Product Information: Deprenyl

One of the most important anti-aging medicines

Product Information
Deprenyl also known as selegiline has shown the ability to increase life expectancy of animals after a series of famous experiments in the 1960’s by Professor Joseph Knoll. He showed that deprenyl improves the availability of dopamine, and slows its age related decline by acting as a selective MAO-B inhibitor and even more importantly (according to Professor Joseph Knoll), it has an enhancer effect and helps maintain healthy brain cells (particularly in the dopamine producing neuron area of the brain called the substantia nigra).

Deprenyl is noted to have anti depression properties and an aphrodisiac effect (more so for men) and to improve sexual dysfunction.

It's approved use is to treat Parkinson's disease (because this is a disease that affects the brain levels of dopamine), but it is also being used more and more in other dementias and even cancers. Parkinson and Alzheimer's disease patients are often treated with very high doses of 20mg daily (often along with other drugs of course). Anti-aging doses (dependent on age and condition) are more likely to be 2.5mg to 5mg once, twice or three times a week. Or better still 1-3mg per day with occasional breaks.

Deprenyl tablets are selegiline hydrochloride, which is seligiline bonded to an in-organic molecule, however liquid deprenyl citrate (LDC) is seligiline bonded to an organic molecule, one reason why the liquid deprenyl citrate is considered to be superior. This form is generally recognized as the most pure and potent form of deprenyl available. It also allows precise titration for anti-aging purposes, as each ml drop in the bottle is equivalent to 1mg deprenyl citrate. The manufacturer recommends 1mg two times a week for 30 to 35 years olds up to 10mg daily for 80 year olds plus (an age/ dosage list in English is enclosed with order).

Ward Dean MD recommends reducing deprenyl doses after several months to lower levels.

Caution: Deprenyl hydrochloride is a controlled substance in Japan.

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Manuracturers Insert
Deprenyl Liquid - Selepryl

Selepryl contains selegiline citrate and purified water.

Selegiline was first synthesized in Hungary in 1965. While studying its pharmaceutical effects, Dr. Joseph Knoll discovered the exceptional antidepressant properties of Selegiline. During the 808, 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 Selegiline have been at hand on hundreds of medical reports, since its inception almost four decades ago!]-
Since 1991, Cyto Pharma DE Mexico S.A., a., company with 30 years of experience in the chemical and pharmaceutical field, has committed itself to the research of Selegiline. DE MEXICO, S.A. The result: Selepryl, Selegiline in citrate form, easily administrable in increment levels of I mg, highly pure and of almost immediate absorption.

Benefits of the preventive use of Selepryl:

• Selepryl 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 Selepryl 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. . Selepryl counteracts the depressive emotional conditions that are frequent in patients suffering from degenerative diseases, such as cancer, chronic fatigue, diabetes, lupus erythematosus, arthritis, etc.
• Other tests have demonstrated that Selepryl dramatically increases the motor ability, awareness, activity and the general well being of elder 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.
• Selepryl 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.

Age Dosage

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

Quality of life usage indications and dosages:

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

Alzheimer's Disease: May be helpful in treatment.

Dosage: 5 mg in the morning and 5 mg in the afternoon.
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 I mg per day until reaching proper dose for age. If tremors return, increase dose by I mg a day, until they disappear again, and continue at that dosage. Do not exceed 10 mg per day.

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 I mg per day until reaching proper dose for age. If high blood pressure returns, increase dose by I mg a day, until it disappears again, and continue at that dosage. Do not exceed 10 mg per day.

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

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.

Manufacturers Insert
Deprenyl Tablets - Jumex

Chemical: Selegiline Hydrochloride

Excipients: Lactose, cornstarch, polyvinyl pyrrolidone, monohydric citric acid, magnesium stearate.

Adverse Effects and Precautions: Selegiline is often given as an adjunct to levodopa therapy and many of the adverse effects reported can be attributed to enhanced levodopa activity- dosage of levodopa may have to be reduced. Adverse effects have included hypertension, nausea, confusion, psychosis, hallucinations, and increased dyskinesias. Unlike non-selective monoamine oxidase inhibitors such as phenelzine, selegiline is reported not to interact with tyramine in food at usual doses.

Interactions: Although selegiline is less likely than non-selective monoamine oxidase inhibitors to interact with tyramine in food, like other monoamine oxidase inhibitors it can produce life-threatening reactions when given with pethidine. Zornberg GL, et al. severe adverse interaction between pethidine and selegiline. Lancet 1991- 337: 246. Correction. ibid.- 440.

Uses and Administration: Selegiline hydrochloride is a selective inhibitor of monoamine oxidase type B, an enzyme involved in the metabolic degradation of dopamine in the brain. It enhances the effects of levodopa and is used in Parkinson's disease as an adjunct to levodopa therapy, usually when fluctuations in mobility have become a problem. It is administered in a daily dose of 10 mg, either as a single dose in the morning or in 2 divided doses of 5 mg at breakfast and lunchtime. Addition of selegiline to levodopa therapy may enable the dosage of levodopa to be reduced by an average of 30%. Selegiline may also be given alone in early Parkinson's disease in an attempt to slow disease progression (see under Parkinsonism, below). A dose of 10 mg of the hydrochloride daily has been suggested for this purpose.

Dementia: Double-blind studies (1,2) indicate that selegiline may produce beneficial effect in-patients with Alzheimer's disease but it has been suggested that improvements in mood and cognitive function may be due to a reduction in tension and depression. (3) 1. Piccinin GL, et al. neuropsychological effects of L-deprenyl in Alzheimer's type dementia. Clin Neuropharmacol 1990- 13: 147-63. 2. Mangoni A, et al. Effects of a MAO-B inhibitor in the treatment of Alzheimer disease. Eur Neurol 1991- 31: 100-107. 3. Anonymous. Drugs for Alzheimer's disease. Drug Ther Bull 1990- 28: 42-4.

Depression: Several studies have suggested that like non-selective monoamine oxidase inhibitors such as phenelzine, selegiline may be of some benefit in depression. Mendlewicz and Youdim reported a marked improvement in 14 patients with unipolar or bipolar depression who received selegiline hydrochloride 5 mg three times daily for 40 days compared with 13 patients given placebo. (1) Similarly, Birkmayer et al. reported benefit in an uncontrolled study in 102 outpatients and 53 inpatients with unipolar depression who received selegiline hydrochloride 5 to 10 mg daily in association with phenylalanine 250 mg daily- about 70% of these patients, in whom conventional antidepressants were not effective, were reported as having complete remission. (2) The benefit was not thought to be due to the amphetamine metabolites of selegiline. Benefit has also been reported in-patients with atypical depression who received selegiline hydrochloride in doses of 10 to 40 mg daily. (3) At high doses the specificity of inhibition is reported to be lost and restriction of tyramine in the diet becomes necessary as with more conventional monoamine oxidase inhibitors- in this study there was little evidence of such a loss of specificity. 1. Mendlewicz J, Youdim MBH. L-Deprenil, a selective monoamine oxidase type B inhibitor, in the treatment of depression: a double-blind evaluation. Br J Psychiatry 1983- 142: 508-11 2. Birkmayer W, et al. L-Deprenyl plus L-phenylalanine in the treatment of depression. J Neural Transm 1984- 59: 81-7. 3. Quitkin FM, et al. l-Deprenyl in atypical depressives. Arch Gen Psychiatry 1984- 41: 777-81.

Parkinisim: Early attempts to prolong the actions of dopamine in the brain by administration of monoamine oxidase inhibitors were unsuccessful because of intolerable side effects and the risk of potentially catastrophic hypertension. However, the discovery that monoamine oxidase (MAO) exists in at least 2 forms, A and B, and the realization that dopamine in the brain is metabolized predominantly by MAO-B led to the identification of selegiline, which could delay oxidative diminution of dopamine in the brain without provoking a `cheese-reaction'. (1) When given to patients experiencing fluctuations in levodopa's effect due to `wearing-off' or `end-of-dose' effects selegiline ameliorates the fluctuations in about 50 to 70% of patients, and permits a reduction in levodopa dosage of up to about 30%. (2,3) However the benefit is usually modest, and declines after 6 to 12 months in most patients with complete loss of benefit usually in 12 to 24 months. (2) More severe fluctuations in mobility associated with the `on-off' effect in advanced Parkinsonism are unlikely to respond to adjuvant selegiline. (3) More recently much interest and controversy has surrounded the possibility that selegiline given in early Parkinson's disease may retard disease progression. Several uncontrolled studies had reported that long-term administration of selegiline with levodopa prolonged the period of responsiveness to the latter and resulted in increased life expectancy of parkinsonian patients. (4,5) Furthermore, a theoretical basis for benefit exists in the model of Parkinsonism caused by methylphenyltetrahydropyridine (MPTP) which relies on conversion by monoamine oxidase type B to the active methylphenylpyridinium (MPP (+)) radical to produce damage to the striatum. (3,6) More recently, controlled studies by Tetrud and Langston (in 54 patients) (7) and by the Parkinson Study Group (the DATATOP study, involving 800 patients) (8) have shown a significant prolongation in the time to reach a level of disability requiring commencement of levodopa therapy. Although some critics have suggested that selegiline is simply providing symptomatic relief in disease which continues to progress (9-11) the promising preliminary results have been suggested by others to justify the prescription of selegiline 10 mg daily to patients, especially younger ones, in the early stages of Parkinson's disease, in the hope of impeding progression. (12)

1. Anonymous. Deprenyl in Parkinson's disease. Lancet 1982- ii: 695-6. 2. Anonymous. Pergolide and selegiline for Parkinson's disease. Med Lett Drugs Ther 1989- 31: 81-3. Golbe LI, et al. Selegiline and Parkinson's disease: protective and symptomatic considerations. Drugs 1990- 39: 646-51. 4. Birkmayer W, et al. (-)-Deprenyl leads to prolongation of L-Dopa efficacy in Parkinson's disease. Mod Probl Pharmacopsychiatry 1983- 19: 170-6. 5 Birkmayer W, et al. Increased life expectancy resulting from addition of L-deprenyl to Madopar treatment in Parkinson’s disease: a long term study. J Neural Transm 1985- 64: 113-27. 6. Steventon G, et al. Monoamine oxidase B and Parkinson's disease. Lancet 1990- 335: 180. 7.