Articles on Selepryl:

Key to life extension

Enhance mental clarity, mood and libido with Selepryl.

Selepryl (also known as Cyprenil) – a key to life extension

What is Selepryl?

Selepryl or Cyprenil as it is also commonly known, is a liquid that contains selegiline citrate (otherwise known as deprenyl). Selegiline was first synthesized by Hungarian Professor Joseph Knoll in his Budapest laboratory in 1961. It forms part of a class of medications - monoamine oxidase inhibitors or MAOIs - that act as powerful antidepressants.

There are two forms of MAOIs –type A (MAO-A) inhibitors and type B (MAO-B) inhibitors. Selegiline is a selective MAO-B inhibitor and breaks down dopamine into compounds which are then excreted. By inhibiting MAO-B, the breakdown of dopamine is reduced, thereby increasing the amount of dopamine available.

Why is Dopamine so Important?

Although dopamine is found in many parts of the body, it is found in the greatest concentration in a part of the brain called the basal ganglia. The basal ganglia (a mass of grey matter at the base of the brain that plays an important role in regulating bodily movement) includes the substantia nigra and it is the neurons (or nerve cells) of the substantia nigra (called dopaminergic neurons) that produce dopamine.

Dopamine is an important and essential neurotransmitter in the brain. Neurotransmitters act as the brains messengers. Neurons are able to communicate by the movement of chemicals across small gaps or synapses. It is these chemicals that are neurotransmitters. When a dopaminergic neuron transmits a message to another dopaminergic neuron, it does so by emitting dopamine. Some of the dopamine is absorbed by the second neuron, some is lost in the process and some is recovered by the transmitting neuron. To keep the brain functioning properly, there has to be just the right amount of dopamine in balance with other chemicals. If there is too much or too little dopamine, the brain will fail to function properly.

Dopamine has a wide variety of important functions in the brain including roles in behaviour and cognition, fine motor control, motivation and reward, sexual behaviour, inhibition of milk production, sleep, mood, attention, learning and immunological function. For example, dopamine is often associated with the pleasure system of the brain, providing you with feelings of enjoyment and reinforcement which gives you the motivation to perform various activities. In the frontal lobes of the brain, dopamine controls the flow of information from other areas of the brain. Dopamine disorders in this region of the brain can cause a decline in neurocognitive functions, especially memory, attention and problem solving.

A healthy brain produces enough dopamine to allow the brain to carry out a whole range of complicated activities. However, as we have already seen, MAO- B prevents the accumulation of dopamine within the neurons. Unfortunately, as we age the amount of MAO-B enzymes increase, which in turn means the amount of dopamine reduces.

MAO-B is also responsible for the release of free radicals which may damage neurons and other healthy cells. Researchers have been able to establish that these free radicals may damage the substantia nigra. This is particularly relevant in Parkinson’s Disease. In a healthy brain, the substantia nigra produces an enzyme to break down and neutralize these free radicals. However, in Parkinson’s Disease, this enzyme is drastically depleted resulting in free radical damage to the substantia nigra.

What is Selepryl used for?

Given its ability to inhibit the actions of MAO-B and therefore affect dopamine levels, selegiline (which is found in Selepryl) can be used for a variety of reasons. Since it was first synthesized by Joseph Knoll back in the early 1960’s, selegiline’s properties and uses have been the subject of many studies. There can be no doubt now that it is a powerful and exceptional medication not only for the treatment of specific conditions such as Parkinson’s Disease and depression, but also for general well being, particularly as we age.

Treatment of Parkinson’s Disease

Selegiline is approved for, and routinely prescribed for, the treatment of Parkinson’s Disease as part of a therapy regime. Whilst Parkinson’s Disease cannot be cured, segeliline has been found to be very effective in not only treating the symptoms of the disease but also in slowing it’s progress and expanding the lifespan of those suffering from the disease.

Parkinson's Disease is believed to be caused by a deficiency of dopamine. Generally, Parkinson’s Disease is not diagnosed until a person has lost more than 80 % of dopaminergic neurons in the substantia nigra.

Needless to say, a significant amount of research has been carried out in this area with dramatic results. For example, in one study carried out in the USA and Canada in 1989, the researchers halted the trials halfway through because the Parkinson’s Disease patients receiving deprenyl (selegiline) were doing so much better than those in the control group who were just receiving a placebo.

Treatment of Alzheimer’s Disease

Patients suffering from Alzheimer’s Disease also face monamine neurotransmitter disturbances caused by the activity of MAO-B. As with Parkinson’s Disease patients, these disturbances manifest themselves as dramatic declines in memory, movement, co-ordination and sex drive. Armed with this knowledge, scientists have been exploring the use of selegiline as a treatment for Alzheimer’s Disease because of its ability to inhibit MAO-B. Early results were promising although further research into whether selegiline can improve memory and behaviour and slow brain degeneration in Alzheimer’s patients has yet to prove conclusive.

Depression and Mood Enhancement

As an MAO-B inhibitor, Selepryl falls into a class of medications known to be anti-depressants. Reports have shown that Selepryl can counteract the depressive emotional conditions often found in people suffering from degenerative diseases such as cancer, diabetes and lupus.

In tests involving older people, it has been demonstrated that Selepryl can drastically improve their general well being, as well as increasing their motor ability, awareness and activity.

Selepryl is also known to be an aphrodisiac, particularly for men.

Ageing

It is perhaps in the area of slowing down the ageing process, that the use of selegiline is most exciting. As we age, the volume of essential chemicals in our bodies declines. Unfortunately, the dopaminergic neurons in the substantia nigra are the fastest ageing cells in the body, which leads to declining levels of dopamine as we grow older. This means that from the age of about 35, our dopamine levels fall at a rate of about 13% per decade.

Elderly people suffer from many of the same symptoms as those found in Parkinson’s Disease patients. This is because exactly the same neurons are being destroyed – it’s just that in Parkinson’s Disease, the destruction is at a much faster rate than in the normal ageing process.

It was during his research into the use of selegiline for the treatment of Parkinson’s Disease that Professor Knoll, first realised its implications in terms of slowing down the ageing process and expanding lifespan. He injected 24 month-old rats (65 years in human terms) 3 times a week with 0.25mg/ kg of deprenyl (selegiline), whilst the control animals received saline injections. The injections were continued until the animals died. The rats lived to an age equivalent in human terms of 150 years!

The results of Joseph Knoll’s remarkable study were later confirmed by a team from the University of Toronto in 1989. Using rats aged 24-25 months, the researchers studied the effects of the administration of 3 injections per week of a solution of 0.25% deprenyl (selegiline). A control group received saline injections. As with Professor Knoll’s study, the rats that had received the deprenyl (selegiline) lived significantly longer than the control group - on average the control group survival time was 133.7 days compared with the control average survival time of 114.7 days. Indeed, one rat in the deprenyl (selegiline) group lived to 315 days compared to a 251 day maximum in the control group. The researchers concluded that the deprenyl (selegiline) had delayed the ageing of the animals’ organs and the animals themselves were healthier than the controls.

Although there were variations between the two studies – for example different strains of rats were used and the life extension achieved by the Toronto team was not as great as that produced by Professor Knoll – the inevitable conclusion to draw is that selegiline may indeed be a key to life extension by protecting the deterioration of the brain cells over time. As Professor Knoll noted in his work “History of Deprenyl – the first selective inhibitor of monoamine oxidase type B”:-

“... it may be advisable to combat the age-related decline of the nigrostriatal dopaminergic neurons in man by taking 10-15 mg of deprenyl weekly during the post-developmental phase of life. Prophylactic deprenyl medication may improve the quality of life in the latter decades, delaying the time of natural death and decreasing the susceptibility to age-related neurological diseases.”

Why take selegiline in the form of Selepryl?

Selepryl is a liquid containing selegiline citrate. Unlike deprenyl tablets, which contain selegiline hydrochloride (selegiline bonded to an in-organic molecule) selegiline citrate is seligiline bonded to an organic molecule. This form is generally recognized as the most pure and potent form of selegiline available. Furthermore, it allows for the precise titration for anti-ageing purposes, as each ml drop in the bottle is equivalent to 1mg deprenyl citrate.

Dosage

For anti-aging purposes, dosage is age dependent:-

Selepryl solution is available in 12 ml bottles. 1 mg is equal to 1 drop. If dosage is more than 5 mg/ day, divide by two (morning and afternoon).

Quality of life usage indications and dosages:

1. Parkinson's Disease: Indicated as a treatment adjuvant. Dosage: 5 mg in the morning and 5 mg in the afternoon.

2. Alzheimer's Disease: May be helpful in treatment. Dosage: 5 mg in the morning and 5 mg in the afternoon.

3. Tremors: Helpful in the relief of symptoms. Dosage: 5 mg in the morning and 5 mg in the afternoon, for 30 days. For maintenance, reduce amount by 1 mg per day until reaching proper dose for age. If tremors return, increase dose by 1 mg a day, until they disappear again, and continue at that dosage. Do not exceed 10 mg per day.

4. High Blood Pressure: Effective in hypertension reduction. Dosage: 5 mg in the morning and 5 mg in the afternoon, for 30 days. After this period, reduce amount by 1 mg per day until reaching proper dose for age. If high blood pressure returns, increase dose by 1 mg a day, until it disappears again, and continue at that dosage. Do not exceed 10 mg per day.

5. Motion Sickness: Dosage: from 5 to 10 mg a day.

6. Depression: Dosage: 5 mg in the morning and 5 mg in the afternoon, for 30 days. After this period, reduce amount by 1 mg per day until reaching proper dose for age. If depression returns, increase dose by 1 mg a day, until it disappears again, and continue at that dosage. Do not exceed 10 mg a day.

Side effects and warnings.

In daily doses of 10mg or less, Selepryl has no known side effects.

In normal clinical doses selegiline acts as a selective irreversible MAO-B inhibitor. However, in larger doses (>20 mg) it loses its specificity and also inhibits MAO-A. Dietary restrictions are common for MAOI treatments, but since selegiline is selective for MAO-B, special dietary restrictions for lower doses have been found to be unnecessary.

Enhance mental clarity, mood and libido with Selepryl.

Selepryl is a brand of Deprenyl, also known as Selegiline, was first discovered in the 1960s by Professor Joseph Knoll.  It has since become known for its antidepressant properties, and its effectiveness in treating Parksinson’s disease.

How Does It Work?

Deprenyl improves the availability of dopamine in the brain and slows its age related decline, by acting as a selective MAO-B inhibitor.  It achieves this by enhancing and maintaining healthy brain cells (particularly in the dopamine producing neuron area of the brain called the Substantia Nigra).

It is thought to be effective in treating depression, and has an aphrodisiac effect, in terms of improving sexual function.”

Its approved use is for treating Parkinson's disease (which affects the brain levels of dopamine), as well as other dementias and even cancers. Parkinson and Alzheimer's disease patients are often treated with very high doses of Selepryl.  However, anti-aging doses (which are dependent on age and condition) tend to be much lower.

Many physicians and patients have gone on record to state that they prefer liquid deprenyl citrate (LDC) forms such as Selepryl. Certainly in a LDC form, it is easy to administer and titrate the small doses used in antiaging medicine.

Deprenyl Research Concludes:

·        Deprenyl protects against age related deterioration in the substantia nigra, which is responsible for sexual behavior, fine motor control, immunological function and motivation.

·        It is effective in preventing and treating Parkinson's and Alzheimer's disease.

·        The unique antioxidant properties of deprenyl protect brain cells from deteriorating over time.

·        The latest study on rats by the University of Toronto revealed that deprenyl may delay the aging of other organs, in addition to the brain and protect kidney function.

·        Deprenyl counteracts depressive emotional conditions that are related to degenerative diseases, such as cancer, chronic fatigue, diabetes, lupus erythematosus, arthritis, etc.

·        Deprenyl dramatically increases the motor ability, awareness, activity and general well being in older people. It may also be effective in the treatment of Multiple Sclerosis.

 GI - 09/20/2007