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LE Magazine July 1997

Picamilon Draws Attention
This New Russian Drug Rapidly Penetrates
The Blood-Brain Barrier, Producing A Beneficial Effecton The
Brain's Metabolism
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 neurotransmitter systems.
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.
Independent researchers in 16 medical centers in Russia carried
out a clinical trial with Picamilon in a great number of patients.
Picamilon was prescribed two or three times a day in doses
of 20 to 50 mg. The course of therapy ranged from two weeks
to three months.
Significant Neurologic Improvement
Picamilon proved to be quite effective in patients with acute
brain syndrome. On 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-asthenodepression,
and asthenohypochondriac disturbances that accompany fear,
anxiety, fatigue, emotional and vegetative instability, and
sleep disturbances.
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 symptoms.
Alcohol Withdrawal Aided
The effectiveness of Picamilon was compared with other similar
drugs, including nootropyl, phenazepam, diazepam, vinpocetin,
complamino and papaverin. It was noted that the psycho-stimulant
effect of Picamilon was greater than nootropyl (piracetam).
After taking Picamilon the patients felt significantly better.
Giddiness and tremor disappeared quicker.
Most patients preferred Picamilon to nootropyl. It normalized
the behavior of patients faster and more completely than nootropyl.
In another study, Picamilon acted faster than vinpocetin 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. In persons suffering
from chronic alcoholism, Picamilon may be used to relieve
the symptoms of withdrawal.
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