This is the first in a two-part series on coenzyme Q10, which is sometime referred to as The Miracle Nutrient. In fact, The Miracle Nutrient: Coenzyme Q10 is the title of a book that was written by Emile Bliznakov, MD, who was one of the first scientists to research and report the benefits of coenzyme Q10 to the non-scientific population of the world. CoQ10 has been known of for 60 years. There are two forms: an oxidized form (Ubiquinone) and a reduced form (Ubiquinol). The ubiquinol form is unstable and has only been in the USA market since 2006. The ubiquinone form had been in the USA market since 1974. Ubiquinol is poorly researched while there are more than 2000 scientific articles on ubiquinone.

Coenzyme Q10 or CoQ10, was discovered by biochemist Fred Crane at the University of Wisconsin in 1957. Coenzyme Q10 is a yellow crystalline substance that belongs to a class of compounds called quinones. Since all living things create some form of this compound for energy production, it was given the chemical name ubiquinone, which is a contraction of ubiquitous (meaning everywhere) and quinone.

Dr. Crane sent a sample of the yellow crystals he had isolated from beef heart mitochondria to Dr. Karl Folkers for analysis and confirmation. At the time, Folkers was a leading biochemist at the pharmaceutical company Merck, Sharpe and Dohme. In 1958, Dr. Folkers determined the exact structure of CoQ10 and conducted some preliminary studies, which suggested that CoQ10 had enormous potential as a cardiovascular drug. When Folkers made his recommendations to Merck’s top management, they were not interested because Merck had recently launched a new blood pressure-lowering drug named Diuril. Since Merck had already trained their drug sales force and committed a huge budget to marketing and advertising Diuril, they did not want to introduce another cardiovascular drug into the marketplace that would compete with their own newly launched drug. Subsequently, Merck sold the patents rights on CoQ10 to a Japanese firm.

It took the Japanese about ten years to learn how to develop the technology that enabled the production of pure coenzyme Q10 in quantities that were adequate to support clinical trials in heart failure patients in Japan. During this ten year development time period, some small trials revealed that the ubiquinol form of CoQ10 was also a powerful antioxidant. As an energizer and an antioxidant, CoQ10 was found to be an effective natural product for the management of individuals with congestive heart failure.

Coenzyme Q10 and Energy Production:
Coenzyme Q10 in the oxidized form (ubiquinone) is required for energy production in the mitochondria of all cells except the red blood cells. Specifically, CoQ10 is required in several steps of what is called the electron transport chain in mitochondrial inner membranes, which is where cellular energy, knows as ATP, is produced. In the 1960s, biochemist Peter Mitchell, Ph.D. first put forth his theories on how coenzyme Q10 participates in and is required for energy production in mitochondria. In 1978, Dr. Mitchell was awarded the Nobel Prize in Chemistry for his discovery. Peter Mitchell is still recognized as the scientist who revolutionized coenzyme Q10 research and educated the world about CoQ’s central role in the production of energy in all living organisms.

Coenzyme Q10 deficiency and the resulting decline in energy production quickly affects systems in the body that have high metabolic energy requirements such as the lungs, kidneys, brain, immune system and muscles. Yes, especially muscles. Since the heart is the most energy-demanding muscle in the body, one of the first effects of CoQ10 deficiency is a weakening of the heart.

Coenzyme Q10 Deficiency And Congestive Health Failure:
Because CoQ10 deficiency reduces the ability of the heart to generate energy, some of the first observations regarding this newly discovered nutritional substance were that patients with congestive heart failure had low levels of coenzyme Q10. Based on these early findings, some of the first clinical trials with CoQ10 involved patients with chronic heart failure, which is also known as congestive heart failure. And, CoQ10 therapy in patients with heart disease turned out to be ASTOUNDINGLY successful. In fact, the author of one study felt compelled to call CoQ10 therapy a scientific breakthrough in the management of chronic heart failure.¹

Initially, coenzyme Q10 was introduced in Japan as a prescription drug for the treatment of various forms of cardiovascular disease. It remained one of the top-selling cardiovascular drugs in Japan for over twenty years. In 1991 coenzyme Q10 was taken off prescription drug status and made available as an over-the-counter product to the general public. Almost immediately, use of CoQ10 in Japan skyrocketed, which caused a world-wide shortage of supply and resulted in a substantial increase in its price.

Coenzyme Q10: A Critical Antioxidant
Coenzyme Q10 in the reduced form (Ubiquinol) is a fat-soluble antioxidant that is made in all cells throughout the body. In fact, CoQ10 is the ONLY fat-soluble antioxidant that is made in the body, which results from the enzymatic conversion of ubiquinone to ubiquinol. CoQ10’s (Ubiquinol) most important functions are its ability to inhibit oxidative free radical damage to the fats that comprise the structure of cellular membranes throughout the body.²

For decades cardiologists have prescribed statin drugs in the belief that elevated LDL-cholesterol is a major risk factor for cardiovascular disease. There is increasing skepticism regarding the level of risk associated with elevated LDL-cholesterol and the frequent prescribing of statins. However, it is well accepted that when LDL-cholesterol undergoes free radical damage, it becomes a “damaged” molecule that is referred to as oxidized LDL-cholesterol. Oxidized LDL-cholesterol is capable of causing damage to the lining of the blood vessels. In a simplification of a complex process, we can simply say that the body creates plaque deposits in an effort to repair this damage. So, it is really oxidized LDL-cholesterol that initiates plaque build-up and increases the risks of heart attacks and strokes.

In a 1997 study on coenzyme Q10 and statin drugs, cardiologist Svend Mortensen made the following important statement. Dr. Mortensen announced that CoQ10 is an antioxidant that is “packaged into the LDL & VLDL fractions of cholesterol.” This means that the LDL cholesterol molecule is the primary method by which coenzyme gets transported around the body. Thus, when CoQ10 is being transported on the LDL cholesterol molecule, CoQ10’s antioxidant properties enable it to protect LDL cholesterol against oxidative damage. This is one way that CoQ10 reduces cardiovascular disease risks.³

Coenzyme Q10 Lowers Elevated Blood Pressure
In 1980, Dr. Folkers reported treating 16 patients with high blood pressure (10 already taking BP meds and 6 untreated) with CoQ10 14 of 16 patients achieved significant lowering of systolic blood pressure and 11/16 achieved significant lowering of diastolic blood pressure. In the patients who had elevated blood pressure even though they were taking BP-lowering drugs, 9 of 10 achieved reductions that brought their blood pressure readings into the normal range.⁴

Another study that demonstrates coenzyme Q10’s blood pressure lowering ability was conducted by cardiologist Peter Langsjoen. He selected 109 of his patients with hypertension and added CoQ10 (average dose was 225 mg/day) to their existing medications. The average time of from initial diagnosis was 9.2 years and many patients were taking two or three blood pressure-lowering medications to keep their pressure within the acceptable range. Within six months of initiating high-dose CoQ10 therapy, 55 of 109 (51 percent) of the patients experienced reductions in their blood pressure readings that enabled them to discontinue taking their blood pressure medications.⁵

More recently, a meta-analysis of 12 clinical trials reported that CoQ10 lowered systolic blood pressure by 17 points and it lowered diastolic blood pressure approximately 10 points.⁶ Thus, the blood pressure lowering effect of coenzyme Q10 is sufficient to keep hundreds of thousands of individuals with borderline hypertension from having to take blood pressurelowering medications.

The FDA Inhibits Education
Utilization of coenzyme Q10 in the United States has lagged behind that of Japan and European countries for several reasons. Nearly 2,000 studies have been published in which either coenzyme Q10 or CoQ10 appear in the title of the study. However, in the United States, FDA policy prohibits nutritional supplement companies from making ANY reference to ANY health claims regarding a nutritional product. This greatly inhibits the public's access to educational information about the benefits of nutritional supplements. Also, pharmaceutical companies are not interested in promoting information about CoQ10 or CoQ10 products because it is a natural product, which means a drug company cannot have an exclusive patent on it. Another reason drug companies don't want the word to get out about coenzyme Q10 is the fact that it is SAFER and MORE EFFECTIVE than most cardiovascular drugs on the market, which is a multi-billion-dollar market for the pharmaceutical industry.

Coenzyme Q10 And Statin Drugs:
In 1987 the FDA approved the first statin drug named lovastatin, which was marketed by Merck under the brand name Mevacor. Statins work by blocking an enzyme in the liver named HMGCoA reductase, which is required for the biosynthesis of cholesterol. When a statin drug blocks HMG-CoA reductase, the synthesis of cholesterol is inhibited and cholesterol blood levels decline fairly rapidly.

Lovastatin's success at lowering cholesterol levels resulted in other drug companies bringing their version of a statin drug to the market. Statin drugs became a "goldmine" for the pharmaceutical industry. There are currently seven statin drugs available in the United States and statins became one of the best-selling classes of drugs in history. In 2011, global sales of statin drugs exceeded $39 billion. Also, in 2009 and 2010, Lipitor (atorvastatin) was ranked as the #1 selling drug in the world with 2009 sales of $11 billion and 2010 sales of $10 billion.

The Dark Side of Statin Drugs:
It is estimated that about 32 million Americans (about 25 percent of people aged 45 and older) are taking statin drugs. In February 2016, The FDA mandated the addition of new warnings regarding potential statin drug side effects which include increased risks of liver damage, confusion and memory loss, type 2 diabetes and muscle weakness.

One of the most serious side effects of statin drugs is something that the FDA has still refused to address. The HMG-CoA reductase enzyme that is critical for cholesterol synthesis is also required for the synthesis of coenzyme Q10. Multiple studies document the fact that in addition to lowering cholesterol levels, statin drug therapy also causes a dramatic decline in coenzyme Q10 levels.^7,8

Drugs That Deplete Coenzyme Q10:
In addition to statins, the following other classes of commonly prescribed drugs deplete coenzyme Q10; oral contraceptives, hormone replacement therapy (HRT), oral hypoglycemic drugs such as metformin for the treatment of type 2 diabetes, thiazide diuretics, beta-blockers and tricyclic antidepressants. Because they inhibit the production of CoQ10, these drugs induce low energy syndromes resulting in reduced muscle function.

Next month, in Part 2 of this series we will discuss coenzyme Q10's role in the prevention and treatment of cancer and various other diseases, its function as an effective anti-aging nutrient, and issues related to CoQ10 recrystallization and the relative absorption and effectiveness of various CoQ10 products on the market.

References

1. Morensen SA. Coenzyme Q10: clinical benefits with biochemical correlates suggesting a scientific breakthrough in the management of chronic heart failure. Int J Tissue Teact. 1990;12(3):155¡V 62.
2. Littarru GP, Bioenergetic and Antioxidant Properties of Coenzyme Q10: Recent Developments. Molecular Biotechnology. Sept. 2007; 37(1):31-7.
3. Mortensen SA. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med. 1997;18 Suppl:S137-44.
4. Folkers K. Bioenergetics in clinical medicine. XVI. Reduction of hypertension in patients bytherapy with coenzyme Q10. Res Comm Chem Pathol Pharmacol. 1981 Jan;31(1):129-40.
5. Langsjoen P. Treatment of essential hypertension with coenzyme Q10. Mol Aspects Med. 1994;15 Supp:S265-72.
6. Rosenfeldt FL, el al. Coenzyme Q10 in the treatment of hypertension: a meta-analysis of the clinical trials. Journal of Human Hypertension. 2007 apr;21(4):297-306.
7. Mortensen SA. Dose-related decrease of serum coenzyme Q10 during treatment with HMG-CoA reductase inhibitors. Mol Aspects Med. 1997;18 Suppl:S137-44.
8. G. Ghirlanda, et al., "Evidence of Plasma CoQ10-lowering Effect by HMGCoA Reductase Inhibitors: A DB PC Study," J Clin Pharmacol. March 1993; 33(3): 226-9

I consider the benefits of most medications used to lower cholesterol (called “statin medications”) to be modest at best in those without known heart disease (called “primary prevention”). These medications lower heart attack death risk by less than two percent. To put this in perspective, having optimal thyroid levels, even when normal, is associated with a 69 percent lower risk of heart attack death. Even owning a cat is associated with a 30 percent lower risk. Despite these minimal benefits, the relatively high expense (costing the health care system over $12 billion a year), and the aggravating pain and fatigue that accompany their use in some patients, they are being heavily pushed — even being heavily marketed to pediatricians now.

I suspect this would not be happening if the medications were not so profitable, as controlling high blood pressure, decreasing excess sugar intake, exercising, stopping smoking and even eating fish are likely more heart protective than the medications — but simply less profitable.

A 2010 meta-analysis using data from 13 clinical trials with 91,140 participants shows these medications are associated with a nine percent increased risk of developing diabetes.¹

It is a good idea, of course, to follow your doctor’s advice. But it’s also okay to recognize that they are being targeted with massive amounts of drug company promotion, including conferences described by some as “advertisements masquerading as scientific activities.”

If you have a known heart problem, the benefits of these medications go way up. If not, it is okay to ask your doctor if improving diet, avoiding sugar, exercising, eating oily fish (tuna and salmon 3–4x week) and stopping smoking may be more beneficial.

References:

1. World J Diabetes. 2015 Mar 15; 6(2): 352–357.

Sometimes blind faith leads to a disaster. Sometimes a miracle. Where will you end up? If you're one of the millions of people diagnosed with high cholesterol, you will more than likely be given a prescription "statin" pill. These work well to reduce cholesterol: Lovastatin for Mevacor, atorvastatin for Lipitor, pravastatin for Pravachol, fluvastatin for Lescol, simvastatin for Zocor, pitavastatin for Livalo, and rosuvastatin for Crestor.

Statins affect many pathways in the body. They are strong anti-inflammatories and are being tested for their use in cancer patients. As for cholesterol reduction, they work by crushing a natural enzyme in your body that would otherwise produce cholesterol. I want you to make a mental note, statins do not suck out gooey cholesterol from your arteries, nor does it negate cheese fries. No, these drugs merely suppress new production of cholesterol. Here's where blind faith (take this pill and you'll feel better) collides with scientific research.

This month a study was published (in the Expert Review of Clinical Pharmacology), entitled, Statins stimulate atherosclerosis and heart failure: pharmacological mechanisms. Repeat: "Statins stimulate atherosclerosis and heart failure." Whoa! The researchers concluded, "The epidemic of heart failure and atherosclerosis that plagues the modern world may paradoxically be aggravated by the pervasive use of statin drugs." What an irony! The problem is that many other studies have found similar disastrous effects on the heart. It has to do with mitochondrial dysfunction, which means that the little generators in your heart cells get sick.

Your heart is a very high energy muscle. It requires thriving, mitochondria in order to churn out ATP, your energy molecule. Statins are toxic to mitochondria because they deplete coenzyme Q10 which is needed for healthy mitochondria. Statins also deplete a special protein called "Heme A" that totes oxygen and iron to your heart. The long-term depletion interrupts ATP production and leads to cellular fatigue among other major problems. You cannot survive long-term without adequate ATP production so it needs to be restored. Fatigue, cramps, muscle weakness, memory loss, depression, cancer… you must have ATP in your body or else! (Biting my lip)

Statins inhibit the biosynthesis of vitamin K2 which we manufacture if we have healthy intestinal gut flora. Do you? I don't know anyone who has a perfect gut. K2 also comes from fermented veggies. It protects our arteries from calcium plaques or atherosclerosis. Without enough K2, statin-induced or not, we are compromised. (Eyes rolling now).

Today, we know statins block very special, powerful selenium-containing proteins known as selenoproteins, the most famous of those is called glutathione peroxidase, which protects muscle tissue from free radical damage (oxidation).

What's the busiest muscle in your body? It has to work 24/7. It's your heart! (Smacks forehead).

Your heart muscle cells are 'burned' form all the oxidation (due to the impairment of selenoprotein biosynthesis) and this is a factor in congestive heart failure. This reminds me of Keshan's disease which is heart failure due to low selenium.

If you have to take statins, please use the lowest dose possible. Be diligent about putting back the nutrients that statins interfere with such as the coenzyme Q10, selenium, and vitamin K2, along with other heart healthy nutrients. There are exceptions to taking these nutrients so ask your doctor (yes, the same one that gave you the statin) This is a classic case of drug mugging, and I hope you will consider replenishing some of the affected nutrients, especially if you have uncomfortable or new symptoms. Talk to your physician about dosages of these vitamins, because this is a highly individual.