Arts and Sciences
 

C0Q10 and Statins: The Vitamin C Connection 

by Owen R. Fonorow © 2003

"We are now in a position to witness the unfolding of the greatest medical tragedy of all time -  never before in history has the medical establishment knowingly created a life threatening nutrient deficiency in millions of otherwise healthy people." – Peter H. Langsjoen, MD

Ubiquinone (CoQ10) is a popular heart medication. Until 2001, it was only available by prescription in Japan. The public is hardly aware that an increasingly popular class of cardiovascular drugs called statins (HMG-CoA reductase inhibitors) interfere with the body's synthesis of CoQ10. Top selling statin drugs, such as Lipitor® and Zocor®, earn their makers in excess $20 billion per year. These drugs lower the endogenous production of cholesterol and are often touted as "life saving" by cardiologists and the Media.

Are the statin drugs really good for us, or are cardiologists mistaken? How can drugs that lower the body's production of CoQ10 benefit heart patients?  Are the health benefits attributed to CoQ10 supplementation hype or is it that there is something fundamentally wrong with the thinking and science being used by those who market statin drugs?

COQ10 BASICS

Coenzyme Q10 is a vitamin-like fat-soluble antioxidant found everywhere in the body; the highest concentrations have been measured in vital organs such as the heart and pancreas. At age 20, the heart has a higher CoQ10 level than other major organs. At age 80 this is no longer true, with the heart levels cut by more than half. More than 35 controlled clinical trials in Japan, Europe and the U.S. have proven that CoQ10 therapy is highly effective in treatment of congestive heart failure, angina and ischemic heart disease, and myocardial infarction. It is now believed that CoQ10 is the key nutrient for generating 95 percent of the total energy required by the human body.

A healthy, youthful human body can make its own CoQ10. Endogenous production or biosynthesis of CoQ10 has 17 steps, requiring at least seven vitamins (vitamin B2 – riboflavin, vitamin B3 – niacinamide, vitamin B6, folic acid, vitamin B12, vitamin C, and pantothenic acid) and several trace elements.

The pharmaceutical giant Merck has known for more than 15 years that statin drugs interfere with CoQ10 biosynthesis; leading to low serum levels which cause muscles to atrophy. The following claim from one of two 1990 Merck patents (4,933,165) is to add CoQ10 to statin drugs in order to overcome statin induced myopathy:

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.

This invention has never been implemented, probably because the entire world supply of CoQ10 is limited and current production would only supply one-sixth of the world's statin users.

VARIOUS HEALTH BENEFITS ATTRIBUTED TO COQ10

The CoQ10 science has accelerated from its discovery in 1957 until the present day and appears excellent. The following headlines summarize the many clinical studies that have shown CoQ10 supplementation beneficial in disease conditions ranging from Parkinson's disease to cataracts. Dosages studied range from 30 mg to 1200 mg daily. Higher dosages have generally been found to be more beneficial.

  • CoQ10 gives complete protection against stroke
    • Since 1972, in studies of stroke in three animal models (dog, rat, gerbil) ubiquinone (coq10) was the only agent giving complete protection and this was over two times more often than the next best agent (naloxone) of the many tested to date.
  • CoQ10 benefits Cardiovascular Disease
    • CoQ10 levels in heart tissue decline disproportionately with age. CoQ10 pioneer Karl Folkers (1985), in agreement with earlier Japanese studies, found lower CoQ10 levels in patients with more severe heart disease and showed that CoQ10 supplements significantly raised blood and heart tissue levels of CoQ10 in these patients.
  • CoQ10 improves high blood pressure
    • "At least six clinical trials have shown a blood pressure-lowering effect of CoQ10."
  • CoQ10 for Parkinson's disease
    • "Less disability developed in subjects on CoQ10 than in those on placebo, and the benefit was greatest in people receiving the highest dosage."
  • CoQ10 benefits people with kidney failure
    • "Because CoQ10 has the potential to revolutionize the treatment of chronic renal failure, a large-scale, long-term study should be initiated as soon as possible." – Alan Gaby
  • CoQ10 for youthful skin
    • "Just recently scientists have also discovered that this natural supplement may even slow down the skin's aging process. Gerson Unna confirmed that, like vitamin E, Co-Q10 slows down tissue damage by decreasing the effect of free radical molecules. In a placebo-controlled study, researchers at Beiersdorf discovered that after six weeks of daily treatment on crow's feet (eye wrinkles), wrinkle depth was reduced by 27 percent; after 10 weeks, fine lines and wrinkles were reduced by a surprising 43 percent. The enzyme also has been effective in the reduction and fading of age spots and is touted by Beiersdorf for its lack of toxicity.
  • CoQ10 Effective for Migraine Prevention
  • CoQ10 Therapy can improve glucose control in Type 2 diabetics
  • 400 mg CoQ10 reportedly induced cancer remissions

Science has uncovered even more benefits of supplemental CoQ10.

COQ10 SUPPLEMENTATION IS NECESSARY AS WE AGE

Researcher Dr. John Ely, of the University of Washington, holds that CoQ10 supplementation is essential in the aged.  Most people make approximately 500 mg of Coq10 daily in the body, at least up until age 21. Between ages 21 and 30, levels of CoQ10 begin to drop, perhaps because of aging. This causes the degeneration of cells, which may contribute to age-related diseases and conditions such as high blood pressure, arthritis, heart disease and the breakdown of skin tissue. Statin drugs and deficiencies in several other vitamins also cause blood levels of CoQ10 to drop.

According to Dr. Ely,

"Possibly the most important details not reported previously are those related to CoQ10 body pool and turnover rate that mandate human supplementation. Adult human body pool has been found to be approximately 2 grams and requires replacement of about 0.5 grams/day based on its average turnover rate of about 4 days in various tissues. This must be supplied either by endogenous synthesis or from exogenous sources. Synthesis decreases progressively in humans above age 21. Furthermore, the average ubiquinone content of the western diet is less than 5 mg/day. Thus, ubiquinone supplementation appears to be the only way for older people, and certainly the ill, to obtain the major proportion of the 0.5 gram/day need. Failure to supplement by the aged, ill or stressed, can have tragic consequences in the form of irreversible damage in the brain, other organs and mitochondria everywhere."(http://faculty.washington.edu/ely/turnover.htm)

CoQ10 pioneer Karl Folkers claimed that the primary source of CoQ10 in man is biosynthesis. Folkers argues that "...suboptimal nutrient intake in man is almost universal causing subsequent secondary impairment in CoQ10 biosynthesis." According to CoQ10 expert Peter H. Langsjoen, MD. "This means that average or 'normal' levels of CoQ10 are really suboptimal and the very low levels observed in advanced disease states represent only the tip of a deficiency ice berg."

The Vitamin C Connection

Vitamin C is a "natural" HMG-CoA reductase inhibitor. It was observed experimentally that when vitamin C levels are low, cholesterol becomes elevated, and when more vitamin C is consumed, cholesterol levels decline. The mechanism by which vitamin C lowers cholesterol was discovered circa 1985. High Vitamin C levels inhibit the same the HMG-CoA Reductase enzyme as the statin drugs. The inescapable conclusion is that vitamin C does what statins do – lowers cholesterol – without side-effects. If the statin drugs were patterned after Vitamin C, they lack many other benefits of the vitamin. For example, vitamin C promotes the production of coenzyme Q10 and lowers Lp(a).

It is interesting that in addition to vitamin C, our bodies require many B vitamins to synthesize CoQ10. Voluminous research has found beneficial effects from ascorbic acid supplementation similar to the effects found from smaller dose CoQ10 supplementation. For example, in a recent study, hydro soluble CoQ10 supplementation was shown to lower circulating levels of Lp(a). We speculate that some of these similar effects may be due to increased endogenous CoQ10 synthesis induced by the ascorbic acid along with generally better all around nutrition. 

Every human body makes up to 500 mg of CoQ10 daily; no human body can make vitamin C. As important as CoQ10 is for health, vitamin C is more important, perhaps an order of magnitude. That fact is that most mammals synthesize ten times more vitamin C than they do CoQ10, when adjusted for body weight. Under normal circumstances the daily amount of ascorbic acid produced by mammals lies between 3,000 mg and 15,000 mg, with an average of 5,400 mg, when adjusted for comparison to the weight of the average male human being.  

We conclude that everyone should supplement 3,000 mg to 6,000mg vitamin C daily from birth, including during pregnancy. On the other hand, healthy, well-nourished children will usually synthesize their own CoQ10. With the possible exception of athletes, persons taking vitamin C should not have to supplement CoQ10 until the fourth or fifth decade of life. Athletes have a high requirement for CoQ10 and may benefit from supplementation earlier in life.

The Statin Dilemma

The question persists, how can statin drugs that deplete levels of CoQ10 be "life saving?" Not only do statins used to treat elevated blood cholesterol levels by blocking cholesterol biosynthesis also block CoQ10 biosynthesis, but most CoQ10 and vitamin E molecules circulate through the bloodstream attached to LDL particles.

According Dr. Langsjoen,

"The resulting lowering of blood CoQ10 level is due to the partially shared biosynthetic pathway of CoQ10 and cholesterol. In patients with heart failure this is more than a laboratory observation. It has a significant harmful effect which can be negated by oral CoQ10 supplementation."

So, are "safe" statin drugs the next "aspirin?" There is considerable hype in reporting the science behind cholesterol lowering drugs. We found, chasing down many of the media stories suggesting benefit, that most stories are either hoaxes or highly speculative. In the world of media hype, an estimated 0.4% reduction in plaque creates worldwide news. Furthermore, it is difficult to formulate an overall theory that explains the reported benefits.

The first "red flag" one encounters researching the statin studies are that the raw mortality data is being kept a closely guarded secret. The data is summarized, but it is surprisingly hard to inspect the raw data of studies published in peer-reviewed journals; mortality data that allegedly supports the "life saving" claims made for statins. This is true of the so-called Heart Protection Study (HPS) managed by Oxford University. 

According to statistician Eddie Vos, after millions of statin pills, in those studies that have summarized or released the data, there is no change in mortality curves – the graphs of the placebo and statin groups touch.

"Massive benefits proclaims Oxford University about its 2002 HPS study, 'the world's largest cholesterol-lowering trial'. 75% of heart attacks still happen and 300 people on the drug for 12 months to postpone the death of just 1 of them. Massive drug use, few lives saved. The next European study claiming benefit in high-risk elderly, PROSPER, found 6 lives saved but 24 more cancer deaths, and more new cancers in each of 4 years in a group with 52 fewer smokers. Zero 'anything' benefit was next found in the ALLHAT trial in 10 year younger North Americans: 1 death postponed per 1.1 million $3-pills taken!  Next was Lipitor's ASCOT study: also no mortality benefit. From 10 years ago: cholesterol lowering by any means caused 150 more deaths per 100,000 patient-years of intervention." (www-health-heart.org)

The HPS paper published in the Lancet medical  journal makes me wary of the claims made by the authors. HPS reportedly had four study groups, 1) a placebo group, 2) a placebo-plus-antioxidant-vitamins group, 3) a statin group and 4) a statin-plus-antioxidant-vitamins group. A second paper devoted to the antioxidant vitamins was published; implying that claims of "massive benefit" in the first paper is between the statins and placebo. However, the paper is written without even a summary of the supporting data, and these results could very well have been between the statins-plus-antioxidants group 4 against the placebo group 1. The authors carefully avoid this issue.

The HPS paper does not discuss the differences between the statins group 3 and statins-and-antioxidants group 4 versus placebo, an obvious point of interest. Instead, they published the second paper diverting attention from this issue. The refusal to publish and share the data indicates that there is something to hide.

British author/researcher Malcolm Kendrick, MD, comments about HPS study:

"In the Heart Protection Study (HPS), a major study in which the rate of deaths was (reportedly) reduced in patients taking a statin (simvastatin), at post-mortem, the people who had been taking the statin had bigger and more complex plaques than those who had not."

VITAMIN C AND MORTALITY

Vitamin C's proven effect on mortality stands in stark contrast to the statin drugs. According to author Bill Sardi, "Vitamin C is the only vitamin repeatedly proven to increase the human life span when taken in doses that exceed dietary levels of this vitamin." This observation was recently confirmed in Britain, again.

Low Blood Vitamin C Concentrations in the Older British Population Strongly Predict Mortality

In November 2003 the British Centre for Ageing and Public Health, London School of Hygiene and Tropical Medicine, United Kingdom (astrid.fletcher@lshtm.ac.uk) published their findings of a direct correlation between low vitamin C and increased mortality.

"We found a strong inverse relationship for blood ascorbate (vitamin C) concentrations with all-cause and cardiovascular disease mortality, which were only marginally reduced after adjustment for confounders or supplement use. Those in the lowest fifth (< 17 micromol/L) had the highest mortality, whereas those in the highest fifth (> 66 micromol/L) had a mortality risk nearly half that (hazard ratio = 0.54; 95% CI: 0.34, 0.84). Similar results were found after the exclusion of those subjects with cardiovascular disease or cancer at baseline (hazard ratio = 0.51; 0.28, 0.93). In fully adjusted models, there was no evidence for an influence of alpha-tocopherol (vitamin-E), beta-carotene, or retinol (vitamin-A) on total mortality. Dietary antioxidants measured by the food-frequency questionnaire were not associated with all-cause or cardiovascular disease mortality."

Adverse Side Effects of Statin Cholesterol Lowering Drugs:

The following headlines from BOLENREPORT.COM reveal the many little-known side effects of the 'artificial' Statin drugs, some of which are required to be reported in Canadian statin drug ads, but not the U. S. versions.

Statin Cholesterol Lowering Drugs:

  1. Deplete the ubiquinone (vitamin-like) Coenzyme Q10 causing cardiomyopthy and heart failure
  2. Change, weaken, damage or destroy muscle (depending on dose and concomitant use of other drugs)
  3. Do not slow atherosclerosis
  4. Induce sudden total memory loss
  5. Increase eye cataract risk
  6. Suppress immune function
  7. Are linked to cancer
  8. Have been linked for 10-years with Rhabdomyolysis and Myoglobinuria
  9. Have been linked with elevated transaminase (indicator of liver and kidney damage)
  10. Are linked to nerve damage
  11. Induce muscle pain
  12. Do not extend life
  13. Increase serum Lp(a) concentrations** (Increasing odds of heart attack or stroke up to 70% SOURCE: CIRCULATION)
  14. Reduce left ventricular function
  15. Elevate the lactate to pyruvate ratio
  16. Enhance LDL cholesterol oxidation
  17. Would be expected to interfere with any function (e.g. sex hormone production, hair growth, sleep, or proper brain and nerve function) that depends on cholesterol or CoQ10
  18. Are prescribed to 13 million (in the U.S., 25 million worldwide) creating a $20b market
  19. Are MORTAL (else will cause 65,000 predicted myopathies Source: Merck Patent)

NOTE: Biopsy only reliable test for statin induced myopathy
 
Supplemental Vitamin C and CoQ10 are completely nontoxic and would lessen or eliminate most of these statin-induced effects. More headlines from BOLENREPORT.COM illustrate the health benefits of Vitamin C:

  1. HARVARD: VITAMIN C ONLY 1 OF 880 SUBSTANCES TO REGENERATE HEART MUSCLE FROM STEM CELLS
  2. 15-YEAR HARVARD STUDY OF 85,000 FINDS SINGLE VITAMIN C PILL REDUCES HEART DISEASE ALMOST 30%
    • THE RISK OF STROKE WAS 70% HIGHER AMONG THOSE IN THE LOWEST QUARTILE FOR SERUM VITAMIN C THAN AMONG THOSE IN THE HIGHEST
  3. VITAMIN C INHIBITS LIPID OXIDATION IN HUMAN HDL
  4. MORE VITAMIN C AS PILLS REDUCE CATARACTS BY 77%
  5. HIGH-DOSE VITAMIN C COMPLETELY PREVENTED DRUG-INDUCED AMNESIA IN MICE
  6. CARNITINE, ITS BUILDING BLOCKS VITAMIN C AND LYSINE, INCREASE MUSCLE STRENGTH
  7. MATTHIAS RATH CLAIMS CANCER HALTED WITH VITAMIN C/LYSINE/PROLINE AND GREEN TEA EXTRACT
  8. VITAMIN C BOOSTS IMMUNE SYSTEM IN AS LITTLE AS 5 HOURS (NIH)
  9. VITAMIN C PILLS EXTEND LIFE 6-YEARS (USC)
  10. VITAMIN C (AND LYSINE) HALT ATHEROSCLEROSIS
  11. IV VITAMIN C REVERSES ENDOTHELIAL DYSFUNCION
  12. VITAMIN C - NEW TREATMENT FOR OSTEOPOROSIS
  13. VITAMIN C CAN (1) PREVENT THE DETERIORATION COMPLETELY; AND (2) CURE EVEN LARGE AORTIC ANEURYSMS WITHOUT SURGERY.

Conclusion

Apparently a 20 billion dollar market has blinded some scientists.  Merck and the other pharmaceutical companies have known about the CoQ10 biosynthesis "issue" for more than a decade. (Few medical doctors in the U.S. are aware of this problem.) There exists no theory that justifies the use of statin drugs. This author has seen no data or evidence that demonstrates any real health benefit for statin drug use in most people that overcomes the proven detriment of hampering the production of CoQ10.  

How could the existing claims for the statin drugs have ever been approved by the FDA?  Apparently the dosage of a statin is important. At lower dosages, the "bad" effects are reduced such that the mortality curves between the control and statin groups are similar. The studies rarely try to quantify muscular aches and pains, and instead usually focus on lowered cholesterol as the end-point. Ergo, if the drug lowers cholesterol, beneficial effects on heart patients are assumed. 

According to Dr. Langsjoen,

"In my practice of 17 years in Tyler, Texas, I have seen a frightening increase in heart failure secondary to statin usage, 'statin cardiomyopathy.' Over the past five years, statins have become more potent, are being prescribed in higher dosages, and are being used with reckless abandon in the elderly and in patients with "normal" cholesterol levels. We are in the midst of a Congestive Heart Failure epidemic in the US with a dramatic increase over the past decade. Are we causing this epidemic through our zealous use of statins? In large part I think the answer is yes. We are now in a position to witness the unfolding of the greatest medical tragedy of all time - never before in history has the medical establishment knowingly create a life threatening nutrient deficiency in millions of otherwise healthy people."

POSTULATE: No human who consistently consumes 10,000 mg or more Ascorbic Acid (vitamin C) and 300 mg or more of ubiquinone (CoQ10) daily has heart disease.
 
PREDICTION: Studies that purport to show that statins benefit heart patients either has mischaracterized the data or, eventually, will be shown to be fraudulent.
 
We defy any researcher to find a contrary example to our postulate, and we stand by the prediction. Cardiologists, as a rule, are highly trained professionals, yet they are being duped by drug company efforts to expand markets. They love these statin drugs, and why not, patients keep coming back?

It is unconscionable that editors of mainstream medical journals, elements of the U. S. government and the news media continue to hide the explosive research results on vitamin C and CoQ10 from U.S. doctors.  Disregarding malpractice, the continuance of ignoring vitamin C and CoQ10, while marketing and prescribing statin drugs – for heart patients – is criminal.
 
Owen R. Fonorow, Ph.D., Naturopath
Vitamin C Foundation
www.VitaminCFoundation.org
www.PaulingTherapy.com
fonorow@foxvalley.net
Fax: (630) 416-1309

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