High Cholesterol Treatments and Medications

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. 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. 

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, LDL (“bad”) cholesterol, HDL (“good”) 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 looking for 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 lifestyle changes alone are not able to lower cholesterol levels, healthcare providers 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

• 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 significantly reduce LDL cholesterol levels. 

Medications

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

Types of high cholesterol medication

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 cholesterol. Also called HMG-CoA reductase inhibitors, statins like atorvastatin, rosuvastatin, and simvastatin block an enzyme the liver needs to manufacture cholesterol, which can significantly reduce LDL cholesterol. Statins may help reduce the risk of heart attack and stroke. 

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 acid sequestrants, such as cholestyramine, colesevelam, and colestipol, are sometimes prescribed in addition to statins or when statins aren’t tolerated because of side effects. They help lower LDL cholesterol. 

Fibrates

When statins are not successful, fibrates (fenofibrate, fenofibric acid, and gemfibrozil) may be added to the treatment plan. Fibrates are effective at lowering triglycerides and also mildly lower LDL cholesterol. 

Niacin

Niacin (nicotinic acid) is a vital nutrient called vitamin B3. It can help reduce LDL cholesterol and raise HDL cholesterol.

PCSK9 inhibitors

PCSK9 inhibitors are injectable drugs that reduce LDL cholesterol. The FDA has approved three PCSK9 inhibitors. Repatha (evolocumab) and Praluent (alirocumab) are usually prescribed as a single injection every two weeks. Lipfendra is a once-daily oral tablet.

Omega-3 fatty acids

Prescription omega-3 fatty acids, such as omega-3 acid ethyl esters and icosapent ethyl (IPE), are often prescribed to lower triglyceride levels. 

Nexletol

Nexletol (bempedoic acid) is known as an ACLY inhibitor. It works by blocking cholesterol production in the liver. Nexletol is often prescribed with other medications to lower cholesterol. 

Over-the-counter cholesterol medicine

There are no over-the-counter medicines that treat high cholesterol. Some dietary supplements may help support healthy cholesterol levels, but they are not a substitute for medication prescribed by your healthcare provider. Always check with your healthcare provider before adding a supplement to your routine.

Treatment of high cholesterol depends on several variables, so there is no “best” medication for high cholesterol. Some 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 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. 

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Best medication for high cholesterol