Dr. Sahelian's Deprenyl
Experience
I have noticed that deprenyl (selegiline) provides a sense of wellbeing
with slightly brighter vision and libido. High doses may induce
heart palpitations
or irregularities. Periods of alertness and sleepiness are possible.
Deprenyl Availability
Deprenyl is a prescription medicine but can be obtained from overseas.
Side effects
Adverse effects include heart rhythm disturbances, sleepiness at times during
the day and insomnia at night.
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Deprenyl Research
Update
Pharmacological aspects of (-)-deprenyl.
Curr Med Chem. 2004 Aug;11(15):2017-31.
Deprenyl, the selective irreversible inhibitor of monoamine oxidase-B (MAO-B),
has been synthesised as a potential antidepressant, however, due to its dopamine
potentiating capacity, became a registered drug in the treatment of Parkinson's
disease. Deprenyl possesses a wide range of pharmacological activities; some of
them are not related to its MAO-B inhibitory potency. Beside its dopamine potentiating effect, it renders protection against a number of dopaminergic,
cholinergic and noradrenergic neurotoxins with a complex mechanism of action. By
inducing antioxidant enzymes and decreasing the formation of reactive oxygen
species, deprenyl is able to combat an oxidative challenge implicated as a
common causative factor in neurodegenerative diseases. In a dose substantially
lower than required for MAO-B inhibition, deprenyl interferes
with early apoptotic signalling events induced by various kinds of insults in
cell cultures of neuroectodermal origin, thus protecting cells from apoptotic
death. Deprenyl requires metabolic conversion to a hitherto unidentified
metabolite to exert its antiapoptotic effect, which serves to protect the
integrity of the mitochondrion by inducing transcriptional and translational
changes. Pharmacokinetic and metabolism studies have revealed that deprenyl
undergoes intensive first pass metabolism, and its major metabolites also
possess pharmacological activities. The ratio of the parent compound and its
metabolites reaching the systemic circulation and the brain are highly dependent
on the routes of administration. Therefore, in the treatment of
neurodegenerative diseases, reconsideration of the dosing schedule, by lowering
the dose of deprenyl and choosing the most appropriate route of administration,
would diminish undesired adverse effects, with unaltered neuroprotective
potency.
l-Deprenyl prevents lipid peroxidation and memory deficits produced by cerebral
ischemia in rats.
Cell Mol Neurobiol. 2004 Feb;24(1):87-100.
1. The present work shows the results on behavior and on biochemical
parameters of l-deprenyl (0.1, 5, and 10 mg/kg, p.o.) administered daily for 5
days to rats submitted to global cerebral ischemia. 2. The transient global
ischemia was carried out by clamping the animals bilateral common carotid
arteries for 20 min. The parameters studied were memory acquisition and memory
retention, locomotor activity and thiobarbituric acid reactive substances, as an
index of lipid peroxidation. 3. l-Deprenyl treatment significantly improved
memory deficits as compared to the ischemic group as measured by the elevated T
maze test. A similar result was observed on the passive avoidance test where l-deprenyl
improved late but not early memory as compared to the ischemic group. Except for
an increased locomotor activity observed in the group treated with 5 mg/kg, no
other alteration was detected in this behavioral test. Rats submitted to
transient global ischemia (and without l-deprenyl) showed an increase in MDA
levels in the hippocampus and the treatment with l-deprenyl (5 or 10 mg/kg)
significantly reversed this effect bringing values close to those of the
sham-operated controls. A similar profile was observed with nitrite levels. 4.
In conclusion, the work showed a significant protective effect of l-deprenyl on
memory deficits and lipid hyperperoxidation observed after cerebral ischemia.
Possibly, the drug is acting at least in part through its antioxidant activity.
Deprenyl medication emails
Q. I am considering purchasing some of
your products, one being sam-e. I understand that sam-e has some
neurotransmitter effects. Would there be any adverse interactions between sam-e
(approx 1 g/ed) and deprenyl at 1-2.5 mg/d, or can they be taken together
with no problems?
A.
SAM-e has a stimulatory nature and even 200 mg can be a lot for some people.
Deprenyl can stimulate dopamine levels, the combination may be too much and
overly energizing, however if dosages are kept very low for both, it may work,
under medical supervision.
Q. I am trying deprenyl at 1-2.5 mg day in the morning
and I think I get the side effect you mention: "Periods of alertness and
sleepiness are possible. "Can you please point me to some resource to understand
this or give me a brief explanation?
A. I'm guessing that this may be due to the effect of dopamine on the
sleep/awake centers in the brain. There are times during the day when dopamine
may actually cause sleepiness, and also there are areas in the brain where
dopamine would lead to sleepiness whereas other parts of the brain exposed to
dopamine would cause alertness.
I have read where deprenyl is
currently being prescribed both as a preventive and as a cure for Parkinson's
Disease? Can you share what information you have regarding this drug?
This medication is helpful in some patients with PD, but it
is not a cure.