Centrophenoxine Articles:
• Centrophenoxine - "the product that reverses aging!"
• Centrophenoxine – Don’t Wait For Age To Affect Your Brain!
• A new approach for prevention and protection against Alzheimer’s disease
By Phil Micans, MS, PharmB
The burden of Alzheimer’s disease
This statement has wide ranging implications because Alzheimer’s disease (AD) is the most common of the senile dementias affecting 5% of all persons in their 60s, 20% in their 70s and an incredible 50% in their 80s.
Furthermore, due to the aging of the so-called baby boomers, it is these age groups that are set to expand greatly over the next 20 years, with World Health Organisation figures stating that the over 80s are expected to rise in number by 400%! Clearly then, senile dementias like Alzheimer’s are going to be a major burden to individuals, their families and society at large.
To put these statistics into “real” numbers, today more than 4,000,000 Americans are already diagnosed with Alzheimer’s and each year an additional 360,000 develop the disease. If you then add in those who have a dementia not yet diagnosed, (but nonetheless having a memory problem that has a debilitating effect on everyday life), then one can see that AD can be considered a virtual epidemic.
Some very famous persons have contracted AD, including President Ronald Reagan and the actors Charlton Heston, Rita Hayworth and Charles Bronson- to name but a few. So fame and fortune are not necessarily the savours from developing this disease.
Current approved therapies
Today in the USA there are essentially 4 medications that are prescribed to treat AD; these are typically based on acetylcholinesterase inhibitors. As the cholinergic neurons in the brain are known to decline in their activity with AD, (possibly through a loss of the neurotransmitter acetylcholine, which is abbreviated to ACh), the drugs donepezil (Aricept®), rivastigmine (Exelon®) and Galantamine (Reminyl®/ Razadyne®) help to prevent the breakdown of ACh, thus increasing the concentration of ACh and aiding the support of the cholinergic neurons.
The only other current “approved” method of treating AD in the USA is using Memantine (Ebixa®/ Namenda®) which works through a different mechanism. It essentially blocks the action of excitotoxins in the brain, thus delaying and preventing damage to the neurons themselves.
In fact Memantine remains to-date the only drug that has been clinically proven to be efficacious in the late stages of AD, making improvements to daily living such as being able to eat and drink unaided etc.
In general, the approved drugs for Alzheimer’s are used in the mild to moderate stages of the disease; however it should be noted that none of these approved drugs has an indication for delaying or halting the progression of the disease itself, rather only to improve the symptoms.
Centrophenoxine
This therefore makes Dr. Nagy’s proposal regarding Centrophenoxine most fascinating- the fact that it may be able to prevent the damage that leads to the development of AD, this by itself makes it different from all the current approved drugs.
Centrophenoxine is a combination of DMAE (dimethylaminoethanol), a substance found in fish-particularly sardines, (and is likely to be one of the key substances behind the common thinking that fish is brain food) and PCPA (parachlorphenoxyacetic acid), which is a form of plant “growth hormone” called auxins.
Centrophenoxine’s uses in European and Asian countries have been centred on its ability as a neuroenergizer and it has been officially used in disorders relating to brain injury, memory disturbances, barbiturate intoxification, alcoholism and cognitive decline.
Animal studies have shown that centrophenoxine has a great affinity to help remove a toxin from brain cells called lipofuscin, (this toxin accumulates with age and particularly so in AD patients). It is believed that this action was responsible for the significant increases seen in the life-span of centrophenoxine treated animals, as well as improvements to their learning abilities compared to their age-related controls.
Thus the preventative role of centrophenoxine for humans can be related to a reduction in lipofuscin plague levels in the brain, resulting in improved cell and neuronal performance. As AD victims have extremely high levels of lipofuscin this can be seen in a very real sense as a preventative measure.
Remember that centrophenoxine is partly made up of DMAE and it is well known to improve choline levels, which in turn leads to improved ACh levels. However DMAE by itself is relatively ineffective, particularly for those who are at a pre-Alzheimer or indeed diagnosed Alzheimer level. Thankfully clinically studies have shown that centrophenoxine delivers much more DMAE into the brain than DMAE alone. It is believed that its counterpart PCPA plays a role in helping it to cross the blood-brain barrier, which is always a significant obstacle for most supplements to do.
In addition, the presence of DMAE in brain neurons is also considered to play a significant role as a free radical scavenger, particularly for oxygen related species, a major cause of oxidative damage in the brain itself.
So it may be construed that centrophenoxine has the ability to improve cognition and protect against a senile dementia such as Alzheimer’s in three distinct ways:
Furthermore, if you have an understanding of the methodology of Professor Nagy’s membrane hypothesis of aging (MHA), then you can understand that whilst free radical activity plays a part in the destruction of cell integrity, that it is a theory in its own right. The MHA concentres on the ability of the membrane of cells to communicate and that efficiency is measured by its ability to move sodium and potassium ions as well as heat, (an often overlooked factor in the aging process) in and out of the cell.
To this end centrophenoxine has displayed a remarkable ability to help slow and even reverse aspects of the MHA; this may be one of the reasons that Professor Imre Zs.-Nagy himself has been taking 500 mg of centrophenoxine daily since 1976.
Human results with centrophenoxine
Professor Nagy himself reports that those who use centrophenoxine regularly “have better mental and physical performance compared to the counterparts. “
In a double blind placebo controlled trial of 50 patients, with an average age of 76 and all suffering from a “medium” level of dementia, reported that 50% of them had much better behavioural and psychometric markers within just 8-weeks of 250 mg centrophenoxine ingestion twice daily.
Indeed a very interesting effect of centrophenoxine supplementation is a considerable rehydration of the intracellular mass, in other words the patients’ body content becomes more watery and less solid. This is a very important antiaging benefit, namely because aging leads to dehydration and dehydration leads to worsening cell performance, for example enzymes work much more efficiently in watery environments.
In fact I will add something that is not in Professor Nagy’s submitted article; that is after a few months these benefits with centrophenoxine go “beyond” the brain environment. Apart from the brain, lipofuscin deposits can be found in the lungs, heart and the skin. Centrophenoxine supplements can improve oxygen uptake and carbon dioxide output from the lungs, a sign that the cells in the lungs are performing better (and perhaps a significant factor behind the physical improvements felt under centrophenoxine supplementation). Plus there can also be a reduction in the number and the size of “age spots” (partly made up of lipofuscin) found in skin. This has been noted by our patients and the improved retained water content also helps to rehydrate the skin and make it appear more plumped and youthful.
Thus centrophenoxine displays benefits for both outward appearance and inward performance.
On a personal note I will add that I have experienced much faster memory recall abilities whilst using centrophenoxine.
Side Effects
Centrophenoxine has been available in parts of Europe and Asia for decades and in that time has displayed very few side effects. Professor Nagy, his family and friends have been using it daily for over 30 years and he notes that there have been no negative effects noted to date.
Of course it is possible that when combined with other ACh increasing drugs that over agitation may take place and in some individuals’ centrophenoxine can act to “over stimulate.” In such cases issues such as headache, muscle aches or agitation may appear. This is not a toxicity issue but an indicator that ACh levels have been raised too far. The answer is to reduce the centrophenoxine dose to a level where these side effects are eradicated.
There is some reasoning that ACh stimulation is not beneficial for persons with mania or Parkinson’s disease, in these cases centrophenoxine use should be avoided unless under the care and direction of a physician.
Conclusion
Let us return to our original proposal of the possibility of centrophenoxine playing a significant role in the prevention and alleviation of Alzheimer’s disease.
Professor Nagy states: “Since centrophenoxine is able to retard or even avoid the age-dependent deterioration of the brain functions, one can assume that it may act also as a useful drug in retarding (or even avoiding?), the structural and functional declines of typical brain diseases like Alzheimer’s disease.”
It is clearly understood that the true answer to the treatment of senile dementias such as Alzheimer’s is their avoidance, but this will take a shift of policy from the current- wait till it develops then treat it practice, to a let’s recognise the earliest symptoms and prevent it focus. The latter is of course the nature of antiaging medicine.
We here at IAS consider centrophenoxine to be one of the most important antiaging/ nootropic supplements currently available.
Centrophenoxine (also called Meclofenoxate) is often considered to be “an ageing reversal drug”. It is one of the original anti-ageing, neuro-energizing drugs. Having been developed at the French National Scientific Research Centre in 1959, it has been studied and used for many years.
Centrophenoxine forms part of a class of drugs known as nootropic drugs, often popularly referred to as "smart drugs", "smart nutrients", "cognitive enhancers" and "brain enhancers". The word nootropic itself is derived from the Greek words ”noos”, or ”mind” and ”tropein”, which means to bend or turn. Nootropic drugs seek to improve the functions and capacities of the brain. Centrophenoxine itself has been found to be very effective in the treatment of brain damage due to old age and is used to treat the symptoms of senile dementia and Alzheimer’s Disease. It is also used where brain damage has resulted from stroke, physical injury caused by chemicals and drugs, or excessive alcohol consumption. Centrophenoxine has the ability to protect against toxic environmental chemicals.
What is Centrophenoxine?
Centrophenoxine is a compound of two other biochemicals- dimethyl-aminoethanol (DMAE) and parachlorphenoxyacetic acid (pCPA). DMAE is a natural substance found in certain foods, especially fish. It is also produced in the human brain - a natural metabolite of choline (trimethylaminoethanol). The fact that high levels of DMAE are found in fish, may be the very reason why fish has for so long be known as “brain food”. pCPA, on the other hand, is synthetic. It is a man-made version of a group of plant growth hormones called “auxins”. As with DMAE, pCPA is a precursor to the neurotransmitter acetylcholine.
One of the benefits of using Centrophenoxine is that it is well absorbed orally. Once absorbed by the body, the liver breaks down some of the Centrophenoxine into it’s two constituent parts – DMAE and pCPA. The liver converts the DMAE to choline. Choline is an organic compound, usually grouped within the Vitamin B complex. It is used in many biochemical processes in the body, and, in 1998, it was classed as an essential nutrient by the Food and Nutrition Board of the Institute of Medicine (U.S.A.). It is this “acetylcholinesterase-stimulating influence of (Centrophenoxine that) is likely to be implicated in the pharmacological reversal of the age related decline of the cholinergic system. This effect of the drug may also mediate its effects on cognitive and neuronal synaptic functions."
The remaining Centrophenoxine that has not been processed by the liver, circulates throughout the bloodstream. It eventually enters, in particular, the heart and the brain.
Why is Centrophenoxine so beneficial?
Centrophenoxine has been shown to be beneficial in a number of significant ways:
1. Reducing lipofuscin levels
Centrophenoxine has the ability to reduce lipofuscin levels. Lipofuscin, sometimes referred to as an ageing pigment, is a brownish pigment that is left over from the breakdown and absorption of damaged blood cells. It’s found in the brain, the heart muscle and the smooth muscles of the body. As we age, lipofuscin levels increase inside the cells, which, in turn, causes the cells to become less and less able to work properly. Eventually, once a critical level is reached, cell death may occur rapidly. Lower levels of Centrophenoxine are also important for retaining learning abilities and memory function. Studies on animals have shown that using Centrophenoxine for just a few weeks can significantly reduce lipofuscin levels and with it improve cell functionality.
2. Increasing choline levels
As mentioned above, taking Centrophenoxine leads to an increase in the body’s production of choline. Choline is an essential nutrient, critical in a number of biochemical processes. Maintaining a good choline level is vital for the body and the brain if they are to function at their optimal levels. The body derives most of its choline supply from diet although a choline-rich diet of meats, liver and eggs might not necessarily be that popular, particularly for those with high cholesterol. Junk foods and vegetarian diets provide the body with very little choline.
The obvious solution would appear to be to simply take a choline supplement such as choline chloride or bitartrate. Unfortunately, the problem with this approach is that as much as 60% of choline supplements are digested by bacteria in the intestines making it a very inefficient way of increasing choline levels. This is where Centrophenoxine comes in to its own. Intestinal bacteria do not digest the DMAE from the Centrophenoxine allowing far more of it to be available to the body which ultimately maybe converted into choline.
Choline can be used to make other valuable biochemicals, such as the major learning/memory neurotransmitter acetylcholine. Indeed, it is this “acetylcholinesterase-stimulating influence of (Centrophenoxine that) is likely to be implicated in the pharmacological reversal of the age related decline of the cholinergic system. This effect of the drug may also mediate its effects on cognitive and neuronal synaptic functions.”1
Choline can also be converted into betaine (trimethylglycine) through a process known as oxidization. Betaine is beneficial in that it assists the body in ridding itself of homocysteine. Homocysteine can be toxic to the heart and arteries. A high level of blood serum homocysteine is a powerful risk factor for cardiovascular disease.
Insufficient levels of choline may also be linked to the beginnings of Alzheimer’s Disease. Choline either flows from the brain cells to the bloodstream (when levels fall below 14 micromoles) or from the bloodstream into the brain (when levels are above 14 micromoles). Unfortunately, when choline flows from the brain cells to the bloodstream, it is derived from auto-cannibalization. In this situation, the choline contains membrane phospholipids as it is these membrane phospholipids that have been broken down by the brain cells to provide the choline to enter the bloodstream. Research now suggests that if, over a lifetime, blood choline levels are too low and the brain cells are therefore forced to continually produce choline by way of auto-cannibalization, such auto- cannibalization may contribute to Alzheimer's disease.
3. Acting as an anti-oxidant
The use of Centrophenoxine has powerful antioxidant effects on the brain. As we have seen above, Centrophenoxine provides the body with a very effective way of getting DMAE incorporated into brain cell membranes. Once there, it acts as a very powerful hydroxyl free radical scavenger which is good news given that hydroxyl radicals are the most damaging of the free radicals/oxidants common in living cells.
4. Acting as a neuro energiser
As we age, neuronal RNA and protein production (essential for facilitating memory and repairing cell damage) decline. Taking Centrophenoxine, however, increases their production, therefore reversing this decline. Centrophenoxine also helps to “wake up” the brain by increasing the uptake of glucose (the major source of energy used by the brain) and oxygen.
How much Centrophenoxine should I take?
Fortunately, Centrophenoxine is an extremely safe, non-toxic drug. Dosage levels depend on the reason why you are taking Centrophenoxine. If you are going to take Centrophenoxine to give you a cognitive boost, raise your choline levels and help protect your brain from the damage ageing brings, you will only require 1 or 2 Centrophenoxine tablets (250mg each) daily taken with breakfast or lunch. The dosage requirement for treating the elderly suffering significant intellectual decline or loss of vigour is between 3 to 6 Centrophenoxine tablets per day (250mg each), again taken with breakfast and lunch. Combining Centrophenoxine with deprenyl may prove useful in the treatment of those in the early stages of Alzheimer’s Disease. Centrophenoxine can also be used to boost the effects of Piracetam.
Centrophenoxine should not be taken by pregnant women and anyone suffering from major depression, mania, seizure disorders or Parkinson's disease.
Finally, although considered to be a very safe drug, occasionally Centrophenoxine can cause problems by increasing acetylcholine too much. Excessive acetylcholine levels can lead to headaches, neck, jaw and shoulder muscle tension, insomnia, irritability and hyper excitability, agitation and restlessness. Simply stopping Centrophenoxine for a few days and then resuming on a reduced dosage should rectify any such situation.
AB
Centrophenoxine is used to treat the symptoms of Senile Dementia and Alzheimer’s disease. It is known for its ability to effectively fight cerebral aging and is therefore an effective weapon in tackling many age related diseases. Read on to discover more about how Centrophenoxine works and how it could help you.
How Does Centrophenoxine Work?
Lipofuscin is a type of metabolic waste product, made from fragments of damaged proteins and fatty acids, that accumulates in the brain, heart, lungs and skin cells. Centrophenoxine is extremely effective at reducing it. The more lipofuscin that is present within a cell, the less functional it becomes, and once it reaches a critical stage, the cell may die. Human and animal studies have demonstrated that low lipofuscin levels correlate with healthy cellular function, and high levels are associated with poor cellular health.
Professor Imre Zs. Nagy of the University of Debrecen (Hungary,) is the author of the ‘membrane’ theory of aging. He discovered that the cells that make up young bodies comprise 92% water and lipids, and 8% dry mass. Conversely, elderly bodies comprise only 40% water and lipids, and 60% dry mass. This vast difference has significant implications for the ability of cells to communicate via chemical and electrical signals. Professor Nagy developed and used Centrophenoxine to modify the cell structure of elderly animals by removing lipofuscin build-up, and by changing the water and lipid/dry mass ratio to that of younger animals. His experiments were so effective, that, in addition to a number of behavioral improvements, the longevity of the treated animals increased by up to 40% compared with the controls.
A range of animal experiments has been conducted, measuring their learning and memory abilities. Aged animals whose high lipofuscin levels were reduced by Centrophenoxine, had their memory and learning abilities restored to a level similar to that of healthy young animals.
A human clinical trial involving 76 healthy, elderly patients suffering from significant intellectual deterioration, found that Centrophenoxine increased storage of new, long term memory information, while increasing vigilance and alertness. These results were noted after only several weeks of treatment.
Research has shown that Centrophenoxine improves the use and metabolism of glucose and oxygen in the brain which, in turn, benefits concentration and attention levels. So, if you want to keep your brain active, fit and healthy, try Centrophenoxine for a thorough mental “spring clean”.