David Leonardi, M.D. ABAAM, CNS

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Muscle Side Effects of Statins And How to Avoid Them

David Leonardi, M.D., ABAAM, CNS

How much information would you like?

Choose:

Section A: Just the bullet points with scientific references

Section B: A detailed explanation with references

Section A. Bullet Points:

  • Like every medication ever invented, statins have potential side effects. Chief among these are muscle problems, including pain, aching, soreness, cramps or even muscle tremors1,2,3.
  • This condition boils down to depletion of energy production and energy supply within muscle cells1,2,3.
  • This statin-related reduced energy supply is caused by depletion of two important nutrients: Coenzyme Q104,5,6,7 and creatine28,29.
  • Supplementing CoQ10 has been shown effective against statin-related muscle problems in some studies8,9,10 but not in others11,12. But either way, if you take a statin you MUST supplement CoQ10 because statins deplete the body’s levels of CoQ10. Low levels of CoQ10 have been linked to a debilitating and dangerous condition called congestive heart failure14,15, which, in many people, can be reversed by CoQ10 supplementation17,18,19,20.
  • Statins also reduce the transport of energy-critical creatine into muscle cells29.
  • Supplementing creatine reversed statin-related muscle problems in eight of ten people who were previously intolerant of a statin due to pain30.

It is for the above reasons that we developed Statin Sidekick™. Statin Sidekick is a proprietary blend of CoQ10 and a specially buffered creatine in the optimum ratio based on published evidence on statin side effects and our own research at the Leonardi Institute. To read a brief paragraph about Statin Sidekick, click here.

 

Section B. For those who want to understand all the science and see all the evidence.

Table of Contents

Pain (Myalgia) and Dysfunction (Myopathy)

Myopathy as related to CoQ10

Myopathy as related to Creatine

The Advantage of Buffered Creatine

The Simplest and Most Economical Solution

 

Pain (Myalgia) and Dysfunction (Myopathy)

At the same time, statins can also rob us of quality of life by way of side effects. By far, the most common side effects of statins are those occurring in muscle, including pain, aching, soreness, cramps or even muscle tremors1,2,3. Doctors call these problems by two names: myopathy (muscle dysfunction) or myalgia (muscle pain). Technically, the term myopathy refers to a more severe condition than muscle pain wherein the serum level of a muscle enzyme called creatine kinase is elevated ten times above its upper normal limit4. But for purposes of this article its best we just use myopathy to mean muscle dysfunction, which could be pain, soreness, aching, weakness, cramps or tremor. Because many people are unaware that statins can cause these problems, they might go to great lengths seeking help for muscle problems such as back or neck pain before realizing that their statin is the culprit. And the converse can be true: one might implicate a statin without considering other causes such as a joint problem, exercise-induced pain, or an injury. So it is prudent to consider all possibilities. Statin-related discomfort is most commonly felt in central muscles of the body such as the low back, neck, buttocks or thighs, but can be felt in any muscle. Over the past 20 years, many studies have been done to determine the source of statin-induced myopathy. Much has been learned. This condition boils down to depletion of energy production and energy supply within muscle cells1,2,3. With inadequate energy to meet demands, muscle cells not only perform poorly but also become painful.

This statin-related reduced energy supply is caused by depletion of two important nutrients: Coenzyme Q104,5,6,7 and creatine28,29. Below is what we know about this relationship thus far.

 

Myopathy as related to CoQ10

All cells, including muscle cells,  contain energy  factories called mitochondria. It is in the mitochondria where sugar and fats are burned to produce energy in the form of adenosine triphosphate (ATP). For example, when sugar is broken down, a compound called NADH is created. High-energy electrons are then passed from NADH down an assembly line of proteins called the electron transport chain. At each step, energy is extracted from the electrons. One of the key proteins involved in this energy production is Coenzyme Q (also known as CoQ10). Statins reduce the body’s production of CoQ105,6,7,8. Statin users have up to 40% lower CoQ10 levels in the blood  compared to non-users8. The reason is that Co Q 10 is made in the body by the same enzyme that makes cholesterol (HMG CoA reductase) and statins are specifically designed to block this enzyme4,5,6,7. Since CoQ10 is a critical link in energy production in muscle cells and statins deplete us of CoQ10, it’s no surprise that statins would cause muscle dysfunction. The obvious solution, then, would simply be to supplement CoQ10. However, it’s not that simple. Studies on the use of CoQ10 for the treatment of statin myopathy are mixed. That is, some have shown significant benefit in relieving statin-associated pain9,10,11 and others studies show no benefit12,13. That’s because there are genetic differences among us in regard to exactly where in our biochemistry statins invoke their energy interference within the muscle cell14. Some of us have susceptibility in one aspect of our chemistry and other’s of us in another aspect. That’s why creatine and vitamin D3 are so important and will be discussed below. But even if you find that CoQ10 doesn’t resolve your statin muscle pain, you should be aware of two other reasons to supplement it. First, CoQ10 depletion can cause muscle weakness or discomfort mild enough to be beneath your radar. In other words, you may be weaker than you should be without even realizing it. Second, CoQ10 is critically important for normal function of heart muscle. Low levels of CoQ10 have been linked to a debilitating and dangerous condition called congestive heart failure due to reduced energy production in heart muscle15,16 and CoQ10 has been shown to correct it17,18,19,20. Finally, even in people not using statins, CoQ10 levels decline with age and even that normal depletion compromises heart function21,22. You don’t want to go through life with CoQ10 depletion.

 

Myopathy as Related to Creatine

As I’ve stated, there is another nutrient important for energy supply in muscle – creatine. Creatine is responsible for a major supply chain of energy production in muscle cells by a completely different chemical pathway than CoQ1023,24. All cells, including muscle cells, ultimately use ATP (created from glucose using the electron transport chain) as an energy source. A muscle cell has enough ATP to sustain contraction for only about 6 seconds. At that point, all the stored ATP (adenosine tri-phosphate) is depleted into low-energy adenosine di-phosphate (ADP). High-energy phosphate molecules are desperately needed to turn ADP back into ATP to prevent immediate and complete muscle failure. Of course, our muscle cells don’t fail after 6 seconds of contraction, so we know that our muscle cells can obtain those phosphate groups to restore ATP. And the source of that phosphate group is creatine23,24. Scientists call this supply line the creatine-phosphate shuttle. When creatine enters the cell it collects a phosphate molecule via an enzyme called creatine kinase (CK) and can transfer (shuttle) that phosphate to ADP when needed to form ATP. You can find more about this on www.Wikipedia.org  or your favorite search engine. In fact, elite athletes have been supplementing creatine for decades because of studies showing improved muscle strength and athletic performance25,26,27,28.

Now, there is strong evidence that in addition to depleting CoQ10, statins block the transport of creatine from the blood stream into the muscle cell29. This is yet another hit to muscle cell energy. Less creatine within muscle cells means poor function of the creatine phosphate shuttle and less formation of ATP. How about the use of creatine to prevent statin-related muscle pain? Does it work? Only one clinical trial of creatine for this purpose has been performed as of this writing (July, 2013). It was done on patients with statin myopathy so severe that they literally could not tolerate any statin due to muscle pain. They had elected to quit taking statins as a result, despite losing the benefit of reduced risk of heart attack. The pain was just too unbearable. When these statin intolerant patients were treated with creatine, 80% of them became fully tolerant of statins and were able to resume their statin therapy with no muscle pain30.

 

The Advantage of Buffered Creatine

Now, there is an important caveat here. Not all creatine is created equal. When creatine is consumed, before it’s absorbed into our system, much of it is immediately transformed to creatinine (note the extra “in” syllable in creatinine), a waste product of muscle that, when it accumulates, is poisonous. The names are very similar as are their chemical structures but they have a very different effects on the body. Creatine is the energy supply link in muscle cells and creatinine is a waste product that is poisonous at higher levels. When you take standard creatine, such as creatine monohydrate, you lose some of the benefit of the creatine because of its rapid conversion to creatinine and additional strain is placed on the kidneys, required to eliminate that extra creatinine. At the Leonardi Institute, we did a pilot study comparing the effect of standard creatine to a special buffered creatine, designed for maximal absorption into the body with little or no conversion to creatinine. We looked at the blood levels of creatine and creatinine before and after taking standard and buffered creatine. We compared the affect of a daily dose of 9 grams of standard creatine monohydrate to only 3 grams of buffered creatine on blood levels of creatine and creatinine in a crossover trial with a washout period in between. After a week of supplementation, here is what we found.

Creatine Type
Percent increase in
blood creatine per gram ingested per day
Percent increase in
blood creatinine per gram ingested per day
Ordinary14-3.2
Buffered52-8.5

Per gram of product ingested each day, ordinary creatine monohydrate increased the blood creatine level by 14% while the buffered creatine increased it by 52%, a 3.6-fold difference. Meanwhile, gram for gram, neither the ordinary creatine monohydrate nor the buffered creatine increased the poisonous blood creatinine level but it dropped by more than double, gram for gram of creatine intake, using the buffered creatine (i.e. buffered creatine had a far more favorable impact). This would imply that, long term, the buffered creatine would be safer.

Clearly, the buffered creatine does more at a lower dose to bring creatine to the muscle cell via the blood stream with no increase in blood level of the potentially harmful creatinine. And there is a very practical advantage: two capsules of buffered creatine can replace seven capsules (or a heaping teaspoon) of creatine monohydrate.

Myopathy as Related to Vitamin D Deficiency

Very low levels of vitamin D (even in the absence of statin use) are associated with muscle dysfunction and muscle pain31,32,33. Low levels of vitamin D are common throughout the world, including in developed countries and certainly including the U.S.34,35,36.  My best estimate of the prevalence of vitamin D insufficiency (levels below 30 ng/ml) in the U.S. is about 50% of the population! What relationship does vitamin D have to statin-related myopathy? There are studies showing a correlation between low vitamin D levels and statin-associated muscle pain37,38 and others showing no such association39,40. Therefore, low vitamin D cannot be the simple answer to statin-associated muscle problems for everyone. However, if you take those with statin-associated muscle pain and a low level of vitamin D, stop their statin and boost the level of vitamin D, most will be able to restart their statin with no pain41,42. Therefore, a low vitamin D status may be the cause of statin-associated muscle pain in some people and vitamin D repletion, therefore, may be helpful. The simple solution is in the next paragraph, so if you’re feeling confused or frustrated, please read on.

 

The Safest, Most Economical and Simplest Solution

As a result of the overwhelming benefits of both CoQ10 and buffered creatine we’ve discussed, along with the benefit of vitamin D3 in those with insufficient levels, I decided to combine CoQ10, buffered creatine and vitamin D3 into one convenient nutritional supplement called Statin Sidekick™. I believe Statin Sidekick is critically important for anyone taking a statin medication along with anyone physically active and interested in insuring a steady supply of energy to muscle and brain cells. Two capsules of Statin Sidekick provides a proprietary blend of buffered creatine and CoQ10 totaling 1,500 mg. along with 2,000 iu of vitamin D3. These three ingredients are included in the most optimal ratio based on published clinical trials, our original research and our patient experience at the Leonardi Institute. The recommended dose is 2 to 3 capsules of Statin Sidekick twice a day (always with food) for the first week (called a “loading dose”) followed by 1 to 2 capsules twice a day thereafter. There appears to be a benefit in stopping your statin for the first week while taking the loading dose of Statin Sidekick but we don’t recommend this without first checking with your practitioner. If you notice muscle aching that you feel is related to your statin while taking Statin Sidekick™, simply increase the dose back up to 3 capsules twice a day. Of course, you should also notify your physician that your statin is causing you pain. You may adjust the dose of Statin Sidekick up and down to see what dose you personally require to eliminate statin-related muscle aching while optimizing muscle energy availability and performance. In unusual circumstances, a few people may even require 4 capsules twice a day. Detailed dosing instructions are included with each order. If 4 capsules of Statin Sidekick twice daily doesn’t relieve your statin side effects, the next logical step might  be to discuss with your practitioner, either an alternative statin or a lower dose of the same statin while continuing Statin Sidekick. If 4 capsules of Statin Sidekick twice daily doesn’t relieve your statin side effects, the next logical step might  be to discuss with your practitioner, either an alternative statin or a lower dose of the same statin while continuing Statin Sidekick. If you’re unsuccessful with that approach you may want to discuss statin alternatives with your practitioner.

Statin Sidekick is an essential nutrient for anyone taking a statin. It provides that margin of safety and peace of mind that you’re getting the best possible performance from your muscles while reducing the risk of muscle pain and muscle dysfunction that can accompany statin use. If you would like to order Statin Sidekick, it is available on our Cycle-Breakers.com website by clicking here.  Statin Sidekick is carefully tested and manufactured in full compliance of U.S. government Good Manufacturing Processes (GMP).

Statin Sidekick Supplement Facts

Serving size 2 capsules

Servings per Container 30 (60 capsules)

Active Ingredients
Amount per Serving
% DRV
Vitamin D32,000 iu500
A proprietary blend of Kre-Alkalyn® (buffered creatine) and Coenzyme Q101500 mgDRV not established

Directions: Take 2-3 capsules twice daily WITH FOOD (within 45 minutes of a meal). You may reduce the dose after the first week if you remain free of statin side effects, or increase the dose if needed.

References

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