I started Picamilon around 10 years ago. The effect was
amazing. I have brain injury stemming from TB meningitis as
a child and all my life my brain has tended to fog up. When
I started taking picamilon, it was like fog burning away.
David in Sydney
Picamilon is working very well for me... stopping
depression and anxiety. It has a tranquilizing action plus mood enhacement.
I ordered your Picamilon recently
and after just a few days I notice a huge
difference. I've suffered from anxiety/panic/depression for years and I now
believe the missing link was GABA. Literally within a couple days my anxiety
is gone and so is the rest of my depression. This is easily the best
supplement I've ever tried and is the only one that lives up to it's claims.
I'll definitely be ordering more in the future. Thanks!
Picamilon has worked very well for me and I regularly order extra bottles to give to
someone I think may need it. My doctor had not been the same person since
his wife died 3 years ago. He agreed to try the bottle of picamilon that I
gave him and he later said,
"Picamilon has transformed my life. Life has taken on new meaning for me."
Another person I know was in a suicidal depression and I convinced him to take
the picamilon I gave him. Within 3 days he came out of his depression.
Another doctor I persuaded to take picamilon said, "I don't know if the
picamilon is responsible but I feel so much better since I started taking it."
Picamilon has given me a new lease on life. It took 6-8 weeks for me to feel the
effects but now every day is a pleasure and I'm on top of the world.
Picamilon works well for both anxiety and depression.
Picamilon helped my anxiety when none
of the drugs the doctor prescribed worked for me.
Las Vegas, NV
Picamilon is the best product I've ever used.
I have tried Paxil, Zoloft, SAMe, and Rhodiola. SAMe worked well for
awhile but then didn't seem to work anymore.Rhodiola is good but nothing
compares to Picamilon.
Long Beach, CA
by A.L. Karayev
The chemical modification of widely used vitamins is one
of the fundamental trends in the search for new pharmaceutical agents. The main
advantages of vitamin-like drugs are the broad spectrums of action, the easy
penetration through cellular membranes, the low toxicity, and the rare side
effects. The broad spectrum of action of these agents is connected not only with
their influence on unspecific metabolic processes, but also on various
In experiments, Picamilon decreases cerebral blood-vessel
tone and increases intracranial circulation rate. The drug exceeds in force and
duration the effects of GABA and niacin alone. In small doses, Picamilon shows
tranquilizing action to prevent the negative effects of emotional stress. As
with diazepam, it depresses motivative aggression. The tranquilizing influence
of the drug on negative emotions expressed through the hypothalamic system has
been proved. Picamilon is characterized by a tranquilizing effect, without a
sedative component but with elements of stimulant action.
The drug effectively counteracts stress and lowers the depressing influence of
ethanol on the behavior of animals. It rapidly penetrates through the
blood-brain barrier and improves the functional state of the brain by producing
a beneficial effect on its metabolism.
Picamilon has been found to have low toxicity during
experiments on animals. The median lethal dose is more than 10 gram per kilogram
of body weight and more than 6 g/kg intravenously. The low toxicity was
demonstrated during six months of chronic toxicity testing when the drug
displayed no allergenic, carcinogenic, teratogenic or embryotoxic action.
Significant Neurologic Improvement
Picamilon proved to be quite effective in patients with acute brain syndrome.
the second or third day after taking the medicine, the patients showed
significant neurologic improvement. The positive dynamics of the cerebral signs
were noted. The effect increased when taking the drug, especially during the
second and third week of treatment. In this case, objective methods of
examination were used to document the increase of cerebral circulation, and the
normalization of cerebrovascular resistance.
Picamilon was effective in patients with mild-to-moderate impairment during
subacute and early convalescent periods. It improved emotional conditions,
speech and memory. Patients showed increased general activity, and better work
and social adaptation.
Picamilon stimulated physical and psychic rehabilitation
from various asthenic (weakening) disorders due to mental and somatic pathology.
Picamilon was effective in patients with neurotic disorders in which the leading
signs were asthenic-astheno-depression, and astheno-hypochondriac disturbances
that accompany fear, anxiety, fatigue, emotional and vegetative instability, and
Picamilon reduced anxiety and hyperesthesia (whereby
normal touch creates pain) without sedative effects, which improved sleep.
According to the majority of researchers, usage of Picamilon employed as a means
of correcting neuroses, manic-depressive syndrome, involutional depression and
schizophrenia enabled doctors to decrease doses of psychotropic drugs used in
the treatment of these conditions. The combining of Picamilon with conventional
treatments accelerated reduction of the psychopathological signs when compared
to conventional treatments alone.
Improvement in A Week
Picamilon also was effective in patients with psycho-organic syndromes including
cerebral atherosclerosis, brain injury from physical trauma, and toxic lesions
of the brain. The condition of these patients took a turn for the better by the
end of the first week.
The effectiveness of Picamilon in patients with migraine
headache was studied. It has been established that the drug has a pronounced
effect on painful hemicrania-pain or headache in one side of the head-by
decreasing its intensity and mitigating or stopping any accompanying symptoms.
In persons suffering from chronic alcoholism, Picamilon alleviated withdrawal
Alcohol Withdrawal Aided
The effectiveness of Picamilon was compared with other similar drugs, including
piracetam, phenazepam, diazepam, vinpocetine, xanthinol nicotainate and
papaverin. It was
noted that the psycho-stimulant effect of Picamilon was greater than piracetam.
After taking Picamilon the patients felt significantly better. Giddiness and
tremor disappeared quicker.
Most patients preferred Picamilon to piracetam. It normalized the behavior of
patients faster and more completely than piracetam. In another study, Picamilon
acted faster than vinpocetine in treating withdrawal symptoms in patients
suffering from chronic alcoholism.
According to clinical studies, Picamilon is recommended
for the treatment of cerebrovascular diseases in subacute and early convalescent
periods, as well as for transient brain damage, neurocirculatory dystonia, and
chronic cerebral circulatory insufficiency. The drug is recommended as a
tranquilizer possessing no sedative action. Picamilon can be prescribed in cases
of asthenic (weakening) syndrome and disorders due to various psychotic and
somatic pathology. It is used in the treatment of depressive disorders in the
elderly and as therapy for senile psychoses. It also is recommended for the
prevention and treatment of anxiety and stress. Picamilon may be used to relieve the symptoms of
How And Why Picamilon Works
by R. P. Kruglikova
Drugs that normalize the gamma aminobutyric acid (GABA)
system consist mainly of substances that activate GABA receptors, inhibit GABA
utilization or increase the permeability of the blood-brain barrier to GABA.
One-way of creating preparations of this kind is to use substances that are
carriers of the GABA molecule, including vitamins or their derivatives and, in
particular, nicotinic acid (niacin).
Niacin has been chosen as the carrier because of its
valuable pharmacological properties, its low toxicity, and its high biological
availability. It has therefore been suggested that a combination of niacin and
GABA in the same molecule would increase the potency of each component.
Picamilon (nicotinyl-y-aminobutyric acid) was first synthesized at the All-Union
Vitamin Research Institute in 1970. It is a white crystalline powder that is
odorless, highly hygroscopic (takes up moisture readily), and readily soluble in
In studies in animals Picamilon has been shown to have
positive action on the cerebral circulation, and also exhibits the properties of
a tranquilizer with a stimulating component. Unlike tranquilizer drugs,
Picamilon does not induce muscle relaxation, drowsiness or lethargy.
The action of the compound on cerebral circulation and on
neural regulation was studied in anesthetized cats; conscious, unrestrained
cats; and on unanesthetized rabbits. Picamilon stimulated cerebral circulation
and lowered vascular tone in both arterial systems of the brain. The increase in
the blood supply to the brain in conscious animals took place to a more marked
degree than in cats under general anesthesia. The drug also lowered blood
pressure. It must be emphasized that these effects manifested themselves after
both intravenous and oral administration of the compound. In all the animals,
Picamilon increased blood flow.
In the strength and duration of its cerebrovascular
effect, Picamilon is much superior both to GABA and to niacin. Under the same
experimental conditions, GABA in a dose of 10 mg/kg (intravenously) caused no
change in cerebral blood flow, and only when given in a dose of 300 mg/kg did it
increase blood flow, with the effect lasting three to five minutes. Niacin in
large doses (50 to 100 mg/kg) increased cerebral blood flow by 5 to 10 percent.
Brain Blood Flow
In its effect on cerebral circulation, Picamilon was shown to be more effective
than papaverine, nialamide, xanthinol nicotinate, and
An essential role in the mechanism of action of Picamilon
is its effect on nervous control of the cerebral circulation. It weakens changes
in cerebral blood flow during the vasomotor reflex, considerably inhibits
constrictor responses of vessels in the carotid and vertebrobasilar basins due
to stimulation of afferent fibers of somatic nerves, and causes gradually
developing inhibition of tonic and reflex activity in sympathetic nerves.
Neuropharmacological screening tests on Picamilon have demonstrated its
tranquilizing properties in small doses. For instance, at a dose of 1 mg/kg,
Picamilon prevents the negative consequences of emotional stress (in cats it
normalizes the orienting reaction when disturbed by the response to rage and
fear). Like diazepam, it has an inhibitory effect on motivated aggression,
associated with fighting for territory in rats.
Investigation of Picamilon's effect on the threshold of
"self-stimulation" showed that in higher doses (80 and 160 mg/kg), in
contrast with small doses, which have a tranquilizing effect, Picamilon lowered
the "self-stimulation" threshold (like amphetamine), but at the same
time reduced the number of self-stimulation. The stimulating action of the drug
also has been shown in general anesthesia. For instance, at a dose of 100 mg/kg,
Picamilon reduced by 1.7 times the duration of the sedative effect of
hexobarbital sodium and reduced by half the duration of thiopental anesthesia.
Unlike tranquilizer drugs (chlorodiazepoxide, diazepam, relanium, phenazepam),
Picamilon does not induce muscle relaxation, drowsiness or lethargy. Clinicians
have stated that the drug closely resembles vinpocetine (the ethyl ester of
apovincamic acid), but comparison of the properties of the two compounds showed
that Picamilon is superior.
After the administration of Picamilon at a dose of 5
mg/kg, defense-conditioned reflexes (jumping onto a rod) were restored after
their disappearance due to fatigue (by 130 percent, compared with 12 percent in
the control). Given to rats at a dose of 50 mg/kg it restored physical working
capacity during a rest period of one hour by 76 percent, compared with 38
percent in the controls.
In a model of shock-induced amnesia of the conditioned
passive avoidance reaction, like other GABA-ergic drugs (sodium hydroxy
butyrate, fenibut, pantogam), Picamilon exhibited anti-amnesiac properties.
hypoxic states, the compound was found to have anti-hypoxic activity. The
presence of anti-amnesiac and anti-hypoxic properties in the spectrum of action
of Picamilon places it in the group of nootropic agents.
There is evidence that activation of the GABA-ergic system
in various kinds of stress can prevent damage to the body when exposed to
various stimuli. In confirmation of this hypothesis, scientists who studied the
effect of GABA derivatives on the development of toxic (nicotinic) cerebral
edema (fluid on the brain), showed that Picamilon in a dose of 500 mg/kg,
injected 30 minutes before nicotine (40 mcg/kg), prevented the development of
edema. If Picamilon was given at a dose of 200 to 300 mg/kg, the density of
the brain tissue was increased, but not up to the control level, and the total
water content had no significant change. They suggested that the mechanism of
the anti-edematous action of Picamilon is linked with a change in energy
metabolism in neurologic tissue.
Quickly through The Blood Barrier
Thirty minutes after injections of Picamilon into rats at a dose of 100 mg/kg (intraperitoneally)
the concentration of the oxidized form of nicotinamide adenine dinucleotide (NAD)
in the brain rises by 67 percent above the control level, and that serum lactate
dehydrogenase activity falls by 23 percent, with glutamateoxalate transaminase
activity showing no significant change. A more prolonged action of the compound
led to normalization of the NAD level in the rats' brains.
The study of the effect of Picamilon on active GABA uptake by synaptosomes in
the rat cerebral cortex showed that it moderately inhibits GABA uptake by
synaptosomes, whereas niacin has no appreciable inhibitory action on this
Scientists at the Department of Biochemistry, Odessa University, found that
Picamilon passes quickly through the blood-brain barrier. As early as 30 minutes
after subcutaneous injection, the compound was found in the brain, penetrating
it by an order of magnitude more rapidly than GABA. The time course of
accumulation of Picamilon in the brain correlated with its blood level. Accumulation of the compound in muscle tissue one to two hours after injection
was greater (10 times) than that of GABA. Picamilon is retained in the body
longer than GABA.
A six-month toxicity study showed that Picamilon does not change the behavior or
condition of rats when administered in doses of three to 75 mg/kg, and causes no
significant changes in the blood, urine and internal organs of the animals. Some
morphological changes were found in the kidneys of rats receiving Picamilon in a
dose of 75 mg/kg (15 times higher than the therapeutic dose). A microscopic
study of the kidneys indicated manifestations of glomerulonephritis and
nephrosclerosis, which led to the consideration of renal pathology as a
contraindication to Picamilon. However, during clinical studies with Picamilon-
even when administered over a long period or in repeated courses-no disturbances
were found in the kidneys or the urinary system.
Adverse Effects Few
Picamilon produces no allergenic, teratogenic, embryotoxic or carcinogenic
effects. On this basis, the pharmacological committee of the Ministry of the
Health (Russia) recommended clinical trials of Picamilon for cerebrovascular
disturbances, as a daytime tranquilizer, as a stimulant in depressive and
asthenic (weakening) states, and to improve physical and mental working
capacity. Picamilon was studied in a large number of scientific facilities
within Russia. The total number of patients under observation was 984. Picamilon
tablets were prescribed two to three times a day at a dose of 20-50mg, and in a daily dose
40-300mg grams. Courses of treatment lasted
from two weeks to one-and-a-half months. The effectiveness of treatment was
assessed by clinical and laboratory tests. Cerebral blood movements were
evaluated by objective methods, including echopulsography, echoencephalography,
rheo-encephalography, ultrasonic scanning, biomicroscopy of the conjuctiva, and
In patients with acute cerebrovascular disturbances, improvement occurred on the
fourth or fifth day, when the severity of neurologic symptoms was reduced.
Later, headache, dizziness, noise in the head and memory disorders were reduced,
motor and speech disorders began to regress rapidly, sleep improved, and
irritability, emotional stress and anxiety were reduced. The velocity of
cerebral blood flow was increased.
Administration of Picamilon to patients suffering from the results of
cerebrovascular disturbances (more than a month later) proved effective after
the second or third day of treatment. The patients' emotional background, speech
and memory were improved, and levels of enzyme activity (AST, ALT, LDH) and
lactate concentration were restored to normal. Scientists who studied the
effects of GABA derivatives on the development of toxic cerebral edema (fluid on
the brain) showed that Picamilon in specific doses prevented the development of
In chronic cerebral insufficiency, Picamilon improved the mood and memory of the
patients, reduced irritability and tearfulness, abolished autonomic vascular
manifestations, and reduced metabolic disturbances. In patients with memory
disorders (global amnesia), considerable improvement in memorization and recall
was observed on the fifth to seventh day of treatment, and the patients were
able to return to work.
In patients with astheno-neurotic anxiety and depression, activation of mental
functions and motor activity was observed, including improved speed and quality
of operative activity, concentration of attention and mood, relief of anxiety,
improved working capacity, and so on. The use of Picamilon in depression, along
with moderate doses of tricyclic antidepressants, enabled the doses of the
latter to be reduced. In patients with alcoholism, Picamilon abolished many
withdrawal symptoms, especially apathy, weariness and lethargy. The patients
later become more tranquil, less fussy and anxious, and their working capacity
Lowers Blood Pressure
The effect of Picamilon on cerebral blood flow was compared with that of
papaverine and xanthinol nicotinate. The scientists found that Picamilon had a stronger
blood pressure-lowering effect than papaverine; xanthinol nicotinate mainly affects the
peripheral circulation, and it exhibits neither tranquilizing nor stimulating
Picamilon is an approved drug in Russia. It is intended for use in adults
as a vasoactive (effecting the caliber of blood vessels) and nootropic
(benefiting cognition and nerves) agent for acute cerebrovascular disturbances
of mild severity, chronic cerebrovascular insufficiency, and vegetovascular
dystonia (an imbalance between sympathetic and parasympathetic influences on
vascular tone). The drug is indicated as a tranquilizer for states of anxiety,
fear, increased irritability and emotional stress. Picamilon is
recommended for depressive disorders in the elderly and for senile psychoses.
In management of drug addictions, the compound can be used to abolish withdrawal
symptoms in chronic alcoholics.
translated from Russian
Picamilon increases blood supply and functional state of the brain, increases
microcirculation and hemodynamics of the eyes, and enables improved arterial
blood supply to internal organs. It possesses nootropic, anti-hypoxic and
antioxidant properties, and is retained for a long time in body tissues. In addition, Picamilon renders tranquilizing (not causing
myorelaxation, sleepiness or apathy), and psychostimulating effects, restores
physical and mental working ability after overwork, and lessens the suppressing
influence of ethanol on the central nervous system.
Indications for use
Picamilon is used in the capacity of a nootropic and vasoactive agent for acute
ischemic disturbances of the cerebral blood circulation of mild to moderate
severity; and also during various stages of the restorative period, for
discirculatory encephalopathy, vegetative dystonia, craniocerebral traumas and
neuroinfections. It is recommended for prevention and stopping assaults of the
simple form of migraine.
Preparation is indicated by conditions accompanied by
anxiety, fear, and elevated irritability; by the asthenic states caused by
various neuro-psychological illnesses or connected with increased physical and
mental stress, depressive disorders of the elderly, or senile psychosis.
It is used in complex therapy for stopping acute alcoholic
intoxication. With chronic alcoholism—for decreasing asthenic and
asthenoneurotic, post-psychotic, pre-relapse states, and also for alcoholic
In opthalmological practice, for primary open-angle
glaucoma with normalized intraocular pressure, and for diseases of the retina
and the optic nerve.
In urological practice Picamilon is used in children and
adults with urinary disorders for the purpose of an improvement in the adaptive
function of the urinary bladder.
Methods of treatment and dosage
For discirculative encephalopathy, 20-50mg 3 times per
day. A course of treatment lasts from 1-2 months, and may be repeated after 5-6
For prevention of migraine, tablets of 50mg 3 times per
day; for treating an attack use 100mg in a single dose.
For asthenic states, 40-80mg per diem, in unusual cases
up to 200-300mg per day, for the duration of 1 to 1.5 months.
For depressive states in the elderly, 40-200mg per day in
2-3 doses, for the duration of 1.5 to 3 months.
For restoration of working ability and with increased
workload, 60-200mg per day for 1 to 1.5 months; for athletes the same dose for
2 weeks of the training period.
For alcoholism in a period of abstinence, 100-150mg per
day for the duration of 6-7 days; for more prolonged breakdowns or relapses a
daily dose of 40-60mg.
For treatment of primary open-angle glaucoma, 50mg 3
times per day for the duration of 1 month. In opthalmological practice after
intramuscular or parabulbar introduction, depending on conditions, from 20-50mg 3 times per day, or
60-150mg per day for duration of 1 month.
For functional disorders of urination in children, 20mg 2
times per day for children 3-10 years; 20mg 3 times per day for children over
10 years. For organic disorders of urination caused by myelodysplasia, 20mg 3
times per day for children under 10 years; 50mg 2 times per day for children
11-15 years; and 50mg 3 times per day for children over 15 years. A course of
treatment is 30 days.
For disorders of urination in adults, 50mg 3 times per
day. A course of treatment is 4-6 weeks.
Use of Picamilon is contraindicated in cases of acute sensitivity to the
preparation, or acute severe illnesses of the kidneys.
A Unique Domestic Preparation With a Wide Spectrum of Action
Translated from Russian
The beginning of the 1970s and subsequent years is
characterized by the appearance of a new class of medicinal preparations, called
nootropics, which are finding increasingly wider applications in various areas
of medicine. Nootropic preparations are applied successfully for breakdowns of
memory, attention, learning, and for treatment of loss of brain blood
circulation, brain trauma, chronic alcoholism and other disorders. Among the
medicinal properties of this group a notable place is occupied by the domestic
preparation Picamilon, synthesized in 1969 by the All-Union Scientific Research
Institute and studied in the NII pharmacological RAN . By chemical structure Picamilon is a derivative of the gamma-amino-butyric acid (GABA) and nicotinic
acid. The preparation was introduced in medical practice in 1986, and to the
present time has achieved sufficiently large experience in its application.
The great interest of clinicians in Picamilon may be
attributed to the unique combination of its pharmacological properties. It
possesses high cerebrovascular activity, which exceeds the effect of cinnarizine,
papaverine, xanthinol niacinate, and piracetam. One of the most important
components in the spectrum of psychotropic activity is its nootropic effect,
which determines its clinical use to a significant degree. The preparation has a
unique tranquilizing effect (the manifestation of action is inferior to
diazepam); in this case the preparation does not cause a myorelaxation effect.
The important property of Picamilon is the ability to quickly restore mental and
physical fitness for work, which was lost through overstress. Clinical
experience with application of Picamilon shows that it is effective for ischemic
disturbances of cerebral blood circulation, discirculatory encephalopathy,
vegetative dystonia, and for prevention and treatment of the simple form of
migraine. Picamilon has proven an effective medicinal treatment for patients
with disorders of a neurotic level, with accompanying manifestations of anxiety,
fear, emotional and vegetative instability. Picamilon finds a use in the complex
treatment of alcoholism and acute alcoholic intoxication. At this time the list
of indications for prescription of Picamilon is constantly growing. Clinical
studies have shown that Picamilon possesses favorable properties in
opthalmological practice in the treatment of primary open glaucoma, diseases of
the retina and the optic nerve of vascular genesis. It has been adapted also in
urological practice for treatment of neurological disorders of urination in
children and adults. It is important to note that the use of this preparation
does not cause habituation, but its safety is proven for 10 years in wide and
intensive clinical application. Picamilon is prescribed both in mono-preparation
and in combination with other medicinal agents.
The fact of the varied spectrum of therapeutic action,
noted by many clinicians, testifies to the possibility of a wider application of
Picamilon in the capacity of a medicinal and preventative agent.