|
Idebenone
– The ultimate anti-aging drug?
by James South MA
Idebenone is a synthetic analog
(variant) of one of life's most essential biochemicals, coenzyme Q10 (CoQ10).
CoQ10 is an important antioxidant component of the lipid (fatty) membranes that
surround all cells, as well as the lipid membranes surrounding the various
organelles ("little organs"), such as mitochondria and microsomes,
inside cells.
CoQ10 is also an important member
of the "Electron Transport Chain" (ETC) within mitochondria, which are
the "power plants" of the cell. Most of the oxygen we breathe is used
inside the electron transport chain to produce much of the ATP bioenergy that
powers virtually every activity of our cells and bodies.
Without CoQ10, or a good
substitute, human life quickly ends, and Idebenone is a "better CoQ10"
that has been extensively researched the past 15 years.
CoQ10’s pro-oxidant action
When blood flow is seriously
reduced to any part of the body, as in a heart attack, stroke, trauma, shock, or
chronic poor blood circulation- cellular/ mitochondrial oxygen (O2) levels
quickly drop in the affected region. Yet because oxygen is seven to eight times
more soluble in the lipid zones of cell membrane, compared to the watery
compartments of the cell, there is still sufficient oxygen remaining in the
membranes of cells and organelles, as well as in the electron transport chain,
to auto-oxidize CoQ10. As the CoQ10 auto-oxidizes, hydrogen peroxide, superoxide
and hydroxl free radicals are rapidly formed in massive numbers. These free
radicals quickly damage cell/ organelle structure and function, as well as
rapidly halt ATP energy generation by the electron transport chain.
Brain and spinal cord cells are
especially prone to such damage, and may be irreparably damaged or even
destroyed within minutes.
Why Idebenone is superior to
CoQ10
Enter Idebenone to the rescue!
Studies have shown that under the same cellular low oxygen conditions that cause
CoQ10 to act as a pro-oxidant producer of damaging free radicals, Idebenone
prevents the free radical dam-age and maintains relatively normal cell ATP
levels. In short, while Idebenone can effectively substitute for CoQ10's
positive and life essential functions, it doesn't have CoQ10's free radical
producing and energy crashing "dark side" which occurs under hypoxic
(low oxygen) conditions.
Idebenone's potential benefits
fall into five categories; antiaging, energy enhancement, cognition enhancement,
organ protector and protector against excitatory amino acid neurotoxicity.
Idebenone – The anti-aging
benefits
The mitochondrial power plants
produce over 90% of all cellular ATP bioenergy. They are also generally the
richest sites in CoQ10 (or Idebenone). Mitochondrial DNA (mtDNA) allows
mitochondria to reproduce them-selves.
While the DNA in a cell nucleus
comes from both our parents, mtDNA comes exclusively from our mother's mtDNA.
There are typically two or three
copies of mtDNA in each mitochondrion, with average 1000 mitochondria per cell.
Because mtDNA exists in the "heart of the fiery furnace" where
electron "sparks" are constantly leaking as ATP is produced in the
electron transport chain, mtDNA is far more prone to free radical electron
damage than is the DNA in our cell nuclei that contains the
"blueprint" for our entire organism.
At the same time, the repair
capacity of mtDNA is much less than that of our cell nucleus DNA. As a
consequence, over the course of a lifetime our mtDNA becomes ever more damaged,
and the mitochondria produced therefrom become ever more ineffective at energy
generation.
Studies comparing heart tissue
from young people with that from elderly people have shown almost no significant
mitochondrial dysfunction in young hearts, with significant, often severe
mitochondrial dysfunction in elderly hearts.
The cells that are most
susceptible to mitochondrial energy depletion with advancing age are the brain,
skeletal muscle and heart muscle cells. Idebenone thus offers a prime anti-aging
effect here in several ways. Unlike CoQ10, even under the low oxygen conditions
that may occur periodically over a lifetime, Idebenone will serve as a powerful
mitochondrial free radical quencher, lessening the ever-increasing mtDNA damage
that occurs with age. Idebenone will work even better than CoQ10 within the
electron transport chain to keep energy production high, even under hypoxic
conditions. This is especially critical to brain and heart cells that may be
rapidly damaged during low ATP production episodes that occur due to poor tissue
oxygenation.
Idebenone – Energy enhancement
Iron is a "dual edged
sword." It is absolutely essential for life, it plays a central role in ATP
generation in the electron transport chain. Yet iron can also be a powerful
initiator of free radical production and cell structural damage, especially
under low oxygen conditions.
This occurs, for example, during
stroke, and during the gradual onset of Parkinson's disease. Studies have shown
that Idebenone can tightly couple oxidation to energy production. This prevents
iron ions from wastefully and toxically, diverting oxygen to producing free
radicals inside the mitochondria, instead of energy.
Studies have shown that Idebenone
can almost completely eliminate this, diverting 10% of cellular oxygen away from
toxic iron induced free radical generation, to beneficial ATP energy production
under hypoxic conditions.
Mild cellular hypoxia can occur
even from intense exercise, or even from mild exercise done by out of shape
"couch potatoes."
Idebenone – Cognition
enhancement
A variety of studies using brain
cells, (animal and humans) have shown Idebenone's ability to enhance brain
structure and function.
Human and animal studies have
demonstrated that Idebenone can enhance serotonin production, even under far
less than optimal conditions, as e.g. with a very low tryptophan diet, or in
patients with cerebrovascular dementia.
Idebenone has enhanced
cholinergic nerve function and consequent learning ability even under hypoxic
conditions, or when an anti-cholinergic drug (Scopolamine) was administered.
Idebenone has increased cellular
catecholamine (dopamine, adrenalin and noradrenanlin) production by enhancing
cellular uptake of the precursor amino-acid tyrosine.
Idebenone enhances long term
potentiation in hippocampal nerve cells, a key part of memory formation and
consolidation. Idebenone has restored glucose (brain fuel) utilization and ATP
production in ischemic (poor blood flow) rat-brain.
Idebenone has been shown to
enhance general cerebral metabolism, lessen the damage from strokes, and has
been used to treat Alzheimer's and other dementias.
And like the original nootropic
drug; piracetam, Idebenone has been shown to promote information transfer across
the corpus callosum, the membrane separating the right and left brain
hemispheres.
This is turn may promote the
union/ integration of the logical (yang) and intuitive (yin) halves of the
brain/ mind.
Idebenone – Organ protector
As our organs age or are damaged,
we age and are damaged. Over a lifetime, blood flow to our organs diminishes due
to arteriosclerosis and less efficient heart pumping. This reduces oxygen
dependent energy production needed for repair, reproduction and normal function
of the organ cells. Free radical damage accumulates over time, leaving ever more
dead, dying or dysfunctional cells within organs.
At some point a critical
threshold is reached when too many cells within an organ are dysfunctional, and
they can no longer sustain the organ's life and function. Then the organ- heart,
brain, liver etc. fails.
Idebenone protects organs in many
ways, it cushions them against hypoxic (low oxygen) and/ or ischemic (poor blood
flow) damage. Idebenone enhances both normal and hypoxic ATP energy generation.
Each cell in our organs must
produce the energy it needs for life and health, cells cannot "borrow"
energy from each other.
Idebenone – The free radical
quencher
Idebenone is a powerful
antioxidant, more so than CoQ10, and in some studies is 30 to 100 times more
effective, than vitamin E or vinpocetine as a free radical quencher within the
brain cells.
Idebenone lessens the free
radical induced mtDNA damage that accumulates acceleratingly over a lifetime,
slowing organ damage and aging.
A 1995 study in the Journal of
Transplantation compared the organ preserving effects of CoQ10 and Idebenone.
The study measured various factors, such as free radical membrane lipid damage,
cell protein damage and cellular energy production under hypoxia conditions.
The results showed Idebenone to
be dramatically more effective than CoQ10 at preserving liver tissue under
conditions identical to that endured by whole livers "harvested" and
stored (briefly) before transplant to another person.
The study recommended using
Idebenone to increase the transplant viability of human livers donated for organ
transplant. Why not use Idebenone to increase your own organ viability, while
you still have the use of them!
Protection against excitatory
amino acid (EAA) neuro toxicity
Glutamic acid and aspartic acid
are the two chief excitatory amino acid neurotransmitters in the human brain.
Without them we would be "mental vegetables."
Yet under certain conditions,
e.g. stroke or traumatic brain injury- excessive amounts of excitatory amino
acids accumulate in the fluid surrounding brain cells, causing damage and even
death to nerve and glial cells through free radical mechanisms.
Excitatory amino acid toxicity is
at least partly responsible for the neurotoxicity of the recreational drug
"Ecstasy or MDMA." Studies over the past 30 years have also shown that
excessive dietary intake of excitatory amino acids may also damage brain
structure/ function, especially in children or excitatory amino acid sensitive
adults.
The two main dietary sources of
excitatory amino acids are the flavor enhancer MSG (monosodium glutamate) and
the artificial sweetener aspartame (Nutrasweet). Also many processed foods (e.g.
canned soups, dry roasted spiced peanuts, beef/ chicken bouillon, canned tuna,
spices etc.) contain "hydrolized vegetable protein, yeast extract, soy
protein isolate" and similar ingredients that are mostly excitatory amino
acids.
In studies with various types of
nerve cell, as well as oligodendroglial cells (which make up the protective
myelin sheaths surrounding many nerves, the so-called "white matter"
of the brain). Idebenone has shown dramatic protective effects against glutamate
toxicity.
Summary
With all these powers, Idebenone
should now rightfully take its place in the first rank of anti-aging/ nootropic/
energizer drugs, along with Hydergine, piracetam, vinpocetine, deprenyl and GH3/
KH3 (and it's one of my personal favorites!)
So who can benefit from Idebenone?
The answers are,
1.
Healthy people wishing cognitive enhancement and brain energizer effects (it
synergizes well with piracetam, vinpocetine and Hydergine). 2 or 3 tablets (45mg
each) daily.
2.
Stroke victims wishing to improve memory, emotional or speech disturbances. 3 to
6 tablets (45mg each) daily.
3.
Alzheimer's and cerebrovascular dementia patients. 4 to 6 tablets (45mg each)
daily.
4.
Those preparing for major surgery, especially brain, heart, liver or kidney.
Synergizes well with Hydergine. 4 to 6 tablets (45mg each).
5.
People with heart energetics problems, e.g. cardiomyopathy, ischemic heart
disease, congestive heart failure. 3 to 6 tablets (45mg each) daily.
6.
People with myelination problems, e.g. multiple sclerosis or "white
matter" stroke injury. 3 to 6 tablets (45mg each) daily.
7.
Those seeking to increase their general energy and vitality levels. 2 to 3
tablets (45mg each) daily.
8.
People with especially high endurance energy needs, e.g. cross country skiers,
long distance runners, cyclists, swimmers etc. 3 to 4 tablets (45mg each) daily.
9.
Those
at risk of excitatory amino acid brain damage, e.g. people who routinely consume
large amounts of aspartame sweetened foods/ drinks, or those who routinely eat
MSG or "hydrolyzed vegetable protein" containing restaurant or
prepared foods. 2 or 3 tablets (45mg each) daily.
10.
People wishing to enhance the brain serotonin benefits of tryptophan or
5-hydroxy-tryptophan supplements or SSRI drugs, such as Prozac, Paxil, Zoloft, or
Luvox etc. 2 to 4 tablets (45mg each) daily.
11.
Those suffering acute or chronic liver damage from poison mushrooms, toxic
chemicals, hepatitis etc. 2 to 4 tablets (45mg each) daily.
12.
People desiring a "long haul" broad-spectrum anti-aging drug.
Synergizes well with deprenyl, Hydergine, GH3/ KH3. 2 or 3 tablets (45mg each)
daily.
Because of its synergy with other
life extension drugs, those also taking any or all of Hydergine, piracetam (and
its analogues), vinpocetine, deprenyl, GH3/ KH3 may benefit from even just one
45mg tablet a day, especially if taken regularly on a long-term basis. Because
idebenone is fat soluble, it is best taken with a fat rich meal, or with lipid
absorption enhancing agents such as lecithin or phosphatidyl choline.
Numerous studies have shown that
idebenone is well distributed through-out the body after absorption,
accumulating in cellular and organelle membranes, as well as in the electron
transport chain, exactly where it does the most good!
HOME
to order
References
www.idebenone.org
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
Ranen
NG and colleagues, "A controlled trial of idebenone in Huntington's
disease" Mov Disord 1996 Sep; 11(5):549-554
Ikejiri
Y, Mori E, Ishii K, Yasuda M, Sasaki M, "Idebenone improves cerebral
mitochondrial oxidative metabolism in a patient with MELAS" Neurology
1996; Aug 47(2); 583-585.
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.
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.
Bergamasco
B, Scarzella L, "Idebenone, a
new drug in the treatment of cognitive impariment in patients with dementia of
the Alzheimer type." Funct Neurol 1994; May;9(3):161-168.
Nitta
A, Hasegawa 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.
Suno
M, Nagaoka A, "Inhibition of brain mitochondrial swelling by
idebenone."
Arch Gerontol Geriatr 1989 May; 8(3):299-305.
Ihara Y, Namba S, Shiraba T, "Mitochondrial
encephalomyopathy (MELAS), pathological study and successful therapy with
coenzyme Q10 and idebenone." J Neurol Sci 1989 May; 90(3):263-271.
Lerman-Sagie T, Rustin P, Lev D, "Dramatic improvement
in mitochondrial cardiomyopathy following treatment with idebenone."
J Inherit Metab Dis 2001 Feb;24(1):28-34.
Gutzmann H, Hadler D., "Sustained efficacy and
safety of idebenone in the treatment of
Alzheimer's disease: update on a 2-year double-blind multicentre study."
J Neural Transm Suppl 1998;54:301-10.
Yamada K, Nitta A, Hasegawa T, "Orally active NGF synthesis stimulators:
potential therapeutic agents in Alzheimer's disease."
Behav Brain Res 1997 Feb;83(1-2):117-22.
Bergamasco B, Scarzella L, "Idebenone, a new drug
in the treatment of cognitive impairment in patients with dementia of the
Alzheimer type."
Funct Neurol 1994 May-Jun;9(3):161-8.
Clinical evaluation of Idebenone in the long-term
treatment of Alzheimer's disease
Hans Gutzmann, Dietrich Hadler
Retzdorffpromenade 3 D-12161 Berlin, Germany
The 2-year efficacy and safety of idebenone were studied in a prospective,
randomized, double-blind multicentre study in 3 parallel groups of patients with
dementia of the Alzheimer type (DAT) of mild to moderate degree. A total of 450
patients were randomized to either placebo for 12 months followed by idebenone
90 mg tid for another 12 months (n = 153) or idebenone 90 mg tid for 24 months
(n = 148) or idebenone 120 mg tid for 24 months (n = 149). The primary outcome
measure was the total score of the Alzheimer's Disease Assessment Scale (ADAS
Total) at month 6. Secondary outcome measures were the ADAS cognitive (ADAS-Cog)
and noncognitive score (ADAS-Noncog), the clinical global response
(CGI-Improvement), the SKT neuropsychological test battery, and the Nurses'
Observation Scale for Geriatric Patients (NOSGER-Total and IADL subscale).
Safety parameters were adverse events, vital signs, ECG and clinical laboratory
parameters. During the placebo controlled period (the first year of treatment),
idebenone showed statistically significant dose-dependent improvement in the
primary efficacy variable ADAS-Total and in all the secondary efficacy
variables. There was no evidence for a loss of efficacy during the second year
of treatment, as a further improvement of most efficacy variables was found in
the second year in comparison to the results of the 12 months visit. Also, a
clear dose effect relationship was maintained throughout the second year of
treatment. This suggests that idebenone exerts its beneficial therapeutic
effects on the course of the disease by slowing down its progression. Safety and
tolerability of idebenone were good and similar to placebo during the first year
of treatment and did not change during the second year.
ALL INFORMATION IS EDUCATIONAL AND
SHOULD NOT REPLACE THE ADVICE OF
YOUR PHYSICIAN.
The above article is
copyrighted and may not be copied without the written permission of
International Antiaging Systems, Les Autelets Suite A, Sark
GY9 0SF, Channel Islands, UK.
HOME
James South articles
1. centrophenoxine,
the brain booster
2. deprenyl,
extending lifespan
3. depression with
alternative antiaging treatments
4. DHEA
5. Excitotoxins
the ultimate brain slayer
6. GHB, the elixir of life
7. Growth Hormone,
the real fountain of youth
8. Idebenone
the ultimate anti-aging drug?
9 James South's supplement
program
10. Laetrile (B17) the answer
to cancer
11. Lucidril - the neuro-energizer
12. NADH, the
body and mind energizer
13. nootropics,
reviewing the smart drugs
14. piracetam - the
original nootropic
15. pregnenolone
the role of the "happy" hormone
16. pyritinol,
the oldest smart drug?
17. resveratrol anti-heart,
anti-cancer
18. SAMe,
for mood, liver, heart, and brain
19 silver for internal
and topical infections
20. thymus Gland: its vital but
overlooked role
21. Tired of being tired?
22. tryptophan,
nature’s answer to Prozac
23. vinpocetine,
cerebral enhancer
| 
