Idebenone, a Drug with a Myriad of Antiaging Benefits

Idebenone, a Drug with a Myriad of Antiaging Benefits

When the coenzyme (the active part of a vitamin)- CoQ10 was first discovered and discussed and found to have heart, blood and energy improvement it soon became apparent that it was a most important supplement.

Now there is also a synthetic variant available called Idebenone, it has all the qualities of CoQ10 but with an even greater range and depth of protection. It protects the precious tiny mitochondria (the energy producing cells) and even has brain-enhancing qualities.

It is, if you like, the "ultimate" CoQ10 and as such qualifies as an important anti-aging supplement.

Mitochondria, Oxygen and Energy Production

There are literally thousands of mitochondria in every cell of our body. Their primary role is to produce pregnenolone (see the same)- the precursor to the steroids and to produce ATP (adenosine triphosphate)- the "raw energy" that powers virtually every activity of our bodies.

In the process of producing ATP, the mitochondria utilize oxygen and CoQ10 in a process of energy production called the "electron transport chain" or ETC.

Unfortunately oxygen can also be a potent free radical (unstable- out of control- molecules). As a result of the amount of oxygen used inside the mitochondria (in fact most of the oxygen we breathe is used inside the ETC to produce ATP), a lot of free-radical damage can occur.

Free radicals therefore have to be "mopped up" by free radical scavengers and protected from occurring by anti-oxidants. If left "unchecked" free radical damage inside the mitochondria will eventually lead to its malfunction and eventually cessation. As cells cannot "borrow" energy from one another, in the end, the organ they " provide" for becomes damaged and ultimately this will lead to organ failure and possibly death.

Whilst under "normal" circumstances CoQ10 provides protection and free radical scavenging, this can change under the condition of ischemia (poor blood flow).

This can take happen during a heart attack, stroke, trauma or shock, it can even be affected by general poor blood supply due to "aging" affecting the condition of the heart's pumping capabilities. As a result of poor blood supply the oxygen levels drop and this causes CoQ10 to oxidize itself, effectively turning itself into another free radical! Under more extreme conditions a large presence of free radicals can cease ATP production and therefore create a life threatening condition.

This is one key-area where Idebenone has been shown to be much more effective than CoQ10. Under the same hypoxic (low oxygen) conditions that cause CoQ10 to become oxidized- Idebenone prevents free radical damage and maintains relatively normal ATP production.

Idebenone should therefore be the supplement of choice for those concerned with stroke, heart conditions, shock, trauma and mitochondrial failure/ conditions.

Slowing Aging

The mitochondria are key life-preserving cells producing over 90% of ATP bio-energy. As we've seen their vast use of oxygen exposes them to free radicals and therefore over a lifetime they become ever more damaged and therefore inefficient.

The mitochondria most at risk from aging- free radical damage are those in the heart, brain and skeletal muscles. Therefore a key aspect of current anti-aging thinking is to slow down/ prevent damage from occurring to mitochondrial function. According to the research, Idebenone is the current- most effective drug capable of performing this task.

Dementia, Memory and Cognition

Nerve Growth Factor (NGF) plays an important role in the survival and maintenance of cholinergic neurons in the central nervous system (CNS).

In dementia's such as Alzheimer's, it is known that learning and memory are impaired by the loss of neurons in an area of the brain called the magnocellular cholinergic neuronal system.

Nerve Growth Factor cannot cross the blood brain barrier and in scientific experiments, it has only been able to be utilized when it is injected directly into the brain. However, animal experiments have shown that oral use of Idebenone tablets induce an increase in NGF and improve choline- acetyltransferase activity.

One rat study demonstrated that Idebenone stimulated NGF synthesis and recovered reduced NGF content in aged rat brains. After 21 days of successive Idebenone supplementation the NGF brain quantity of aged rats was increased to an amount similar to young rats.

As a result of these studies, Idebenone is being used in the treatment of senile dementias, particularly Alzheimer's disease. In a German clinical study, 90mg of Idebenone was administered for 6 months; Alzheimer patients thereafter showed statistically significant improvement.

Treatment with Idebenone was found effective on memory, attention and orientation. Perhaps most importantly of all, Idebenone slowed down the natural progression of the disease.

Furthermore, there were so few (and minor) side effects that the study ended with "... results demonstrate the efficacy and safety of Idebenone in the treatment of Alzheimer's disease patients."

Once again, as with most nootropics, clinical trials indicate that patients with mild dementia seem more likely to respond, than those with greater functional decline.

It's the old story, catch it and treat it early before it becomes a major problem.

Comparing CoQ10 and Idebenone

  1. Idebenone is so much more potent than CoQ10 in its anti-oxidant abilities. In fact, studies indicate that Idebenone is 30-100 times more effective than vitamin E or vinpocetine as a free radical quencher.
  2. Idebenone protects under hypoxic conditions, a situation where CoQ10 can become quite the reverse.
  3. Idebenone (unlike CoQ10) has been shown to increase Nerve Growth Factor and enhance cholinergic activity, thereby showing it to have cognitive enhancement abilities.
  4. Idebenone is a superb anti-oxidant for protecting the all important mitochondria, by both "mopping up" free radical activity and protecting the unique mitochondrial DNA (mtDNA)- unique because it is only derived from our mother's genes.

In fact when organs are "harvested" for transplant to another patient, very often it is Idebenone that is used to protect it from damage. That is the level of free radical protection offered by Idebenone.

However, rather than switching from CoQ10 to Idebenone, some studies have suggested that adding Idebenone to a CoQ10 supplement is the best way to "cover all the bases."

Side Effects and Contraindications

Side effects have been rare and usually of mild intensity when they do occur. Those noted have been insomnia, gastralgia, nausea and anxiety. There are no known contraindications, but it is known that concurrent use of anti-convulsants will affect/ impede its pharmacokinetics.

Doses and Uses

Idebenone may be useful in the treatment and prevention of all the following,

  • Stroke.
  • Alzheimer's disease.
  • Liver, kidneys, heart or brain disturbances.
  • Multiple Sclerosis.
  • Chronic fatigue.
  • Persons in need of "high-energy" quotas.
  • Anti-aging protection.

Normal anti-aging doses may be considered at 45mg to 90mg daily, (normally one or two tablets). For specific treatment purposes dosages of 45-90mg three times a day may be required. It is suggested that late evening use by avoided in order to help prevent insomnia.

CoQ10 was one of the "earth-shattering" discoveries in recent years and as such has become a well-known and demanded supplement. Idebenone with its even greater and broader range of uses is (we feel), also likely to impact onto the general public's attention. This is going to occur as soon as the word spreads and the momentum has reached a certain point.

Ed.- The above article is extracted with kind permission from the International Guide to AntiAging Drugs (available from IAS).

References

  1. Parnetti L, Senin U, Mecocci P, "Cognitive enhancement therapy for Alzheimer's disease. The way forward." Drugs 1997 May; 53(5):752-768.
  2. Weyer G, Babeji-Dolle RM, Hadler D, Hofmann S, Herrmann WM, "A controlled study of 2 doses of Idebenone in the treatment of Alzheimer's disease." Neuropsychobiology 1997; 36(2):73-82
  3. Ranen NG and colleagues, "A controlled trial of Idebenone in Huntington's disease" Mov Disord 1996 Sep; 11(5):549-554
  4. Ikejiri Y, Mori E, Ishii K, Nishimoto K, Yasuda M, Sasaki M, "Idebenone improves cerebral mitochondrial oxidative metabolism in a patient with MELAS" Neurology 1996; Aug 47(2); 583-585.
  5. Pisano P and colleagues, "Plasma concentrations and pharmacokinetics of Idebenone and its metabolites following single and repeated doses in young patients with mitochondrial encephalomyopathy." Eur J Pharmacol 1996; 51(2):167-169.
  6. Gillis JC, Benefield P, McTavish D, "Idebenone, a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in age-related cognitive disorders." Drugs Aging 1994; Aug;5(2): 133-152.
  7. Bergamasco B, Scarzella L, LaCommare P, "Idebenone, a new drug in the treatment of cognitive impariment in patinets with dementia of the Alzheimer type." Funct Neurol 1994; May;9(3):161-168
  8. Nitta A and colleagues "Oral administration of Idebenone induces nerve growth factor in the brain and improves learning and memory in basal forebrain-lesioned rats." Dept of Neuropsychopharmacology, Nagoya University, Japan.
  9. Nitta A, Hasegawa T, Nabeshima T, "Oral administration of Idebenone, a stimulator of NGF synthesis recovers reduced NGF content in aged rat brain." Neuosci Lett 1993 Dec 12; 163(2):219-222.
  10. Kakihana M, Yamazaki N, Nagaoka A, "Effects of Idebenone on the levels of acetylcholine, choline, free fatty acids and energy metabolites in the brains of rats with cerebral ischaemia." Arch Gerontol Geriatr 1989 May 8(3);247-256
  11. Ihara Y, Namba S, Sato T, Shiraba T, "Mitochondrial encephalomyopathy (MELAS), pathological study and successful therapy with coenzyme Q10 and Idebenone." J Neurol Sci 1989 May; 90(3):263-271.
  12. Suno M, Nagaoka A, "Inhibition of brain mitochondrial swelling by Idebenone." Arch Gerontol Geriatr 1989 May; 8(3):299-305.

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