What are statins?
Statins are drugs that help improve your lipid levels. They do so, primarily, by reducing levels of LDL cholesterol – commonly referred to as “bad” cholesterol.
Statins available include:
- Atorvastatin (Brand name: Lipitor)
- Fluvastatin (Lescol)
- Lovastatin (Mevacor)
- Pravastatin (Pravachol)
- Pitavastatin (Livalo)
- Simvastatin (Zocor)
- Rosuvastatin (Crestor)
High LDL cholesterol levels are linked to atherosclerosis – the hardening and narrowing of your arteries – which subsequently increases your risk of chest pain (angina), coronary heart disease, heart attacks, strokes, and other cardiovascular complications. Statins, by lowering your LDL cholesterol levels, are therefore used to reduce your risk of such heart problems.
Statins usually come in tablet form, although some are available as capsules (such as fluvastatin) or oral suspensions (such as simvastatin).
Statins may be used alone or in combination with another drug, such as ezetimibe. Additionally, doctors will usually recommend lifestyle improvements that can improve cholesterol levels and reduce the risk of heart problems, including dietary improvements, exercise, reducing alcohol consumption, and quitting smoking.
How do statins work?
Statins work by reducing cholesterol production in your body.
Cholesterol itself is a fatty substance that is vital for human life; it is found in every cell in your body. Cholesterol is transported around the body in lipoproteins (which also carry another fat called triglycerides). Lipoproteins come in different shapes and sizes and have different characteristics.
Cholesterol carried by low-density lipoproteins (LDL cholesterol) has long been linked to the development of atherosclerosis, which is the build-up of plaque on the artery walls. Atherosclerosis is a major risk factor for cardiovascular diseases, including chest pain (angina), coronary heart disease, heart attacks, and strokes. This is why LDL cholesterol is often referred to as “bad” cholesterol.
High-density lipoproteins (HDL cholesterol) have been found to protect you from heart disease, largely by collecting excess cholesterol from circulation and transporting it to the liver for disposal. You cannot have too much “good” HDL cholesterol.
According to Cleveland Clinic, target lipid values are:
HDL cholesterol:
◦ Greater than 40 ml/dL
LDL cholesterol:
◦ Lower than 70 mg/dL for those at very high risk of heart disease
◦ Lower than 100 ml/dL for those at high risk of heart disease
◦ Lower than 130 ml/dL for those at low risk of heart disease
Triglycerides:
◦ Lower than 50 mg/dL
Statins’ primary mechanism of action is blocking an enzyme called HMG-CoA reductase from converting HMG-CoA to mevalonate, a necessary step for cholesterol synthesis. Inhibiting the enzyme slows down cholesterol synthesis. That is why statins are also called HMG-CoA reductase inhibitors.
In general, this mechanism has been found to reduce levels of LDL cholesterol and triglycerides, while boosting levels of HDL cholesterol.
What are statins used for?
Statins are used to improve cholesterol levels, particularly for people living with a heart condition (cardiovascular disease or CVD), such as coronary heart disease, angina, or peripheral artery disease, and those who have suffered from a heart attack or stroke.
Statins are also often prescribed to people who have not been diagnosed with heart conditions but are at risk of developing them.
In recent years, researchers have increasingly investigated the potential use of statins in a broad range of conditions, including autoimmune disease, neurodegenerative diseases, chronic inflammatory diseases, and certain cancers. However, no statins are yet approved for treating these disease clusters.
Are all statins the same?
Although all statins work in fundamentally the same way, some differences may influence your doctor’s decision regarding which to prescribe. Statins can be grouped by generations:
- First-generation: Lovastatin, pravastatin, fluvastatin
- Second-generation: Simvastatin, atorvastatin
- Third-generation: Rosuvastatin, pitavastatin
Each subsequent generation of statins has been found to have greater LDL cholesterol-lowering effects than the previous generation. Additionally, there is evidence that second- and third-generation statins improve HDL cholesterol levels and reduce triglyceride levels.
The differences in the chemical makeup of statins can have other consequences. Third-generation statins, for example, have been found to be less prone to drug interactions due to their chemistry.
The desired outcomes of your treatment (based on your lipid profile) and your personal circumstances, such as comorbidities and any other medications you take, will help your doctor decide which statin is most suitable for you.
Some other ways statins differ include:
- Cost. Although the majority of statins are available as generics, there is still some deviation in prices.
- Form. Statins usually come as tablets. However, some are also available as capsules and oral suspension, which may be preferable for certain people. For example, an oral suspension (such as simvastatin, sold under the brand name FloLipid), may be prescribed to people with swallowing difficulties.
- Release time. Some statins, including fluvastatin and lovastatin, are available in extended-release formulas. There is evidence that extended-release versions are more effective in reducing LDL cholesterol levels than regular-release versions of the same drug. However, they are usually more expensive, so they are often prescribed only to people whose cholesterol levels are particularly high.
- Time they should be taken. Several statins should be taken at night. However, some (such as atorvastatin) can be taken at any time during the day (albeit at the same time each day). This may be preferable for some people.
- Combination therapy. Some medications contain both a statin and another cholesterol-lowering agent, such as simvastatin/ezetimibe. This may be prescribed to people whose cholesterol level is not lowered by the desired amount with statins alone.
This is not an extensive list of the differences between statins. If you have any questions or concerns about your treatment, you should speak to your doctor.
Should I take statins at night?
Some statins should be taken in the evening. This is because cholesterol synthesis takes place mostly overnight and some statins have a relatively short half-life (the time it takes for half of the drug to be eliminated from your body). The FDA recommends the following statins should be taken in the evening:
- Fluvastatin (Lescol)
- Lovastatin (Mevacor & Altoprev)
- Simvastatin (Zocor)
Statins that have a longer half-life, and therefore stay in your body longer, can be taken at any time throughout the day (but at the same time each day). They include:
- Atorvastatin (Lipitor)
- Fluvastatin extended-release (Lescol XL)
- Pravastatin (Pravachol)
- Pitavastatin (Livalo)
- Rosuvastatin (Crestor)
For more information on how and when to take your medication correctly, you should speak to your doctor or read the patient information label.
What are the side effects of statins?
Statins are generally very well tolerated. However, they can cause some side effects, including:
- Headache
- Dizziness
- Muscle cramps or spasms
- Nausea
- Musculoskeletal pain (myalgia)
- Abdominal pain
- Trouble sleeping
- Fatigue
- Skin rash
These side effects are often mild and will go away as your body gets used to the medication. However, if side effects are more severe, persistent, or get worse, you should speak to your doctor as soon as possible.
Several statins also carry warnings for more serious side effects, including:
- Rhabdomyolysis: a serious syndrome that is caused by the breakdown of skeletal muscle fibers. This can lead to a protein called myoglobin to be released into your blood, which can damage your kidneys and potentially cause acute renal failure. Rhabdomyolysis is a very rare side effect of statins.
- Myopathy: elevated levels of an enzyme called creatine phosphokinase (CPK) can cause muscle pain, tenderness, and weakness.
- Liver dysfunction: statins can occasionally impair liver function, particularly in people with a history of liver disease or who drink substantial quantities of alcohol.
If you notice unexplained muscle weakness, pain, or tenderness, particularly if coupled with fever or malaise (feeling of overall discomfort, illness, or weakness), you should speak to your doctor immediately. If you believe you are at risk of liver dysfunction, you should speak to your doctor about the best course of action, which may involve periodically testing your liver function.
This is not a comprehensive list of the possible side effects of statins, nor is it specific to any individual medication. You should speak to your doctor and read the information label to learn more about the side effects of the specific statin you are taking.
Why do statins cause muscle pain?
It is not fully known why statins can cause muscle pain and other muscle complications (as mentioned in the answer to the previous question: What are the side effects of statins?)
It is possible that statins affect proteins or enzymes relating to muscle growth and energy production. A study published in 2019 suggested that muscle pain could be caused by irregular leaks of calcium from within muscle cells. The authors suggest that most people can tolerate this leak, but genetic or lifestyle factors may lead to pain in some people.
Many instances of muscle pain are attributed to a “nocebo” effect, which is when people’s negative expectations of a drug lead to greater instances of side effects. According to Mayo Clinic, nearly 30% of people in a trial stopped taking a placebo pill because of perceived muscle aches. The article states that:
“A strong predictor you'll experience muscle aches when taking statins could be whether or not you read about the potential side effect.”
Nonetheless, you should speak to your doctor if you experience muscle weakness, pain, or tenderness.
Can I lower cholesterol without taking statins?
Depending on your lipid levels and personal circumstances, your doctor may recommend lifestyle changes before the use of statins or other medications. Even if you are prescribed statins, the same lifestyle changes are usually recommended to help improve their effectiveness. Diet, exercise, and alcohol consumption are a few of the lifestyle factors that can affect your cholesterol levels and risk of heart problems.
You can read about the effects your diet can have on cholesterol levels and cardiovascular health here:
You can read about how exercise can improve your cholesterol levels here:
You can read about alcohol – and the commonly held belief that a glass of wine improves cholesterol levels – here:
Doctors do not usually recommend lifestyle improvements with the singular aim of improving cholesterol levels. Rather, positive lifestyle choices – such as those relating to exercise, diet, alcohol, smoking, etc. – will have a wide range of health benefits, among which are improving cholesterol levels and mitigating the risk of heart problems.
Whether you have been prescribed statins or not, therefore, positive lifestyle choices can help improve your cholesterol levels, reduce your risk of cardiovascular diseases, and have a host of other health benefits.
If you have any concerns or questions about your lifestyle, you should speak to your doctor or a health professional for advice. For dietary advice, you can also consult national dietary guidelines, such as those published by the USDA here.
The content on this page is provided for informational purposes only. If you have any questions or concerns about your treatment, you should talk to your doctor, pharmacist, or healthcare professional. This is particularly important if you are taking multiple medications or have any existing medical conditions.
