If you’ve recently been diagnosed with high cholesterol, you may be wondering what treatments are available to you. Your doctor will discuss options for how to lower your high cholesterol. Most people can manage their cholesterol with lifestyle changes, but medications may also be used in cases where these modifications aren’t enough. It’s important to maintain healthy cholesterol levels in order to avoid cardiovascular complications such as heart disease and stroke.¹

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What is High Cholesterol?Clinical Trials for Cholesterol

Medications for High Cholesterol

High cholesterol levels cause fats and other substances to build up in your arteries. This condition is known as atherosclerosis, and it increases your risk of other cardiovascular complications.² To keep your heart and body healthy, your doctor may recommend one or more medications to lower your cholesterol and/or triglyceride levels.

Statins

Statins are a class of medications used by millions of Americans to lower their low-density lipoprotein (LDL or “bad cholesterol”) levels. These medications help significantly reduce LDL levels by blocking the function of the HMG CoA reductase enzyme. This enzyme is essential for your body’s cholesterol production — in fact, your body makes nearly all of the cholesterol it needs. By blocking the enzyme, your body makes much less, and your cholesterol levels quickly fall.³

Some statins also help raise your high-density lipoprotein (HDL or “good cholesterol”) levels, which help your body get rid of excess cholesterol. Together with recommended lifestyle changes such as eating a healthy diet and exercising, statins are the preferred treatment for high cholesterol levels.

Studies show that statins also help reduce the risk of health complications associated with high cholesterol, including heart disease. These medications may help stabilize plaques and prevent them from breaking off, reducing your risk of blood clots and stroke.⁴

Types of Statins

The U.S. Food and Drug Administration (FDA) has approved several statin medications, including:³

Atorvastatin (Lipitor®)
Simvastatin (Zocor®)
Rosuvastatin (Crestor®, Ezallor^TM)
Pravastatin (Pravachol®)
Lovastatin (Altoprev®, Mevacor®)
Pitavastatin (Livalo®, Zypitamag®)
Fluvastatin (Lescol® XL)

Some statins may also be combined with other drugs to boost their cholesterol-lowering effects. These include:

Lovastatin-niacin (Advicor®)
Simvastatin-ezetimibe (Vytorin®)
Atorvastatin-ezetimibe (Liptruzet^TM)

Side Effects of Statins

Most people who take statins tolerate them well and have few side effects. You’re more likely to experience side effects when first starting statins, and they should go away as your body begins to adjust. Common side effects include:³

Muscle pain and/or cramping
Achy joints
Headaches
Nausea
Constipation or diarrhea
Dizziness or lightheadedness

Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors help reduce the amount of cholesterol absorbed by your intestines. This class of medications limits cholesterol delivery to the liver — as a result, your body clears more cholesterol from your blood and liver.^5,6

Ezetimibe (Zetia®) is currently the only FDA-approved cholesterol absorption inhibitor. Studies show that it can reduce LDL cholesterol levels by 13 to 20 percent. Ezetimibe may be prescribed alone or together with other medications. Two formulations have also been approved in combination with statins (Vytorin® and Liptruzet^TM). Exetimibe is also combined with bempedoic acid (Nexlizet®), which reduces cholesterol made by the liver.

Side Effects of Cholesterol Absorption Inhibitors

Common side effects of ezetimibe include:⁵

Runny nose
Sore throat
Headache
Fatigue
Body aches and pains
Diarrhea
Joint pain

Bile Acid Sequestrants

Bile acid sequestrants, also known as bile acid resins, are another class of cholesterol-lowering medications. As their name suggests, they bind to the bile acids in your small intestine. This prevents them from being absorbed, and they’re excreted from your body. Your liver is then forced to use cholesterol to make more bile acids, which lowers your cholesterol levels.⁷

Studies show that bile acid sequestrants can lower your LDL levels by up to 30 percent. These medications are typically prescribed in addition to statins or other medications to help better control cholesterol levels.⁸

Types of Bile Acid Sequestrants

The FDA has approved three bile acid sequestrants to treat high cholesterol. They include:

Cholestyramine (Prevalite®, Questran®)
Colesevelam (Welchol®)
Colestipol (Colestid®)

These medications are available as pills or as powders to mix with water, soups, or other liquids.

Side Effects of Bile Acid Sequestrants

The most common side effect reported while taking bile acid sequestrants is constipation. Other side effects you may experience include:⁷

Gas or bloating
Nausea
Heartburn
Diarrhea
Achy muscles

PCSK9 Inhibitors

PCSK9 inhibitors are a newer class of medications used to treat high cholesterol. Specifically, they block the proprotein convertase subtilisin/kexin type 9 (PCSK9) protein. These medications are only prescribed in cases where statins and other medications aren’t effective, or in people who have a genetic condition known as familial hypercholesterolemia.⁹

The more PCSK9 you have, the higher your cholesterol levels tend to be. This is because PCKS9 breaks down your LDL receptors. These receptors are found on many cells throughout your body, but they’re highly concentrated in the liver. The more LDL receptors on your liver cells, the faster LDL is removed from your body.

PCSK9 inhibitors block the PCSK9 protein, preventing it from breaking down the LDL receptors in your liver. As a result, the receptors are able to attach to LDL cholesterol and remove it from your body. Studies show that PCSK9 inhibitors may reduce your LDL cholesterol by nearly 70 percent — they can also decrease your risk of a heart attack by over 30 percent.¹⁰

Types of PCSK9 Inhibitors

Currently, the FDA has approved three PSCK9 inhibitors — evolocumab (Repatha®), alirocumab (Praluent®), and inclisiran (Leqvio®). Two are laboratory-engineered antibodies (known as monoclonal antibodies) designed specifically to attach to the PSCK9 protein. Inclisiran is a siRNA (short interfering RNA) that interferes with the production of PCSK9. Because these drugs are proteins, they must be given as injections to be effective. Injections are given every one to six months.¹⁰

Side Effects of PCSK9 Inhibitors

In general, PCSK9 inhibitors are well tolerated and many people experience mild side effects, including:¹⁰

Muscle soreness or pain
Fatigue
Redness or swelling at the injection site

Treatments for High Triglycerides

Triglycerides are a different type of fat from cholesterol. Your triglyceride levels may be high if you eat high-fat foods such as oils or butter. Your body also stores extra calories as triglycerides in fat cells to be used later. Depending on your total cholesterol levels, your doctor may prescribe a statin or a treatment specifically for lowering your triglyceride levels.¹¹

Fibrates are a class of medications that help lower your very-low-density lipoprotein (VLDL) levels. VLDL cholesterol is responsible for carrying triglycerides through your bloodstream. Fibrates also boost the production of other proteins that help your body make HDL or “good cholesterol,” which helps your liver get rid of “bad cholesterol.” Studies show that fibrates can lower triglyceride levels by up to 50 percent, and they can also increase HDL cholesterol by around 20 percent.

Examples of FDA-approved fibrates include:

Fenofibrate (Fibricor®, TriCor®, Lofibra®)
Clofibrate (Atromid-S®)
Gemfibrozil (Lopid®)

Common side effects you may experience while taking fibrates include abdominal pain, headaches, leg cramps, constipation, or diarrhea.

Your doctor may also recommend over-the-counter (OTC) treatments, such as fish oil (omega-3) or niacin (vitamin B3). (A purified form of marine fatty acid called Vascepa® is availble by prescription for high triglycerides.) If you’re interested in starting an OTC treatment or supplement, be sure to consult your doctor first to ensure it doesn’t interfere with your other medications.¹²

Lifestyle Modifications for High Cholesterol

Your doctor will likely recommend that you make lifestyle modifications to help lower your cholesterol. For some people, these changes are enough — for others, they can help boost the effects of cholesterol-lowering medications. The Mayo Clinic recommends five heart-healthy modifications you can make:¹³

Limit fats and enjoy a heart-healthy diet: Extra cholesterol typically comes from your diet, so be sure to limit saturated fats and cut out trans fats. Eating foods high in fiber and protein can help your body clear excess LDL cholesterol.
Maintain a healthy weight: Excess weight can contribute to high cholesterol levels. Choosing healthier foods and beverages and getting more exercise can help you reach a healthy weight.
Quit smoking: Smoking causes inflammation and damages your blood vessels, making it easier for plaques to form. Quitting smoking has been shown to boost your HDL levels and reduce your risk of cardiovascular complications.¹⁴
Get more exercise: Increasing your activity level can help raise your HDL cholesterol. With your doctor’s permission, try to get at least 30 minutes of exercise five days a week by walking, biking, or swimming.
Drink alcohol in moderation: While some research shows that alcohol may boost HDL levels, the benefits don’t necessarily outweigh the risks. Increased alcohol consumption has been linked to heart disease and stroke.¹⁵

Doctors and researchers continue to look for new ways to treat high cholesterol, including studying interventions in clinical trials for cholesterol management.