How do I choose my cholesterol medication?

How can you control your cholesterol levels?

For some people, lifestyle changes, such as a healthier diet and more exercise, may prevent or treat unhealthy cholesterol levels. For others with high cholesterol, medication may also be needed.

Work with your doctor to develop a treatment plan that works for you. If you need to take medication, be sure to take it as prescribed. The potential benefits to your health are worth making these medications part of your daily routine.

Cholesterol-lowering medications

Various medications can lower blood cholesterol levels.

Statins are recommended for most patients and are directly associated with a reduced risk of heart attack or stroke. In most cases, statins continue to provide the most effective lipid-lowering treatment.

The guidelines recommend that anyone in these groups discuss the risks and benefits of statin therapy with their physician at

• Adults with a history of cardiovascular disease, including stroke, caused by atherosclerosis
• Those with LDL-C level of greater than 190 mg/dL
• Adults 40-75 years with diabetes
• Adults 40-75 years with LDL-C level of 70-189 mg/dL and a 5% to 19.9% 10-year risk of developing cardiovascular disease from atherosclerosis and risk-enhancing factors
• Adults 40-75 years with LDL-C level of 70-189 mg/dL and a 20% or greater 10-year risk of developing cardiovascular disease from atherosclerosis

Some people who don't fall into these categories may also benefit from statin therapy.

It's important to talk to your healthcare professional about your 10-year or lifetime risk. They will assess your risk factors to determine your level of risk and work with you to choose the best treatment.

This section summarizes some of the major types of commonly used cardiovascular drugs. We have included generic names and major trade names to help you identify the medications you may be taking. Please understand that the American Heart Association does not recommend or endorse any particular product. If your prescription medication is not in this list, your doctor and pharmacist are your best sources of information. It is important to discuss all medications you take with your doctor and to understand their expected effects and possible side effects. Never stop taking a medication or change the dose (or frequency) without first consulting your doctor. Some cholesterol-lowering medications may interact with grapefruit, grapefruit juice, pomegranate, and pomegranate juice. Please discuss any potential risks with your doctor.

Statins

This class of drugs, also known as HMG CoA reductase inhibitors, works in the liver to prevent cholesterol from forming. This reduces the amount of cholesterol circulating in the blood. Statins are most effective at lowering LDL (bad) cholesterol. They also help lower triglycerides (blood fats) and raise HDL (good) cholesterol.

Talk to your doctor about the possible side effects before starting statins. Most side effects are mild and go away as your body adjusts. Muscle problems and liver abnormalities are rare, but your doctor may order regular liver function tests. Women who are pregnant or people who have active or chronic liver disease should not take statins. 

Statins available in the U.S. include:

• Atorvastatin (Lipitor®)
• Fluvastatin (Lescol®)
• Lovastatin (Mevacor®, Altoprev™)
• Pravastatin (Pravachol®)
• Rosuvastatin Calcium (Crestor®)
• Simvastatin (Zocor®)

If statins don’t help you enough, or if you develop side effects, your doctor may recommend different medications.

Statins are also found in the combination medications Caduet® (atorvastatin + amlodipine) and Vytorin™ (simvastatin + ezetimibe).

If you have CVD and are already taking the highest tolerated statin and your LDL-C is still 70 or above, one or more of the following medicines may be prescribed. They all can be taken in combination with a statin.

Ezetimibe (cholesterol absorption inhibitors)

Prevents cholesterol from being absorbed in the intestine. It’s the most commonly used non-statin agent.

Bile Acid Sequestrants

Also called bile acid-binding agents, cause the intestine to get rid of more cholesterol. 

Those available in the U.S. include:

• Cholestyramine (Questran®, Questran® Light, Prevalite®, Locholest®, Locholest® Light)
• Colestipol (Colestid®)
• Colesevelam Hcl (WelChol®)

PCSK9 inhibitors

PCSK9 inhibitors are powerful LDL-lowering drugs. They bind to and inactivate a protein on cells found in the liver to lower LDL (bad) cholesterol. Some names are alirocumab and evolocumab.

Adenosine triphosphate-citrate lyase (ACL) inhibitors*

ACL inhibitors work in the liver to block the production of cholesterol. They are used in combination with lifestyle changes and statins to further decrease LDL cholesterol in adults with familial heterozygous hypercholesterolemia and patients with heart disease that need to further lower their LDL.

• Bempedoic acid (Nexletol)
• Bempedoic acid and ezetimibe (Nexlizet)

The following triglyceride-lowering drugs have mild LDL-lowering action, but data doesn’t support their use as an add on to statins.

Fibrates

Fibrates are especially good for lowering triglyceride (blood fat) levels and have a mild LDL-lowering action. 

Fibrates available in the U.S. include:

• Gemfibrozil (Lopid®)
• Fenofibrate (Antara®, Lofibra®, Tricor®, and Triglide™)
• Clofibrate (Atromid-S)

Niacin (nicotinic acid)

Niacin is a B vitamin that limits the production of blood fats in the liver. Take this only if your doctor has prescribed it. It lowers triglycerides and has mild LDL-lowering action.

Niacin side effects may include flushing, itching and upset stomach. Your liver functions may be closely monitored because niacin can cause toxicity. Nonprescription immediate-release forms of niacin usually have the most side effects, especially at higher doses. Niacin is used cautiously in diabetic patients because it can raise blood sugar levels.

Niacin comes in prescription form and as a dietary supplement. Dietary supplement niacin must not be used as a substitute for prescription niacin because of potentially serious side effects. Dietary supplement niacin is not regulated by the Food and Drug Administration and may contain widely variable amounts of niacin – from none to much more than the label states. The amount of niacin may even vary from lot to lot of the same dietary supplement brand. Consult your doctor before starting any niacin therapy.

Omega-3 Fatty Acid Ethyl Esters

These are derived from fish oils that are chemically changed and purified. They’re used in tandem with dietary changes, to help people with high triglyceride levels.

Omega-3 Fatty Acid Ethyl Esters available in the U.S. include:

• Lovaza®
• Vascepa™
• Epanova®
• Omtryg®

Marine-Derived Omega-3 Polyunsaturated Fatty Acids (PUFA)

Commonly referred to as omega-3 fish oils or omega-3 fatty acids, are used in large doses to lower high blood triglyceride levels. They help decrease triglyceride secretion and clear triglycerides. The amount of marine-derived omega-3 PUFAs needed to significantly lower triglyceride (2 to 4 g) is hard to get from a daily diet alone, so supplementing with capsules may be needed.

Use these supplements only under a doctor’s direction and care, because large doses may cause serious side effects. These can include increased bleeding, hemorrhagic stroke and reduced blood sugar control in diabetics. Negative interactions with other medications, herbal preparations and nutritional supplements are also possible. People with allergies to fish, shellfish or both may have a severe adverse reaction to using these supplements.

If diet and exercise aren't enough, you may also need to take medication to help lower your cholesterol.

Choose your cholesterol medication

A healthy lifestyle is the first line of defense against high cholesterol. But sometimes diet and exercise aren't enough. You may also need to take cholesterol medications to help.

• Lower low-density lipoprotein (LDL) cholesterol, the "bad" cholesterol that increases the risk of heart disease
• Lower triglycerides, a type of fat in the blood that also increases the risk of heart disease
• Increase your high-density lipoprotein (HDL) cholesterol, the "good" cholesterol that can prevent heart disease

Your doctor may recommend a single medication or a combination of cholesterol medications. The following outlines the advantages and disadvantages of common classes of cholesterol medications.

Drug class	Benefits	Possible side effects
Statins Atorvastatin (Lipitor) Fluvastatin (Lescol XL) Lovastatin (Altoprev) Pitavastatin (Livalo) Pravastatin (Pravachol) Rosuvastatin (Crestor) Simvastatin (Zocor)	Decrease LDL and triglycerides; slightly increase HDL	Muscle pain, increased blood sugar levels, constipation, nausea, diarrhea, stomach pain, cramps, elevation of liver enzymes
Cholesterol absorption inhibitor Ezetimibe (Zetia)	Decreases LDL; slightly decreases triglycerides; slightly increases HDL	Stomach pain, diarrhea, fatigue, muscle soreness; avoid during pregnancy and lactation
PCSK9 inhibitors Alirocumab (Praluent) Evolocumab (Repatha)	Decrease LDL; usually reserved for people who have a genetic condition that causes very high LDL levels or people with heart disease who cannot tolerate statins or other cholesterol lowering drugs	Itching, swelling, pain or bruising at injection site
Citrate lyase inhibitors Bempedoic acid (Nexletol) Bempedoic acid-ezetimibe (Nexlizet)	Decrease LDL	Muscle spasms and joint pain, including acute gout
Bile acid sequestrants Cholestyramine (Prevalite) Colesevelam (Welchol) Colestipol (Colestid)	Decrease LDL; may slightly increase HDL	Constipation, bloating, nausea, gas, heartburn
Combination cholesterol absorption inhibitor and statin Ezetimibe-simvastatin (Vytorin)	Decreases LDL and triglycerides; increases HDL	Stomach pain, fatigue, gas, constipation, abdominal pain, cramps, muscle soreness, pain and weakness
Combination calcium channel blocker and statin Amlodipine-atorvastatin (Caduet)	The statin component decreases LDL and triglycerides; the calcium channel blocker lowers blood pressure	Facial and neck flushing, dizziness, heart palpitations, muscle soreness and pain, increased blood sugar levels, constipation, nausea, diarrhea, stomach pain, cramps, elevation of liver enzymes
Fibrates Fenofibrate (Antara, Lipofen, others) Gemfibrozil (Lopid)	Decrease triglycerides; modestly decrease LDL; increase HDL	Nausea, stomach pain, muscle pain
Niacin Prescription niacin (Niacor, Niaspan)	Decreases LDL and triglycerides; increases HDL	Facial and neck flushing, itching, stomach upset, increase in blood sugar
Omega-3 fatty acids Prescription versions include Lovaza, Omacor and Vascepa	Decrease triglycerides; may increase HDL	Belching, fishy taste, indigestion; may increase risk of bleeding

In many people, muscle pain commonly associated with statins may not actually be caused by the drug. In studies in which participants did not know whether they were taking a statin or a placebo, muscle pain was a common complaint in both groups. It seems that the anticipation of side effects makes it more likely.
Most cholesterol medications can lower cholesterol with few side effects, but the effects vary from person to person. It is also important to follow a healthy diet and get enough exercise. Cholesterol medications and lifestyle choices can work together to help reduce the risk of heart attack and stroke.

References：

1. Statin - Wikipedia

2. Atorvastatin - Wikipedia

See also:

1. Cholesterol care