Tranquilizers and sedatives in sport

Anxiolytic agents (tranquilizers) with the medical purpose to athletes prescribe only in need of elimination of alarm, internal emotional tension which can arise at the athlete as a result of an unsuccessful performance.

Tranquilizers are the psychotropic medicines promoting elimination of alarm, a pavor, concern, an internal strain. Apply them at neurotic and borderline cases. Having appeared in 1955, these drugs are in the lead on use frequency today. The main effects of action of these agents — tranquillium tranquilizing (Latin — tranquility, rest), anxius anxiolytic (Latin — alarming, full of phobia, captured by a pavor), (from Greek ataraxia — coolness, a peace of mind), anti-phobic (from Greek phobos — a pavor) allow to apply widely them for correction of psychoemotional condition of the person.

Tranquilizers affect the emotional sphere of the person, causing feeling of serenity and tranquility, take out sensation of fear, concerns, alarm. The main effects are characteristic of all groups of these agents (anxiolytics or antialarming agents): anxiolytic (anti-phobic), hypnotic (simplification of offensive of a dream), (central muscle relaxation) and anticonvulsant. All tranquilizers differ among themselves based on the ratio of influence on these four components, as causes their choice for clinical use. The mechanism of action of tranquilizers is bound to decrease of excitability of subcortical areas of a brain (limbic system, a thalamus, a hypothalamus) which control emotional reactions in a human body, slowing down reactions between subcortical formations and a cortex of larger hemispheres, and also block spinal reflexes that is the reason of muscle relaxation. They poorly affect systems.

Some of them influence Gamkergichesky and benzodiazepine receptors (Aminalonum) while others influence cholinergic systems of a brain. There are also other molecular mechanisms of action of tranquilizers which are activly discussed by experimental and clinical pharmacologists. Long uncontrolled reception of tranquilizers can cause medicinal dependence. Drugs of this group exponentiate influence of alcohol on an organism. Aren't recommended to drivers of transport.

Tranquilizers, as well as neuroleptics, exert the oppressing (depriving of bonuses) impact on a CNS, but, unlike neuroleptics, have no the expressed antipsychotic effect, they promote elimination of various neurotic and neurosis-like disturbances, reducing psychoemotional coloring of behavior of the person.

On a chemical structure tranquilizers can be divided into the following groups:

1) benzodiazepine derivatives (benzodiazepines) — Chlozepidum (Chlordiasepoxidum, Elenium), Sibazonum (Diazepamum, Relanium), to gidazepa, Phenazepamum, Nozepamum (an oxazepam, Tazepamum), Mezapamum (Medazepamum, Rudotelum), Lorasepamum (Laurent), to bromazepa, alprazola (κρΰνΰκρ), Tofizopamum (Grandaxinum), to estazola, clorazepate, to klobaza, tetrazepa;

2) carboamine Aethers of the replaced pro-pan-diol — Meprotanum (Meprobamatum);

3) derivatives of a difenilmetan — Amizylum, Hydroxyzinum;

4) derivatives of a bupiron — ασροθπξν;

5) tranquilizers of various chemical groups — Mebicarum, Phenibutum (νξξτεν), Trioxazinum, oksolidin.

In clinical practice tranquilizers often divide into two groups: typical and atypical. Carry benzodiazepine derivatives to the first, considering the greatest study of their action, appreciable distribution and use; to atypical — derivatives of other chemical classes. Benzodiazepine derivatives (typical tranquilizers) which are very often used in clinical practice owing to hypotoxicity, determine by the term "tranquilizers" though it and isn't absolutely correct.

It is interesting that the term "tranquilizer" (uspokoitel) appeared in France more than 100 years ago and first had no relation to pharmacology. To them designated a special chair to which tied the patients with psychomotor exaltation who aren't giving in to arrangements. When for the first time in 1954 in the USA the first tranquilizer Meprobamatum was released, its consumption only in one year made several billion tablets (about 30 tablets on each resident of the USA). Drug gained popularity from sick and healthy people as an agent of correction of psychoemotional state at various somatopathies, neurosises, vital failures, the conflicts, shyness, etc. There were reports of advertizing character which said that, at last, medicine against the main illness of the 20th century — a stress is found. Instructions which obliged not to prescribe tranquilizers to pilots, drivers, operators, etc. were at the same time developed. However the first two years of use of tranquilizers dispelled this myth. At the same time the boom of use of tranquilizers didn't decrease, and now on use frequency they came out on top in the world among other medicines (among tranquilizers the most benzodiazepine derivatives). Only in recent years accurate strategy and tactics of their clinical use, and also a possibility of correction of mentality of the healthy person are developed.

Speaking more specifically about benzodiazepine derivatives, it should be noted that they are obliged by the opening to accident. Several hundreds of milligrams of chemical lay all the Hoffman-La Roche laboratories forgotten somewhere in a corner after J1 were for the first time synthesized. Other projects in laboratory became more important, and only two years later when cleaning the forgotten substance was revealed for the second time and is subjected to analyses. The new chemical called was capable to tame aggressive animals without obvious sedative effect. New medicine was put on the market by Roche under the name "librium", and the era of benzodiazepines began. By 1963 Roche monopolized the market, having issued the second benzodiazepine — diazepam (Valium) which became the most often appointed medicine of this kind, and also a standard for the whole class of sedative pharmacological means. Safety, especially in case of overdose, became a key argument for sale, however it was found and Valium cause dependence. Same treats also the third benzodiazepine of Roche — to nitrazepam (mogadon) put on the market in 1965 as sleeping pill. In total it is described more than 2000 pharmacological active derivatives of benzodiazepine, from them over 100 are issued in the world in the form of medicines. Derivatives of benzodiazepine constitute the greatest group of psychotropic medicines on number. Most of them are derivative 1,4 benzodiazepines, but also derivative 1,5 benzodiazepines are applied.

The most effective are benzodiazepine derivatives: khlozepid (chlordiazepoxide, elenium, librium), diazepam (sibazon, seducsen, relanium, Valium), to fenazepa, nozepa (tazepa, oxazepam), to mezapa (rudotel, medazepa).

Pharmacokinetics. Derivatives of benzodiazepines are well soaked up from digestive tract, form complexes with proteins. Accumulate in fatty tissue and from it arrive in blood. Are metabolized in a liver, are allocated generally with a stake.

Pharmakodinamiks. The main action of tranquilizers on TsNS is connected with influence on structures of limbic system and bark of big hemispheres. These medicines strengthen GAMK-ergichesky braking of nervous cages, interacting with benzodiazepinovy receptors, the allosterichesky regulatory centers of the Gamkergichesky receptor complex. Derivatives of benzodiazepines increase sensitivity of GAMKA of a receptor to the mediator. In the center of this receptor there is a chloric channel which opens in case of activation of a receptor. The strengthened entrance to a cage of ions of chlorine causes increase in potential (hyperpolarization) of a membrane, at the same time activity of neurons in many departments of a brain decreases. The sedative effect is connected with influence on other type of the receptors (less sensitive to benzodiazepines) localized in formation of a trunk of a brain, in nonspecific kernels of a thalamus.

Meprotin possesses the similar mechanism of action.

Amizil and hydroxywinters block central M-holinoretseptory. Buspiron mainly influences receptors, is partial agonist 5HT1 of A-receptors.

Pharmakodinamika. The main effects of tranquilizers — anxiolytic, ataraktichesky, antifobichesky, sedative, vegetostimuliruyushy. At diazepam hypotensive, antiarhythmic action is noted. Tranquilizers are also capable to lower a tone of skeletal muscles, to reduce concentration of attention, some possess somnolent action or promote development of a dream, exponentiate effect of hypnotic drugs, sedative, drugs, show anticonvulsive activity. Nebenzodiazepinovy tranquilizers exert more specific impact on TsNS, have no other effects (feninut, mebicar, etc.).

Possesses the most expressed anxiolytic action, its sedative effect surpasses that at other medicines.

To "day tranquilizers" — to medicines which don't possess or have insignificant somnolent effect, don't reduce working capacity, mezapa can carry (rudotel). Medicine possesses less expressed sedative and somnolent action. Treat them to gidazepa, tofizopa, mebicar.

Indications to use: neurosises and neurosis-like states, the epileptic status, an epilepsy, a muscle hyper tonus, reactive states, sleeplessness, premedication before operations.

Side effects: at prolonged use of tranquilizers development of accustoming and medicinal dependence is possible (mental and physical), the withdrawal is characteristic; it is also necessary to note emergence of a sleepiness, memory impairment and opportunities to concentrate, retardation of neuromuscular reaction, emergence of uncertainty when walking and orientation disturbance. Derivatives of benzodiazepine can reduce a potency and break a menstrual cycle.

Thus, in an arsenal of the doctor there is a large number of the most various tranquilizers by means of which it is possible to functions of a cerebral cortex, subcortical educations, the subthalamic centers, a reticular formation, spinal transfer, the central and peripheric autonomic nervous system. The doctor can choose drug necessary for the patient according to its individual properties and a pharmacodynamics of a tranquilizer.

And in practice of sports preparation application in sports medicine

The main indication to use of benzodiazepines is mental disadaptation at which psychopathological violations of neurotic level prevail. Promoting balancing of mechanisms at violation of mental adaptation, tranquilizers show universal influence on various psychopathological manifestations of neurotic character. In the course of treatment there is not only a reduction of emotional components in structure neurotic and violations, but also the vegetative dysfunctions, neurotic violations, frustration of a dream and other manifestations characteristic of the majority of adjacent forms of mental disorders decrease. Serious side effect of tranquilizers of group of benzodiazepines is the fast-arising mental dependence in this connection even in medical practice their application is limited.

As dopes tranquilizers are applied in sports, for example, at implementation of the obligatory program in figure skating and others (different types of firing), to removal of sensation of fear, uncertainty in themselves. Application cases for this purpose of nitrazepam, sibazona, fenazepama are known. It is a little cases of disqualification of athletes for the use of tranquilizers. In particular, in 1986 the pentathlonist L. Norwood has been convicted of reception of tranquilizers.

Certainly, owing to the fact that tranquilizers cause mental dependence their uncontrolled reception is inadmissible. Nevertheless in the presence of medical indications purpose of these medicines to athletes is quite justified — equally, as well as to any other persons having medical indications to reception of tranquilizers. It is obvious if not restrictions of "prohibitive" character, tranquilizers would have to take not the last place in an arsenal of the sports doctor, and besides not as doping means at all; at the same time it would be necessary to pay attention to the "day" tranquilizers which aren't causing drowsiness (to gidazepa, etc.).

Sedatives

To athletes at development of neurosises, vegetososudisty dystonia, sleeplessness more often appoint the sedatives increasing braking process.

Classification of sedative medicines

1. Bromine medicines — sodium bromide, bromine-validol, the adonis bromine, bromkamfor.

2. Monomedicines of plants — tinctures and dry extract of a valerian, motherwort tincture, peony tincture.

3. Barbiturates in a combination with medicines of other groups — korvakdin valocordin, korval-tab, Corvalol.

4 Melatonin (Vit melatonin, melokson).

5. The other combined medicines — dorminlact, new οΰρρθς, florised-health, gerbion — the calming drops, persen, triflumen, fitosed, etc. sedavit, seduksen-forte.gerbion

The mechanism of their action is connected with strengthening of processes of braking, tamponada of sodium channels, increase in a role of GAMK is characteristic of valerian.

The medicines having sedative properties are applied tranquilizers much earlier and strengthen brake process in TsNS, effect of hypnotic drugs and means. Don't exert impact on phobias as tranquilizers and don't cause medicinal dependence. In small doses sleeping medicines have similar effect, medicines of a phytogenesis and bromides concern to them. The last are used for correction of a motive in army and other isolated contingents. The main sedatives are provided in table 2.25.

Whenever possible and in case of an adequate current of neurotic conditions it makes a sense to begin treatment with sedatives, and then to pass to tranquilizers.

Forms of release of medicines

• Chlozepidum — tablets and a dragee on 0,005 g
• Diazepam — tablets on 0,005; 0,001 and 0,002 g; ampoules on 2 ml of 0,5% - γξ solution
• Phenazepam — tablets on 0,00025 and 0,001 g
• Mezapamum — tablets on 0,01 g
• Natrii bromidi — solution 1; 2 and 3%
• Rhizoma cum rhadicibus Valerianae — in packaging on 100 g or in briquettes on 75 g;
• tincture (Tinctura Valerianae) in bottles on 30 ml;
• dense extract (Extr. Valerianae) tablets on 0,02 g;
• liquid extract (Extr. Valerianae fluidum) for preparation of mixtures 1: 2
• Herba Leonuri — in packaging on 100 g;
• tincture (Tinctura Leonuri) — in bottles on 25 ml;
• extract liquid 1: 2 (Extr. Leonuri fluidum)
• Rhizoma cum rhadicibus Polemonii coerulei — a rhizome with roots cut on 100 g
• Corvaldinum — drops in bottles on 25 ml