Can't Tolerate Statin?

Cholesterol is good for us because it helps with the production of estrogen, testosterone, cortisol and helps us with repairing inflammation. Our body naturally creates just enough cholesterol for our body distribution, however, if you eat  food with high saturated or trans fat, it can cause an excess amount of cholesterol in your body. An excess amount of cholesterol can cause plaque build-up in our arteries making it harder for blood to pump through our body. This can lead to heart diseases like hypertension or coronary artery disease (CAD).

Clinically, some medications have been used for years to help individuals lower their cholesterol levels, specifically their LDL (low-density lipoprotein). One of the most common medications would be statins. Statins stop the production of cholesterol by blocking the enzyme that creates cholesterol. This will lower the amount of cholesterol available in our bloodstream (Bonetti, P. O., Lerman, L. O., Napoli, C., & Lerman, A., 2003). However, over the past few years, many patients have noticed bad side effects from taking statins. Some of the common side effects are myalgia (muscle pain and aches). Most patients would endorse mild discomfort that does not affect daily activities. However, some patients would have moderate symptoms making it impossible to tolerate (Mayo Clinic, 2022). 

Our liver makes a protein called proprotein convertase subtilisin/kexin type 9 (PSCK9). This protein is used to help regulate how many LDL receptors we have and is involved in the breakdown of these receptors. These receptors would attach to LDL cholesterol that is then carried into our lives where the liver breaks it down and gets rid of it. PCSK9 inhibitors are used to block that protein from breaking the LDL receptors down therefore there will be more receptors on the outside of cells and as a result reduce LDL cholesterol (Dadu, R. T., & Ballantyne, C. M., 2014). Currently one of the most common PCSK9 inhibitors medications is Repatha. Patients would take an injection every two weeks. Clinically, it has been shown to lower LDL by an average of 55% to 72% in just a few months (Rosenson, R. S., Hegele, R. A., Fazio, S., & Cannon, C. P., 2018). I believe that this is a good alternative for patients who can not tolerate statins with fewer side effects. However, it could be expensive and many insurances won’t approve it so hopefully one day it becomes genetic and more affordable for patients. 

Bonetti, P. O., Lerman, L. O., Napoli, C., & Lerman, A. (2003). Statin effects beyond lipid lowering—are they clinically relevant?. European heart journal, 24(3), 225-248.

Dadu, R. T., & Ballantyne, C. M. (2014). Lipid lowering with PCSK9 inhibitors. Nature Reviews Cardiology, 11(10), 563-575.

Mayo Foundation for Medical Education and Research. (2022, September 2). Statin side effects: Weigh the benefits and risks. Mayo Clinic. Retrieved November 27, 2022, from https://www.mayoclinic.org/diseases-conditions/high-blood-cholesterol/in-depth/statin-side-effects/art-20046013 

Rosenson, R. S., Hegele, R. A., Fazio, S., & Cannon, C. P. (2018). The evolving future of PCSK9 inhibitors. Journal of the American College of Cardiology, 72(3), 314-329.