Medications to Lower Cholesterol and Triglyceride Levels

Managing cholesterol and triglyceride levels is crucial to coronary artery disease (CAD) prevention

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Several medications are regularly prescribed to treat high cholesterol and triglyceride levels, from statins like Lipitor (atorvastatin), to PCSK9 inhibitors like Repatha (evolocumab), to niacin.

Which is most appropriate for you depends on several factors, but it’s likely your healthcare provider will want you to begin taking prescription medication if diet and exercise are not enough to lower your levels, or if your risk for cardiovascular disease is particularly elevated.

This article will help you learn about the possible prescription options your healthcare provider might suggest so you can take an active role in your treatment discussions and decisions.

Man sitting on couch taking medication
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Statins

Statins are the mainstay of therapy for cholesterol. These oral drugs inhibit the action of an enzyme called HMG-CoA reductase, reducing the liver’s ability to make cholesterol.

Some of the body’s cholesterol is produced by the body rather than ingested through diet. Thus, inhibiting this enzyme lowers cholesterol through a process different from dietary strategies.

Statins also reduce vascular inflammation, decrease vascular thrombosis, and improve overall vascular function.

Statins are usually well tolerated, but you can experience side effects. The most notable one is muscle pain or weakness, which occurs in 0.3% to 33% of patients who take these drugs.

Currently available statins include:

  • Crestor (rosuvastatin)
  • Lescol XL (fluvastatin)
  • Lipitor (atorvastatin)
  • Livalo (pitavastatin)
  • Altoprev (lovastatin)
  • Pravachol (pravastatin)
  • Zocor (simvastatin)

PCSK9 Inhibitors

PCSK9 inhibitors are a newer class of cholesterol-lowering drugs than statins.

They work by inhibiting PCSK9, an enzyme that destroys the receptor proteins that help remove low-density lipoprotein (LDL or “bad” cholesterol) from circulation.

The effect of these drugs is a therapeutic reduction of bad cholesterol.

PCSK9 inhibitors, administered by injection and combined with other lipid-lowering medications like statins, can drive LDL cholesterol to deficient levels. They are often prescribed for those who have familial hypercholesterolemia or LDL cholesterol levels that remain significantly elevated despite treatment with statins.

Available PCSK9 inhibitors include:

  • Leqvio (inclisiran)
  • Praluent (alirocumab)
  • Repatha (evolocumab)

Ezetimibe

Ezetimibe reduces cholesterol absorption from the intestines, causing the liver to get more cholesterol by removing it from the bloodstream. As a result, blood levels of LDL cholesterol are reduced.

Clinical trials with ezetimibe have been fairly disappointing, and the drug is not used often in clinical practice. It is mainly prescribed for people who have continued high cholesterol levels despite statin therapy or those unable to take statins.

Available versions of this drug include:

  • Vytorin (ezetimibe)
  • Zetia (ezetimibe/simvastatin)

Bile Acid Sequestrants

Bile acid sequestrants prevent the reabsorption of cholesterol-containing bile acids from the intestine. This causes the liver to remove more cholesterol from circulation.

Bile acid sequestrants include:

  • Cholestid (colestipol)
  • Questran (cholestyramine)
  • Welchol (colesevelam)

While these drugs also effectively reduce LDL cholesterol levels, they tend to cause gastrointestinal side effects that limit usefulness.

Clinical studies have yet to show that they improve outcomes.

Fibrates

Fibrates inhibit the production of triglyceride-rich lipoproteins in the liver. They are most effective at reducing triglyceride blood levels (by up to 50%). They also increase HDL cholesterol levels and reduce LDL cholesterol levels to some extent.

Despite their favorable effect on blood lipids, several randomized trials have failed to show any improvement in clinical outcomes with fibrates. They are mainly used to treat severe hypertriglyceridemia.

Available fibrates include:

  • Antara (gemfibrozil)
  • Lopid (fenofibrate)

The most common side effect of fibrates is that they can cause muscle toxicity, mainly when used with statins.

Summary

Several types of prescription medications are available to treat cholesterol and lower triglyceride levels. Statins are the first-line therapy for reducing cholesterol. These drugs work by reducing the liver's ability to make cholesterol. Other options include a newer class of drugs called PCSK9 inhibitors, as well as ezetimib, bile acid sequestrants, and fibrates.

13 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
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Additional Reading
Richard N. Fogoros, MD

By Richard N. Fogoros, MD
Richard N. Fogoros, MD, is a retired professor of medicine and board-certified in internal medicine, clinical cardiology, and clinical electrophysiology.