Cyprenil, Selepryl, Deprenyl
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cyprenil

This product is know as Cyprenil, Selepryl, Deprenyl (L-Deprenyl)

Category: Antidyskinetic

History:
Cyprenil (Depreyl/Selegiline) was first synthesized in Hungary in 1965. While studying it's pharmaceutical effects, Dr. Joseph Knoll discovered the exceptional antidepressant properties of Selegiline. During the 80's, he also became aware of its effectiveness in the prevention and treatment of Parkinson's disease. Since then, numerous studies have been made on Selegiline, demonstrating its therapeutic action on various diseases.
Now we know that the preventive use of this drug has positive effects on many other health areas, improving the quality of life (or general well being). For at least 15 years, numerous accounts of the benefits of Selpryl have been at hand on hundreds of medical reports, since its inception almost four decades ago.

Benefits of the preventive use of Cyprenil
Cyprenil protects against age related deterioration in the substantia nigra, the part of the brain where dopamine is produced. This crucial neurotransmitter is responsible for the primary functions such as sexual behavior, fine motor control, immunological function and motivation.
It is effective in the prevention and treatment of Parkinson's and Alzheimer's disease.
To Dr. Knoll, the studies of humans with Parkinson's disease, as well as his studies on rats, all lead to one conclusion: "We now have a safe, selectively acting drug, that for the first time can slow down the most rapidly aging neuronal machinery in our brain".
The unique antioxidant properties of Cyprenil protect brain cells from deteriorating over time.
The latest study on rats by the University of Toronto revealed that Selegiline may delay the aging of other organs, in addition to the brain, and has a protective effect on kidney function. Cyprenil counteracts the depressive emotional conditions that are frequent in patients suffering from degenerative diseases, such as cancer, chronic fatigue, diabetes, lupus erythematous, arthritis, etc.
Other tests have demonstrated that Cyprenil dramatically increases the motor ability, awareness, activity and the general well being of elderly people. It may also be effective in the treatment of multiple sclerosis.
When Dr. Knoll's research was later duplicated by scientists at the University of Toronto, further evidence was provided that Selegiline can increase the average life span.
Cyprenil has no side effects in daily doses of 10 mg or less.

Conclusion:
Recent studies in both animals and humans have demonstrated that Selegiline has a variety of beneficial results against the deterioration of the brain due to aging, without toxic side effects. There is now evidence of the effectiveness of this drug as an antidepressant, of its benefits as an adjuvant in the treatment of Parkinson's disease, its encouraging results for Alzheimer's disease, and in anti-aging therapy.

Description: Cyprenil (selegiline citrate), contains 300 mg of selegiline base in
12 ml (1+ oz.) solution (not tablets or capsuls)

Dosage: (1ml = 32 drops)
Age                     Dosage
45-49 years       1 drop/day
50-54 years       2 drops/day
55-59 years       3 drops/day
60-64 years       4 drops/day
65-60 years       5 drops/day
70-74 years       6 drops/day
75-79 years       8 drops/day
80-85 years       9 drops/day
over 85 years   10 drops/day
                 Note: 1 btl of 12 ml contains approx. 384 drops; 38 doses at 10 drops per day



Cyprenil (Selegiline), is a drug used as an adjunct therapy of Parkinson's disease due to it's anti-neurodegenerative properties it is biochemical defined as a selective monoamine oxidase type B (MAO B) inhibitor, Selegiline was originally developed as an antidepressant agent. To date Selegiline has only been medically approved by regulatory agencies for use on treatment of Parkinson's disease. However recent testing has indicated that Selegiline may have some effect on increasing sexual response in aging animals, an observed retardation of normal age dependent deterioration of renal function and cognitive abilities, including spatial learning ability.

 

Cyprenil {L-Deprenyl (Selegiline [seh-LEDGE-ah-leen])} works on the brain, not the body whose approved uses are treatment of Alzheimer's & Parkinson's disease. It is also used as a "smart drug" and as such improves motivation, short term memory and to a slight degree aggression. Selegiline seh-LEDGE-ah-leen is used in combination with levodopa or levodopa and carbidopa combination to treat Parkinson's disease, sometimes called shaking palsy or paralysis agitans. This medicine works to increase and extend the effects of levodopa, and may help to slow the progress of Parkinson's disease.

 

SELEGILINE AS A SELECTIVE MONOAMINE OXIDASE INHIBITOR

Monoamine oxidase inhibitors became more widely used in the late 1950's, and their mechanism of action became better understood. Like other enzymes, monoamine oxidase is a protein that catalyses and regulates the chemical reaction necessary for the efficient functioning of most of the body's cells.
Of all the thousands of enzymes in the body, monoamine oxidase is the most ubiquitous and the one that has the most captured the curiosity and fascination of scientists. Monoamine oxidase is everywhere in the body, in the liver, the stomach, the intestines and other organs. In 1973 it was discovered that monoamine oxidase also occurred in the brain.

SELEGILINE IN ALZHEIMER'S DISEASE

Alzheimer and Parkinson are both neurodegenerative diseases, several studies have been conducted to demonstrate the effects of Selegiline on Alzheimer's. The brain is not composed of discrete components; it is an organ of interdependent parts. The question arose weather Selegiline, by improving the tone of the dopaminergic system, might be useful in treating other neurodegenerative diseases.


CONCLUSION:

Selegiline has a unique selectivity to the nigrostriatal dopaminergic neurons, and for the time being is the only promising tool for this purpose in humans because of the following reasons:

  • Given concurrently with levodopa and a peripheral decarboxylase inhibitor (-) Selegiline is now widely used in Parkinson's disease, it is an effective antidepressant and is beneficial effect on Alzheimer's disease was recently demonstrated to be free of significant side affects.
  • The supplementation of (-)Selegiline to Madopar significantly prolonged the survival of parkinson patients as compared to those on Madopar alone indicating that (-)Selegiline protected somehow the nigrostriatal dopaminergic neurons in these patients.
  • Selegiline exerts its specific pharmacological effect in animals with an excellent safety margin.
  • Selegiline turned out to be an efficient inhibitor of the uptake of dopamine in the striatum and this effect was found to play an important role in the facilitation of the activity of the nigrostriatal dopaminergic neurons in animals treated continuously with (-)Selegiline.
  • Selegiline in striking contrast with the MAO inhibitors used previously inhibits the noradrenaline releasing effect of indirectly-acting amine in vascular smooth muscle. This latter effect of (-)Selegiline, which is not shared even with other known selective inhibitors of the B type MAO, is the reason of its safety It is at present, the only MAO inhibitor free of the "Cheese effect".
  • The selectivity of (-)Selegiline, in the small dose range, to the nigrostariatal dopaminergic neuron is also supported by our findings that whereas the turnover rate of noradrenaline and unchanged level of this amine in the brain stem were found.

 

Before you use this medicine...

Allergies -
Tell your doctor if you have ever had any unusual or allergic reaction to selegiline. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes.

Pregnancy -
Selegiline has not been studied in pregnant women. However, this medicine has not been shown to cause birth defects or other problems in animal studies.

Breast-feeding -
It is not known whether selegiline passes into the breast milk.

Children -
Studies on this medicine have been done only in adult patients and there is no specific information about its use in children. Therefore, be sure to discuss with your doctor the use of this medicine in children.

Older adults -
In studies done to date that included elderly people, selegiline did not cause different side effects or problems in older people than it did in younger adults.

Other medicines -
Although certain medicines should not be used together at all, in other cases 2 different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking selegiline, it is especially important that your health care professional know if you are taking any of the following:

  • Antidepressants, tricyclic (amitriptyline [e.g., Elavil], amoxapine [e.g., Asendin], clomipramine [e.g.,
  • Anafranil], desipramine [e.g., Norpramin], doxepin [e.g., Sinequan], imipramine [e.g., Tofranil], nortriptyline [e.g., Pamelor], protriptyline [e.g., Vivactil], trimipramine [e.g., Surmontil]) or
  • Fluoxetine (e.g., Prozac) or
  • Fluvoxamine (e.g., Luvox) or
  • Meperidine (e.g., Demerol) or
  • Nefazodone (e.g., Serzone) or
  • Paroxetine (e.g., Paxil) or
  • Sertraline (e.g., Zoloft) or
  • Venlafaxine (e.g., Effexor) - Using these medicines together may increase the chance of serious side effects


Other medical problems -
The presence of other medical problems may affect the use of selegiline. Make sure you tell your doctor if you have any other medical problems.

Proper Use of This Medicine
Take this medicine only as directed by your doctor . Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

Dosing -
The dose of selegiline will be different for different patients. Your doctor will determine the proper dose of selegiline for you. Follow your doctor's orders or the directions on the label .

For the treatment of Parkinson's disease, the usual dose of selegiline is 5 mg two times a day, taken with breakfast and lunch. Some patients may need less than this.

Missed dose -
If you miss a dose of this medicine, take it as soon as possible. However, if you do not remember the missed dose until late afternoon or evening, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage -
To store this medicine:

  • Keep out of the reach of children.
  • Store away from heat and direct light.
  • Do not store in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause the medicine to break down.
  • Do not keep outdated medicine or medicine no longer needed. Be sure that any discarded medicine is out of the reach of children.

Precautions While Using This Medicine
When selegiline is taken at doses of 10 mg or less per day for the treatment of Parkinson's disease, there are no restrictions on food or beverages you eat or drink. However, the chance exists that dangerous reactions, such as sudden high blood pressure, may occur if doses higher than those used for Parkinson's disease are taken with certain foods, beverages, or other medicines. These foods, beverages, and medicines include:

  • Foods that have a high tyramine content (most common in foods that are aged or fermented to increase their flavor), such as cheeses;
  • Fava or broad bean pods;
  • Yeast or meat extracts;
  • Smoked or pickled meat, poultry, or fish;
  • Fermented sausage (bologna, pepperoni, salami, summer sausage) or other fermented meat;
  • Sauerkraut;
  • or any overripe fruit. If a list of these foods and beverages is not given to you, ask your health care professional to provide one.
  • Alcoholic beverages or alcohol-free or reduced-alcohol beer and wine.
  • Large amounts of caffeine-containing food or beverages such as coffee, tea, cola, or chocolate.

Any other medicine unless approved or prescribed by your doctor. This especially includes:

  • Nonprescription (over-the-counter [OTC]) medicine, such as that for colds (including nose drops or sprays), cough, asthma, hay fever, and appetite control;
  • “Keep awake” products;
  • or products that make you sleepy.

Also, for at least 2 weeks after you stop taking this medicine, these foods, beverages, and other medicines may continue to react with selegiline if it was taken in doses higher than those usually used for Parkinson's disease.

Check with your doctor or hospital emergency room immediately if severe headache, stiff neck, chest pains, fast heartbeat, or nausea and vomiting occur while you are taking this medicine. These may be symptoms of a serious side effect that should have a doctor's attention.

Dizziness, lightheadedness, or fainting may occur, especially when you get up from a lying or sitting position. Getting up slowly may help. If the problem continues or gets worse, check with your doctor.

Selegiline may cause dryness of the mouth. For temporary relief, use sugarless candy or gum, melt bits of ice in your mouth, or use a saliva substitute. However, if your mouth continues to feel dry for more than 2 weeks, check with your medical doctor or dentist. Continuing dryness of the mouth may increase the chance of dental disease, including tooth decay, gum disease, and fungus infections.

When you start taking selegiline in addition to levodopa or carbidopa and levodopa combination, you may experience an increase in side effects. If this occurs, your doctor may gradually reduce the amount of levodopa or carbidopa and levodopa combination you take.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Stop taking this medicine and get emergency help immediately if any of the following side effects occur:

  • Symptoms of unusually high blood pressure (caused by reaction of higher than usual doses of selegiline with restricted foods or medicines) Chest pain (severe)
  • Enlarged pupils
  • Fast or slow heartbeat
  • Headache (severe)
  • Increased sensitivity of eyes to light
  • Increased sweating (possibly with fever or cold, clammy skin)
  • Nausea and vomiting (severe)
  • Stiff or sore neck

Check with your doctor as soon as possible if any of the following side effects occur:

  • More common Increase in unusual movements of body mood or other mental changes
  • Less common or rare Bloody or black, tarry stools
  • Difficult or frequent urination
  • Difficulty in breathing
  • Difficulty in speaking
  • Dizziness or lightheadedness, especially when getting up from a lying or sitting position
  • Hallucinations (seeing, hearing, or feeling things that are not there)
  • Irregular heartbeat
  • Lip smacking or puckering
  • Loss of balance control
  • Puffing of cheeks
  • Rapid or worm-like movements of tongue
  • Restlessness or desire to keep moving
  • Severe stomach pain
  • Swelling of feet or lower legs
  • Tightness in chest
  • Twisting movements of body
  • Uncontrolled chewing movements
  • Uncontrolled movements of face, neck, back, arms or legs
  • Vomiting of blood or material that looks like coffee grounds
  • Wheezing

Symptoms of overdose Agitation or irritability

  • Chest pain
  • Convulsions (seizures)
  • Difficulty opening mouth or lockjaw
  • Dizziness (severe) or fainting
  • Fast or irregular pulse (continuing)
  • High fever
  • High or low blood pressure
  • Increased sweating (possibly with fever or cold, clammy skin)
  • Severe spasm where the head and heels are bent backward and the body arched forward
  • Troubled breathing

Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome:

  • More common Abdominal or stomach pain
  • Dizziness or feeling faint
  • Dryness of mouth
  • Nausea
  • Trouble in sleeping
  • Vomiting

Less common or rare Anxiety:

  • Back or leg pain
  • Blurred or double vision
  • Body ache
  • Burning of lips, mouth, or throat
  • Chills
  • Constipation
  • Diarrhea
  • Drowsiness
  • Headache
  • Heartburn
  • High or low blood pressure
  • Inability to move
  • Frequent urge to urinate
  • Increased sensitivity of skin to light
  • Increased sweating
  • Irritability (temporary)
  • Loss of appetite
  • Memory problems
  • Muscle cramps
  • Nervousness
  • Numbness of fingers or toes
  • Pounding or fast heartbeat
  • Red, raised, or itchy skin
  • Restlessness
  • Ringing or buzzing in ears
  • Slow or difficult urination
  • Slowed movements
  • Taste changes
  • Uncontrolled closing of eyelids
  • Unusual feeling of well-being
  • Unusual tiredness or weakness
  • Unusual weight loss

With higher doses, Clenching, gnashing, or grinding teeth or sudden jerky movements of body may occur.

Other side effects not listed above may also occur in some patients.

If you notice any other effects, check with your doctor.

 

A further Note about Dopamine (DA) and Cyprenil (Deprenil [selegiline])

This important neurological transmitter chemical is produced by special DA cells like serotonin cells. We have only a few thousands (30-40) of DA producing brain neurons. DA is broken down by MAO-B specifically. The potent free radicals breakdown intermediate products normally produced are very toxic. In humans dopamine production is gradually reduced in almost a linear fashion throughout life due either to a slow reduction of viable DA producing neurons or to increasing MAO-B activity.

When the amount of DA gets small enough in aging the person gets Parkinson disease. This seemingly is what Parkinson's disease is. The amount of dopamine reduction for Parkinson's is around 70-80%. It has been speculated that most people will get Parkinson's if they live long enough. Some speculate that gradual age related reduction of DA production (about 10-13% per decade of adult life) is directly related to long term accumulated free radical damage to the Dopamine cells where it is produced and re-uptaken and then broken down by MAO-B..

The anti-aging drug (Deprenil or selegiline) has shown so much promise in mice as it acts by specifically slowing down MAO-B activity. ) Cyprenil (Deprenil/Deprenyl) has a lot of other benefits but it increases the amount of DA in the brain to more youthful levels and helps the brain run better.

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