Prescription Drugs for Cholesterol and Triglycerides

From statins like Lipitor (atorvastatin) to PCSK9 inhibitors like Repatha (evolocumab) to niacin and beyond, there are several kinds of medications that are regularly prescribed for treating high cholesterol and triglyceride levels. Which is most appropriate for you depends on several factors, but it's likely that your doctor will want you to begin taking prescription medication if diet and exercise are not enough to lower your levels, or your risk for cardiovascular disease is particularly elevated.

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.

It can help to learn about all of the possible prescription options your doctor might suggest so you can take an active role in your treatment discussions and decisions.

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:

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

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 the 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 that are available, which were approved by the U.S. Food and Drug Administration (FDA) in late 2015, are:

• Praluent (alirocumab)
• Repatha (evolocumab)

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 levels are reduced.

Clinical trials with ezetimibe have been fairly disappointing, and the drug is not used very often in clinical practice. It is used 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 prevent the reabsorption of cholesterol-containing bile acids from the intestine. This causes the liver to remove more cholesterol from the 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 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.

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

Fibrates include:

• Antara (gemfibrozil)
• Lopid (fenofibrate)

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

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 doctor about your case and why they are recommending a particular course of treatment.