By Barry Keate
Barry Keate, has lived with tinnitus over 40 years and has published 150+ research articles on numerous aspects of tinnitus. He is an expert on the condition and a well-known advocate for those with tinnitus.
High levels of cholesterol in the bloodstream, especially the LDL “bad cholesterol”, can lead to heart disease, heart attack, or stroke. Statin medications, such as Lipitor, Mevacor, Crestor, Zocor, and others, are frequently prescribed to lower cholesterol levels. A major side effect is they significantly reduce the level of Coenzyme Q10 (CoQ10) in the body resulting in deficiency of this critical compound.
Statin drugs are very expensive and come with significant side effects. The statin drug class is the largest and most profitable of all prescription medications, costing $22 billion per year in the US. This represents 8% of the total American drug cost of $270 billion.
In this article we will explore the effect of statin drugs on critical ailments including tinnitus and how the compound Coenzyme Q10 (CoQ10) can mitigate the deleterious side-effects of these popular prescription medications.
History of CoQ10
To fully appreciate the tinnitus – CoQ10 connection it is important to review the recent history of this important enzyme and its relationship to disease states.
CoQ10 was discovered in 1957 by Frederick Crane, PhD at Purdue University in Indiana. Four years later, Peter D. Mitchell, PhD, of the University of Edinburgh, figured out how CoQ10 produces energy at the cellular level and won the 1978 Nobel Prize in chemistry for this discovery.
CoQ10 is a fat-soluble compound and is found in virtually every cell in the body. It is required for the conversion, or burning, of fats in the mitochondria of the cells to produce energy in the form of adenosine triphosphate (ATP). ATP is the energy powerhouse of the cells and provides energy for all cellular and biological operations. Without ATP production the cells and eventually the entire organism will die. CoQ10 is also a powerful antioxidant.
CoQ10 is a member of the ubiquinone family of compounds. Vitamins are coenzymes and both are necessary for fostering thousands of essential biochemical processes. Since the human body can synthesize coenzyme Q10 from food, it is not considered to be a vitamin. The name ubiquinone refers to the ubiquitous presence of these compounds in all living organisms. Now there is evidence that CoQ10 supplementation can be helpful for a certain subset of tinnitus patients, those who are deficient in the enzyme.
Most commercial CoQ10 consists of ubiquinone, which provides satisfactory absorption for most people. As we age, we are not able to absorb CoQ10 as readily as younger people. Also, those with advanced congestive heart failure are not able to absorb this properly due to fluid retention, or edema, which occurs in the liver and intestines in these critically ill patients.
CoQ10 is synthesized in the body primarily from amino acids. These are found mainly in organ meats, poultry and fish with smaller amounts coming from soybean and canola oil, and nuts. Adequate vitamin B6 nutrition is essential for CoQ10 biosynthesis. The average dietary intake of CoQ10 in the western world is estimated at 3-5 mg/day.
CoQ10 and Aging
According to the free radical and mitochondrial theories on aging, oxidative damage of cells by reactive oxygen species (ROS), often called free radicals, plays an important role in the functional declines that accompany aging. 1 ROS are generated by mitochondria as a byproduct of ATP production. If not neutralized by antioxidants, ROS damage mitochondria over time, causing them to function less efficiently and to generate more damaging free radicals in a self-perpetuating cycle. Eventually the damaged cells are unable to continue operating and die. CoQ10 plays a central role in mitochondrial ATP production and also functions as an antioxidant in mitochondrial membranes, neutralizing the free radicals. Tissue levels of CoQ10 have been reported to decline with age. 2
CoQ10 and Cancer
Two medical journal articles suggest tremendous promise in the treatment of cancer. One study conducted on 10 cancer patients who were also given CoQ10 for heart failure showed survival for periods of five to 15 years. 3 Another study using CoQ10, antioxidants and essential fatty acids for 32 breast cancer patients found that all patients survived for 24 months when about 6 deaths would have been expected. One patient had a tumor removed surgically. It returned but stabilized at 1.5 – 2 cm after the patient began taking 90 mg CoQ10 daily. One month after increasing the dose to 390 mg, the tumor completely disappeared, confirmed by mammography. 4
CoQ10 and HIV/AIDS
One of the most remarkable findings was that CoQ10 supplementation can extend the lifespan of patients with Acquired Immune Deficiency Syndrome (AIDS). In 1986 researchers began treating seven patients with HIV or AIDS. Not all the patients consistently took the CoQ10 but “treatment was very encouraging and at times even striking… All 7 patients felt better soon after starting on CoQ10.” 5
CoQ10 and Cardiovascular Disease
Oxidation of low-density lipoproteins (LDL, the “bad” cholesterol) in arterial walls is thought to represent an early condition leading to the development of atherosclerosis (excessive plaque build-up in blood vessels). CoQ10 inhibits the oxidation of LDL. Studies with atherosclerotic mice found that CoQ10 supplementation significantly inhibited the formation of atherosclerotic lesions (arterial plaque). 6
Human studies also show that CoQ10 is a valid adjunct treatment for cardiovascular disease. In particular, a study of heart attack patients showed that compared to placebo, supplementation with 120 mg per day of CoQ10 reduced secondary cardiac events by 45% and significantly reduced the number of cardiac deaths. All of these heart attack patients were prescribed a statin drug to lower cholesterol levels. The active group was taking both statin drugs and C0Q10 while the placebo group took only a statin medication. The major adverse effect of statin treatment was fatigue that occurred in 40.8% of the statin-only group but only 6.8% of the patients supplemented with CoQ10 expressed fatigue. 7
Massive advertising by drug companies has resulted in millions of Americans taking statin drugs every day. Statins have now become the most profitable drug class in the world. While statin drugs do lower cholesterol, there is controversy as to how effective these drugs are in extending overall life span.
Peter H. Langsjoen, MD, a Texas cardiologist, is the foremost authority on the use of CoQ10 in the treatment of heart disease. His numerous research studies can be found in the world’s most prestigious scientific journals.
In 1990, the Proceedings of the National Academy of Science published Dr. Langsjoen’s studies on the safety of statin drugs. Dr. Langsjoen explained that the mechanism by which statin drugs lower cholesterol also inhibits the natural biosynthesis of CoQ10 in the liver. He wrote that he conducted these studies to learn “If lovastatin (Mevacor) were to reduce levels of CoQ10, this reduction would constitute a new risk of cardiac disease, since it is established that CoQ10 is indispensable for cardiac function.” Dr. Langsjoen then reported that his animal and human studies showed that lovastatin does indeed lower levels of CoQ10. He went on to describe case histories of his lovastatin patients who suffered from progressive cardiac degeneration but whose heart function improved after oral administration of CoQ10. 8
By July of 2002, Dr. Langsjoen had become a vocal critic of statin drugs and published a new paper titled “Statin-Induced Cardiomyopathy.” In an excerpt from this paper, Dr. Langsjoen describes his 17-year experience with statin drugs as follows:
“I have seen a frightening increase in heart failure secondary to statin usage…. Over the past five years, statins have become more potent, are being prescribed in higher doses, and are being used with reckless abandon in the elderly and in patients with normal cholesterol levels.” 9
Dr. Langsjoen attributes these heart failure cases as being caused by “statin-induced CoQ10 depletion” that is preventable if stain drug users supplement with CoQ10.
The evidence supporting CoQ10 as an antidote to statin drug complications is so clear that in 1989 and 1990 Merck patented the use of CoQ10 in combination with statin drugs to both prevent and treat these complications. However, Merck has neither exercised these patents nor educated physicians or patients about the necessity of taking CoQ10 along with statin drugs. One of the two Merck patents states that:
“Since Coenzyme Q10…is of benefit in congestive heart failure patients, the combination with HMG-CoA reductase inhibitors (statin drugs) should be of value in such patients who also have the added risk of high cholesterol. 10
Based on the overwhelming body of evidence of CoQ10 depletion from statin drugs, Julian Whitaker, MD, filed a petition in 2002 against the FDA that meticulously documented the many lethal effects that would occur if patients prescribed statin drugs were not supplemented with CoQ10. The object of this petition was to force the FDA to mandate on the package insert that patients taking stain drugs should also take CoQ10.
Dr. Whitaker asserts that most patients and doctors do not realize that stain drugs block the production of CoQ10. He went on to describe how CoQ10 has been found to be essential for cellular energy production as well as for the functioning of the heart muscle. His petition stated, “Statin drugs have proven in clinical trials to deplete Coenzyme Q10, the ‘sparkplugs’ of the human body. Patients who take statin drugs without Coenzyme Q10, particularly those with a history of heart disease, are especially prone to developing complications that can have fatal consequences. 11
The FDA has ignored the petition and, to this date, has not responded.
The Tinnitus Connection
As far back as 1988, researchers were aware that CoQ10 was effective in promoting recovery from acute sudden deafness. A Japanese study was conducted on guinea pigs with acute sensorineural hearing loss artificially induced by hypoxia (lack of oxygen) conditions. The results showed that CoQ10 “is effective in promoting recovery from damage in auditory hairs as well as preventing respiratory metabolic impairment of hair cells due to hypoxia.” 12
Based on recent findings that CoQ10 can also be effective for treating hypertension, muscular dystrophy and neurodegenerative diseases, researchers in Berlin, Germany decided to study its effects on people with tinnitus. 13 The study involved 20 patients with tinnitus and lasted for 16 weeks. Researchers recorded CoQ10 levels before the study began and used the Tinnitus Handicap Inventory (THI) to evaluate efficacy. Patients were given 100 mg three times daily.
At the end of the study, they found mean plasma concentration of CoQ10 significantly increased and was still elevated 4 weeks after the study ended. No statistical differences in the THI scores were recorded.
However, a subgroup of 7 patients (out of 20) had significant reductions in questionnaire scores from 38 to 24. These responders had a reduction in all dimension of the THI score compared with their initial values except for the dimension of emotional distress. The people in this group who responded well had a much lower level of CoQ10 before the study began than non-responders. Moreover, the increase of CoQ10 levels was significantly higher in responders than in non-responders. These results showed a significant improvement in tinnitus in those who initially had the lowest CoQ10 levels.
Everyone who is taking prescription statin drugs to lower cholesterol should be also taking supplemental CoQ10 to prevent damaging side-effects of the medication. Those who also have tinnitus, which most of our readership presumably has, should also use it for the potential of improving the condition.
There are many safe and effective ways to reduce cholesterol without resorting to statin medications. Diet and exercise are both highly effective for this and also for reducing tinnitus. Many herbs, vitamins and other supplements are also helpful.
Ubiquinone vs Ubiquinol
For many years the only form of CoQ10 on the market has been the ubiquinone form. This is the oxidized form of the molecule and the body must neutralize it before it can be absorbed and utilized. In 2007, the ubiquinol form was developed, which is the reduced form (not oxidized) which can be immediately absorbed and used by the body.
This is very important because people with chronic heart conditions and other illnesses are not able to fully absorb the ubiquinone form of CoQ10. The ubiquinol form is both water and fat soluble and is fully absorbed and utilized by these people.
Ubiquinol is more expensive than ubiquinone but that is offset by the fact that it is up to 8 times more absorbable and less can be used.
You may have seen the TV ads for Qunol CoQ10. This is advertised as being the most absorbable form of CoQ10. This is because is it consists of ubiquinol rather than the older ubiquinone. There are many other brands of ubiquinol on the market that are less expensive than Qunol.
Alternative Treatments for High Cholesterol
Omega-3 fatty acids found in fish oils reduce the risk of heart attack and lower cholesterol levels. Garlic does much the same. As discussed in last month’s article, B vitamins lower homocysteine, improving the health of arterial lining and preventing damage from plaque build-up. Niacin, or vitamin B3, is also known to lower cholesterol and, in high doses, can also help remove cholesterol from plaque in arterial linings.
Ginkgo biloba (found in Arches Tinnitus Formula®) also protects blood vessels and lowers cholesterol levels. A recent study into the effects of Ginkgo biloba found that it significantly lowers free circulating cholesterol. 14
Arches Tinnitus Formula for Tinnitus
Arches Tinnitus Formula is also very helpful for most people with tinnitus. It acts as an antioxidant, improves blood flow and reduces glutamate, an excitatory neurotransmitter that causes hyperactivity and tinnitus.
We do not advocate discontinuing any prescribed medication without the express approval of the prescribing physician. However, the addition of other therapies and supplements will help lower cholesterol and may lead to a reduced need for prescription medications.
1 – Beckman KB, Ames BN. Mitochondrial aging: open questions. Ann N Y Acad Sci. 1998;854:118-127.
2 – Kalen A, Appelkvist EL, Dallner G. Age-related changes in the lipid compositions of rat and human tissues. Lipids 1989;24(7):579-584.
3 – Folkers K, Brown R, Judy WV, Morita M. Survival of cancer patients on therapy with coenzyme Q10. Biochem Biophys Res Commun. 1993 Apr 15;192(1):241-5.
4 – Lockwood K, Moesgaard S, Folkers K. Partial and complete regression of breast cancer in patients in relation to dosage of coenzyme Q10. Biochem Biophys Res Commun. 1994 March 30;199(3):1504-8.
5 – Folkers K, Langsjoen P, Nara Y, et al. Biochemical deficiencies of coenzyme Q10 in HIV infection and exploratory treatment. Biochem Biophys Res Commun. 1988 Jun 16;153(2):888-96.
6 – Witting PK, Pettersson K, Letters J. Stocker R. Anti-atherogenic effect of coenzyme Q10 in apolipoprotein E gene knockout mice. Free Radic Biol Med. 2000;29(3-4):295-305.
7 – Singh RB, Neki NS, Kartikey K, et al. Effect of coenzyme Q10 on the risk of athero-sclerosis in patients with recent myocardial infarction. Mol Cell Biochem. 2003 Apr;246(1-2):75-82.
8 – Folkers K, Langsjoen P, Willis R, et al. Lovastatin decreases coenzyme Q levels in humans. Proc Natl Acad Sci USA. 1990 Nov;87(22):8931-4. Available at http://www.redflagsweekly.com/features/2002_july08.html. Accessed December 1, 2003. Brown MS. Coenzyme Q. sub. 10 with HMG-CoQ reductase inhibitors. United States Patent 4,933,165. June 12, 1990.
9 – Whitaker JM, MD. Citizen petition before the Department of Health and Human Services Food and Drug Administration, November 24, 2002.
10 – Sato K. Pharmacokinetics of coenzyme Q10 in recovery of acute sensorineural hearing loss due to hypoxia. Acta Otolaryngol Suppl. 1988 (458):95-102.
11 – Khan M, Gross J, Haupt H, et al. A pilot clinical trial of the effects of coenzyme Q10 on chronic tinnitus aurium. Otolaryngology-Head and Neck Surgery 2007(136):72-77.
12 – Yao ZX, Han Z. Drieu K. Papadopoulos V. Ginkgo biloba extract (EGb 761) inhibits beta-amyloid production by lowering free cholesterol levels. Nutr Biochem. 2004 Dec;15(12):749-56.
13 – Khan M, Gross J, Haupt H, et al. A pilot clinical trial of the effects of coenzyme Q10 on chronic tinnitus aurium. Otolaryngology-Head and Neck Surgery 2007(136):72-77.
14 – Yao ZX, Han Z. Drieu K. Papadopoulos V. Ginkgo biloba extract (EGb 761) inhibits beta-amyloid production by lowering free cholesterol levels. Nutr Biochem. 2004 Dec;15(12):749-56.