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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, but see below
under Interactions.
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. 
Cyprenil 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: Cyprenil, 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 Cyprenil:
o 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.
o .It is effective in the prevention
and treatment of Parkinson's and Alzheimer's disease.
o 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".
o The unique antioxidant properties of Cyprenil protect
brain cells from deteriorating over time.
o 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 erythematosus, arthritis, etc.
o Other tests have demonstrated that
Cyprenil 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.
o 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.
o 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.
Age Dosage
45- 1 mg/ day
50- 2 mg/ day
55- 3 mg/ day
60- 4 mg/ day
65- 5
mg/ day
70- 6 mg/ day
75- 8 mg/ day
80- 9 mg/ day
80 over 10mg/
day
Cyprenil 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:
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 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.
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 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.
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.
Keep
this and all other medicines safely out of the reach of children. DEPRENYL
TABLETS/ JUMEX®: 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.
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