65 and older). Researchers found no reason to believe that the use of statins in older adults causes any different side effects, risks or concerns than it does in younger adults. In fact, study results find that statins significantly reduce the rates of death and coronary events in elderly patients. This is an important piece of information since other research has revealed that statins are underused in the elderly population. There is some evidence to suggest that the risk of developing a severe complication called rhabdomyolysis is higher in elderly patients taking statins. However, this potentially fatal side effect is still extremely rare. Patients are encouraged to discuss their concerns with their physicians.
Questions for your doctorPatients may wish to ask their doctors the following questions related to statins:
- Why are you recommending a statin for me?
- What are the benefits of a statin over another cholesterol-reducing drug?
- Which statin are you prescribing for me?
- What is my targeted cholersterol level?
- How quickly can I expect to see results with the statin?
- Will the statin interact with other medications I am taking?
- What side effects might I experience with this drug?
- Which side effects indicate the need to contact you immediately?
- Will you change the statin if I have problems with the drug?
- How long will I need to take this medication?
- What other lifestyle changes should I make to reduce my risk of heart problems?
- What will be used for treatment if I can't take a statin?