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This Russian Drug Picamilon Rapidly Penetrates The Blood-Brain Barrier, Producing A Beneficial Effect on The Brain s Meta!olism
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. n experiments, !icamilon decreases cerebral blood-vessel tone and increases intracranial circulation rate. The drug exceeds in force and duration the effects of "A#A and niacin alone. n small doses, !icamilon shows tran$uili%ing action to prevent the negative effects of emotional stress. As with dia%epam, it depresses motivative aggression. The tran$uili%ing influence of the drug on negative emotions expressed through the hypothalamic system has been proved. !icamilon is characteri%ed by a tran$uili%ing 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. t rapidly penetrates through the blood-brain barrier and improves the functional state of the brain by producing a beneficial effect on its metabolism. !icamilon has been found to have low toxicity during experiments on animals. The median lethal dose is more than &' gram per kilogram of body weight and more than ( 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. ndependent researchers in &( medical centers in *ussia carried out a clinical trial with !icamilon in a great number of patients. !icamilon was prescribed two or three times a day in doses of +' to ,' mg. The course of therapy ranged from two weeks to three months.

"ignificant #eurologic $mpro%ement !icamilon proved to be $uite effective in patients with acute brain syndrome. -n 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. n this case, ob.ective methods of examination were used to document the increase of cerebral circulation, and the normali%ation of cerebrovascular resistance. !icamilon was effective in patients with mild-to-moderate impairment during subacute and early convalescent periods. t improved emotional conditions, speech and memory. !atients showed increased general activity, and better work and social adaptation. !icamilon stimulated physical and psychic rehabilitation from various asthenic /weakening0 disorders due to mental and somatic pathology. !icamilon was effective in patients with neurotic disorders in which the leading signs were asthenicasthenodepression, and asthenohypochondriac disturbances that accompany fear, anxiety, fatigue, emotional and vegetative instability, and sleep disturbances. !icamilon reduced anxiety and hyperesthesia /whereby normal touch creates pain0 without sedative effects, which improved sleep. According to the ma.ority of researchers, usage of !icamilon employed as a means of correcting neuroses, manic-depressive syndrome, involutional depression and schi%ophrenia enabled doctors to decrease doses of psychotropic drugs used in the treatment of these conditions. The combining of !icamilon with conventional treatments accelerated reduction of the psychopathological signs when compared to conventional treatments alone. $mpro%ement in A &ee' !icamilon also was effective in patients with psycho-organic syndromes including cerebral atherosclerosis, brain in.ury 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 !icamilon in patients with migraine headache was studied. t 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. n persons suffering from chronic alcoholism, !icamilon alleviated withdrawal symptoms.

Alcohol &ithdra(al Aided The effectiveness of !icamilon was compared with other similar drugs, including piracetam, phena%epam, dia%epam, vinpocetine, xanthinol nicotinate, and papaverin. t was noted that the psychostimulant effect of !icamilon was greater than piracetam. After taking !icamilon the patients felt significantly better. "iddiness and tremor disappeared $uicker. 1ost patients preferred !icamilon to piracetam. t normali%ed the behavior of patients faster and more completely than piracetam. n another study, !icamilon acted faster than vinpocetine in treating withdrawal symptoms in patients suffering from chronic alcoholism. According to clinical studies, !icamilon is recommended for the treatment of cerebrovascular diseases in subacute and early convalescent periods, as well as for transient brain damage, neurocirculatory dystonia, and chronic cerebral circulatory insufficiency. The drug is recommended as a tran$uili%er possessing no sedative action. !icamilon can be prescribed in cases of asthenic /weakening0 syndrome and disorders due to various psychotic and somatic pathology. t is used in the treatment of depressive disorders in the elderly and as therapy for senile psychoses. t also is recommended for the prevention and treatment of anxiety and stress. n persons suffering from chronic alcoholism, !icamilon may be used to relieve the symptoms of withdrawal.
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