Cholesterol medication: types, benefits, and side effects

Millions of adults in the United States and Europe have a current diagnosis of elevated blood cholesterol levels, otherwise known as hyperlipidemia. And that number is rising (Hill, 2021).

Cholesterol is a fat-like molecule found in every cell in your body. Your body uses it to make essential substances such as hormones, steroids, cell membranes, and bile acids used for digestion. However, having high cholesterol levels can put you at increased risk of health complications, particularly heart disease (Pappan, 2021).

Fortunately, high cholesterol is very treatable with lifestyle modifications and medications that lower the amount of cholesterol in your blood (Hill, 2021).

There are many different types of cholesterol-lowering medications available. They vary in how they work, the kind of cholesterol they treat, and their potential side effects. Let’s dive in. 

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When people talk about testing your cholesterol levels, they are referring to measuring several different substances. These are (Pappan, 2021):

• Low-density lipoprotein cholesterol (LDL)

• High-density lipoprotein  cholesterol (HDL)

• Triglycerides

The current guidelines for cholesterol levels are as follows (Lee, 2020):

LDL cholesterol levels

• Optimal: less than 100 mg/ dL

• Near-optimal/above optimal:100 to 129 mg/dL

• Borderline high: 130 to 159 mg/dL

• High: 160 to 189 mg/dL

• Very high: greater than 190 mg/dL

HDL cholesterol levels

• Low: less than 40 mg/dL

• Optimal: greater than or equal to 60 mg/dL

Fasting triglyceride levels

• Normal: less than 150 mg/dL

• Mildly elevated: 150 to 499 mg/dL

• Moderately elevated: 500 to 886 mg/dL

• Severely elevated: greater than 886 mg/dL

As you can see above, you want your HDL cholesterol to be high. It's your LDL cholesterol, triglycerides, and your total amount of cholesterol that can harm your health if they are elevated for long periods.

Some common risk factors for high cholesterol levels are (Pappan, 2021):

• Genetics (also called familial hypercholesterolemia—if you have a first-degree relative with high cholesterol, you’re more likely to have it, too)

• Tobacco use

• Physical inactivity

• Obesity 

• Insufficient consumption of fruits, vegetables, and nuts/seeds

• High consumption of saturated fats

Cholesterol-lowering drugs are a safe and effective way to get your levels back to where they should be and improve your heart health.

There are several different types of cholesterol medications approved by the U.S. Food and Drug Administration (FDA). They work in different ways to lower your LDL cholesterol, total cholesterol, or triglycerides; some can even help raise HDL cholesterol. 

Your healthcare provider may prescribe one or more of these medications to help lower your risk of cardiovascular disease in combination with other diet and lifestyle changes.

Statins

Statins are the most commonly used type of medication to lower LDL cholesterol. They work by preventing the liver from making cholesterol, which lowers your overall levels. Multiple randomized controlled trials have shown that statins are highly effective, safe, and well-tolerated. They can reduce your risk of heart attack, stroke, and death. You can take them even if you already have plaque build-up in your arteries (Toth, 2019).

Common examples of statins include: 

• Atorvastatin (Lipitor)

• Fluvastatin (Lescol)

• Lovastatin (Mevacor, Altoprev)

• Pravastatin (Pravachol)

• Rosuvastatin Calcium (Crestor)

• Simvastatin (Zocor)

Fibrates

Fibrates are used to lower cholesterol levels in combination with a lipid-lowering diet. Unlike statins, fibrates not only lower triglycerides but also help raise HDL cholesterol. Fibrates work by reducing the availability of the materials used to make triglycerides in the liver. They also encourage the breakdown and clearance of LDL cholesterol from the body (Singh, 2021).

Common examples of fibrates include: 

• Gemfibrozil (Lopid)

• Fenofibrate (Antara, Lofibra, Tricor, Triglide)

• Clofibrate (Atromid-S)

PCSK9 inhibitors

PCSK9 stands for proprotein convertase subtilisin/kexin type 9, but don’t be intimidated by that complicated name. All that means is these medications work by blocking a protein called PCSK9. They make it easier for your liver to clear out LDL cholesterol from your blood. This newer class of cholesterol-lowering medication is generally well tolerated and very effective at lowering your cholesterol levels. Unfortunately, because it’s a newer drug, it comes with a hefty price tag, which is a barrier for many patients. They are also currently available as injections  (Karatasakis, 2017).

There are just two PCSK9 inhibitors on the market: 

• Alirocumab (Praluent)

• Evolocumab (Repatha)

Bile acid sequestrants

Your body uses cholesterol to make bile acids in the liver.  These bile acids move through the gallbladder and intestines to help your body digest the fats you eat. These bile acids are then recycled in the body, but bile acid sequestrants block the bile from being reabsorbed. When that happens, the bile acids get excreted from the body along with some of the undigested fat. Your liver then has to remove cholesterol from the blood to make new bile acids, reducing cholesterol levels in the process (U.S. National Library of Medicine, 2021).

Examples of bile acid sequestrants include: 

• Cholestyramine (Questran, Questran Light, Prevalite, Locholest, Locholest Light)

• Colestipol (Colestid)

• Colesevelam Hcl (WelChol)

Absorption inhibitors

Cholesterol absorption inhibitors decrease the amount of cholesterol that your small intestine absorbs from food that you eat. This helps lower how much cholesterol ends up in your blood (U.S. National Library of Medicine, 2021).

There’s just one absorption inhibitor available: 

• Ezetimibe (Zetia)

Niacin

Niacin, also known as nicotinic acid, is a form of Vitamin B3 that can help lower LDL cholesterol and triglycerides and raise HDL cholesterol. It is available over the counter, without a prescription. However, you should still talk to your healthcare provider before taking it. Large doses of niacin can cause serious side effects, which we’ll discuss below (U.S. National Library of Medicine, 2021).

All medications have a risk of some side effects. Most of the time, these are mild. Sometimes, these go away once you have been on the medicine for a little while. Other times, your healthcare provider can suggest changes to reduce the side effect. These can include changing the time of day you take it or switching you to a new medication if need be. 

Always talk to your healthcare provider about the risks and benefits of any medications or supplements that you take.

Here are the most common side effects for the different types of medications to lower cholesterol (Chhetry, 2020): 

• Statins carry a small risk of muscle pain and injury. 

• Fibrates commonly cause indigestion. They may also cause fatigue, vertigo, decreased blood cells, and elevation of some liver function tests.

• PCSK9 inhibitors can cause injection site reactions such as redness, pain, or bruising.

• Bile acid sequestrants cause stomach upset, including nausea, bloating, or cramping. They may also cause an increase in liver enzymes. 

• Ezetimibe can cause flu-like symptoms, diarrhea, joint pain, or elevation of some liver function tests. 

• Large doses of niacin can cause flushing in up to 80% of people. This flushing is uncomfortable but not dangerous. Other potential side effects include itching, nausea, increased blood sugar, increased bleeding time, and low blood pressure (when taken with other blood pressure-lowering medications).

Most people with high cholesterol won’t experience any adverse symptoms at first. This might make you think you don’t need to worry about your cholesterol levels, but this isn’t the case.

Untreated high cholesterol puts you at increased risk of significant health problems, some of which can be fatal. These complications include (Hill, 2021):

• Coronary artery disease

• Peripheral artery disease

• Heart attack

• Stroke

• Diabetes

• High blood pressure

Clinical trials have shown that if you and your provider decide to use a cholesterol-lowering medication, you can cut your risk of heart disease by as much as 20–30% (Hill, 2021).

High cholesterol is often a lifelong condition, but it is usually easily managed through a heart-healthy diet, lifestyle changes, and cholesterol medications. Talk with your healthcare provider about when to have your cholesterol levels tested and whether starting on a cholesterol-lowering medication is right for you.

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Every article on Health Guide goes through rigorous fact-checking by our team of medical reviewers. Our reviewers are trained medical professionals who ensure each article contains the most up-to-date information, and that medical details have been correctly interpreted by the writer.

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Current version

July 19, 2021

Written by

Ellyn Vohnoutka, BSN, RN

Fact checked by

Steve Silvestro, MD

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About the medical reviewer

Steve Silvestro, MD, Ro

Dr. Steve Silvestro is a board-certified pediatrician and Associate Director, Clinical Content & Education at Ro.