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[Pharmacological effects of the new psychotropic preparation, mebikar].

By its effects mebicar -- a derivative of bicyclic bis-ureas -- may be refered to psychotropic drugs occupying a middle position between tranquilizers and neuroleptics. The drug inhibits the orientation reaction in albino mice, potentiates the action of narcotic hypnotics, abolishes the conditioned reflex reaction of avoidance, displays central adrenolytic activity, interferes with the norepinephrine metabolism in the brain stem and modifies the permeability of the blood-encephalic barrier, like this is done by the known neuroleptics. The substance is little toxic, does not exert any direct spasmolytic action on the isolated organs.

Amphetamine↗

[Characteristics of the psychotropic spectrum of action of mebicar].

Under group interaction in cats, a new Soviet tranquilizer mebicar eliminates fear-alarm induced by stimulatin of the emotiogenic zone of the hypothalamus. This action is not associated with myorelaxant or hypnotic action. Mebicar decreases the brain noradrenaline level, exerts no effect on the dopaminergic systems, increases the brain serotonin level, and does not elicit cholinolytic action.

Aggression↗

[Comparative analysis of the behavioral, neurochemical and autonomotropic effects of mebikar and diazepam].

It has been shown that the tranquilizers, diazepam (a 1,4-benzodiazepine derivative) and mebicar (a derivative of bicyclic bisureas) produce one-line inhibition of the production of the conditioned reflex of active avoidance in rats and of their "open-field" motor activity. Both the drugs change the balance of neuroactive amino acids in the animals' brain. However they produce different changes: diazepam increases the content of asparaginic and glutamic acids, while mebicar raises that of gamma-butyric acid. No interrelationship was found between psychotropic and vegetotropic effects of the tranquilizers.

Animals↗

[Effect of tranquilizing agents on the blood level of endogenous ethanol in alcoholics].

Experiments on alcohol addicts blood were made to study the time course of the endogenous ethanol level after a single administration of mebicar (1.5 g), a derivative of bicyclic bisuria, 50 ml of 5% sodium hydroxybutyric syrup, a derivative of gamma-hydroxybutyric acid, and 20 mg diazepam, a derivative of 1,4-benzodiazepines. The clinical effect was recorded simultaneously. It was established that different tranquilizers stimulate the increase in the endogenous ethanol level as regards the spectrum of psychotropic activity. This effect was the most pronounced with mebicar and to a less measure with diazepam.

Adult↗

[Effect of the meat of farm animals fed new nitrogen-containing food additives on the morphologic features of the internal organs in the rat].

A study was made of the internal organs of rats fed the meat of agricultural animals whose diet included non-protein nitrogen-containing compounds--urea, isobutylidene diurea and a polymer, carbamide with polyacrylamide. Morphological studies have demonstrated that inclusion into the diet of experimental rats of the meat of young bulls given isobutylidene diurea and urea leads to structural alterations in the internal organs of rats, the most pronounced alterations being detected in experiments with the use of the meat of young bulls given isobutylidene diurea. The feeding of experimental rats with the meat of animals grown with the use of the polymer did not affect the morphofunctional status of their organs.

Animal Feed↗

[Disorders in brain levels of macroergic substances during chronic stress and their correction by psychotropic agents].

The content of adenylic nucleotides (ATP, ADP and AMP) in different structures of the rat brain (cortex, limbic system, medulla oblongata) was studied in experimental chronic stress (anxiety) as was its correction with psychotropic agents--the derivatives of different chemical compounds. Stress was shown to lead to a dramatic decrease in the content of macroergic constituents in an excess-catabolic stage, largely at the expense of ATP, thereby reducing the adenylate charge. These changes were the most demonstrable in the limbic system. The medulla oblongata was little responsive to stress in this stage. Prophylactic administrations of the tranquilizers exerted a pronounced stress-protective action and made the content of macroergic constituents return to normal. GABA and nicotinic acid derivatives had the highest therapeutic effect.

Adenine Nucleotides↗

[Regulation of oxidative phosphorylation as a possible method of normalizing cerebral metabolism].

Experiments were performed to study the effect of chronic emotional painful stress on oxidative phosphorylation in different structures of rat brain at varying times of the development as well as after pretreatment with psychotropic agents. During the stage of excess catabolism, stress was demonstrated to dramatically inhibit and dissociate oxidative phosphorylation. This led to the impairment of macroerg synthesis and to the reduction of the brain macroerg content. Prophylactic administration of the derivatives of nicotinic acid and GABA markedly stimulated oxidative phosphorylation making it return to the initial level. Mebicar and meprobamate were less powerful. Chlorodiazepoxide aggravated stressful effects on tissue respiration and oxidative phosphorylation. It has been demonstrated that energy metabolism of the brain may return to normal at the expense of stimulation of oxidative phosphorylation.

Animals↗

[Mechanisms of the antishock action of mebikar].

The tranquilizer mebicar produces an antishock action, normalizes different links of mediator, acid-base and oxygen homeostasis. Mebicar decreases arterial pressure and the tone of peripheral vessels insignificantly and for a short period.

Animals↗

[Clinical pharmacokinetics of mebikar].

Twenty-two patients admitted to the narcological clinic of an industrial enterprise were examined for the clinical effect and pharmacokinetic parameters after intake of a single dose of a Soviet psychotropic drug mebicar. The clinical status was assessed by means of psychometric mapping and concurrent recording of the EEG. The correlation of the pharmacodynamic and pharmacokinetic data can be used for the choice of minimal effective concentrations applied in further calculations of individual dosage regimens.

Absorption↗

[GABA-ergic component in the action of the tranquilizing agent mebikar].

The paper is concerned with studies into the effect of the tranquilizer mebicar, a derivative of tetra-N-alkyl bicyclic bisureas, on the GABA-ergic system. The drug in doses of 250-1500 mg/kg (1/15-1/2 LD50) increased the preconvulsive period upon thiosemicarbazide administration, inconsistently changed the effects of picrotoxin and displayed antagonism in regard to bicucullin. Upon 2-week administration the drug reduced the GABA content in the rat brain. A hypothesis is advanced of mebicar-associated facilitation of the inhibitory GABA-ergic transmission.

Animals↗

[Protective effect of the psychotropic preparations diazepam, sodium oxybutyrate and mebikar in experimental arrhythmias].

It was shown that the psychotropic agents diazepam (1-2 mg/kg), sodium hydroxybutyrate (50-100 mg/kg) and mebicar (250-500 mg/kg) exert a protective action in experimental arrhythmias. This effect is determined by the ability of the drugs to reduce intoxication phenomena, as well as by their antihypoxic and stress-protective properties. On the other hand, the drugs exert an antiarrhythmic effect proper, interfering with potassium ion balance. The protective effects of diazepam, sodium hydroxybutyrate and mebicar enable their application in combined therapy of arrhythmias of varying genesis.

Animals↗

[Correlation between the stress-protective and vegetotropic action of mebikar].

Mebicar, a tranquilizer of the group of tetra-N-alkyl bicyclic bis-ureas, under acute emotional stress in cats (confrontation with a dog), simultaneously with tranquilizing effect on behavior also improves central baroreflex control and reduces hypertensive reaction of the arterial pressure. In rats, it normalizes disorders of individual and intraspecies behavior induced by the stress of a long-term social isolation. It decreases the degree of ulcer injury of the stomach during the immobilization stress.

Animals↗