Bemitil

The first well studied aktoprotektor — bemitil (2 ethylthiobenzimidazoles hydrobromide) — derivative benzimidazole. It is widespread in Ukraine under trademark of Antikhot from Power MAX. Antikhot active ingredient was result of the scientific research conducted in Army medical college (Leningrad) on search of the connections increasing intellectual and physical working capacity.

In recent years tens of aktoprotektor were synthesized. All of them can be divided into two big groups: benzimidazole derivatives (bemitil) and derivatives of an adamantan (bromantane). From these medicines in Ukraine it is registered only bemitit, and generally entered clinical practice so far only bemitit also bromantane (the last was forbidden as doping medicine recently). Within this chapter we will consider only benzimidazole derivatives on the example of a bemitil.

Bemitil is issued in tablets on 100 mg and is appointed from 2 to 4 tablets a day. Anti-jotas contains 200 mg of active agent and 200 mg of fructose in each tablet. As medicine possesses a capability to accumulate in an organism, it is possible to accept it no more than 6 days in a row then do a three-day break. In case of repeated acceptances positive action of a bemitil amplifies within several days, and then the surplus of working capacity is steadily supported at the reached level all term of use of medicine. Bemitil (anti-jotas) significantly increases general endurance and body weight. Its action of subjects is stronger, than physical activity is higher. Increase in working capacity under the influence of a bemitil can reach 200%, especially in the conditions of a lack of oxygen. Medicine increases resistance to high temperatures what received the trade name Anti from - against, Hot - a heat.

The mechanism of action of a bemitil activation of synthesis of protein, to be exact is the cornerstone of RNA that reminds basic mechanisms of action of anabolic means (therefore aktoprotektor and are considered among the permitted anabolic medicines). RNA synthesis strengthening bemitil results probably from interaction of medicine with a genome thanks to a certain structural similarity of derivatives of benzimidazole to the purin bases of nucleinic acids — adenine and a guanine. Bemitil isn't, obviously, primary activator of specific genes, and only nonspecific by means of the unknown so far of the mechanism strengthens the reactions of synthesis of RNA which are naturally proceeding at present in various fabrics. It is confirmed by strengthening of processes of synthesis of protein only in those bodies which actively function during presence of medicine at an organism and in which such processes happen intensively. Among the proteins which are actively formed under the influence of bemitil the greatest value has a number of short-lived proteins, in particular gluconeogenesis enzymes. On modern representations, such proteins can play a key role in adaptation processes — disadaptations: their first fast synthesis causes development of initial signs of adaptation, and the earliest decrease in content serves as a starting link in fabrics the shifts.

Bemitil, being benzimidazole derivatives, has structural similarity to the purinovy bases that allows it to make active a cage genome, to strengthen synthesis of RNA and proteins-enzymes (in particular, enzymes of gluconeogenesis and mitochondrial oxidation) therefore in a cage power products, utilization of exchange "slags" and antioxidant protection raise (formation of hydroperoxides of lipids, the diyenovykh of conjugates, etc. decreases).

Glyukoneogenez passing in the basic in a liver and bark of kidneys represents resynthesis of carbohydrates from products of their disintegration (a lactate and a piruvat), and also from some amino acids (first of all, an alanin and a glutamine) and a glitserola. In case of physical activity the role of gluconeogenesis consists also in utilization of the produced lactic acid — one of the main factors reducing working capacity. This process is integrated also to a glyukozolaktatny cycle (Cory's cycle) and to a glyukozoalaninovy cycle. The last promotes neutralization and removal not only a lactate, but also nitrogenous products of disintegration (ammonia, etc.). Glyukoneogenez, thus, brings big, and often decisive contribution to maintenance of physical working capacity: during gluconeogenesis the metabolites which are formed in case of physical activities and negatively influencing working capacity (lactate) are utilized; very restricted stocks of carbohydrates in an organism which are obligatory are at the same time recovered, and in case of intensive muscular loadings — the main source of energy. Glyukoneogenez in close interface to a glyukozoalaninovy cycle and reactions of exchange of a glutamine performs also other functions important for working capacity maintenance (reduction of formation of a lactate and ammonia in muscles, utilization and removal from an organism of nitrogenous products of disintegration, removal of hydrogen ions). Gluconeogenesis activation bemitily is observed both during physical activities, and in renewal period. It also constitutes, according to numerous experimental data, the main link in the increase mechanism working capacity medicine.

Mechanism of a positive impact of a bemitil on intellectual and operator activities is studied less. Here too can have some value activation of synthesis of protein, but already in structures of nervous system. It is also revealed that Antikhot makes favorable impact on brain vessels. At last, increase in working capacity in case of the specified types of activity can be partly secondary, for example, after physical activities when it in a certain measure is a consequence of improvement of a functional condition of an organism in case of loadings and after them under the influence of bemitil.

To important components of the mechanism of action bemitit decrease in need of an organism for oxygen and heat production reduction belong. Thin mechanisms of these effects aren't opened yet. There are data on suppression by medicine of some ways of free nefosforiliruyushchy oxidation, and also about maintenance of mitochondrions in more integrated condition, especially in case of the impacts on an organism (in particular, heavy physical activities) leading to dissociation of oxidation and phosphorylation. Such effect is connected probably with protective influence of a bemitil on structure of mitochondrions which, in turn, can partially be a consequence of strengthening of synthesis of components of mitochondrial membranes. Protective effect of medicine on membranes is shown sometimes and suppression of processes the FLOOR, i.e. a certain antioxidant effect. All listed links of the mechanism of action causing oxygen consumption reduction by an organism and formations of warmth explain outstanding performance of a bemitil as means of increase in working capacity in the conditions of a hypoxia and high temperature of the environment.

Direct anabolic action of a bemitil on muscular tissue is expressed poorly, however medicine possesses the strong mediated action as allows to increase sharply loadings which give such effect. Under the influence of a bemitil content of a glycogen in muscles, a liver and heart increases. Efficiency of tissue respiration increases.

Bemitil, thus, is anabolic steroid of indirect action.

Besides, reducing Saccharum level in a blood a little, bemitit somewhat promotes rising of secretion of Somatotropinum. Aktoprotektora in general also bemitit in particular are bonds of ekonomiziruyushy action, promoting performance of a certain amount of works with the minimum expenses. They reduce rate of working disintegration of proteins, fats and carbohydrates. At the same time in a liver rate of synthesis of the short-lived proteins responsible for urgent adaptation of an organism is enlarged.

In medicine bemitil it is applied at a chronic hypoxia of a different parentage (especially by sports preparation, during high exercise stresses and other extreme influences, and also after them to acceleration of recovery processes), at a mental asthenia of any genesis, to aftertreatment of the patients who transferred an acute hepatitis (the mass of a liver is quicker restored, expression and duration of disturbances of its functions) or a radial illness, for treatment of neuromuscular diseases decreases (the progressing myodystrophy, secondary myopathies and so forth), vestibular disorders, an epilepsy (prescribe only in a complex with antiepileptic agents), a recurrent erysipilatous inflammation.

Thus, rather physiologic influence of a bemitil on an organism allows to use with success it in clinical practice for maintenance recovering, treatments of asthenias of various nature. At the same time thanks to activation of synthesis of protein drug can strengthen reparative processes in various organs that also accelerates maintenance. Such double medical effect is especially brightly shown at liver pathology (for example, during aftertreatment after a viral hepatitis) as this organ is characterized by the high potential of neogenesis, and reparative processes include restoration of one of key mechanisms of maintenance of working capacity here — normalization of system of a gluconeogenesis. Bemitil doesn't cause dangerous side effects, sometimes at reception irritant action on mucous digestive tract is on an empty stomach observed.

Results of testing demonstrate that bemitil is an effective remedy of increase in physical working capacity both in regular, and in extreme conditions. Effect of medicine is shown already in 1 — 1,5 h after single acceptance. By efficiency in usual conditions bemitil it is quite comparable to a psychomotor stimulator sidnokarby, at the same time its action is more physiologic; the negative effects peculiar to a sidnokarb — excitement with elements of euphoria, decrease in mental stability, excessive stimulation of functions of cardiovascular system aren't observed. In the complicated conditions (a hypoxemic hypoxia, threat of an overheat) bemitit exceeds not only on physiology of action, but also by efficiency: the positive impact of a sidnokarb in such conditions decreases by working capacity or is even transformed in negative, and the positive effect of a bemitil becomes more noticeable.

Bemitil, as it was already mentioned, can increase working capacity in case of intellectual and operator activities. These effects in general are less expressed in comparison with influence on physical working capacity, but too are shown more brightly in the complicated conditions.

Bemitil

Bemitil (anti-jotas) — original domestic medicine; has the psychostimulating effect, has anti-hypoxemic activity, increases resistance of an organism to a hypoxia and increases working capacity in case of physical activities. It is slowly soaked up in case of intake. Bemitil strengthens synthesis of antioxidant enzymes (a catalase, SOD). It possesses also immunostimulating and anti-mutagen action.

Anti-jotas appoint the adult in case of asthenic conditions, neurosises, after the postponed injuries and in case of other conditions in case of which stimulation of mental and physical functions is shown. There are data on the immunostimulating action of bemitil and, with respect thereto, its efficiency in complex therapy of some infectious diseases.

Indications to use

Shablon: spravochnik Povysheniye and maintenance, including in extreme conditions (serious loads, a hypoxia, an overheating, etc.); acceleration and consolidation of adaptation to influence of various extreme factors; asthenia (various nature): somatopathies, infections and intoxications, before - and the postoperative period; ChMT consequences, memory depression.

As an immunomodulator Bemitil it is possible to use at the secondary immunodeficiency accompanying acute and chronic bacterial and viral infections.

Contraindications

Hypersensitivity, hypoglycemia, the expressed abnormal liver functions, pregnancy, the lactemia period, epilepsy, arterial hypertension, glaucoma, ischemic heart disease, arrhythmias.

Side effects

Unpleasant feelings in a stomach and a liver, it is rare - nausea, vomiting, allergic reactions (a dermahemia of the person, a rhinitis, a headache). In these cases it is necessary to reduce a dose or to stop reception.

Overdosage

Symptoms is a hyperexcitability, disturbance of a night dream. Treatment: a gastric lavage, reception of absorbent carbon, if necessary - symptomatic therapy, it is necessary to reduce a dose or to stop administration of drug.

Course and doses

Inside, after food, on 0,25 g 2 times a day. If necessary the daily dose is enlarged to 0,75 g (0,5 g in the morning and 0,25 g after a lunch), to persons with the big body weight (over 80 kg) - to 1 g (on 0,5 g 2 times a day). A course of treatment - 5 days, a break between courses 2 days (in order to avoid a drug cumulation). The quantity of courses depends on medical effect and averages 2-3 (more rare than 1 or 4-6) a course. For rising of working capacity in extreme conditions accept in 40-60 min. prior to the forthcoming load in a dose 0,5-0,75 g. At further work - repeated reception in 6-8 hours in a dose of 0,25 g. The maximum daily dose shouldn't exceed 1,5 g, in the next days - 1 g. For maintenance of high level of working capacity for a long time (several weeks) and for activation of adaptic processes prescribe according to the scheme: 5-day courses of reception with 2-day breaks, in a dose of 0,25 g 2 times a day. At the expressed abnormal liver function (an acute viral hepatitis, a cirrhosis, toxic lesions of a liver) the dose is reduced.

Special indicatings

Don't accept in the evening (possibly backfilling disturbance). During treatment the diet rich with carbohydrates is recommended.

Medicinal interaction

Strengthens effects of HP of metabolic type of action - nootrop (Pyracetamum, etc.), antioxidants (an alpha tocopherol, etc.), antigipoksant (ِْوٌمْـهولوٍ), nonsteroid anabolic HP (Riboxinum), an asparkam, glutaminic acid, vitamins, and also anti-anginal HP (Sodium nitritums, beta adrenoblockers). At use together with the HP reducing activity the mikrosomalnykh of enzymes of a liver (for example, Cimetidinum), rising of concentration of etiltio-benzimidazole in a blood is possible.