This Russian Drug Picamilon Rapidly Penetrates The Blood-Brain Barrier, Producing A Beneficial Effect on 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
piracetam, phenazepam, diazepam, vinpocetine, xanthinol nicotinate, 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. In persons suffering from chronic alcoholism, Picamilon may be used to relieve the symptoms of withdrawal.