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Deprenyl Review Article

 

Parkinson’s diseaseDeprenyl, deprenyl selegiline, first intended as an antidepress­ant, is commonly used in the treatment of Parkinson’s disease, and also as a life-extension drug. It is also being applied in the treatment of a range of other conditions. It enhances and protects mental function, and helps in retaining libido and a positive mood. Thus, particularly in its life-extension role, not just the length of life is increased, but also the quality of life. Deprenyl, which is also known by the name of Deprenyl Selegiline, is an antidepressant that is widely used in the treatment of Parkinson’s disease. The main function of Deprenyl is to assist in the protection and development of mental functions thereby assist in maintain a good mood by retaining the libido. It is said to increase the quality of life also along with the length of life, which is why it is also known as life extension drug. Deprenyl is said to be a modification of phenyl ethylamine, also known as PEA. PEA belongs to the same family to which neurotransmitters dopamine and noradrenalin belongs. Deprenyl is available in different forms like Ldeprenyl, better known as Selegiline, and deprenyl citrate. Continue reading...

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Deprenyl is a medicinal drug that is said to have life extending properties because of which it is used in the treatment of many diseases like Parkinson’s disease. It has the ability to boost mental function and improve the quality of life along with its length. However, other than its life saving properties it has many side effects also like dry mouth, dizziness, muscle pain, constipation and sleep troubles.

How deprenyl works

It was suggested by Professor Knoll, the drug's developer, that the action of deprenyl was due to the fact of it being an inhibitor of the action of a group of enzymes called monoamine oxidase-B (MAO-B). These are scavenger substances responsible for metabolising "used" neurotransmitter chemicals so that they can be excreted. MAO levels tend to increase with age, causing a resultant decrease in amounts of monoamine neurotransmitter substances such as dopamine. Consequently, inhibition of the MAO action can correct the natural age-related decrease in levels of these vital substances.

The MAO-B enzymes break down dopamine inside the brain. However by using this drug dopamine can be preserved, because the action of the enzymes is inhibited by deprenyl. Fortunately however, it is at the same time very selective in its action (although if taken in large doses it loses its specificity). Thus other key enzymes in the body, such as the MAO in the digestive system, remain unaffected by this drug. Deprenyl can be regarded as the only potent MAO-B inhibitor currently available which is selective in this way. Deprenyl also inhibits the uptake of noreprinephine, dopamine and epinephrine into the neuronal cells.

Deprenyl is partly metabolized to produce low levels of variant forms of amphetamine and methamphetamine, although these isomers are not considered psychoactive and have little abuse liability, even with excess doses of deprenyl. At the same time, possibly they may beneficially contribute to the stimulatory effect on locomotor activity and dopamine synthesis. Nevertheless in this context it should be noted that due to these metabolites, deprenyl has the potential to cause false positives for amphetamine or methamphet­amine in drug tests.

Certain tyramine-containing foods like cheese, chicken liver, yeast, herring, and some wines, tend to cause the neural uptake of tyramine. This sometimes leads to a hypertensive reaction in the brain which can prove dangerous. This, comm­only known as the "cheese effect", is prevented by MAO inhibitors. Neverthe­less, as a precaution certain dietary restrictions may be advised when taking high doses of deprenyl; although deprenyl is much better than other MAO inhibitor drugs in this respect. With low doses of deprenyl, such attention to diet is considered to be unnecessary.

Deprenyl was the first selective MAO-B inhibitor to be described. More recent research however indicates that deprenyl may also possess a number of unique properties, apart from its MAO-B inhibition activity. Dr Knoll has shown that by blocking the MAO-B enzymes, deprenyl also helps in the formation of higher levels of natural antioxidants in the brain. These antioxidants in turn protect the nerve cells and further aid in extending life-expect­ancy. In particular, deprenyl has been found to act as a promoter of the anti-oxidant enzymes superoxide dismutase (SOD) and catalase (CAT).


Antiaging effect

Deprenyl for many years remained a relatively obscure drug, officially approved in Europe and elsewhere as an adjunctive treatment for Parkinson's disease. Then in 1988 a sensational scientific article on a different effect of the drug was published in a specialized small-circulation medical journal. In the article, Professor Knoll reported the results of longevity experim­ents on rats which had been given deprenyl. In his studies, Knoll found that rats treated with deprenyl lived up to 40% longer than the "control" rats which were given a dummy substance instead. In particular, not just the average lifespan was improved, but there was a dramatic increase in maximum lifespan for the very oldest animals – an indication of a genuine antiaging effect.

Most subsequent studies (by Knoll and other investigators) have confirmed the longevity-enhancing effects of deprenyl. Although the recent studies have not shown results as dramatic as achieved in the original report, Knoll believes this can be explained by the various differences in experimental details which led to non-optimal dosages.

Professor Knoll has said that he himself takes deprenyl tablets twice per week – and that in his opinion, nearly everyone over the age of 45 would benefit by taking deprenyl as a preventative against aging.


TextOther applications

In addition to its potential as a life-extending drug, deprenyl also appears to have a number of other beneficial effects. Apart from the general anti-aging action, undoubtedly one of the most significant for the general population is a libido-promoting or aphrodisiac effect, in both men and women. Professor Knoll and colleagues first reported indications for the drug's potential in this area in the 1980s in animal experiments, showing that it was particularly effective in older males.

In the USA its use for Parkinson's disease was for a long time the only FDA-approved indication for deprenyl. However, there are a number of ongoing clinical studies evaluating its efficacy in the treatment of Alzheimer's disease; and beyond this, anecdotal reports have been accumulating of its ability to give dramatic improvements in an impressive number of other diseases.

Although in some cases this is still a matter of controversy, conditions for which deprenyl may reportedly be therapeutic or ameliorative include depression, learning difficulties, (stopping) smoking, senile dementia, hypertension, stroke, certain hormonal inadequacies, multiple sclerosis, amyotrophic lateralizing sclerosis (Lou Gherig's disease), fatigue, chronic pain, gastric ulcers, sexual dysfunction, blepharospasm, and cancer.

In relation to cancer Dr. Clyde Reynolds, who specializes in the metabolic therapy of cancer, has discovered that cancer patients invariably have imbalances of the neuro­transmitters epinephrine, norepinephrine and serotonin. He believes that a normal balance of these neurotransmitters is necessary for the effective treatment of all cancers – and he has found that Deprenyl has a highly effective action in achieving this balance.


Deprenyl and healthy brain cells

As already mentioned, the brain contains neurotransmitter substances that in effect form the messengers for brain impulses or signals. Deprenyl boosts the levels of these neurotransmitters in the brain, offsetting their natural decline in older persons, and thereby finds its place in the field of anti-aging medicine. In a particularly important example, brain activity retains its youthfulness by reducing the loss of dopamine which would occur due to the natural aging process.

Deprenyl was initially developed as a psychic energizer – it was designed to combine some amphetamine-like brain effects with the action of an antidepressant. It was found however that deprenyl also has the beneficial effect of protecting or shielding neurotransmitter cells from the action of neurotoxins – chemical agents that kill or reduce the activity of such cells. Dopamine availability is improved, and the nerve cells are maintained in good health by being protected from being damaged by the stressful conditions which occur as the body ages. In this way deprenyl acts as an antiaging agent. Professor Knoll in his life-extension research showed that the average human life-span could potentially be increased by some 15 years by regular usage of deprenyl.


Treatment with deprenyl

Dosage

The appropriate dose of deprenyl selegiline varies from one patient to another, and can only be effectively determined by the doctor. The dosage varies with age and medical condition of the patient, but also depends on many other factors. For example, studies indicate that the biological uptake for oral dosage is considerably increased (by an order of magnitude) in women taking oral contraceptives. Furthermore, a high dose is not necessarily more effective (in fact, may be less effective) than a lower one. Therefore it is very important to act according to the doctor's recommend­ation. Thus the figures below should be taken only as rough guidelines. For people aged in the range 30-35 years, a dose of 1 mg twice a week is suggested by the manufact­urer. Those aged above 80 years are sometimes prescribed up to 10 mg a day. For treat­ment of Parkinson’s disease and Alzheimer’s disease a typical dosage is about 20 mg a day, which is higher than for any of the other applications. Usually for other purposes the dose is between 2.5-5 mg, taken 1-3 times a week. A lower dose of about 1-3 mg, but taken more frequently (on alternate days), is suggested in some other cases.

The dosage of Deprenyl varies from person to person depending on severity of the condition. Other than condition of the patient there are other natural factors involved in deciding dose of Deprenyl in patient like for example high doses are required in some patients for more benefit. However, it is advised to act as per the instruction of your doctor. For the people who are in the age group of 30 to 35 years, the average dose is said to be 1 mg two times in a week and for those who are above the age group of 80 years, are prescribed a dosage of 10 mg in a single day. In case of treatment for Parkinson’s disease and Alzheimer’s disease, the dosage recommended is around 20 mg in a day. While in some other purposes, the average dosage varies from 1 mg to 3 mg on alternate days.
Deprenyl is available in both liquid and tablet form but if compared, liquid form is considered more beneficial for its quick effect when taken in form of injection.

Side effects

It is possible that some people may experience side effects from this drug. These may include digestive problems such as heartburn, upset stomach and nausea. In others, side effects like hyper-excitability, irritability and psychomotor agitation along with insomnia have been found. Certain neurotransmitter substances that affect sleeping and calmness of mood may be over-activated by deprenyl, and this may account for the above-mentioned disorders. Dietary supplementation with magnesium, tryptophan or 5-HTP can be used to overcome such side effects.
In younger people, dopamine levels remain fairly stable. However, even in healthy individuals, after about age 45 average dopamine levels in the brain start to decrease, by about 13% for each 10 years of life. On this basis, by approximately age 130 the dopamine content would decline to around 30% of normal – which is typically the level seen in patients with early Parkinson's disease. (When the level has fallen to 10% of normal, death is likely to ensue.)

Thus some neuroscientists have said that if we were to live long enough, everyone would ultimately suffer Parkinson's disease symptoms. In healthy persons, if the rate of decline could be slowed even modestly (perhaps down to 10% per decade, instead of 13%), then a very significant life-extension would be possible. It is believed that this can be achieved by regular usage with deprenyl.

There is a possibility that some of the people consuming Deprenyl may feel certain side effects. Some of which may be related to digestion like heartburn, upset stomach and nausea. While other side effects include irritation, hyper-excitement and psychomotor agitation along with the problem of insomnia have been found. Other than that, there are certain neurotransmitters that can affect calmness and sleeping of mood and these are over activated by Deprenyl and lead to the disorders that are mentioned above. However, consumption of dietary supplements that have magnesium, tryptophan or 5- HTP is beneficial in overcoming the side effects.

Cautions

Although there are no particular that a person needs to maintain while using Deprenyl but its suitability on pregnant and breast feeding women is still doubted. Therefore, it is better to continue the treatment under the supervision of a doctor.

Deprenyl (generic name: selegiline) is believed to be a versatile drug that has life-extending properties. This drug is usually used for treating Parkinson’s disease and for life-extension. It is also being used in treating many other different conditions. It guards and boosts mental function and assists in preserving libido and positive mood. It is also very safe to use. Deprenyl does not only lengthen the life span but also improves the quality of life. This drug is a variation of phenyl ethylamine or PEA which belongs to a class of neurotransmitters along with dopamine and nonradrenaline. Side effects of this drug may include dry mouth, dizziness, muscle pain, constipation, difficulty in staying or falling asleep, and rash.

This drug is very well-established, having been developed in the early 1960s as an antidepressant by Professor Joseph Knoll, in Hungary. Later, in the 1970s, it was found that when deprenyl was administered as an adjunct to other drugs such as levodopa in the treat­ment of Parkinson's disease, significantly improved results were achieved in such patients.

Parkinson's disease

Parkinson's disease is a degenerative brain illness in which the patient suffers progr­ess­ively worsening dementia, unsteady gait, and tremor. Ultimately it is fatal. The disease is thought to be caused by a reduction in the numbers of a special type of cell in a portion of the brain called the substantia nigra. These cells are responsible for producing dopamine, a stimulatory neurotransmitter substance; and the consequence is that the body suffers a progressively more severe dopamine deficiency, leading to the well-known symptoms of the disease.

Deprenyl selegiline was initially developed as a psychic energizer – it was designed to combine some amphetamine-like brain effects with the action of an antidepressant. It was found however that deprenyl also has the beneficial effect of protecting or shielding neurotransmitter cells from the action of neurotoxins – chemical agents that kill or reduce the activity of such cells. Dopamine availability is improved, and the nerve cells are maintained in good health by being protected from being damaged by the stressful conditions which occur as the body ages. In this way deprenyl acts as an antiaging agent. Professor Knoll in his life-extension research showed that the average human life-span could potentially be increased by some 15 years by regular usage of deprenyl.


 

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