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Depression
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2 New Drug Treatments
Tianeptine,
the Novel Serotonin Activator
 Interestingly,
the new drug tianeptine (brand name Stablon®) is chemically related to
amineptine (brand name Survector®). Amineptine
was a drug unique in that it was a dopamine
reuptake inhibitor and was proving very popular as an antidepressant,
(as a quick review of any of the internet chat-groups will reveal). Unfortunately, it appeared
that amineptine helped aid orgasm and as such was
considered by the authorities to be a "drug of abuse and
potentially addictive". Many drugs that "interfere"
with dopamine have been shown to improve libido, particularly for men (for
example deprenyl,
L-dopa, and GHB). But perhaps amineptine was even stronger. As a
result, it is my understanding that the FDA pressured the foreign manufacturer
to remove the drug from the market. But
this is hardly the first time such actions have been taken (minaprine and
fipexide for example), and I am sure it won't be the last time.
While
tianeptine is chemically related to amineptine, it is not a dopamine reuptake inhibitor. Instead
it displays another totally unique action. Tianeptine is a serotonin reuptake
accelerator and works exactly opposite to the SSRI’s. Whereas SSRI’s
increase serotonin, tianeptine takes serotonin out of circulation. Yet
tianeptine still works. It
stimulates the uptake of serotonin and reduces the
hypothalamic-pituitary-adrenal response to stress.
Tianeptine-
the Clinical Trials
In trials, tianeptine has
shown to be well tolerated in the short term (3-months) and the tong term
(1-year). In particular it has been noted that tianeptine is effective in
depressed patients who also suffer from anxiety and disturbed sleep. One study suggested that tianeptine can be placed in a middle position in the
bipolar classification, between the sedative and stimulant antidepressants. When
compared in clinical studies to other antidepressants such
as fluoxetine (Prozac®), tianeptine exhibits good efficacy and safety.
Tianeptine
is a new and novel serotonin drug, its antidepressant and anxiolytic properties
and its action on somatic complaints make the drug particularly suitable for the
treatment of the entire range of depressive symptomology.
Tianeptine-
Dosages, Contraindications and Side Effects
Possible side effects have
to date been reported as dry mouth, anorexia, nausea, flatulence and gastralgia. In rare cases were the drug has been administered in the late
evening, insomnia and nightmares have been reported. Further rare side effects include dizziness, faintness and
respiratory discomfort, however taken as a whole the side effects with
tianeptine are few compared to many other of the standard anti-depressants.
Tianeptine should not be
taken with MAO inhibitors, and the maker suggests an interval of at least
15-days between a MAOI and tianeptine use. Although not clearly stated, use with
other anti-depressants, especially those that alter serotonin levels should only
be undertaken under the close supervision of your physician. Dosages have been
12.5mg two or three times a day.
Moclobemide-The
Unique MAO-A Inhibitor
A lot of focus has been
placed over the years on monoamine oxidase (MAO). MAO is an enzyme that helps
break down neurotransmitters, as such inhibiting MAO leads to an improvement in
the availability of the brain neurotransmitters (these inhibitors are
abbreviated to MAOl). At first, the early drug developments were irreversible
MAOIs, these exhibited the so-called cheese effect, whereby the ingestion of
certain foodstuffs containing tyramine (such as aged cheese and red wine) could
cause a life-threatening situation. Gerovital-H3
was noted as being one of the first and most effective mild reversible MAOls to
appear in the marketplace, and is undoubtedly one of the reasons why it has an
anti-depressive effect and remains one of the most popular antiaging medicines
today. Later came the development
of safer reversible MAOI drugs. MAO can be divided into few categories, MAO-A and
MAO-B, the-A form being the more abundant and potent of the two.
All MAO inhibitors inhibit both the MAO-A
and the MAO-B except deprenyl (selegiline) and moclobemide which
only inhibit MAO-B.
Moclobemide (trade name Moclamine®) developed by Roche is a selective, short acting and reversible MAO-A
inhibitor designed as an anti-depressant. It has been shown to increase
brain levels of serotonin and noradrenaline.
Moclobemide’s interaction with dietary amines causes considerably less
increase in blood
pressure than with other MAO inhibitors.
Moclobemide-the
Clinical Trials
Studies
have shown that moclobemide is as effective as the tricyclics and much better
tolerated and is considered to be comparable to the SSRI's in both efficacy and
tolerability. One study compared a 450mg dose of moclobemide and fluoxetine
(Prozac®)
at 20mg daily. Two groups of approximately 60-patients were selected for
either an 8-week trial or a 1-year trial. Within
8-weeks the efficacy data showed there was little difference between the
effectiveness of either moclobemide or fluoxetine
(Prozac®)
with anti-depressive benefit
for 63% and 70% respectively. At
the 1-year stage there were no severe side effects in either group and the study
concluded that in both groups of patients were much or very much improved. The data
from the study also showed that moclobemide produced far fewer
side-effects than fluoxetine.
Moclobemide-
Dosages, Side Effects and Contraindications
There
is little clinical evidence to support the use of other anti-depressants with
moclobemide, however one Australian study suggested that "moclobemide can
have significant interactions with both selective serotonin reuptake inhibitors
(SSRI's) and tricyclic antidepressants (TCAs), even in therapeutic doses."
Therefore combination with any anti-depressants should not be undertaken unless
under the close supervision of your physician. The makers insert also states
that moclobemide should not be used if you suffer from a tumor of the adrenal
glands; and caution also advised if you suffer from a thyroid condition. Under
normal conditions, with the "standard" dosages of 300mg to 450mg daily
side effects have been noted as sleep
disturbances, dizziness, headache, and confusion. But remember that studies have
shown moclobemide to have fewer side effects than standard SSRI drugs and may be
more effective in cases of mild to moderate depression. Dosages are normally
150mg twice or three times a day.
Other
Novel Approaches
That
brings us to the last relatively new drug that is showing promise in the battle
against depression. The drug is Picamilon (sometimes also spelled Pikamilon with or without the e on the end). Officially
it is an anti-anxiety drug, but is also possesses stimulatory properties and
anti-depression qualities. I believe that often times, anxiety is the cause of
depression and vice-versa and I refer back to my original comment in the early
part of this article, where I stated: "The individual's interpretation of
these varied brain imbalances may cause many patients to claim they are feeling
depressed." In other words, we are never taught how to interrupt different
feelings, and so very often the words that the doctor hears are simply "I'm
depressed."
Picamilon-The
Russian Connection
Picamilon (www.picamilon.net)
is a Russian
development, it is in essence the bonding of niacin (vitamin B3) to the amino
acid GABA.
This combination acts very differently and uniquely and can't be compared to taking niacin and GABA
together as individual supplements.
Niacin is very
effective in crossing the blood-brain barrier and has been shown to enhance
cognitive function by protecting the neurons against the effects of diminished
blood flow. GABA on the other hand
has a calming action and possibly helps to stabilize other neurotransmitters.
Picamilon-
Anti-Anxiety, Anti-Depression & Stimulation, All in One?
Picamilon
is a very effective vasodilator (it improves brain blood flow).
In fact Russian research suggests that picamilon is a better vasodilator
than both Hydergine and vinpocetine. I
would consider vinpocetine to be the current industry leader in regard to its
vasodilatation action, so for picamilon to be considered better is indeed
noteworthy.
It
appears that the synergism between niacin and GABA is very strong.
For while picamilon produces vasodilatation (likely the action of
niacin), it also produces a mild tranquilizing effect which helps prevent the
negative effects of emotional stress. The tranquilizing effect is likely
produced by GABA, as it is the basis of the diazepam tranquilizing drugs (such as
Valium®) which inhibit the reuptake of GABA.
But
what makes picamilon unique is that while it counteracts stress and
anxiety, it doesn't have a sedative action. In fact quite the opposite; it can
have
a mild stimulatory action. Picamilon may be the first anti-anxiety drug that doesn't make-you
drowsy. Russian studies going back
to 1989
have compared picamilon with other psycho-stimulant drugs including piracetam, phenazepam, diazepam,
vinpocetine, xanthinol nicotinate, and papaverine. It was noted that the stimulant properties of
picamilon were
greater than that of piracetam. After
taking picamilon the patients felt better and giddiness and tremor disappeared.
Further benefits of picamilon over the traditional tranquilizing
drugs are that it does not display any signs of inducing muscle relaxation,
lethargy, or drowsiness.
Picamilon
has a number of positive benefits. It can reduce anxiety, lower
stress and yet at the same time display a non-sleepy action or indeed even a
stimulatory property. As such, many patients exclaim that they have a "good
feeling" while using the picamilon.
Picamilon-Dosages,
Side Effects and Contraindications
With
over 10 years of use in the former Russian states, picamilon is considered to be very safe.
It has not been shown to produce any
altergenic, teratogenic, embryotoxic, or carcinogenic effects. Most side effects
have been noted as
headache, dizziness and
nausea, it has been stated that at higher dosages picamilon can lower blood
pressure, and while this may be advantageous in some cases those persons with
low blood pressure should be monitored. Due
to its potent properties it is advisable not to use any other vasodilating
agents while using picamilon unless under the supervision of a physician.
Apart
from the known listed drugs this list may also want to include vinpocetine,
ginkgo biloba, niacin derivatives (such as xanthinol nicotinate) and the ergot
preparations such as bromocriptine, Hydergine, and nicergoline.
The
effects of picamilon are fast acting, often within an hour the effects continue for a period of approximately 6
hours.
Accordingly,
dosages have been applied two or three times daily, but late evening use should
be avoided otherwise insomnia may result. Dosages
for anti-anxiety are approximately 100mg 1 to 3 times daily. If a stimulatory
effect is required, the dosage should be increased.
Picamilon
The Conclusion
to
order
Unfortunately,
there hasn't been enough time or space
to elaborate on the many properties and uses of picamilon. To list a few of the
known clinical results, picamilon has shown promise in memory, mood, anxiety,
stress, motor and speech disturbances, sleep, irritability, alcohol withdrawal,
and visual acuity,
The
Conclusion of the New Generation of Brain Drugs and Anti-Depressants
I
hope that what I have managed to achieve in this small article is an idea of the
new directions in which anti-depression treatments are going with the latest
commercially available brain drugs.
The
main hope is that at long last pharmacological treatment for depression is being
looked at on a multi-level, encompassing new and novel approaches. The main
draw-back to the new therapies is the lack of knowledge in how to use many of
these 'different products in unison, in order to take advantage of any potential
synergy. More often than not, any combination is shied away from by the
manufacturer because of concerns of liability. This leaves it in the hands of the physician to use his or
her knowledge and skill.
Hopefully,
in the not-so-distant future we shall see the development of tests that will
enable the physician to determine the precise cause of the depression and treat
it accordingly and not to rely solely upon what's written in the Physician's
Desk Reference.
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