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High cholesterol

High Cholesterol Treatments and Medications

Medically reviewed by Gerardo SisonPharm.D.
Licensed Pharmacist
Updated Apr. 24, 2024  •  Published Dec. 14, 2020
Fact Checked

Cholesterol is important for a healthy functioning body. But if too much cholesterol collects in the bloodstream, heart disease and stroke become a serious risk. Because high cholesterol has no symptoms, keeping cholesterol levels in check requires vigilance, regular blood tests, a healthy diet, exercise, and, if necessary, cholesterol-reducing medications.

What is high cholesterol?

Cholesterol is a wax-like substance that the body uses to build cells, protect nerves, and make hormones. Cholesterol normally circulates in the bloodstream, but too much blood cholesterol contributes to the formation of plaques stuck to the lining of blood vessels. Plaque buildup, or atherosclerosis, can narrow arteries and obstruct blood flow. If a plaque breaks loose, it can completely block an artery to a vital organ, such as the heart or brain, causing a heart attack or stroke.

There are two major types of cholesterol. High-density lipoprotein cholesterol (HDL) primarily serves to transport cholesterol to the liver to be broken down. Called “good” cholesterol, HDL reduces total cholesterol levels in the blood. Low-density lipoprotein cholesterol (LDL) transports fats to cells. Called “bad” cholesterol, LDL cholesterol can build up in the bloodstream.

Some genetic disorders, such as familial hypercholesterolemia, can cause high cholesterol, as can medical conditions such as hypothyroidism or pregnancy. Most people, however, have high cholesterol due to an inactive lifestyle or a diet high in saturated and trans fats.

The Centers for Disease Control and Prevention (CDC) estimates that 93 million adults aged 20 or older in the United States have high total cholesterol levels. For most people, high cholesterol can be managed by rigorously adopting a heart-healthy diet, losing weight, and adding exercise to their daily routine. If that doesn’t work, a variety of medications can effectively bring serum cholesterol back to safe levels.

How is high cholesterol diagnosed?

High cholesterol is diagnosed by blood tests that measure fats and cholesterol in the blood. A physical examination and medical history can help identify possible causes or complications.

High cholesterol does not produce symptoms, so it is first identified through a blood test. The standard test measures total cholesterol level, LDL cholesterol level, HDL cholesterol level, and the concentration of triglycerides (a type of fat) in the bloodstream. A general practitioner or another healthcare provider will evaluate these results and consider other medical conditions or lifestyle habits that may raise the risk of cardiovascular disease. Risk factors such as high blood pressure, diabetes, obesity, smoking, family history of heart problems, and advanced age can help determine what would be considered dangerous LDL cholesterol and total cholesterol levels.

While reviewing your medical history and physical examination, the healthcare provider is not only looking for risk factors, but also sleuthing out possible causes for elevated LDL cholesterol such as:

  • Family history of high cholesterol
  • Diet
  • Lifestyle
  • Pregnancy
  • Medications that raise cholesterol levels
  • Hypothyroidism
  • Kidney problems (nephrotic syndrome)
  • A blocked liver (cholestasis)

In a physical examination, the healthcare provider will also look for evidence of possible complications such as heart disease, stroke, or arterial disease. Further tests may be required if there’s evidence of heart or vascular problems.

High cholesterol treatment options

The initial treatment for high cholesterol is a healthy lifestyle consisting of a heart-healthy diet and exercise plan. If a healthy lifestyle is not able to keep cholesterol at safe levels, doctors will prescribe medications to bring down cholesterol levels.

Lifestyle changes

No matter what causes high cholesterol, the most effective treatment involves adopting a healthy lifestyle:

  • Maintaining optimal body weight
  • Exercising for 30 minutes five times per week
  • Eating a healthy diet low in saturated fats and trans-fatty acids, as well as high in fiber
  • Quitting smoking

In most people with high cholesterol, a healthy lifestyle can dramatically reduce LDL cholesterol levels within two to three months.

Medications

Medications can dramatically reduce LDL cholesterol levels through a variety of mechanisms. Statins are the first-line drug therapy for high cholesterol, but other types of medications can be added if statin treatment is not effective enough or causes bad side effects.

High cholesterol medications

The foundational treatment for high cholesterol is a combination of diet and exercise. When diet and exercise are not sufficient, different types of medications can lower LDL cholesterol and fats in the bloodstream through a variety of mechanisms.

Statins

Statins are the first-line drug therapy for high LDL cholesterol and triglyceride levels in the bloodstream. Also called HMG-CoA reductase inhibitors, statins like atorvastatin, fluvastatin, and simvastatin block an enzyme the liver needs to manufacture cholesterol. Most of the cholesterol in the bloodstream is made by the liver, so by shutting down the liver’s “cholesterol factory,” statins can reduce LDL in the bloodstream by as much as 60%. Statins also protect the heart by reducing inflammation of the blood vessels and preventing blood vessel plaques from breaking up and forming blood clots. Because the liver churns out most of the body’s cholesterol at night, statins are usually taken as a single dose right before bedtime.

Ezetimibe

Usually prescribed along with a statin or other cholesterol-reducing drug, ezetimibe interferes with the digestive system’s ability to absorb cholesterol from food. By blocking the absorption of cholesterol in the small intestines, ezetimibe causes the liver to clear LDL cholesterol from the bloodstream. This action leads to overall reduced cholesterol levels, especially when ezetimibe is added to statin therapy.

Bile acid sequestrants

Bile acids are molecules built from cholesterol in the liver. They are secreted into the intestines where they attach to fats from foods. Without bile acids, the intestines would not be able to bring fats into the body. After bile acids are absorbed into the body, they are then recirculated back to the liver to be reused. Bile acid sequestrants (cholestyramine, colesevelam, and colestipol) attach to bile acids and prevent them from attaching to fats or being reabsorbed by the intestines. Without bile acids to reuse, the liver must make new bile acids from cholesterol, so the effect is reduced LDL cholesterol in the bloodstream. Also called antilipemic agents, bile acid sequestrants can lower serum LDL cholesterol by as much as 30%. They are usually prescribed in addition to statins or when statins aren’t tolerated because of side effects. Bile acid sequestrants are often taken with ezetimibe or niacin. They work best when taken before meals.

Fibrates

When statins are not successful, fibrates (fenofibrate, fenofibric acid, and gemfibrozil) may be added to the treatment plan. Fibrates increase the liver’s uptake and destruction of LDL cholesterol and increase the liver’s production of HDL. They also stimulate cells to clear triglycerides from the bloodstream, reducing triglycerides from 30 to 60%. Fibrates can be taken with or without a meal, but they’re usually taken with meals to reduce stomach upset.

Niacin

Niacin (nicotinic acid) is a vital nutrient called vitamin B3. It is not well-understood how it reduces LDL cholesterol and raises HDL cholesterol, but it is often prescribed with a statin alone or in combination with ezetimibe for high-risk patients. To be the most effective, it is usually administered in high daily doses.

PCSK9 inhibitors

The newest family of cholesterol-lowering medications are monoclonal antibodies that block PCSK9, a protein that stimulates liver cells to break down LDL receptors. These LDL receptors help remove LDL cholesterol from the bloodstream. When the PCSK9 protein breaks down and recycles LDL receptors, there is an increase in LDL cholesterol in the blood. Blocking this protein increases the availability of LDL receptors so they can remove more LDL cholesterol from the bloodstream. The FDA has approved two PCSK9 inhibitors: Repatha (evolocumab) and Praluent (alirocumab). These drugs are usually prescribed as a single injection every two weeks.

What is the best medication for high cholesterol?

Treatment of high cholesterol depends on several variables, so there is no “best” medication for high cholesterol. Many patients can successfully control cholesterol levels by committing to lifestyle and dietary changes. These don’t work in every case, so a combination of lifestyle changes and medications can help reduce blood cholesterol levels. The type and dose of the medication will depend on the drug’s effectiveness, the patient’s tolerance of side effects, and other factors.

Best medications for high cholesterol
Drug Name Drug Class Administration Route Standard Dosage Common Side Effects
Lipitor (atorvastatin) Statin Oral 10 to 80 mg once per day Joint pain, pain in the extremities, diarrhea
Zocor (simvastatin) Statin Oral 5 to 40 mg once per day in the evening Headache, abdominal pain, constipation
Lescol XL (fluvastatin) Statin Oral 20 to 80 mg once per day Indigestion, nausea, headache
Lopid (gemfibrozil) Fibrate Oral 600 mg once in the morning and once in the evening 30 minutes before a meal Abdominal pain, indigestion
Fibricor (fenofibric acid) Fibrate Oral 105 mg once per day Nausea, back pain, headache
Tricor (fenofibrate) Fibrate Oral 160 mg once per day with food Nausea, abdominal pain, back pain
Questran (cholestyramine) Bile acid sequestrant Oral 8 to 16 g per day in divided doses Constipation, abdominal pain, flatulence
Zetia (ezetimibe) Cholesterol absorption inhibitor Oral 10 mg once daily with or without food Diarrhea, upper respiratory tract infection, joint pain
Niacor (niacin) Miscellaneous cholesterol-reducing drug Oral 1.5 to 2 g per day in divided doses Facial flushing, nausea, vomiting
Repatha (evolocumab) PCSK9 inhibitor Subcutaneous injection 140 mg injected under the skin every two weeks Injection site reactions, upper respiratory tract infection, back pain

Many of the standard dosages above are from the U.S. Food and Drug Administration (FDA). Dosage is determined by your doctor based on your medical condition, response to treatment, age, and weight. Other possible side effects exist. This is not a complete list.

What are the common side effects of high cholesterol medication?

The side effects of cholesterol medications will vary depending on the type of medication. This is not a complete list of possible side effects, so consult with a healthcare professional about any questions or concerns regarding side effects or drug interactions.

Among cholesterol-reducing medications, statins are the safest. The most common side effect of statins is muscle pain. In worst-case scenarios, statins can destroy muscle tissues and precipitate kidney failure. Some statins can also cause common cold symptoms, joint pain, and diarrhea. Other side effects may include liver problems, kidney problems, and elevated blood sugar. Statins may cause rare, adverse effects like behavioral changes and memory problems.

The most common side effects of fibrates include abdominal pain, nausea, and headache. Fibrates may also irritate the liver and increase liver enzymes, which could lead to liver injury. Other side effects of fibrates may include muscle pain, leg cramps, and diarrhea. The risk of muscle pain goes up when fibrates are taken with statins.

The most common side effects of ezetimibe are runny nose, sore throat, headache, muscle aches, joint pain, and diarrhea.

In clinical doses, niacin may produce unpleasant side effects. Four out of five patients will experience facial flushing and one out of five will experience nausea, itching, or a tingling or numbing sensation on the skin. In clinical doses, niacin may increase the risk of high blood sugar levels or bleeding.

Bile acid sequestrants primarily affect the digestive system, so common side effects include constipation, diarrhea, stomach upset, nausea, bloating, cramping, and loss of appetite.

PCSK9 inhibitors are self-injected, so the most common side effects are injection site reactions, such as redness, pain, or bruising. Other common side effects include nasopharyngitis, upper respiratory tract infections, flu, and back pain.

What is the best home remedy for high cholesterol?

The good news about high cholesterol is that lifestyle changes are usually the first recommended form of treatment. Yes, lifestyle changes will require commitment and effort. However, unlike medications, they don’t have side effects.

Eat a healthy diet

The foundation of a cholesterol-reducing diet is to avoid saturated and trans fats, both of which increase LDL cholesterol. Soluble fiber (found in vegetables, fruits, and grains) can help decrease the absorption of cholesterol in the body. Whey protein (found in dairy products) may also help decrease LDL cholesterol in the blood.

Exercise

Exercise increases HDL cholesterol, the lipoprotein that removes cholesterol from the bloodstream. Simply walking for 30 minutes on most days could produce a noticeable drop in LDL cholesterol levels.

Lose weight

It’s hard to lose extra weight. The benefits, however, really do outweigh the effort. Losing excess weight not only reduces LDL cholesterol, it also lowers blood pressure and decreases the risk of heart disease.

Quit smoking

Quitting smoking is always a great idea. It can improve a slew of health problems. For high cholesterol, quitting smoking raises serum HDL, the lipoprotein that carries off cholesterol to be broken down by the liver.

Frequently asked questions about high cholesterol

What reduces cholesterol quickly?

A healthy lifestyle is one of the most effective ways to reduce “bad” cholesterol in the bloodstream. Eating a healthy diet, exercising, losing weight, and quitting smoking can dramatically reduce serum cholesterol in just a few weeks. Genetics, however, do play a role in high cholesterol, so lifestyle and dietary changes are not always enough to do the job. In those cases, people will need to take cholesterol-reducing medications to lower the risk of coronary heart disease or stroke.

What are the symptoms of high cholesterol in the body?

High cholesterol is a silent medical condition. People do not experience symptoms or warning signs. What they do experience are complications of high cholesterol such as cardiovascular disease, arterial disease, blood clots, heart attack, and stroke.

What is a natural way to treat high cholesterol?

An effective, natural way to control high cholesterol is to exercise, lose excess body weight, and eat a healthy diet low in saturated and trans fats.

What is the best medicine for lowering cholesterol?

Statins are the first-line medicine for lowering cholesterol. Most statins can reduce serum cholesterol from 22% to 50% over the course of treatment. They may not work for everyone by themselves, so a healthcare professional may prescribe additional medications such as ezetimibe, bile sequestrants, fibrates, niacin, or PCSK9 inhibitors.

What is the best natural remedy for cholesterol?

The best natural remedy for high cholesterol is a healthy diet combined with daily exercise. For most people with high cholesterol, a diet low in saturated and trans fats and high in fiber may dramatically reduce “bad” cholesterol after a few months.

What should I eat for breakfast to lower my cholesterol?

Soluble fiber, plant stanols, and whey protein can all help to lower “bad” cholesterol. Breakfast foods rich in these substances may include oatmeal, almond milk, low-fat milk, yogurt, fruits, and whole grains.

What is the best cholesterol medication with the least side effects?

Statins are the first-line therapy for high cholesterol. They are the safest of the cholesterol-reducing drugs, but some people can still experience side effects. Side effects are usually mild and go away on their own after starting treatment.

What non-statin drugs are used to lower cholesterol?

If statin drugs do not succeed in sufficiently lowering LDL cholesterol, other medications such as bile sequestrants, ezetimibe, fibrates, niacin, or a new breed of monoclonal antibodies can be added to the statin prescription or used alone.

What is the most common side effect of statins?

The most common side effect of statins is muscle pain. Other common side effects may include headache, common cold symptoms, joint pain, and diarrhea. In a small number of patients, the statin can cause severe muscle pain, which could indicate a condition called rhabdomyolysis where the muscle tissue breaks down.

What happens if you stop taking statins?

When you stop taking statins, LDL cholesterol can return to high levels within a few months.

What is the best drink to lower cholesterol?

Certain drinks with added plant sterols or fiber may help to reduce “bad” cholesterol. If you increase your daily fiber intake, it is important to make sure you drink extra water to prevent constipation. Make sure, though, that the fiber-fortified drink you pull from the shelf is low in saturated or trans fats, both of which can increase “bad” cholesterol in the blood.

How can I check my cholesterol at home?

At-home cholesterol tests can be inexpensive and surprisingly accurate—sometimes almost as accurate as a blood test performed at a clinic. They may be worth considering if you want to monitor how effectively lifestyle changes or medications are lowering blood cholesterol.

Which cholesterol drug is safest?

Statins are considered the safest cholesterol-reducing drugs. Most people are able to tolerate the side effects of statins. However, some people may find that certain side effects are too severe to bear. Consult your healthcare provider for the safest cholesterol drug for you.

Medically reviewed by Gerardo SisonPharm.D.
Licensed Pharmacist

Gerardo Sison, Pharm.D., graduated from the University of Florida. He has worked in both community and hospital settings, providing drug information and medication therapy management services. As a medical writer, he hopes to educate and empower patients to better manage their health and navigate their treatment plans.

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