Prescription Drugs for Cholesterol and Triglycerides

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From statins like Lipitor (atorvastatin) to PCSK9 inhibitors like Repatha (evolocumab) to niacin and beyond, several kinds of medications are regularly prescribed to treat high cholesterol and triglyceride levels.

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.

Man sitting on couch taking medication
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Keeping your lipid—cholesterol and triglyceride—levels from getting too high is an important part of preventing atherosclerosis, coronary artery disease (CAD), stroke, and peripheral artery disease.

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.

Statins

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

Experts agree that some of the body’s cholesterol is produced by the body rather than ingested, so inhibiting this enzyme lowers cholesterol through a different mechanism than 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:

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, which are administered once or twice per month by injection and can be used in combination with other lipid-lowering medications, can drive LDL cholesterol to very low levels. They are often prescribed for those who have familial hypercholesterolemia or LDL cholesterol levels that remain very elevated despite treatment with statins.

The two PCSK9 inhibitors available, approved by the Food and Drug Administration (FDA) in late 2015, are:

  • Praluent (alirocumab)
  • Repatha (evolocumab)

Ezetimibe

Ezetimibe reduces the absorption of cholesterol from the intestines, causing the liver to get more of the cholesterol it needs 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 who are 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 their usefulness. Clinical studies have failed 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, however, several randomized trials have failed to show any improvement in clinical outcomes with fibrates. They are mainly used to treat severe hypertriglyceridemia.

Fibrates include:

  • Antara (gemfibrozil)
  • Lopid (fenofibrate)

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

A Word From Verywell

Several classes of drugs have been shown to have a favorable effect on cholesterol and triglyceride levels.

In 2018, the American College of Cardiology published a set of guidelines on treating cholesterol, with recommendations regarding screening, a heart-healthy lifestyle, and statin and non-statin drugs.

Speak to your healthcare provider about your case and the particular course of treatment that is right for you.

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6 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.
  1. Hla D, Jones R, Blumenthal R, Martin SS. Assessing severity of statin side effects: fact versus fiction. American College of Cardiology.

  2. American Heart Association. Familial hypercholesterolemia (FH). Updated November 9, 2020.

  3. Zimmerman MP. How do PCSK9 inhibitors stack up to statins for low-density lipoprotein cholesterol control? Am Health Drug Benefits. 2015;8(8):436-442.

  4. Cannon CP, Blazing MA, Giugliano RP, et al. Ezetimibe added to statin therapy after acute coronary syndromes. N Engl J Med. 2015;372(25):2387-2397. doi:10.1056/NEJMoa1410489

  5. American Heart Association. Cholesterol medications. Updated November 11, 2020.

  6. Feingold KR, Grunfeld C. Triglyceride lowering drugs. Endotext. Updated April 1, 2021.

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