The most effective treatments for high cholesterol


Editorial Team


June 20, 2024

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Medical Review by Heidi Moawad, MD


  • There are various treatment options available for managing high cholesterol levels including statins, ezetimibe, PCSK9 inhibitors, and bile acid sequestrants.
  • Lifestyle modifications, such as regular exercise, stress management, and adopting a heart-healthy diet can complement medication therapy in managing cholesterol levels.
  • Regular monitoring and adjustment of medications are essential to help you meet your target cholesterol levels and minimize potential side effects and risks.
  • Side effects of cholesterol-lowering medications can include muscle aches, digestive issues, and memory loss. Rarely, serious complications such as liver damage and risk of developing type 2 diabetes can also occur. 

Worried about your high cholesterol? Here’s what you need to know about your treatment options. 

There are various medical treatments available to help combat your high cholesterol levels. We’ll discuss medication options and how simple lifestyle changes can complement medical interventions, empowering you to make informed decisions for a healthier future. Below, we’ll explore the different types of treatments available and how they work to keep you on track toward your health goals. 

Statins: what you need to know

Statins are a class of medications that are widely prescribed for the prevention of cardiovascular diseases such as heart attack and stroke. They are used to lower the levels of low-density lipoprotein, or LDL, cholesterol which is often referred to as ‘bad’ cholesterol in the blood. 

Types of statins include:

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

With statin therapy, clinical trials have shown that LDL cholesterol levels can be reduced by up to 60%, depending on the dosage and type of statin. In both primary and secondary prevention, statins have been shown to significantly reduce the risk of cardiovascular events such as heart attack and stroke. They are one of the best-studied classes of medications and are the most effective drug for the prevention of coronary heart disease. 

Common side effects of statins include:

  • Muscle aches and tiredness
  • Digestive issues
  • Headache

Other less common, but more serious side effects that physician monitor patients on statin for include: 

  • Liver or kidney damage
  • Increase in blood sugar levels
  • Type 2 diabetes
  • Memory loss

Rarely, muscle breakdown (rhabdomyolysis) and liver damage can occur, however, the potential benefit of the treatment  often outweighs the risk for most people. You may want to discuss how to monitor and detect any potential side effects with your healthcare provider.

Statin dosage depends on a variety of factors, such as:

  • Patient’s age
  • Cholesterol levels
  • Medical history
  • Other risk factors

Pregnant and breastfeeding women are generally not recommended for statin therapy due to potential risks to the fetus. 

How statins work

Statins inhibit an enzyme called HMG-CoA reductase, which plays a major part in the production of cholesterol in the liver. At the same time, statins can modestly increase the amount of high-density lipoprotein (HDL) cholesterol, or “good” cholesterol, while also decreasing the levels of triglycerides in the blood. 

Certain medications can negatively interact with statins, so it is important to keep your doctor updated with all of your current prescriptions, supplements, and herbal remedies before you start on your statin journey. 

When combined with a healthy lifestyle, statins can reduce the risks associated with cardiovascular disease and help keep you on the path to improve your overall health. 

How Ezetimibe can help improve your cardiac health

Ezetimibe is a cholesterol absorption inhibitor. Research shows that, in combination with statins, ezetimbe can help some patients control LDL levels and improve their cardiac outcomes. Your healthcare provider may also prescribe ezetimbe if you have a statin intolerance.

PCSK9 inhibitors and how they can help you manage your cholesterol

PCSK9 inhibitors are a type of medication used for managing your cholesterol levels, particularly “bad” low-density lipoprotein cholesterol. PCSK9 (proprotein convertase subtilisin/kexin type 9) is an enzyme produced in the liver; its main role is to regulate the number of LDL receptors on the surface of liver cells. 

How PCSK9 inhibitors work

  1. They bind to LDL receptors on the surface of liver cells and mark them for destruction. This leads to the reduction of the liver’s ability to remove LDL cholesterol from the bloodstream. 
  2. The action of PCSK9 enzymes is blocked, which prevents them from binding to LDL receptors. This allows for more receptors to remain on the surface of the liver cells. 
  3. With more LDL receptors available, the liver can now work to remove more “bad” cholesterol from the bloodstream, which in turn leads to lower levels of LDL cholesterol circulating in the blood. 

Bile acid sequestrants as a cholesterol treatment option

When ingested orally, bile acid sequestrants bind to bile acids in the intestines. These positively charged resins attract the negatively charged bile acids and form complexes that are too large to be absorbed through the intestinal wall and are instead excreted from the body. 

Examples of common bile acid sequestrants include:

  • Cholestyramine
  • Colestipol
  • Colesevelam

How bile acid sequestrants work

As bile acids bind to the sequestrants and are excreted, the amount of bile acids available for re-absorption decreases. This reduction signals to the liver to begin converting cholesterol into bile acid, which removes cholesterol from the bloodstream. By interrupting the circulation of bile acids and increasing the use of cholesterol for bile acid synthesis, bile acid sequestrants can effectively lower “bad” cholesterol levels in the bloodstream, reducing the risk of heart attack and stroke. 

Potential side effects can include:

  • Constipation
  • Bloating
  • Abdominal discomfort 
  • Flatulence
  • Nausea
  • Rarely, gallstones or biliary obstruction

Sequestrants have also been known to interfere with the absorption of fat-soluble vitamins A, D, E, and K, which can lead to deficiencies if not supplemented. Be sure to check in with your healthcare provider if you are pregnant or breastfeeding before starting bile acid sequestrants. 

Some patients may dislike the taste or texture of the sequestrants, which are administered orally as a powder mixed with water. Lipid levels should be assessed regularly to prevent risks from side effects. 

Can combination therapies help you reach your target levels over monotherapy alone?

To achieve optimal levels of LDL cholesterol, combination therapies of different classes of cholesterol-lowering medications can be used, especially if you haven’t hit your target levels with monotherapy.

Different ways they work

  1. Combining a statin, which limits cholesterol synthesis in the liver, with a bile acid sequestrant can result in an increase of LDL-lowering effects. 
  2. Combination therapies can also target triglycerides and high-density lipoprotein (“good”) cholesterol levels. 
  3. Combining a statin with omega-3 fatty acids can work to reduce triglyceride levels and improve HDL cholesterol levels, especially in people with dyslipidemia. 

If you are at high cardiovascular risk, combination therapies for cholesterol treatment can help you reach your target levels, when compared to monotherapy alone. If you have a family history of high cholesterol or a cholesterol disorder such as heterozygous familial hypercholesterolemia, combination therapies offer a valuable approach for optimal limid management.

Lifestyle modifications to aid medication therapy

It is important to consider changes to your lifestyle while taking cholesterol-lowering medication. In conjunction with medication, taking charge of your routine can positively affect changes to your cholesterol levels.

Examples of lifestyle modifications that impact cholesterol include: 

Adopting a heart-healthy diet: Adding in fiber-rich foods such as fruits, vegetables, whole grains and legumes can help lower “bad” cholesterol. Limiting your intake of saturated and trans-fats, commonly found in red meat, full-fat dairy, and processed foods, and incorporating healthy fats like avocados and nuts also work to maintain healthy cholesterol profiles. Limiting alcohol intake and quitting smoking also have positive benefits for cardiovascular health.

Physical activity: Regular exercise is essential, not just for managing cholesterol levels, but for overall cardiovascular health. Exercise helps raise HDL cholesterol levels while lowering LDL cholesterol in the body. Aim for at least 150 minutes of moderate activity, with muscle-strengthening routines on two or more days per week. 

Stress management: Identifying stressors and introducing stress-reduction techniques into your routine can support your overall well-being. Practicing mindfulness and deep breathing exercises, and spending time in nature can encourage a healthier cardiovascular system.  

In addition to medication, small lifestyle changes can have a large impact on your cholesterol levels. Monitoring blood pressure and weight are simple at-home checks that can keep you on track for your cardiovascular goals. Scheduling regular check-ups with healthcare professionals and being compliant with prescriptions will go a long way in improving your heart health. 

Monitoring & adjusting medications

Certain medications and dosages may need to be adjusted if you aren’t meeting your target cholesterol levels. Risk factors and medication complications are taken into consideration so it is important to inform your doctor of any and all medications, supplements, and lifestyle changes and habits. 

It is important to keep compliant with medications and to take them as prescribed. If you have any questions about your treatment plan and the medications prescribed, be sure to ask your healthcare professional. Regular check-ups and addressing concerns also play a part in your overall health.

Weighing the potential risks

Managing cholesterol levels is made easier thanks to a variety of treatment options. However, it is important to note that these treatments are not without their risks. 

It is important to be mindful of the risks associated with cholesterol medications but to also weigh the risks against the benefits. Evaluating treatment goals and working with your healthcare provider to reach those goals will go a long way in minimizing the negative effects of cholesterol medication.

Get started on your journey to healthier cholesterol levels

We’ve discussed a variety of options for treatments to keep cholesterol levels in a healthy, manageable range. From statins and Ezetimibe, to PCSK9 inhibitors and bile acid sequestrants, there are options to help you reduce your risk of stroke and heart attack. Whether using these medications alone or in conjunction with one another, a healthcare professional can assess your needs and work with you to meet your goals for better health. 

Learn about what cholesterol lowering treatments are available at Lemonaid Health. 

Lipitor® is a registered trademark of Upjohn Manufacturing Ireland Unlimited Company, a Viatris Company. 

Crestor® is a registered trademark of the AstraZeneca group of companies. 

Zocor® is a registered trademark of MERCK & CO., Inc. 

Pravachol® is a registered trademark of Bristol-Myers Squibb Company. 

Mevacor® is a registered trademark of Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc. 

Altoprev® is a registered trademark of Covis Pharma GmbH. 

Lescol® is a registered trademark of Novartis Pharmaceuticals Corporation. 

Livalo® is a registered trademark of Kowa Pharmaceuticals America, Inc.

  1. Feingold KR, Anawalt B, Blackman MR, et al. (updated 2024, February 12), Cholesterol Lowering Drugs. National Library of Medicine. Accessed April 24, 2024 at
  2. Hajar R. (2019, April – June). PCSK 9 Inhibitors: A Short History and a New Era of Lipid-lowering Therapy. National Library of Medicine. Accessed April 25, 2024 at
  3. Metkus T S. (2022, Feb 23). Bile acid sequestrants for cholesterol. MedlinePlus. Accessed April 25, 2024 at
  4. Byambaa Enkhmaa, Prasanth Surampudi, Erdembileg Anuurad, & Lars Berglund. (2018, September 11). Lifestyle Changes: Effect of Diet, Exercise, Functional Food, and Obesity Treatment on Lipids and Lipoproteins.;, Inc. Accessed May 10, 2024 at
  5. Garg, P., Ayushi Mendiratta, Banga, A., Carolina, A., Victoria, P., Balakrishnan Kamaraj, Qasba, R. K., Bansal, V., Jyothi Thimmapuram, Pargament, R., & Kashyap, R. (2024). Effect of breathing exercises on blood pressure and heart rate: A systematic review and meta-analysis. International Journal of Cardiology Cardiovascular Risk and Prevention, 20, 200232–200232. Accessed May 10, 2024 at
  6. Grundy, S. M., & Feingold, K. R. (2022, May 28). Guidelines for the management of high blood cholesterol (K. R. Feingold, B. Anawalt, A. Boyce, G. Chrousos, W. W. de Herder, K. Dungan, A. Grossman, J. M. Hershman, H. J. Hofland, G. Kaltsas, C. Koch, P. Kopp, M. Korbonits, R. McLachlan, J. E. Morley, M. New, J. Purnell, F. Singer, C. A. Stratakis, & D. L. Trence, Eds.). PubMed;, Inc. Accessed May 10, 2024 at
  7. Wang C, Wang F, Cao Q, Li Z, Huang L, Chen S. (2018, September 4). Effect and safety of combination lipid‐lowering therapies based on statin treatment versus statin monotherapies on patients with high risk of cardiovascular events. National Library of Medicine. Accessed April 25, 2024
  8. Thomas S. Metkus, MD. (2024, Feb 27). How to take statins. MedlinePlus. Accessed April 25, 2024 at
  9. Sizar O, Khare S, Patel P, et al. Statin Medications. [Updated 2024 Feb 29]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2024 Jan-. Available from:
  10. Pradhan, A., Bhandari, M., & Sethi, R. (2020). Ezetimibe and Improving Cardiovascular Outcomes: Current Evidence and Perspectives. Cardiology research and practice, 2020, 9815016.


Editorial Team


June 20, 2024

This article is for informational purposes only and does not constitute medical advice. The information contained herein is not a substitute for and should never be relied upon for professional medical advice. Always talk to your doctor about the risks and benefits of any treatment or medication.