CoQ10 and Statin Drugs

Statin drugs have become very popular and are being widely prescribed in recent years to lower high blood cholesterol and thus reduce the risk for heart disease. These drugs block cholesterol production in the body by inhibiting the enzyme called HMG-CoA reductase in the early steps of its synthesis in the mevalonate pathway. This same biosynthetic pathway is also shared by CoQ10. Therefore, one unfortunate consequence of statin drugs is the unintentional inhibition of CoQ10 synthesis. Thus, in the long run, statin drugs could predispose the patients to heart disease by lowering their CoQ10 status, the very condition that these drugs are intended to prevent.

Dr. Emile Bliznakov, an authority on CoQ10, recently published a scholarly review on the interaction between statin drugs and CoQ10 (Bliznakov and Wilkins, 1998). He wrote the best-selling book "The Miracle Nutrient Coenzyme Q10" several years ago and it is still being hailed as the best reference book on CoQ10 (Bliznakov, 1987).

The reduction of CoQ10 levels might be associated with myopathy, a rare adverse effect associated with statin drugs. This metabolic myopathy is related to ubiquinone (CoQ10) deficiency in muscle cell mitochondria, disturbing normal cellular respiration and causing adverse effects such as rhabdomyolysis, exercise intolerance, and recurrent myoglobinuria. (DiMuro S., Exercise intolerance and the mitochondrial respiratory chain. Ital J Neurol Sci. Dec. 1999;20(6):387-393).

It is important to note that Coenzyme Q10 supplementation does not interfere with the very important cholesterol-lowering effect of statin drugs such as Lipitor® and Zocor®. Therefore, if you are taking a statin drug, (especially for an extended period of time), you may want to consider discussing CoQ10 supplementation with your health care professional.

The bottom line is that the popular and widely prescribed cholesterol lowering drugs called "Statins" can block the synthesis of Coenzyme Q10 in the body which may lead to sub-optimal CoQ10 levels. Supplementation with Q-Gel CoQ-10 is a prudent approach when undergoing "statin" therapy.

But, don't just take our word for it. One of the world's premier Pharmaceutical Companies and the manufacturer of the 2nd largest selling statin drug has not one but two US Patents regarding the use of Coenzyme Q10 with HMG-COA Reductase Inhibitors (Statins). You can read the full contents of these patents for yourself on the official United States Patent and Trademark Office web site (www.uspto.gov/). It is interesting to note that both of these patents were issued over eleven years ago (May and June of 1990) but that no use of the patented process of combining Coenzyme Q10 with HMG-COA Reductase Inhibitors (Statins) has yet been made or publicized.

The Patent numbers you will want to look up are: Patent Number: 4,933,165 Patent Number: 4,929,437

Below is a verbatim sample from Patent Number 4,933,165.

"What is claimed is:

1. A pharmaceutical composition comprising a pharmaceutical carrier and an effective antihypercholesterolemic amount of an HMG-CoA reductase inhibitor and an amount of Coenzyme Q.sub.10 effective to counteract HMG-CoA reductase inhibitor-associated skeletal muscle myopathy.

2. A composition of claim 1 in which the HMG-CoA reductase inhibitor is selected from: lovastatin, simvastatin, pravastatin and sodium-3,5-dihydroxy-7-[3-(4-fluorophenyl)-1-(methylethyl)-1H-Indole-2yl]- hept-6-enoate.

3. A method of counteracting HMG-CoA reductase inhibitor-associated skeletal muscle myopathy in a subject in need of such treatment which comprises the adjunct administration of a therapeutically effective amount of an HMG-CoA reductase inhibitor and an effective amount of Coenzyme Q.sub.10 to counteract said myopathy.

4. A method of claim 3 in which the HMG-CoA reductase inhibitor is selected from the group consisting of: lovastatin, simvastatin, pravastatin and sodium-3,5-dihydroxy-7-[3-(4-fluorophenyl)-1-(methylethyl)-1H-Indole-2yl]- hept-6-enoate."

To access these patents: Go to the official United States Patent and Trademark Office web site at (www.uspto.gov/). (We certainly hope you'll come back to epic4health.com later!) . From the Patent offices home page "click" on the Patents button, then "click" on "Search Patents", then click on "Patent Number Search". Type in the patent number (4,933,165) in the "Query Box" and "click" on the search button. The Patent number and title will show up, then just click on the patent number and you will be able to read the full documentation, including who is assigned the patent. I've probably made this whole search process sound harder than it really is -- give it a try, you may be surprised by what you learn.

CoQ10 Dosage, Forms and Bioavailability

The daily intake from a typical Western diet is estimated to be about 5 mg. The daily dosage of CoQ10 supplements in healthy individuals is generally in the 15-30 mg range and is taken for general well-being. In patients with heart disease or other chronic conditions, a minimum of 100 mg a day has been used in numerous clinical trials. A dosage in the range of 600-1200 mg is being used in the on-going study on Huntington’s disease, supported by the National Institutes of Health.

Pure CoQ10 is not soluble in water and has limited solubility in oils. Commercially available CoQ10 products come in the form of tablets, powder-filled capsules and oil suspension in softgel capsules. Bioavailability of CoQ10 in these products is poor. A new "hydrosoluble" CoQ10 formulation with superior bioavailability was introduced in 1997 (called Q-Gel®, Tishcon Corp., Westbury, NY 11590) using a patented process (Biosolv) to solubilize CoQ10. In a human study published in 1998, Q-Gel® was shown to be about 3-fold better than any of the other three product types, as assessed by increases in blood CoQ10 levels (Chopra et al, 1988; Bhagavan et al, 2001). This means that lower doses of CoQ10 as Q-Gel® are needed to reach and maintain adequate blood levels.

Q-Gel CoQ10 Dosage Note from Mike Engel

Dosage depends on many different factors. I am NOT an MD so really can not advise any particular individual in this area. However, I can let you know what some of the MD's who buy from us tell their patients -- those with congestive heart failure, they recommend a jump start of 180mg Q-Gel CoQ10 for first 2-3 weeks and then 120mg per day.

If on a statin drug, they suggest 60 to 90mg Q-Gel CoQ10 per day.

No real problems? Want it for prevention and/or antioxidant use? Then 30 to 60 mg Q-Gel CoQ10 per day would be very sufficient. (This is what I do, taking one 30mg in AM with breakfast and one 30mg at lunch -- when I remember!)

Thanks for your interest in Q-Gel CoQ10

*These statements have not been evaluated by the Food & Drug Administration. These products are not intended to diagnose, treat, cure or prevent any disease.

Any questions? Please email, or, in the U.S., call: 1-800-866-0978

In addition, stress and other aspects of one’s lifestyle can deplete bodily levels of coenzyme Q10 (CoQ10), another nutrient needed by the heart. Supplementing one’s intake of red yeast rice with CoQ10 ensures that the body does not become deficient in this essential nutrient.

Every cell in the body must have CoQ10 to produce energy. Dr. Karl Folkers, the man who pioneered research on CoQ10, even said, "We know today that CoQ10 is essential for life to exist." According to Parris M. Kidd, Ph.D. (1988), it sparks energy production in the mitochondria "in every cell of every tissue in every organ of every person during every moment of life."

Heart muscle contains the highest concentration of CoQ10; it provides the energy to drive the heart’s constant, mechanical beating. It’s not surprising, then, that lack of CoQ10, like excessive blood cholesterol, can be a factor in heart problems.

Dr. Folkers and his colleagues confirmed a connection between CoQ10 deficiency and heart disorders. They tested CoQ10 on more than 80 people experiencing various degrees of heart failure and found that CoQ10 significantly improved the strength of their heart muscle and extended the time that these people survived (Kidd 1988).

Other studies have found that using CoQ10 alone can sometimes help control an irregular heartbeat and swelling of the mouth or throat. Even in more complicated heart disorders caused by poor circulation, CoQ10 can help restore heart function partially (Kidd 1988).

This nutrient also functions as an antioxidant as potent as the super-antioxidant vitamin E. It assists in protecting cells against cell-destroying free radical damage and the severe oxygen depletion that can generate vast amounts of free radicals (Kidd 1988).

It was not until 1957, when Dr. Frederick Crane first isolated CoQ10 from beef heart mitochondria, that biochemists were able to decipher how cells obtained their energy. Dr. Crane discovered the secret in the then unknown molecule CoQ10, which functions as the "gasoline" that fuels the cell’s "engine." Every cell in our body has and needs CoQ10.

Dosage Is Everything for L-Carnitine,

A-Lipoic Acid, & CoQ10

You’re throwing your money away if you don’t take CoQ10, L-carnitine, and alpha-lipoic acid in the amounts that researchers and clinicians have found to work.

In his book The Carnitine Miracle, Robert Crayhon, M.S. (1998), comments that people often take low amounts, fail to see results, and then think the nutrient doesn’t work. "This is like throwing a glass of water on a burning building and concluding that water does not put out fires," he points out. "You don’t know the effectiveness of a compound until you use the right dose."

For CoQ10, "The average dose is 200 to 300 milligrams a day," says Dr. Peter Langsjoen (2002), who uses CoQ10 extensively in his Tyler, Texas, cardiology practice.

For L-carnitine, Crayhon says, "There is substantial evidence that, for optimal health, we should be getting at least 250 to 500 milligrams in our diet daily. The real health benefits of carnitine do not come in the amount our body makes or the amount in most people’s diet." Crayhon notes that, when L-carnitine is used for weight loss, a substantially higher amount is needed: at least 1,000 milligrams a day and sometimes as much as 4,000 milligrams a day.

CoQ10 is also known as a ubiquinone (from ubiquitous, meaning "present everywhere"), and researchers noticed that, where CoQ10 levels are low, disease is present. However, according to leading cardiologist Dr. Peter Langsjoen (2002), the exciting thing is that low levels of CoQ10 can be corrected. He says of CoQ10, "When it is taken [as a supplement], we can show normalization of these levels in blood and in tissue. And CoQ10 affects all cells. The entire field of medicine has to be reevaluated in light of this growing knowledge."

CoQ10 May Help Heart Function

Supplementing with CoQ10 may improve heart function across a wide range of parameters. New research shows that, when taken daily for a week beforehand, CoQ10 may even help people recover faster from heart surgery (Pepe 2001).

In his cardiology practice, Dr. Langsjoen (2002) has used CoQ10 for the past 17 years on thousands of patients with heart problems. "It’s almost too good to believe," he says, "but CoQ10 really is more extraordinary than you could imagine, unless you have personally experienced it or have used it in a patient. It’s better than you would get from the literature, because the literature has lagged behind."

Other Health Benefits

Dr. Langsjoen (1994 and 2002) has made various other discoveries regarding the benefits of CoQ10, both published and unpublished:

* CoQ10 seems to improve heart function with virtually no side effects.

* Heart patients on CoQ10 often can reduce the number of medications they take.

* People with heart problems respond even more dramatically and quickly to CoQ10 than do people with heart failure. They often are able to reduce their nitroglycerin use to a fraction of what it was, sometimes within weeks.

* At high doses, CoQ10 may help protect the brain.

"Just from a practical standpoint clinically," says Dr. Langsjoen (2002), "when you treat people who have had, say, heart failure for years, they [see] improve[ment] in [just about] all aspects of their health. They get colds much less frequently, for instance. Their nails get harder, and all kinds of skin lesions disappear. And, people with fragile, bleeding gums always see a big benefit."

What’s Unique About L-Carnitine

L-carnitine’s most beneficial property is its extraordinary ability to collect fats and then drop them off right where the body burns them: the mitochondria, which generate the energy that drives every cellular function.

The heart derives fully two thirds of its energy from fat. When your body is low on carnitine, your heart is apt to suffer first. People taking L-carnitine supplements can experience substantial changes in heart health. L-carnitine has been found to:

* Improve heart function in people with congestive heart failure

* Reduce heart damage when taken soon after a heart attack

* Reduce pain from angina

* Help stabilize heartbeat in people with irregular heartbeat

* Reduce blood-fat levels

* Improve heart-muscle function

* Increase cardiac output

Although the benefits of CoQ10 are well documented, U.S. cardiologists have been slow to incorporate it into their practices. Research has shown that statin drugs, the group of cholesterol-lowering drugs prescribed most often, deplete CoQ10 levels so seriously that they can cause heart failure (Folkers 1990). This is among CoQ10’s most significant possible impacts, according to Dr. Langsjoen (2002). "If we’re causing a clinically significant nutrient deficiency in millions of people [by prescribing statins]," he explains, "we have to be really careful about it."

Because CoQ10 levels decrease with age, it is theorized that increasing the body’s supply of CoQ10 may have a longevity benefit. CoQ10 has two forms and thus two functions within the body: When CoQ10 oxidizes after producing energy in the cell, it quenches itself by reducing back to its antioxidant form. This is an extraordinary property, analogous to a car’s exhaust fumes being able to turn spontaneously into an air filter.

 

 

L-Carnitine Energizes the Heart

CoQ10 is not alone in its extraordinary capacities. L-carnitine, a nutrient whose cardiovascular benefits have been studied since 1937, extracts fatty acids, the heart’s major source of energy, from the blood and transports them to the mitochondria. When the body is low on L-carnitine, the heart suffers first.

Alpha-Lipoic Acid and Aging

In summing up the research on alpha-lipoic acid in his book The Antioxidant Miracle, Dr. Lester Packer (1999) says, "Obviously, these findings have profound implications for healthy aging."

Dr. Packer, the world’s foremost authority on lipoic acid, says that lipoic acid supplements can act as a broad shield against the degenerative health problems associated with heart disease, stroke, and cataracts. Dr. Packer’s work also has shown that alpha-lipoic acid can help strengthen memory and prevent some signs of brain aging.

Low levels of L-carnitine in heart tissue are markers for problems. Supplementing with L-carnitine, however, can bring about dramatic changes, including increases in cardiac output and endurance, improvements in heart muscle function, and lessening of irregular heartbeat (Crayhon 1998).

The benefits do not end there. As a fat-burning nutrient that delivers fat right to the mitochondria, L-carnitine is terribly efficient. It can help increase metabolic rate while maintaining muscle tissue. Crucially for our national epidemic of blood sugar problems, L-carnitine also aids in blood sugar balancing by helping to metabolize carbohydrates.

Relieving Oxidative Stress

Old animals have old mitochondria, and old mitochondria have sluggish energy production. However, preliminary animal experiments suggest that combining L-carnitine with the antioxidant alpha-lipoic acid can improve mitochondrial function: the production of energy (Packer 1999). "Obviously, these findings have profound implications for healthy aging," says Dr. Lester Packer (1999), the world’s foremost authority on alpha-lipoic acid, in his book The Antioxidant Miracle. "In the United States, cutting-edge physicians have already begun to incorporate lipoic acid in the prevention and treatment of diseases related to free radicals."

Alpha-Lipoic Acid: Critical for Energy

Without alpha-lipoic acid, the cells shut down. In addition, it is both fat- and water-soluble, so it can trap free radicals wherever they may be. It even recycles all of the body’s other antioxidants—vitamins C and E, glutathione, and CoQ10—increasing their supply.

Call to All Doctors From

ABC-TV News

Nicholas Regush (2001) of ABC News began his commentary, "Come on, cardiologists! Crack open the medical literature on coenzyme Q10, or CoQ10, a vital nutrient that produces energy in the body. Start reading up on how this powerful substance may be able to help patients with heart problems."

Of course, he didn’t limit his remarks to cardiologists. "Neurologists, too! You also have been slow to respond to tantalizing data suggesting CoQ10 might help fight off degenerative brain diseases and even help slow down the aging process."

Scientists recognize that low antioxidant levels and oxidative stress are the hallmarks of many unhappy conditions. People suffering from blood sugar imbalance, for example, have significantly lower levels of antioxidants than others do. Luckily, alpha-lipoic acid can help stop the progression of blood sugar problems by boosting antioxidant levels and assisting glucose transport in the body. In those suffering this problem, it also can enhance regeneration of damaged nerve fibers. Indeed, it has been used in Germany for more than 30 years to treat peripheral neuropathy.

Alpha-lipoic acid has the added benefit of boosting the body’s defense system against foreign invaders.

A Winning Combination

I’ve seen the powerful effects of using all three nutrients: CoQ10, L-carnitine, and alpha-lipoic acid. Such a mixture could have a huge impact on heart problems, which affect 62 million Americans and are ranked as the number-one killer in the United States. In fact, a protocol is being written right now to test the synergy among these three heart nutrients. The results of this study will be released next year. In the meantime you can look forward to upcoming Journal of Longevity articles on the multiple benefits of CoQ10, L-carnitine, and alpha-lipoic acid as ongoing research becomes available.

Ronald M. Lawrence, M.D., Ph.D., was a member of the National Advisory Council on Aging of the National Institutes of Health and Co-Medical Director of the 1996 Olympic marathons. He has authored 35 scientific and medical papers in the fields of pain and neurophysiology.