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26-01-2015

Picamilone : a beneficial effect on brain metabolism

Picamilone GABA (gamma-aminobutyric acid) has been cleverly combined with niacin (vitamin B3) in a single molecule to produce Picamilon. Chemically bonding these two substances has produced a unique compound that provides a wide range of new health benefits, particularly in relation to cognition. Its effects are more powerful and long-lasting than those of vitamin B3 or GABA taken separately. Studies in Russia show that Picamilon improves blood flow to the brain, control of the nervous system, post-work recovery time, blood pressure and memory. It has been used for problems such as fatigue, irritability, depression, low energy, anxiety and excess alcohol consumption.

Chemically modifying widely-used vitamins is a key trend in research into new therapeutic agents.
The main advantages of vitamin-like substances are their wide-spectrum activity, the ease with which they penetrate cell membranes, their low toxicity and their infrequent side-effects.
These substances’ broad-spectrum activity is linked to their effects both on unspecific metabolic processes, and on various neurotransmitter systems. .
Vitamin B3 was chosen as the carrier for the GABA molecule because of its pharmacological properties, low toxicity and high bioavailability. It was reasonable to assume that combining vitamin B3 and GABA would increase the potency of each component.

Increases blood flow to the brain

Animal studies have demonstrated that Picamilon exerts a beneficial effect on blood flow to the brain.
It is a powerful vasodilator which substantially increases blood flow - Russian research even suggests it is more powerful in this respect than hydergine, vinpocetine or xanthinol nicotate
Its effects on cerebral circulation and nerve cell regulation were studied in conscious and anaesthetised cats and in conscious rabbits. Picamilon stimulated cerebral circulation and lowered vascular tone in both arterial systems in the brain. It increased blood flow in all animals, the rise in blood supply to the brain being more marked in the conscious animals than in the cats under general anaesthesia. It also lowered blood pressure. These effects were observed regardless of whether Picamilon was administered orally or intravenously.
The strength and duration of Picamilon’s vascular effects are much greater than those of GABA or vitamin B3.
Under similar experimental conditions, 10mg/kg of GABA administered intravenously produced no change in cerebral blood flow. A dose of 300mg/kg was required to produce such a change and even then, it lasted for just three to five minutes. As for vitamin B3, an increase in blood flow of 5% to 10% was achieved with high doses (50-100mg/kg)

A non-sedative tranquilliser

At low doses, Picamilon has demonstrated tranquillising properties. At doses of 1mg/kg, it prevents the negative effects of emotional stress. It normalised reactions in cats distressed by anger or fear. Like diazepam, it demonstrated in rats an inhibitory effect on motivated aggression associated with defending territory.
Investigations have shown that at higher doses (80-160mg/kg), Picamilon lowers the threshold for self-stimulation (like amphetamines) and at the same time, reduces its frequency. Picamilon’s stimulant effect has been demonstrated in general anaesthesia use: at a dose of 100mg/kg it reduced by 1.7 times the duration of the sedative effect of sodium hexobarbital and halved that of thiopental anaesthesia.
Unlike tranquillisers, Picamilon does not induce muscle relaxation, drowsiness or lethargy. It is therefore superior to many tranquillisers in terms of enabling normal daily activities to be carried out.
Administering Picamilon at a dose of 5mg/kg restored defence-conditioned reflexes that had been compromised by fatigue (130% compared with 12% in the control group). In rats, a dose of 50mg/kg restored 76% of their physical work capacity during a one-hour rest period compared with 38% in the control group.
Activation of the GABAergic system in certain stressful situations may prevent damage to the body when exposed to various stimuli. Confirming this hypothesis, scientists studied the effects of GABA derivatives on the development of toxic cerebral oedema.
A dose of 500mg/kg of Picamilon injected thirty minutes before nicotine (40 mcg/kg) prevented the development of oedema. When administered at lower doses of 200-300mg/kg, there was an increase in density of brain tissue but not to the level of controls’ and there was no significant change in total water content. The researchers concluded that the mechanism of Picamilon’s anti-oedema effect could be linked to a change in energy metabolism in neurological tissue.

Rapidly crosses the blood-brain barrier

Picamilon rapidly crosses the blood-brain barrier and improves brain function by exerting a beneficial effect on brain metabolism.
Thirty minutes after injecting a dose of 100mg/kg of Picamilon into rat brains, the oxidised form of nicotinamide adenine dinucleotide (NAD) increased by 67% above control levels, lactate dehydrogenase activity fell by 23%, while that of glutamate oxalate showed no significant change. More prolonged Picamilon action led to normalisation of NAD levels in the rat brains.
Researchers at the University of Odessa have shown that Picamilon rapidly crosses the blood-brain barrier. Picamilon was detected in the brain just thirty minutes after sub-cutaneous injection, penetrating faster than GABA. The time it took for Picamilon to accumulate in the brain correlated with its levels in blood.
Two hours after being injected, its accumulation in muscle tissue was ten times greater than that of GABA and it was also retained in the body for longer.

Low toxicity and few side-effects

Toxicity trials on animals have demonstrated that Picamilon has low toxicity. One such study lasting six months showed that doses of between 3 and 75 mg/kg produced no changes in rat behaviour or condition, nor any significant alteration in blood or organs. Some morphological changes were observed in the kidneys of rats injected with 75mg/kg (15 times the therapeutic dose). Microscopic examination of the kidneys revealed signs of glomerulonephritis and nephrosclerosis, suggesting that kidney disease could potentially be a contraindication for Picamilon.
However, tests have shown it to have low toxicity even when administered for long periods and to have no allergic, teratogenic, embryogenic or carcinogenic effects.
Independent researchers from 16 medical centres in Russia conducted clinical studies on Picamilon involving a large number of patients. Treatment duration varied from two weeks to three months and prescribed doses from 20 to 50mg two to three times a day. Efficacy was measured by clinical and laboratory tests. Changes in cerebral blood were monitored using measures such as echopulsography, echoencephalography, electroencephalography, rheo-encephalography and ultrasound scans ...

Clear neurological improvements

Picamilon demonstrated efficacy in patients suffering from acute cerebellar syndrome. Researchers observed a clear improvement in neurological symptoms after the fourth or fifth day of treatment and positive developments in impaired motor coordination. There was a subsequent decrease in headache, dizziness, ‘head noise’ and memory problems. Motor and speech difficulties quickly regressed, sleep improved and irritability, emotional stress and anxiety all decreased. The rate of blood flow also increased.
Picamilon’s effects were cumulative, increasing particularly in the second or third week of treatment.
Objective testing methods were used to record the increase in circulation and the normalisation of cerebrovascular resistance.
Picamilon’s efficacy in patients suffering the effects (more than a month later) of cerebrovascular problems was apparent from the second or third day of treatment. Their emotional state, speech and memory all improved and levels of enzyme activity (ASAT, ALAT and LDH) and lactate concentrations reverted to normal.
In cases of chronic cerebral insufficiency, Picamilon improved the patients’ mood and memory and reduced irritability, the tendency to cry for no reason and metabolic problems. In patients with memory difficulties (general amnesia), significant progress in memorisation and recall was observed between the fifth and seventh day of treatment and they were able to return to work.
Picamilon stimulated physical and psychological rehabilitation following various states of asthenia caused by mental or somatic disease. It improved the speed and quality of activity, concentration, attention and mood, and relieved anxiety, improving capacity for work. It was effective in patients suffering from neuroses in which the main symptoms were asthenia, asthenic-depressive states or asthenic-hypochondriac states accompanied by fear, anxiety, fatigue, emotional instability or sleep disturbances. Picamilon reduced anxiety and hyperesthesia with no sedative effect, resulting in improved sleep.
According to the majority of scientists, administering Picamilon to treat neuroses, manic-depressive syndromes, involutional melancholia and schizophrenia enables lower doses of the psychotropic drugs commonly prescribed for these types of disease to be used. Combining Picamilon with conventional treatments resulted in faster decreases in psychopathological symptoms than conventional treatment alone.
Picamilon’s efficacy in migraine patients has also been investigated. Researchers found that it had a pronounced effect on migraine pain, reducing its intensity and reducing or eliminating some of its associated symptoms. In individuals suffering from chronic alcoholism, it relieved symptoms of withdrawal syndrome. Patients ultimately became calmer, less difficult and anxious and their capacity for work improved.

Improvements seen within one week

Picamilon has also been shown to be effective in psycho-organic syndromes such as cerebral atherosclerosis and physical trauma- or toxin-induced brain damage. The condition of patients began to improve after just one week of treatment.

In Russia

Used in Russia for over 10 years, Picamilon is recommended there for adult use as a vasoactive agent (modifying blood vessel quality) and a nootropic (beneficial for cognition and the nervous system) in mild cerebrovascular problems, chronic cerebrovascular insufficiency and vegetovascular dystonia (imbalance between the sympathetic and parasympathetic influences on vascular tone). Its use as a tranquilliser is indicated in cases of anxiety, fear, increased irritability and emotional stress. It is recommended for depression in older people and for senile psychosis. It can also be used to relieve symptoms of withdrawal in chronic alcoholics.

Rapid action

Picamilon’s effects are generally felt quickly - within an hour for most people - and they normally last for four to six hours after each dose.
At low doses of 50mg three times a day, it produces a mildly tranquillising and mood-stabilising, but not sedative, effect. It prevents the negative psychological effects of emotional stress and is also beneficial in situations of mild anxiety and depressive mood.
Contrary to most tranquillisers, PIcamilon has no sedative effect making it more compatible with carrying out everyday activities. At higher doses of 100mg three times a day, Picamilon has a stimulant effect producing increased energy and stamina. Its stimulant effects on cognition are cumulative and are more evident after several weeks’ daily supplementation.
High doses of Picamilon should ideally not be taken alongside other vasodilators such as Ginkgo Biloba or Vinpocetine unless advised to by your therapist. In general, the same goes for monoamine-oxidase (MAO)-inhibitory drugs or other drug therapies. Picamilon should not be taken by children or women who are either pregnant or breastfeeding.
Picamilon enhences blood flow, Mirzoian RS et al., Gan'shina TS Farmakol Toksikol (URSS) Jan-Feb 1989, 52(1) p23-26.
The results of clinical study of the drug picamilon (an analysis of some data of neurologic and psychiatric clinics, AP Huaichenko et al. The pharmacological committee of the Ministry of health of URSS.
Picamilon and cerebrovascular disorders, Institute of pharmacology, Moscou, URSS.
Picamilon influence on the brain oedema course, Medical Institute, Moscou, URSS.
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Picamilon

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