Everything about Picamilon totally explained
Picamilon is a compound formed by reacting
niacin with
GABA. It was invented in
Russia. Picamilon is able to cross the
blood-brain barrier and activate
GABA receptors, producing an
anxiolytic response. The niacin also acts as a strong
vasodilator, helping to improve awareness.
Studies from Russia demonstrate that Picamilon improves nervous control, recovery time after work,
blood pressure and
memory. The drug even shows benefits in treating
traumatic brain injury.
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 l 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
intracranial 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 and other drugs of
abuse), but at the same time reduced the number of self-stimulation attempts made. 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,
phenazepam), Picamilon doesn't induce muscle relaxation, drowsiness or
lethargy.
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 0.02 to 0.05 grams, and in a daily dose of 0.04 to 0.3 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
electroencephalography.
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 (
aspartate transaminase,
alanine transaminase, and
lactate dehydrogenase) 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 edema.
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 improved.
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