High Cholesterol medications & treatments

Medically reviewed by  Jamie Winn, PharmD

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According to the CDC, almost 94 million adults in the United States are considered to have borderline high cholesterol (hyperlipidemia) with a total cholesterol level higher than 200mg/dl. Over 28 million adults in the U.S. have high cholesterol with levels over 240mg/dl. This condition can also affect children and adolescents. It is estimated that 7% of those aged 6 to 19 in the U.S. have high total cholesterol. 

What is high cholesterol?

Cholesterol is a wax-like substance (lipid) that is naturally produced by your liver. It is involved in important processes such as making vitamin D and hormones. It is transported through your blood by lipoproteins:

• Low-density lipoprotein (LDL). This carries LDL cholesterol, which is referred to as “bad” cholesterol.
• High-density lipoprotein (HDL). This carries HDL cholesterol, which is referred to as “good” cholesterol.

Lipoproteins also carry triglycerides, another type of lipid.

High cholesterol causes

High cholesterol levels are often caused by an unhealthy lifestyle, but can also be caused by genes inherited from your parents. It is usually due to a combination of the following:

• Poor diet. If you eat too many foods that are high in saturated fat or trans fat, it can raise your LDL cholesterol (bad cholesterol). Saturated fats are found in dairy products and high-fat cuts of meat such as skirt steak and rib-eye. Trans fats can be found in fried fast foods and commercially baked foods.
• No regular exercise. Physical activity can increase your HDL cholesterol levels (good cholesterol). Lack of regular exercise can lead to obesity which can increase your cholesterol levels.
• Obesity. For every 10 pounds you are overweight, your body makes an extra 10mg of cholesterol per day.
• Smoking. Smoking cigarettes can lower your level of HDL while raising your LDL levels.
• Alcohol. Drinking more than 2 drinks a day if you are a man or 1 drink a day if you are a woman can raise your total cholesterol level.
• Genetics. There are certain genetic factors or inherited conditions (familial hypercholesterolemia) that can cause you to have high cholesterol levels.
• Certain medical conditions. Your risk of high cholesterol is increased if you have diabetes, chronic kidney disease, hypothyroidism, lupus, or HIV.
• Stress. Some studies have shown that increased levels of stress can cause an increased level of LDL cholesterol.

How is high cholesterol diagnosed?

The majority of people with high cholesterol have no symptoms. Routine screening and blood tests can help you uncover high levels. How often you should be screened will be determined by your family history and other risk factors.

Your doctor will perform a lipid panel to check the levels of the following:

• Total cholesterol
• LDL cholesterol
• HDL cholesterol
• Triglycerides (a type of fat in the blood)

Consult your health care provider to find out what your cholesterol levels should be. Untreated high blood cholesterol can lead to serious complications such as high blood pressure, cardiovascular disease, peripheral artery disease, type 2 diabetes, and stroke.

What are some high cholesterol treatment options?

Treatment for high cholesterol usually consists of a combination of lifestyle changes and/or medications. 

Medications

If diet and exercise do not lower your cholesterol enough, your doctor may prescribe one of the following types of cholesterol-lowering drugs:

• Statins. HMG-CoA reductase inhibitors, which are more commonly known as statins, are the first-line treatment to lower triglyceride and LDL cholesterol levels in your bloodstream. They are the most commonly prescribed medication to treat high cholesterol, according to the American Heart Association. They work by blocking an enzyme in the liver that is needed to make cholesterol. Some examples include Lipitor (atorvastatin), Zocor (simvastatin), Lescol (fluvastatin), and Crestor (rosuvastatin).
• Zetia (ezetimibe). This medication is usually prescribed along with another cholesterol-lowering medication. It works by preventing the absorption of cholesterol from your diet
• Bile acid sequestrants. Bile acids are made in your liver using cholesterol. Medications such as Colestid (colestipol) and Welchol (colesevelam) bind to bile acids in your bloodstream. Without enough bile acids, your body uses any extra cholesterol to make more bile acids, which lower cholesterol levels in your blood.
• PCSK9 inhibitors. These monoclonal antibodies can help the liver absorb more LDL cholesterol by blocking the protein PCSK9. This increases the removal of LDL cholesterol from the bloodstream by LDL receptors. Two of the PCSK9 inhibitors that are approved by the FDA are Repatha (evolocumab) and Praluen (alirocumab).
• Nexletol (bempedoic acid). This medication works by slowing down the production of cholesterol in your liver. This will reduce the cholesterol in your blood.
• Fibrates. Medications such as Lopid (gemfibrozil) and Tricor (fenofibrate) lowers your triglyceride levels and can increase the production of HDL cholesterol.
• Niaspan (niacin). Niacin, or vitamin B3, reduces LDL cholesterol and can raise HDL cholesterol. It is often prescribed with a statin or along with another medication if you cannot take a statin.

What is the best medication for high cholesterol?

The best medication for the treatment of high cholesterol will depend on the individual’s health information including medical condition, medical history, medications that the individual is already taking that may potentially interact with high cholesterol medications, and the individual’s potential response to the treatment. It is advisable to always speak with your healthcare provider about the best medication for you. The table below includes a list of the most prescribed or over-the-counter supplements approved by the Food and Drug Administration (FDA).

Best medications for high cholesterol

Your healthcare provider will determine the right dosage based on your response to the treatment, medical condition, weight, and age. Other possible side effects may exist; this is not a complete list.

What are the most common side effects of high cholesterol medications?

As with all medicines, those used for high cholesterol will have some side effects, depending on the class of drugs you are taking:

• Statins can cause muscle pain, diarrhea, nausea, vomiting, indigestion, constipation, gas, headache, and stomach pain.
• Bile acid sequestrants may cause gas, constipation, nausea, vomiting, diarrhea, headache, and indigestion.
• Fibrates can commonly cause indigestion, stomach pain, diarrhea, fatigue, nausea, vomiting, elevated liver enzymes, and headache.
• PCSK9 inhibitors may cause common cold symptoms, upper respiratory tract infections, back pain, injection site reactions, allergic reactions, and diarrhea.
• Zetia’s (ezetimibe) most common side effects include diarrhea, cough, upper, fatigue, joint pain, and headache.
• Niaspan (niacin) causes facial flushing in the majority of people who take it. It also commonly causes nausea, headache, itching, and tingling sensations.

What are some home remedies for high cholesterol?

Lifestyle changes are typically the first line of treatment for high cholesterol. In some cases, they will lower your cholesterol enough and you won’t need medications.

High cholesterol prevention

These changes can include:

• Eat a healthy diet that’s low in saturated fats and high in fiber.
• Exercise regularly.
• Maintain a healthy weight.
• Stop smoking.
• Limit or avoid alcohol.

Frequently asked questions about high cholesterol

Are there over-the-counter supplements that can lower your cholesterol?

Certain OTC medications may help improve your cholesterol levels. They include niacin, red yeast rice, and fish oil (omega-3 fatty acids). Please contact your healthcare provider before taking any OTC medications.

What foods should I avoid with high cholesterol?

You should avoid foods high in saturated fats and trans fats such as processed or deli-style meats, fried fast foods, processed foods, and fatty cuts of meat.

What foods can I eat to help lower my cholesterol?

You should eat a heart-healthy diet that is high in fiber with fruits, vegetables, legumes (lentils, chickpeas), and whole grains. You can also eat lean, protein-rich meats such as chicken, fish, and some cuts of red meat.

What are some complications of high cholesterol?

High cholesterol levels can lead to serious health problems if left untreated. It can raise your risk of heart disease (the leading cause of death in the U.S.), stroke (5th leading cause of death in the U.S.), and heart attacks.

Related resources for high cholesterol

• High cholesterol symptoms and causes. MayoClinic
• Cholesterol numbers and what they mean. Cleveland Clinic
• What is high cholesterol? NHS
• Everything you need to know about high cholesterol. Healthline
• What is blood cholesterol? National Heart, Lung, and Blood Institute
• About cholesterol. Centers for Disease Control and Prevention
• Causes of high cholesterol. Heart.org