Anxiolytics

22 Dec 2016

Anxiolytics (from the Latin anxietas -. Anxiety, fear + Greek lytikos -. Capable of dissolving, weakening), or tranquilizers (from the Latin tranquillo -. Calm), or ataractics (from the Greek ataraxia -. Equanimity) - psychotropic drugs that reduce the severity of, or overwhelming anxiety, fear, anxiety, emotional stress.

Appearance of the first tranquilizers refers to the 50-th years of XX century. Prior to that, for the correction of anxiety use alcohol, opium, bromides (from the beginning of the XIX century.), Barbiturates (from the beginning of XX century.) And others. Means.

In 1952, during the search of the central muscle relaxant meprobamate was synthesized (meprotan). In 60-ies in a number of clinical trials were found anxiolytic properties (when taken in high doses - 100-400 mg / day) of hydroxyzine (Atarax) - one of the first antihistamines, an antagonist of H1-histamine receptors, is used in dermatology since 1955 The first generation of anxiolytics include also trimetozin (Trioxazine, repealed in 1996), the central anticholinergic benactyzine (Amizyl), atypical anxiolytics mebicar and Benzoclidine (Oxylidin).

Widely used in medical practice, drugs anxiolytics groups have since the 60s of XX century, when the first tranquilizers - benzodiazepine derivatives:. Chlordiazepoxide (Librium, 1960) and diazepam (Valium, 1962).

Historically, can be divided into 3 generations anxiolytics:

• The first generation of anxiolytics (meprobamate, hydroxyzine, benactyzine et al.);
• The second generation of anxiolytics (benzodiazepine drugs);
• The third generation of anxiolytics (buspirone, etc.).

There are several classifications of drugs belonging to the group of anxiolytics: chemical structure, mechanism of action, pharmacokinetic and pharmacodynamic characteristics and others.

According to the classification MD Mashkovskiy anxiolytics represented by several classes of chemical compounds:

• Benzodiazepines (benzodiazepines);
• Esters of substituted carbamic propanediol (meprobamate);
• Diphenylmethane derivatives (benactyzine, hydroxyzine);
• Tranquilizers different chemical groups (benzoklidin, buspirone, mebicar et al.).

According to the classification DA Kharkevich, anxiolytics on the mechanism of action can be divided into the following groups:

• Benzodiazepine receptor agonists (diazepam, Phenazepam et al.);
• Serotonin receptor agonists (buspirone);
• Substances of various types of action (benactyzine et al.).

Mechanisms of action of anxiolytics has not yet been disclosed to the end. Action anxiolytics manifested by decreasing the excitability of the subcortical regions of the brain (the limbic system, thalamus, hypothalamus) responsible for the implementation of emotional reactions, inhibition of interaction of these structures with the cerebral cortex, as well as oppression polysynaptic spinal reflexes.

In the aspect of different neurochemical anxiolytics differ on the specifics of the action. The effect on noradrenergic, dopaminergic, serotonergic system is expressed in their relatively low degree (with the exception of buspirone). The effects of benzodiazepines are mediated effects on brain GABA-ergic system.

Currently leading position in wide use among drug group anxiolytic benzodiazepines continue to hold. Most structures benzodiazepine anxiolytics are 1,4-benzodiazepine derivatives. Basis benzodiazepine chemical structure consists of a benzene ring connected with the seven-membered heterocyclic ring containing two positions 1 and 4 nitrogen atom (diazepine) all used in the clinic benzodiazepine derivatives have also the second benzene ring attached to the carbon at position 5. For the manifestation of activity essential is the presence of a halogen or nitro group at the 7 position. Certain benzodiazepine compounds contain in the molecule the residue of 1,5-benzodiazepine (clobazam) or 2,3-benzodiazepine (Tofisopam).

Due to the easy replaceability radicals on different positions in the molecule benzodiazepine was synthesized and studied for more than 3 million compounds, of which a few dozen registered in different countries as drugs.

In accordance with the substituents in the diazepine ring benzodiazepines can be classified as follows:

• 2-keto-benzodiazepines containing keto-group at the carbon atom in position 2 (diazepam, dipotassium clorazepate, flurazepam * etc.);
• 3-hydroxy-benzodiazepines containing a hydroxy group at the carbon atom in position 3 (* oxazepam, lorazepam, temazepam *);
• Triazolobenzodiazepiny contain triazole ring connected to the diazepine ring through a nitrogen atom in the 1-position and the carbon atom in position 2 (alprazolam, triazolam * * estazolam).

There may be additional substituents and the other in the benzodiazepine structure, for example, imidazo-group (midazolam *), and others.

Electrophysiological studies in the 60-70-ies. XX century., Showed that benzodiazepines enhance GABAergic transmission in the CNS. The mechanism of action of benzodiazepines was clear after in 1977, with the help of the method place radioligand specific binding of benzodiazepines was observed in the brain of humans and animals, so-called benzodiazepine receptors (receptors DB). Later on in vitro experiments and in vivo correlation was found between the ability of different benzodiazepines bind to these regions and their pharmacological activity. The methods of autoradiography and electron microscopy showed that the DB-receptors are localized mainly in the synapses of the CNS, primarily on postsynaptic membranes. It is shown that the heterogeneity of the DB-receptors, which are represented in the mammalian brain by at least two subtypes - BD1 and Sn2.

After detecting the specific binding sites of benzodiazepines began searching for endogenous compounds that interact with a DB-receptors, the so-called endogenous ligands. In a large number of compounds considered as the endogenous ligand-receptor DB: peptides, purines, nicotinamide hypoxanthine, beta-carbolines, diazepam binding inhibitor (DBI) and others, but the nature of the final database receptors endogenous ligand is not clear.

It is now believed that benzodiazepines interact with specific benzodiazepine receptors (agonists of these receptors), members of the postsynaptic GABAA receptor complex in the limbic system of the brain, the thalamus, the hypothalamus, the ascending activating reticular formation of the brain stem and neurons of lateral spinal cord horns. Benzodiazepines increase the sensitivity of GABA receptors to neurotransmitter (GABA) that causes the increase in the frequency of opening the channels in the plasma membrane of neurons to incoming currents chlorine ions. The result is a strengthening of the inhibitory effect of GABA interneurons and oppression transfer in the CNS.

he effect on GABA transmission - the main mechanism of action of benzodiazepine anxiolytics. A role in the implementation of the effects of benzodiazepine anxiolytics can play and other neurotransmitter systems of the brain.

Benzodiazepines have a wide range of pharmacological effects, including anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, amnestic and others.

The effects of benzodiazepines due to the influence on different parts of the central nervous system: amygdala limbic system (anxiolytic), the reticular formation of the brain stem and the nonspecific nuclei of the thalamus, the hypothalamus (a sedative and hypnotic), hippocampus (anticonvulsant).

The main effect, characteristic for all drugs combined into a group of anxiolytics, and makes use of these funds for all types of anxiety disorders, is an anxiolytic (anti-anxiety). The anxiolytic effect is a decrease in anxiety, fear (anti-phobic effect), emotional tension.

Sedative (calming) effect is a decrease in psychomotor excitability, daily activities, decreased concentration, decreased reaction rate, and others.

Hypnotics (hypnotic) effect is to facilitate sleep onset and increase its duration. The inhibitory effect of tranquilizers on the CNS contributes to strengthening the mutual effects of hypnotics, anesthetic and analgesic agents.

Muscle relaxant activity (relaxation of skeletal muscles) is due primarily to inhibition polysynaptic spinal reflexes. Benzodiazepines may also provide and direct depressant effect on motor nerves and muscles function. Myorelaxation effect of the application of tranquilizers is often a positive factor for stress relief, arousal, including motor, but it can also limit the use of drugs in patients who require rapid mental and physical reactions. Note that the muscle relaxant effects can manifest a sense of lethargy, weakness, and others.

The anticonvulsant effect is to suppress the spread of epileptogenic activity occurring in the epileptogenic foci in the cortex, the thalamus, and limbic structures. Anticonvulsant action is connected not only with the effects on the GABAA receptor complex, but also due to the effect on the voltage-gated sodium channels.

Amnestic effect (ability to induce amnesia) occurs mainly with parenteral use (diazepam, midazolam *, etc.). The mechanism of this effect is not yet clear.

The spectrum of action of some tranquilizers sometimes emit additional effects, including vegetative stabilization. Vegetative-stabilizing effect is due to the normalization of the functional activity of the autonomic nervous system. Clinically, this effect can be expressed by a decrease in autonomic manifestations of anxiety (unstable blood pressure, tachycardia, sweating, violation of gastrointestinal function, and others.). Expressed Wegetotropona action have Tofisopam, diazepam, etc. hidazepam.

Benzodiazepine derivatives may exhibit all the characteristics of this group pharmacological properties, however, and the severity of effects at different ratio of benzodiazepines may be different, which makes use of certain features of clinical drugs.

The peculiarities of the clinical actions of benzodiazepine anxiolytics can be divided into 3 groups:

1). Benzodiazepines with a predominance of anxiolytic action.

2). Benzodiazepines with a predominance of hypnotic action.

3). Benzodiazepines with a predominance of the anticonvulsant action.

Anxiolytic effects have Phenazepam (for anxiolytic activity surpasses many benzodiazepines, including diazepam), diazepam, lorazepam, alprazolam, and others. Moderately pronounced anxiolytic effects from chlordiazepoxide, bromazepam, gidazepam, Clobazam, oxazepam and others.

Sedative-hypnotic effect is particularly pronounced in nitrazepam * * flunitrazepam, flurazepam * * temazepam, triazolam * * midazolam, estazolama * et al. And they are used mainly as hypnotics (see. Hypnotics).

Anticonvulsant properties characteristic clonazepam, diazepam, and also (in lesser extent) for nitrazepam etc. *.

Muscle relaxant activity is characteristic of diazepam, chlordiazepoxide, lorazepam, tetrazepam and others.

For some anxiolytics characteristically pronounced anxiolytic effect at relatively low muscle relaxant and hypnotic (Tofisopam, medazepam et al.), In connection with which they are more convenient for use during the day (the so-called daytime tranquilizers).

Benzodiazepine derivatives differ in their pharmacokinetic characteristics, which is also taken into account in the appointment of these drugs. For the duration of action (taking into account the effect of the active metabolites), benzodiazepines can be classified as follows:

• Long-acting (T1 / 2 - 24-48 h): diazepam, chlordiazepoxide, etc .;
• Average duration (T1 / 2 - 6-24 h): alprazolam, oxazepam, lorazepam etc .;
• Short-acting (T1 / 2 - less than 6 hours): midazolam, etc. *.

All benzodiazepines are lipophilic compounds. The lipophilicity of various compounds of this group varies more than 50 times, most of lipophilic benzodiazepines diazepam and midazolam are *.

When administered benzodiazepines are well absorbed from the gastrointestinal tract, mainly from the duodenum (absorption depends on several factors, including by lipophilicity). The most rapidly absorbed diazepam and triazolam *, the least fast - oxazepam, lorazepam. Antacids can decrease rate (but not the extent of absorption) some benzodiazepines, including chlordiazepoxide and diazepam. After intramuscular administration of benzodiazepines are absorbed more slowly than when taken orally (with the exception of lorazepam and midazolam *, which with the / m introduction absorbed quickly).

The time to reach maximum plasma concentration after a single dose for different drugs varies from 30 minutes to several hours. Equilibrium concentration in the blood at course intake of benzodiazepines is usually achieved within a few days after initiation of therapy (for benzodiazepines with short half-life and the mean) or within 5 days - 2 weeks (for drugs with long half-life). Benzodiazepines and their metabolites are characterized by a high degree of binding to blood proteins, ranging from 70% (alprazolam) to 98% (diazepam).

High lipophilicity results in penetration of the drug through the BBB and other biological barriers, as well as a significant rate of redistribution of CNS tissue (adipose tissue, muscle). The volume of distribution of benzodiazepines is quite high.

Benzodiazepines primary metabolism in the liver. Exceptions are dipotassium clorazepate and flurazepam *, which are rapidly metabolized in the gastrointestinal tract and enter the blood system in clinically relevant amounts. Action exert their active metabolites that subsequently undergo biotransformation in liver. Most benzodiazepines subjected to liver microsomal oxidation, mainly by N-demethylation and hydroxylation to active or inactive metabolites. Then metabolites undergo further conjugation or biotransformation. You can also like Phenibut.

In the metabolism of many benzodiazepines same active metabolites are formed, some of them are used as distinct drugs (oxazepam, etc.). The duration of the therapeutic effect of benzodiazepines having active metabolites determined not T1 / 2 of the starting material, and T1 / 2 of active metabolites. For example, T1 / 2 desmethyldiazepam (nordiazepam), which is an active metabolite of chlordiazepoxide, dipotassium clorazepate diazepam and is, according to one more of 30-100 hours, at the other - 40-200 hours, far exceeding half-lives of the starting materials.

Some benzodiazepines do not form active metabolites -. Lorazepam, oxazepam, temazepam *, etc., subject only under the influence of the process of conjugation to glucuroniltransferaze to form a glucuronid.

Benzodiazepines (and their metabolites) are derived primarily through the kidneys as conjugates, less than 2% - unchanged, a small part - through the intestines.

Some benzodiazepines pharmacokinetic parameters depend on age. For example, elderly patients may increase the volume of distribution. Furthermore, elderly patients and children may be extended half-life.

Time of occurrence and duration of the effects of benzodiazepine anxiolytics are not always related to their half-life, but the course intake, these parameters are largely correlated. When receiving repeated doses of the benzodiazepines with long T1 / 2 occurs accumulation of the drug and / or its active metabolites. A related effect is the aftereffect of drugs (diazepam, etc.). The accumulation of benzodiazepines with a short or medium half-life is usually minimal, and they are quickly eliminated from the body after the end of therapy.

The spectrum of anxiolytics clinical use due mainly to their anti-anxiety effect. Benzodiazepines are used in all types of anxiety disorders (which may be indicated for the treatment of anxiety disorders or for the short-term elimination of symptoms of anxiety).

In psychiatric and neurological practice anxiolytics are used in the treatment of neuroses, psychopathy states, accompanied by anxiety, fear, increased irritability, emotional stress. For relief of anxiety and phobic disorders (panic attacks, etc.) With the most effective drugs anxiolytic and anti-phobic effect - alprazolam, lorazepam, Phenazepam. Some benzodiazepine anxiolytics are used for the relief of anxiety syndrome at endogenous mental illness, including in schizophrenia (as an aid in the complex therapy) - diazepam, Phenazepamum and others.

In acute conditions, such as the purpose of the relief expressed psychomotor excitation, effectively parenteral administration of benzodiazepines (diazepam, Phenazepamum et al.).

When acute alcohol withdrawal anxiolytics (diazepam, Oxazepam, Phenazepamum, chlordiazepoxide, etc.) is used in the complex therapy to relieve symptoms such as excitement, nervousness, restlessness, anxiety, tremors, and also to reduce the probability of developing or signs, in Vol. h. hallucinations, emerged acute delirium.

When sleep disorders using benzodiazepines, have, along with anxiolytic, hypnotic action marked (* nitrazepam, flunitrazepam * * triazolam, temazepam * etc.). They relieve emotional stress, reduce anxiety, anxiety and promote sleep onset. Application of sleep disorders benzodiazepines such as diazepam or Phenazepamum advisable in cases when combined with insomnia and daytime anxiety desirable that anxiolytic effects lasted throughout the day.

Benzodiazepines with pronounced anticonvulsive action can be effective in the treatment of epilepsy, status epilepticus (clonazepam, diazepam, etc.), Nitrazepam * - in some forms of seizures, especially in children.

Benzodiazepines, like other anxiolytics, are widely used in many fields of medicine: cardiology, anesthesiology and surgery, dermatology and others.

Some benzodiazepines with marked muscle relaxant action (diazepam, chlordiazepoxide, and others.) Are shown in spastic conditions associated with damage to the brain or spinal cord, and others.

Benzodiazepines are used for sedation before and immediately before surgery and endoscopic procedures for induction of anesthesia, when ataralgezii combined with analgesics (flunitrazepam * * midazolam, diazepam, etc.).

The use of anxiolytics some healthy people may be justified for acute reactive states of stress in extreme situations (fire, industrial disaster, earthquake, etc.). Keep in mind that anxiety or tension associated with everyday stress, are not an indication for anxiolytics purpose, therefore should not be given them in any stressful conditions, particularly in reactions of grief or somatic diseases.

The main contraindications to the appointment of benzodiazepines is an individual hypersensitivity, severe liver failure, myasthenia gravis, glaucoma, severe respiratory failure, ataxia, suicidal tendencies, drug or alcohol dependence (except for the treatment of acute withdrawal syndrome).

Should avoid taking benzodiazepines during pregnancy (especially in I trimester) and lactation.

Benzodiazepines easily pass through the placenta. There is evidence that chlordiazepoxide and diazepam increase the risk of congenital malformations in the appointment in the I trimester of pregnancy. Other drugs in this group may also increase the risk, so the appointment of drugs benzodiazepine during pregnancy should be treated very carefully and use them only in the absence of alternatives, matching the potential risk to the fetus and the benefit to the mother.

In the appointment of benzodiazepines (clonazepam, diazepam and others.) During pregnancy, women with epilepsy should be aware that there are reports of increased incidence of birth defects in children whose mothers took anticonvulsant drugs during pregnancy, however, the causal link between the the facts have not yet been established. On the other hand, in women taking anticonvulsants (e.g., clonazepam), their cancellation before or during pregnancy is possible only in cases where seizures are weak and sparse in the absence of treatment, and if the probability of status epilepticus and withdrawal symptoms is evaluated as low.

The use of benzodiazepines in the III trimester of pregnancy (especially in the last week) can lead to accumulation of the drug in fetal tissues, and as a consequence, to the oppression of the central nervous system in newborns. This can be observed in the newborn muscle weakness, hypothermia, respiratory depression, disturbance of the sucking reflex.

Long-term use of benzodiazepines during pregnancy, including in late stages, it may lead to the formation of the development of physical dependence and withdrawal symptoms in the newborn.

The caution (only on strict conditions) used benzodiazepines during labor, for example, parenteral administration of diazepam in preterm labor or premature detachment of the placenta. Diazepam at low doses, usually has no adverse effects on the fetus, but the use of high doses can cause neonatal heart rhythm disturbances, decrease of pressure, asthma attacks, muscle weakness, etc. hypothermia. Symptoms.

Since benzodiazepines penetrate into breast milk in significant quantities, means that the group should not be applied to nursing mothers. Neonates benzodiazepines metabolized more slowly than adults, resulting in these drugs and their metabolites can accumulate in the body and cause sedation. It is possible feeding difficulties and weight loss in infants.

At therapeutic doses, benzodiazepines do not typically affect the function of respiration, blood pressure did not change. However, in patients with obstructive lung disease, a syndrome of sleep apnea, and others. While taking these drugs may worsen the condition.

Parenteral administration of benzodiazepines, especially in patients with middle and old age, can lead to breathing disorders (apnea) and the cardiovascular system (hypotension, bradycardia up to cardiac arrest).

Benzodiazepines not recommended as a single agent in the treatment of anxiety and depression or in severe depression because possible suicide attempts (benzodiazepines could enhance the expression of depression). However, some of the benzodiazepine anxiolytics structure (alprazolam, lorazepam, oxazepam) are effective in the treatment of anxiety depression on the background of various genesis (usually in combination with antidepressants).

Since most benzodiazepines biotransformation in the liver, in violation of its function may change the duration of the therapeutic effect of these drugs may cause serious side effects. In this connection it should be very careful when assigning benzodiazepines in patients with hepatic impairment.

The use of anxiolytics in children and adolescents under 18 years of age is justified only in exceptional cases, when well-founded indications, with the duration of treatment should be minimal.

Patients elderly, debilitated patients, children (especially small ones) are usually more sensitive to benzodiazepines neurotropic action. In particular to avoid systemic administration of benzodiazepines (especially a long acting) to patients over 65 years as intake of these drugs can lead to undesirable consequences in the form of excessive sedation, dizziness, disorientation and coordination. This may cause patients falls and related fractures.

Adverse side effects when taking benzodiazepines are signs of CNS depression, including daytime sleepiness, lethargy, muscle weakness, blunting of emotion, headache, dizziness, ataxia, and others. It is possible cognitive impairment (eg, chronic administration of diazepam, fenazepama).

In connection with a reduction in speed of psychomotor reactions, weakened concentration should be used with caution in outpatient anxiolytics, including Patients whose work requires quick mental and physical reactions, and is also associated with increased concentration (vehicle drivers and others.).

When receiving benzodiazepine anxiolytics possible paradoxical reactions (severe agitation, anxiety, hallucinations, nightmares, fits of rage, inappropriate behavior), most often seen in children, elderly patients and mentally ill patients. In the event of paradoxical reactions the drug should be discontinued immediately.

After receiving a few, mostly long-acting drugs (eg, diazepam), possible aftereffect syndrome (muscle weakness, decreased performance, and others.).

Application anxiolytics can lead to addiction (reduction effect of chronic administration) and the dosage form according to (physical and / or mental) and occurrence of withdrawal syndrome. The risk of dependence increases with prolonged use (more than 6 months), especially in high doses and in patients with alcohol dependence and drug history.

With a sharp lifting of the drug on a background of drug dependence may be withdrawal symptoms (tremor, convulsions, vomiting, excessive sweating), in severe cases - depersonalization, hallucinations, seizures (sudden elimination in epilepsy).

It should be remembered that treatment with anxiolytics can be conducted only under the supervision of a physician. In the appointment of benzodiazepines to treat anxiety disorders should respect the principle of gradual dose escalation - from the lowest to the optimum effective to produce a therapeutic effect (except for acute conditions). The course of treatment should be as short as possible, and then to re-evaluation of the patient to decide whether to continue therapy. Because of the possibility of addiction and the emergence of drug dependence WHO Conciliation Commission (1996) did not use the drug benzodiazepine continuously for more than 2-3 weeks. If necessary, long-term treatment (months) course should be done by the method of intermittent therapy, stopping the reception for a few days followed by the same dose of individually selected. The lifting should be done by gradual dose reduction, to reduce the risk of withdrawal symptoms.

In the treatment of anxiolytics should take into account the possible drug interactions of this group with other drugs. Anxiolytics potentiate the effects of other CNS depressants (opioids, anesthetic agents, hypnotics, antipsychotics with sedating, antihistamines to sedating effect), muscle relaxants, and others.

When receiving anxiolytics unacceptable consumption of alcoholic beverages, because alcohol increases the inhibitory effect of this group of drugs on the central nervous system (which may be accompanied by severe side effects, including loss of consciousness, respiratory depression), in turn, tranquilizers increase the toxic effect of alcohol on the central nervous system. In an application with alcohol in addition to increased inhibitory effect on the central nervous system are possible paradoxical reactions (psychomotor agitation, aggressive behavior, state of pathological intoxication).

Simultaneous administration of benzodiazepines with other drugs, oppressive central nervous system, as well as alcohol can lead to overdose and life-threatening consequences (in the case of serious overdose require medical intervention).

Symptoms of overdose may be anxiolytics oppression CNS varying degrees of symptoms (from somnolence to coma), including: expressed drowsiness, lethargy, weakness, loss of muscle tone, ataxia, in more severe cases - prolonged confusion, oppression reflexes, coma, and possible hypotension, respiratory depression. When intoxication benzodiazepines, induce vomiting, application of activated charcoal, gastric lavage through the probe (if the patient is unconscious), symptomatic therapy, requires monitoring of vital functions, in / in a liquid (to increase urine output), if necessary - the ventilator. Hemodialysis is an overdose of benzodiazepines is ineffective.

Specific benzodiazepine receptor antagonist is flumazenil - 1,4-benzodiazepine derivative with high affinity to benzodiazepine receptors. It competitively blocks the benzodiazepine receptors and eliminates or reduces the severity of the central effects of substances which excite these receptors, but does not preclude the action on the CNS with other means of depressing effect (barbiturates, opioids, etc.). The use of flumazenil as a specific antidote in overdose of benzodiazepines is possible only in conditions of a hospital. It should be borne in mind that the use of flumazenil as an additional, rather than as a single agent. The on / in the introduction of flumazenil acts quickly, but short-lived (the action of benzodiazepines lasts longer), so can be returned overdose symptoms. In addition, the possible development of epileptic seizures (especially in patients taking benzodiazepines, along with tricyclic antidepressants in patients with epilepsy).

Despite the fact that benzodiazepines has a leading position in the degree of knowledge and breadth of application, also other anxiolytics are used in medical practice.

So far, I have not lost their importance Benzoclidine. Benzoclidine reduces the activity of cortical neurons and inhibits the activity of the reticular formation of the brain stem, reduces the excitability of the vasomotor center, improves cerebral blood flow. It is used in the treatment of anxiety disorders, including anxiety-depressive states (especially mild expressed and associated with cerebrovascular insufficiency). Especially shows elderly patients with atherosclerosis with cerebral disorders, hypertension, paroxysmal tachycardia.

The return of interest to hydroxyzine due to the peculiarities of its pharmacological action. Hydroxyzine is an antagonist of the central m-choline and of H1-histamine receptors. Sedating and mild anxiolytic effect is due to inhibition of the activity of certain subcortical structures of the central nervous system. Hydroxyzine has quite rapid development of anxiolytic action (within the first week of treatment), the absence of amnestic effect. Unlike benzodiazepines, hydroxyzine long-term use does not cause addiction and dependence, withdrawal symptoms were observed, "return." In addition to use in the treatment of anxiety disorders, including psychosomatic diseases, it is used for sedation, relief of alcohol withdrawal syndrome, as well as itching dermatoses.

From other anxiolytics differs significantly benactyzine (diphenylmethane derivative), anxiolytic effect which is caused by reversible blockade of the central M-cholinergic receptors. Due to the pronounced influence of the central structure holino-reaktive benactyzine belong to the group of central anticholinergics. His influence on the central nervous system manifests sedative effect, inhibition of convulsive and toxic effect of cholinesterase and cholinomimetic substances, increasing the action of barbiturates and others. Hypnotics, analgesics and others. At present, due to the presence of effective tranquilizers, as well as due to the undesirable side effects, atropine-related effects (dry mouth, tachycardia, mydriasis, etc.), benactyzine practically applied as anxiolytic.

Propanediol derivative (meprobamate) effect on benzodiazepine and cholinergic receptors has not. Its anxiolytic effects due to the depressing effect on the various departments of the central nervous system, including the thalamus and the limbic system, muscle relaxant effect is due to inhibition of the transfer of excitation in the neurons of the spinal cord lateral horn, thalamus and hypothalamus. Besides the treatment of anxiety disorders, meprobamate used for menopause and premenstrual syndrome. It is less effective than the benzodiazepines, and currently has a limited application.

The third generation of anxiolytics are buspirone, hydroxymethyl-ethylpyridine succinate (Mexidol) and others. Mexidol anxiolytic effect is due to its modulating effect on the membrane, including GABAA receptor complex, and shows improvement in synaptic transmission.

The mechanism of action of buspirone is not completely understood. Buspirone is a partial agonist of the serotonin receptor has high affinity for the serotonin receptor subtype 5-HT1A. Decreases the synthesis and release of serotonin, the activity of serotonergic neurons, including in the dorsal raphe nucleus. In addition, it selectively blocking (antagonist) pre- and postsynaptic dopamine D2-receptors (having moderate affinity) and increases the rate of excitation of the midbrain dopamine neurons. Some evidence about the presence of buspirone effects on other neurotransmitter systems. Buspirone is effective in the treatment of mixed anxiety-depressive states, panic disorders, and others. Anxiolytic effect develops gradually, seen in 7-14 days, and reaches a maximum after 4 weeks. In contrast to benzodiazepines, buspirone no sedative action, adverse effects on psychomotor functions, does not cause tolerance, dependence and drug withdrawal symptoms, do not potentiate the effects of alcohol.

In addition to drugs belonging to the group of anxiolytics, in varying degrees, have anxiolytic action of pharmacological agents of other groups, some beta-blockers (propranolol, oxprenolol, acebutolol, timolol et al.), Alpha-adrenoceptor agonists (clonidine). Thus, propranolol is effective in the treatment of anxiety states associated with hyperactivity of the sympathetic nervous system and is accompanied by considerable severity of somatic and autonomic symptoms, clonidine has the ability to reduce the somatic-vegetative symptoms with withdrawal syndrome opioid addiction.

In the treatment of anxiety disorders, including under compulsion, panic disorders, showing some antidepressants. In severe anxiety disorders pronounced effect gives some drugs from the group of neuroleptics.

There is an ongoing intensive search for new drugs with anxiolytic effects and at the same time safer and more effective than existing drugs. Screening benzodiazepine derivatives aimed at identifying more selectively acting drugs with the most pronounced anxiolytic effect with minimum side effects. Search also held among the substances that affect serotonergic transmission, antagonists of excitatory amino acids (glutamate, aspartate) and others.

Mildronat 500mg

22 Dec 2016

Mildronat 500mg drug in the sport - one of the most discussed topics in the world and domestic media. This drug, once included in the list of permitted substances for athletes, officially recognized Doping World Anti Doping Agency (WADA). Meanwhile, most domestic scholars and experts on sports nutrition does not agree with the decision of the organization and consider Mildronat 500mg a harmless drug, unrelated to the stimulants of physical activity.

Try to understand what Mildronat 500mg is, how this drug works, what the benefits and harms Mildronat 500mg why athletes take it and why Mildronat 500mg is admitted doping. Consider also the history of drug and find out what are the areas of its application.

Mildronat 500mg - General information, history of creation

The drug is a metabolic means known in medicine as "Mildonium". Action of Mildronat 500mg on the body - stimulating and protecting: the substance normalizes cell work exposed hypoxia (oxygen deficiency), or food shortages.

In medicine, the drug Mildronat 500mg is used quite widely: for example, it is part of a comprehensive drug therapy for coronary heart disease (coronary artery disease), heart attack and heart failure. In the Russian Federation in 2012 are included in the list of essential medicines.

Mildronat 500mg was obtained in 1970 in the Latvian SSR in Organic Synthesis Institute. Initially the device was patented as a stimulator of growth of domestic animals and birds and is used in agriculture and industry. The creator of the drug Professor Ivars Kalvins argues that the idea of using Mildronat 500mg at medicine arose after its prolonged use in other industries.

In 1984, the drug Mildronat 500mg was patented in the US, but is banned for use in a few years. Analogs of Mildronat 500mg in the United States there, but to get them in ordinary drugstores practically impossible, although in terms of the effectiveness of medical Mildronat 500mg is no doubt among doctors and pharmacists.

Application of Mildronat 500mg in medicine - readings, release forms, pharmacological action
Mildronat 500mg is a white powder with a pronounced crystalline structure. Preparations available in tablet form – 500 mg.

Indications for use Mildronat 500mg are:
Cardiac ischemia;
Myocardial;
Stroke;
Heart failure;
Nervous and physical exhaustion;
Reduced working capacity as a result of excessive loads;
The postoperative period (to accelerate recovery);
Lack of blood circulation;
Abstinence in alcoholism stages 2-3;
Chronic bronchitis, asthma and other respiratory diseases accompanied by oxygen deficiency;
Ophthalmic (eye) disease (retinopathy, thrombosis, ocular veins, bleeding in the retina);
Complications of diabetes.

Application of Mildronat 500mg in sports is justified by its stimulating effect, but it is believed that perfectly healthy people to use this medication impractical.

The active substance of Mildronat 500mg accelerates the synthesis and movement of ATP in cellular structures, which positively affects the function and energy status of cells and tissues themselves. When myocardial substance slows irreversible necrosis of heart muscle and improves circulation of any etiology in stroke and ischemia. When hypoxia (oxygen deficiency) product helps to deliver oxygen to the cells according to their needs in such.

Tablet form of the drug is well absorbed in the digestive tract. Bioavailability of drugs - 78%, the maximum content of active substance in the blood is reached after 60-90 min. after reception. Withdrawal times of Mildronat 500mg excreted - 12-24 hours, but certain tests can detect a substance in the body even after 120 days after application.

Contraindications of Mildronat 500mg

The drug is contraindicated in pregnant women, children up to 18 years (in the absence of clinical trials), people with individual intolerance to the active component or an auxiliary drug substances. Do not use without a doctor's appointment. When possible overdose gastric disorders, tachycardia, pressure surges, allergic skin reactions such as redness, itching, swelling.

In recent years, seriously study the effect of Mildronat 500mg on the body of diabetics. During animal testing revealed that the substance is able to lower the plasma glucose concentration without affecting the level of insulin. Along the way, it reduces the risk of acidosis and other consequences of metabolic disorders.

Mildronat 500mg - the use in sports

Mildronat 500mg at bodybuilding and sport is used not so long ago. Most athletes until recently referred to the drug as a vitamin agent has no effect on athletic performance. Meldonium Doping scandal changed attitude to the drug in the Russian sport. Now the matter is officially referred to the class of hormones and modulators of metabolism, and its use is prohibited during the competitions and in preparation for it.

Why do athletes take Mildronat 500mg ? Domestic and some foreign experts in sports nutrition and pharmacology claim that Mildronat 500mg has always been used by athletes as a means to adapt to the increased load and speed up recovery after a hard training, but never taken to stimulate and increase physical abilities.

Conclusions

Not all experts agree with the statement that meldonium - it affects the doping and increase performance in athletes. But there are a number of incontestable factors related to this drug. Here are the most important ones:

Meldonium effectively used as medicines for cardiac ailments and other pathologies.
Scale study to confirm the drug's effects (or lack thereof) of endurance, not spent. This casts doubt on the WADA definite conclusions about the presence of meldonium expressed doping properties.
Healthy people should refrain from unauthorized use Mildronat 500mg as a stimulant with physical and mental stress.
The drug has a positive effect on the health of athletes who have medical problems of cardiovascular nature, but does not guarantee victory in the competition.

It is clear that to take Mildronat 500mg for athletes and its analogues is not recommended until after the doping scandal. But the people who are assigned to this group of medicines by qualified doctors, should continue treatment without fear of negative consequences.

Sleep and biorhythm

22 Dec 2016

Somnologist Dr. Doping tells about the occurrence of chronobiology, melatonin and sleep factors.

Modern biological rhythms management concept includes the notion of the main oscillator of the suprachiasmatic nucleus of the hypothalamus, which controls the secondary oscillators up to the individual cells of the body. Interestingly, if the cell, skin fibroblast, highlight, placed in culture medium and observe the change in the activity of the individual cell or group of cells, it appears that during the day the activity of this group of cells will vary.

Epiphysis highlights a very important hormone called melatonin. He begins to stand out in the evening, in the region of 21-22 hours begins to increase its secretion, and it stands out throughout the night, all dark period, and in the morning when the first rays of the sun fall on our eyes, its release is stopped and the day is almost absent. Improve your sleep with Picamilon, Afobazol and Selank.

In recent papers, which say that the use of "blue" screens - all sorts of gadgets, tablets, computers, TVs - results in greater suppression of melatonin production (a hormone that provides a regular alternation of the sleep cycle), somewhere in the 20% . That is, if a person has trouble sleeping, then it is not worth spending a lot of time in the evening in front of TV, as it suppresses the production of melatonin. On the other hand, if he does not have problems with sleep, he can do anything, as long as these problems do not appear.

Gliatilin - choline alfoscerate - Features and Benefits

22 Dec 2016

Gliatilin is an unique donor acetylcholine to restore structure and cholinergic function of the brain:

Gliatilin fills deficit of endogenous acetylcholine
Gliatilin stabilizes the membranes of neurons and neuronal organelles
Gliatilin promotes conservation and restoration of cholinergic receptor field.

Gliatilin: FROM AMBULANCE TO REHABILITATION

• 1.Early recovery of consciousness.
• 2.Gliatilin prevents the expansion of finite size morphological defect of the brain tissue by the end of the acute period.
• 3. Choline alfosceratereduces the level of disability of patients after critical lesions of the nervous system.

The scheme of gliatilin in critical conditions:

• 1.Consciousness disturbance 1d (1 ampoule) 4 times a day at intervals of 6:00 intravenous (bolus or infusion); 1 ampoule of 50 ml of 5% glucose or saline infusion rate of 60-80 drops / min.
• 2.Ischemic, hemorrhagic stroke, traumatic brain injury 1 g (1 ampoule) 1-3 times a day Intravenously or intramuscularly.
• 3.Long flowing surgery; risk patients for cardiac and cerebral pathology of 1 g (1 ampoule) 2-3 times a day in the preoperative period, during surgery and in the postoperative period.

Gliatilin: Returns to the intelligent and active life from birth to old age
Gliatilin reduces neurological deficit.
Choline alfoscerateimproves the ability of patients to self-service.
Choline alfosceraterestores the cognitive, behavioral and emotional functions.
Gliatilin slows down the progression of the disease.

The scheme of gliatilin in the post-critical and chronic conditions

• 1.The early recovery period after a stroke or head injury; rehabilitation period, encephalopathy - 1 g (1 ampoule) 1 times a day intramuscularly, the first 10-15 days, then 400-800 mg (1-2 capsules) in the morning, 400 mg (1 capsule) in the afternoon for 1 to 4 months of taking the capsules 30-60 minutes after ingestion. In case of failure of the injection rate to start with compulsory admission of three (!) Capsules per day.
• 2.Dementia of different origin , Emotional disturbances, cognitive impairment - 1 g (1 ampoule) 1 times a day intramuscularly, the first 10-15 days, then 400-800 mg (1-2 capsules) in the morning, 400 mg (1 capsule) in the afternoon, the course of 2-6 months of taking the capsules 30-60 minutes after ingestion. In case of failure of the injection rate to start with compulsory admission of three (!) Capsules per day.

Gliatilin (Glyceryl phosphoryl choline phosphate) - Thanks to a more efficient neutralization of polar properties of hydrophilic groups, the phosphate form has advantages when entering into the CNS through the blood-brain barrier.

Central cholinergic effects gliatilin
recovery
motor
sensitive
cognitive
Behavioural
Emotional brain functions.

Gliatilin - Choline alfoscerateis Drug with proven central cholinergic activity and lack of peripheral side effects.

Protect Nerves

22 Dec 2016

There are effective compounds peptide able to prevent such terrible diseases such as stroke, Alzheimer's and Parkinson's.

Investigation of mechanisms of functioning of the nervous system cells, and regulatory factors allows them to better understand the process of neurodegeneration associated with such widespread diseases as Alzheimer's, Parkinson's, stroke and others. The Laboratory of Molecular Genetics of somatic cells Institute of Molecular Genetics concerned with the regulation of the nervous system functions, studying peptides - molecules produced in our body as a result of certain chemical reactions and can affect various body functions, in the Soviet Union program "Neuropeptide" was launched, in which actively worked on research of the impact of these molecules on the nervous system.

Scientific reserve

Research scientists at the regulation of the nervous system functions attracted the attention of the military: professionals working on the ground, submarines, guided missile involved needed drugs that improve attention, having anti-stress effect. Errors operators strategically important objects lead to serious consequences, and the possibility of further concentration and memory would have a great importance. In 1978, the experts on the structure and synthesis of peptides IMG Academy of Sciences under the leadership of Vladimir Nezavibatko and Nicholas Myasoedova began work on the creation of the drug having such properties.

It is known that all the regulatory peptides are quickly degraded. A medication based on these molecules needed to make a stable. Scientists have created a few short unique regulatory peptides - fragments of adrenocorticotropic hormone, consisting of seven amino acids. Amino acid sequences have been modified so that the peptides are synthesized in the body decompose more slowly than the natural. After much research and testing necessary to market a new drug Semax was launched - a highly effective brain function correction (including the treatment of severe stroke), the gain of a number of cognitive processes, treatment of optic nerve dystrophy. Today on sale there are two formulations of different concentrations of the drug, "Semax 0,1%", intended for correcting various disorders of attention and memory, some post-traumatic lesions of the nervous system, and "Semax 1%" for the treatment of severe forms of stroke.

Final victory neurodegenerative diseases is impossible. There are several drugs against stroke, but not completely effective. So there is no end of work

Continuing the battle against stroke

Today this work continues in the Laboratory of Molecular Genetics of somatic cells in two ways: as studies actual somatic and stem cells.

- In the fight against stroke already done a lot, but finally win neurodegenerative diseases today is unreal, - says Igor Dimes. - There are several drugs against the disease, but there is no one hundred percent effective. So there is no end of work, and we are working on this problem. It is likely that we will be able to find more effective peptide compounds inhibits or prevent various neurodegenerative processes. Our laboratory has been studying the action is unique regulatory peptides mechanisms, with counterparts not only adrenocorticotropic hormone, and other classes of compounds. We learn what the structure of regulatory peptides may be active, looking for which amino acids must be included in the synthesized structure, so that it is protected from the action of proteolytic enzymes - substances that break down proteins.

These studies led to the 2008 appeal of the laboratory staff to the Federal Target Program "Research and development on priority directions of scientific-technological complex of Russia for 2007-2012".

- We were able to synthesize peptides and explore, and did so, but we needed a system that would allow to quickly select the connection of a certain type of activity, - says Igor. - Chemists synthesize a huge number of derivatives of various classes of compounds, not knowing which of them would be able to eventually treat a particular disease. It is understood that the primary selection is conducted on a fairly simple systems; you need to try as much as possible connections to select promising because when it comes to testing on animals and then on humans, testing will become more expensive, and can not lead to clinical trials of hundreds or thousands of connections. Therefore, the money allocated to the federal program, enabled us to develop a relatively simple and effective system for the screening of compounds that they have neuroprotective activity. For this, we used primary cultures of neuronal and glial cells derived from mammalian brain (in this case, rats). In these models, we analyzed which compound increases cell viability in vitro. This gave the opportunity to test a large enough range of compounds and to select promising. Next, we studied how the selected compounds affect the expression of certain genes, the growth processes, axons and dendrites of nerve cell division and so on. If in the course of fundamental research, we noted that the test compound affects the protein molecules, causing the expression of certain genes, we were talking about this combination as a promising in terms of future development on its basis of the drug that can slow the neurodegenerative processes in a number of pathologies of the nervous system .

The money enabled us to develop a relatively simple and effective system for the screening of compounds that they have neuroprotective activity.

Nerve cells are able to regenerate?

The second direction, which involved employees of laboratory of Molecular Genetics of somatic cells, is associated with the study of the differentiation of embryonic stem cells. While the research is carried out on the model is not human, and mouse cells, however, it is fully possible to trace variations differentiation of mammalian cells.

- Embryonic stem cells are able to multiply indefinitely in the laboratory, and they do not lose their ability to differentiate into all organs and tissues of the body. If we talk about a person, then, as you know, running the embryonic stem cells in a certain type of differentiation, they can be used for transplantation in the affected organs. If the cells take root, there is a regenerative process. We can expect that the affected or lost functions in any way restore the cells differentiated into neurons, although to date there still ambiguous. Despite the fact that the animal model we have seen a partial recovery of disturbed functions in stroke, the problem is very complicated, because unlike other organs - liver, kidney and even heart - brain transplant can not be: it will be a different person. We can only try to fix the affected areas. When transplanting the cells is important not only so that they remain viable, but also to establish the right connections with existing neurons. Only then can we talk about the restoration of brain functions. To this aim, and our research.

It can be expected that the cells differentiated into neurons in any way restore the affected or lost functions, although to date there still ambiguous.

The quality of life

From the research topics we turn to the question of quality of life. The difference in the approaches of the scientists of the Institute of Molecular Genetics, Russian Academy of Sciences and foreign laboratories to modify unique regulatory peptides was outlined in the late 70s, at the beginning of work on this problem.

- Above the structures composed of natural amino acids, at the same time started to work for us and the West - says Igor. - Particularly strong was a school of Dutch scientists led by De View, which is also engaged in analogous regulatory peptides. Which way went the Europeans? They also have modified the sequence of these molecules, but there was added D-amino acids - compounds which do not occur in the human body. Either type of substituents used specific fatty acid residues, carbon chains of different lengths. This could lead to undesirable side effects, including the development of cancer. In our institute we used only natural L-amino acids. With this approach, the body does not introduce anything foreign, and when the drug was divided, were only conventional amino acids, of which our body is largely composed. This is an ideal approach, as they say now, provides the correct quality of life. He was already in full developed in our country, although today it is called differently and believe that these principles work came from the West. In fact, Western civilization is very closed, she wants to take everything from around the world, and particularly from us, but listens only to himself. It is, so to speak, arrogant - in the best sense of the word.

Intellectuals and farmers?

We develop the theme of "Western arrogance".

- They engage in expansion, - says Igor. - If people say every day, you need to eat, "Snickers", and they will eat it. What's on TV? You will find, for example, what percentage of western gear, films show us? I once asked. Up to thirty percent of the Western (particularly American) films. I do not think that on American television may be thirty percent of Russian transmissions. You have to understand the reality: there is no cooperation between us and the West, which is often say no; there is the use of our resources, any - natural, intelligent, others. They do not do anything illegal, just pursue their own goals, and also we need to pursue their. Why walk at the end, and will always trail? Because we do not produce a final product that can be consumed and sold.

Why walk at the end, and we always will? Because they do not produce the final product. I think you should start with the fact that has long been done in Europe and America: with agriculture.

I think you should start with the fact that has long been done in Europe and America: with agriculture. Maybe those words someone rebelled (ostensibly nothing else we do not do), but when a person is hungry, he stops to think about how to feed their families, and thinks like something else to develop. In the meantime, in our conditions, we must begin once again on the same circle. Especially since the only place, where now it is possible to establish, first, clean production, and secondly, no genetically modified additives, it is for us.

There are figures showing that annual global losses from a variety of neurodegenerative diseases, stress, schizophrenia and other diseases of the nervous system account for hundreds of billions of dollars. According to statistics, for example, in Russia in the year there about five hundred thousand strokes. Man has become incapacitated, not come to work - it's a big loss for the state. We are talking about socially important work, we have the venerable national objective: to help people to be healthy. Therefore, research in areas such as oncology, stroke, neurodegenerative and cardiovascular diseases should be state orders. If the scientist is always to look for the money, which means that it is degraded as a scientist and ceases to fully think about the experiment. The Ministry of Education and Science, to a certain extent provides order, but requires more applied output. This is the right direction, but fundamental research is also necessary to develop and maintain.

Great Cognitive Revolution

22 Dec 2016

Technologies associated with the brain, coming out of the walls of laboratories and begin to penetrate into our lives. This is not an abstract science, and specific preparations, systems and devices. They may feel they can be purchased. Great cognitive revolution is happening before our eyes. In our world becomes more and more devices that are configured on a dialogue with the person carefully watching us and studying us.

Introduction

man sitting in a chair, hung with electrodes.

Think of any number, "- he says scientist in a white coat. After a few seconds on the screen appears the figure five. The device is able to read thoughts. And there is nothing sensational about it.

The device for reading thoughts ...
cord management in the distance ...
Prostheses with which it can be seen without the aid of the eye ...
Drugs make a person smarter and bolder ...

Ten years ago, such scenes belong to the genre of sci-fi fiction. Sometimes there were reports in the press, saying that such a professor is going to create a technology that might help ... The future came quickly. Now you can do without "going" and "possible."

Cognitive: remember the word

The word "nanotechnology" has learned all. Even juniors are ready to Having reported that this piece opens the way for us in the future, that "nano" means ten to the minus ninth and that through this console Russia finally able to get rid of oil dependence.

Now it's time to learn a new word - "cognitive". Cognitio in Latin means knowledge. Cognitive science studies how we perceive the world, how to think, what to look for, how to memorize and so on. On the basis of its discoveries constructed cognitive technologies - devices that take into account our state, attentive to our attention, and even watching the work of our brain.

Now the retina of your eye perceives black characters on a white background. Included are neurons that are pulled out from the memory images are activated knowledge. As a result, you understand the meaning of the article (in any case, we are very hope so). A couple of days will be arguing with a friend about the fate of Russian science and possibly retell a piece of text. Make sure all of this chain - one of the tasks of cognitive science. But not the only one.

Under the banner of cognitive since the sixties of the twentieth century began to unite psychologists, linguists, psychologists, mathematicians, computer scientists, and representatives of other sciences. But right now, the results of their studies are starting to turn into a mass technology. And more importantly, cognitive research merge with other, no less cutting-edge areas.

Cognitive interfaces and virtual reality
The first graphical shell programs have emerged in the 80s, and in just a few years occupied the minds of progressive part of humanity. The graphical interface has revolutionized, to make computers an essential complement to the human brain, because the world is on the computer screen has become similar to the objective world, to work with which our brain is set up.

But in its current form, the graphical interface is obsolete and no touch screen position is not saved. The fact that he does not consider user identity, our state interests and goals - he can not adjust to us and maintain a dialogue, as it should any normal robot from the movie.

Alternatives are available - for example, a pilot interface, which is developing an iconic game designer Peter Molyneux. Instead, the desktop - living in the lap of the virtual nature of the boy Milo, getting to know the user is able to determine his mood's expression, understanding it and ready to run any command or just talk about life (in his virtual world, too, some his own life with its events ).

Interfaces of the near future will be able to perceive not only verbal, but also the mental command. Today, these interfaces allow you to interact with the computer and communicate on the network paralyzed people, able to move only his eyes. For a wireless computer control and other devices enough camera, tracking the direction of gaze.

And of course, in the near future interface, as it sounds banal, it becomes three-dimensional. Why, by the way, still has not become? In the cognitive scientists has unexpected answer: to work with three-dimensional displays is very difficult for our brain, occurs quickly seasick (it is now called "simulator sickness") and a strong psychological discomfort. Virtual reality - Cognitive technology based on the use of visual illusion, to deception of our senses. But when leaving the third dimension we have been able to deceive the only part of the mechanisms of visual perception, there is a mismatch of the conflict brainwave programs, and the user hangs up. You head after "Avatar" did not hurt? With the current 3D technology, we will not rest, and tired in the three-dimensional "home theater", which is about to begin the conquest of the market - there is not enough cognitive solutions.

Crowned picture of a bright future interface for interaction with your own brain, allowing, among other things, to strengthen and weaken the desires and emotions. We are waiting for the temptation, in comparison with which any drugs seem child's play! It would not turn into the legendary rat, the owner of the world's first brain control panel, which is all the stings and stings on the pedal, enabling her center of pleasure, until she died from exhaustion. And yet, people should take up the challenge to move on.

Neuroeconomics and neuro-politics

On the basis of conventional image processing with webcams already today it is possible to analyze human emotions. For example, policy advocates, and the system logs and analyzes its facial expressions, and tells us whether the speaker is lying, or simply disingenuous and what his real feelings about what has been said.

Further - more, the smart thing to learn to look to us directly into the brain. A typical experiment of the rapidly growing field of neuromarketing: the subject show commercials, but this time his brain scanning equipment magnetic resonance imaging (fMRI). The reaction of the test on the rollers as a whole or for individual objects and scenes judged by a special color areas of the brain, indicative of their increased or decreased activity. Experimenters are not interested, like the subject or not advertising, it is important how the brain responds. On assurances neyromarketologov, the technology allows to design advertisements so that they cause the most positive reactions of people and how they can be firmly imprinted in the subconscious.

For example, the study of cognitive scientists at Bonn University, titled "What do men want?". The subjects were shown three groups of cars - sports, such as Ferrari, middle class and economy class cars. It turns out that different cars react different structures of the brain. Structures associated with spontaneous emotion sharply intensified in all subjects men, when they showed a sports car, and the other two classes of cars, on the contrary, caused their braking. For the cars easier reacted structures associated with the conscious control of behavior, "reasonable choice." I wonder what brain structures we react to produce a domestic car industry ...

So far, however, fMRI - a very expensive method and apparatus are extremely cumbersome, but remember how to look and how many computers cost a few decades ago. Methods of monitoring the activity of the brain is also developing rapidly, and after 10 years counterparts fMRI can be used in everyday life.

NBIC time

Several years ago the US National Science Foundation, under the auspices of which being the lion's share of research in the United States, released a report that predicts the development of science in the next 50 years. The report was named NBIC, or in Russian NBIC. Abbreviation is not too harmonious, but that it is becoming a major trend in the coming decades.

"H" - a nanotechnology, "B" - biotechnology, "I" - information technology and, finally, the "K" - cognitive technologies. Half a century ago, these four areas are on the sidelines of world science. In any case, it seemed not as important as nuclear physics or chemistry of polymers.

The revolution of information technology began in the '60s, the rapid progress of biotechnology turned in the 90s, in zero, we all ears buzz about nanotechnology, and are now beginning to develop rapidly cognitive technologies.

Now with "nano", "bio", "info-" and "Cogno-" bind future. Thus all four areas should be developed in a dense bundle. Take, for example, information technology. The capacity of electronic media is growing at a breakneck pace. Soon you will be able to get out of the box with the disc "Movie" sign on which all the movies ever made will be recorded by Hollywood. But you'll need some sort of device that allows you to find the information you need, without spending time and nerves. And this is a cognitive technology.

One of the first in Russia fashionable theme of "NBIC" grabbed the Kurchatov Institute, known for its ability to convert new ideas into solid science infusion of public money.

7 cognitive technologies that will change the world

Many developments in the field of cognitive technologies invented in Russian institutes and universities, and then sold on the domestic enterprises. We have identified seven major trends in this area - those without which a few years it will be impossible to imagine life. All of them already exist in the form of actual technologies and some even reached the normal production.

1. Get smart: Cogne-tropic drugs (nootropics)

What is. Our thinking - is a chain of chemical reactions. It means for intelligence and the emotions can be influenced by chemical substances. For centuries, this was done with the help of alcohol, drugs and other muck. But now science is ready to offer a set of effective and relatively safe medications like.

Positive effect on the processes underlying perception, analysis of information, learning and memory ... "- that describe the drug Semax its creators from the Institute of Molecular Genetics, Russian Academy of Sciences. Development began in the 70s by order of the Ministry of Defence. Now semax drop can be found in any drugstore.

The drug does not "change the mind", it only improves cognitive function, brings them back to normal. In order to bury itself in the nose of the substance do not necessarily suffer any disease

healthy people can take semaks to stimulate memory and performance. "

Following Semax appeared on the shelves of pharmacies Selank, which helps to cope with stress, removes the fear and anxiety.

We continue to work on new drugs acting on the central nervous system, cognitive functions. They will have a different structure - shared with "PP" Academician Nikolai Myasoedov who directed these works. - But while the development in the early stages, and that it will turn out, we can not say.

There are also more extravagant ideas. For example, Professor Konstantin Anokhin Institute of Normal Physiology RAMS will release a substance capable of erasing unpleasant memories. And this is not a utopia, a drug already tested on animals.

What will happen. At first, people using smart doping, will benefit over more conservative opponents every GMO and other innovations. Then the society will get used to this "cosmetics for the mind." Tablets that affect thinking, will take everyone - teachers, office workers, police officers. It will be as normal as drinking vitamins today.

2. Transparent Head: neuroimaging

What is. Transparent mouse brain, which Russian scientists have demonstrated Dmitry Medvedev - one of the most vivid symbols neuroimaging, saying, look, thinking is becoming more open to science, and to the authorities.

Our brains for many years was regarded as a "black box." Behavioral psychologists taught: you can only learn what the input, - words, images and other incentives, and that at the outlet, - retaliatory words and actions. What happens inside the skull remained a mystery. Now, there are computerized tomography, magnetic resonance imaging, positron emission tomography, magnetic resonance spectroscopy, and so on - a lot of modern technologies to literally see the work of our consciousness.

This is necessary not only to doctors. In recent years, the fashion is such a thing as neuromarketing. Man shows the options for the new package of oatmeal and watching how the brain reacts to it, which zones are activated and which remain calm.

What will happen. "Peeking" in the brain become traditional procedure in different areas. This will engage and sociologists, and educators and criminologists. Their work will be much more effective. However, recall unsuited dystopia feared not only ordinary people.

3. Artificial senses

What is. Technology can replace the eyes, ears, nose and other organs. In many laboratories of the world is the development of visual prostheses that will make even sighted totally blind people. You do not need to use the eye and the optic nerve - a signal with a miniature camera goes directly to the cerebral cortex, which is implanted a special chip.

On a theoretical level, all the technology is already understood and tested on rats and cats. Now we are talking about the technical details.

That is, the scientists checked how the electrodes will behave in the brain tissue, whether the inflammation, whether corrosion will occur.

What will happen. It is expected that mass cure the blind and the deaf will begin in a few years. A few decades implanted electronics can be more sensitive than living bodies. After all, we see only in a narrow wavelength range, and survey the space of only 180 degrees. The visual prosthesis is theoretically capable of transmitting the image to the brain and in the ultraviolet and infrared, and X-ray ranges. And you can see, not only in front, but the back, side and top.

4. Know the state: cognitive assistants

What is. Good secretary always takes into account the state of his boss - is irritated, tired, or good-natured. But to replace the busty blonde in short skirts is already underway electronics. Various systems are beginning to help the person to monitor their activities.

Begin with a simple - to sleep. A small company "NeurOK", created on the basis of the Institute of Radio Engineering and Electronics, Russian Academy of Sciences, released the driver awake sensors. At least one-third of traffic accidents is due to the fact that the man had fallen asleep for a moment and lost control of the situation. Condition prior to falling asleep can be identified by brain rhythms, eye movements, especially of speech or the electrical conductivity of the skin. The man has not yet had time to fall asleep, and the unit is already beeping and flashing.

And again this is not some kind of experimental design, such devices are already in the cockpits of several thousand Russian locomotives. Soon to begin mass production of such devices for car drivers.

What will happen. Sensors driver wakefulness may enter into a massive turnover in the coming years. It is possible that the Europeans, who are concerned about their safety, require all drivers to install such devices, and then the market of such devices will be in the hundreds of millions. Gradually learn to cognitive systems to help us in all - to drive, to learn foreign languages, to cope with temper tantrums. We will quietly listen to the recommendations of smart organizer:

5. Brain Bashers: Brain-Machine Interfaces

What is. Mind reading is becoming a scientific commonplace. Conduct experiments, published articles, thesis defended. Systems to directly transmit signals from the brain to the computer,

However, not only the brains of a computer controlled, but also vice versa.

What will happen. In two or three years in the computer can be a supermarket to buy a device that allows you to play shooter rpg using the power of thought. And sooner or later it becomes available mental control any device, and such a trifle as computers and mobile phones, move from our pockets directly into the brain connected to the Great Network.

6. Iron thought: intelligent robots

What is. The robot can easily depict the movement of the waiter, janitor or collector circuits. It is much harder to teach him to imitate the way of thinking. Scientists and engineers are trying to make mechanical devices more and more like a person, not only in appearance but also intellectually. Robots must be taught to see (recognize objects, to determine their location), hear (detect spoken language), thinking (quick decisions).

In Russia, too, such developments are under way. By the way, in the area of "intellectual stuffing" we are not so far behind the Americans and Japanese, both in the field of mechanics.

The basis is the emotional behavior of living people - their speech, intonation, facial expressions, behavior. The resulting model algoritmized and converted into program code. As a result, the computer screen is already talking painted men, able and joke, and angry.

What will happen. On "Revolution robots" speak for half a century. It never happened. Instead, there is an evolution: robots penetrate into our lives rather slowly, but surely. For example, according to the forecast of TechCast, by 2022, intelligent robots, sensory environment environment, decision-makers, students, will be used in 30% of households and organizations. And soon for someone robot may be more sensitive companion than a colleague or neighbor in the stairwell.

Analysts will not be needed: automatic analysis of texts

What is. Mankind produces every second, millions of pages of text. And the world is ruled not the one who owns the information and someone who knows how to handle it and filter. Computer systems are not only able to lay out the documents on the shelves, but also try to understand their content.

For example, the company Cognitive Technologies was created by the Institute of System Analysis, RAS. Its profile - creation and implementation of management systems in enterprises. The main feature is considered intelligent analysis of business information: "We have created a new form of description of the document, whose main elements are the so-called semantic units ... In fact, this approach is nothing more than an attempt to abstract the implementation of the mechanism of thinking in artificial intelligence systems." Similar systems are already in place in a very reputable companies such as the "Norilsk Nickel".

Also work everywhere electronic translators or handwriting and voice recognition systems. And if we ask Google find something containing the word "cognition" and "technology", then the system will be wise enough to give us an article on cognitive technologies, despite the fact that the word "cognitive" in them never used.

Ten years from analysts, reporters, translators and many other professionals have to compete with cars. Systems themselves will compare the texts and numbers, and then draw conclusions. And there is a risk that people will lose this fight. Already, the computer is able to digest thousands of pages per second, and when he learns more and analyze this information, people will be in difficulty.

Leuzea: Ancient Doping

22 Dec 2016

Our patient today - a good old adaptogen. The plant, which is native to the mysterious, wild mountainous areas of Siberia. Apparently, once people decide to eat the grass and got a variety of effects, and the rumor leaked thousands of kilometers away from the potential epicenters. Leuzea - a fast adaptogen. Its effects are felt immediately.

About this grass, I learned from his classmate at the university a few years ago, he exploits it until now. One day he introduced me to somehow agent that reduces sleep, increases energy, vitality and simply suppresses almost all available ordinary person sedatives. But everything is always in order.

Leuzea is began to produce and use as a food additive in the 50-ies in the USSR. Maybe someone heard about the soft drinks "Sayan", which contains levzei. This was the beginning of mass improve immunity Union citizens, our response to the western caffeinated cola. Since the substance is firmly stuck among domestic mineral grass.

How does Leuzea act:

• 1.The muscles, stamina, libido.

Our current material includes a plurality of antioxidants, vitamins and trace elements.

Leuzea is rich of ecdysteroids, for this reason forbidding used by athletes. If you are far from the sports pharmacology, then believe in the word that ecdysteroids do not have steroids in the mass consciousness, and there are no corresponding side effects.

The basic ecdysteroid in Leuzea - is ecdysterone. Most likely, this component is the link with Leuzea such effects as increased libido, increase muscular endurance and increase muscle mass by improving protein metabolism. However, no precise unambiguous data that ecdysterone is useful, so do not rely that take Leuzea and shake. But fatigue is indeed less!

Possibly, there is an action on norepinephrine. The precursor of adrenaline. If the system is circulating adrenaline, you can be sure that it is there and norepinephrine. To physically understand and feel how it works, you can imagine yourself a predator while hunting. Tu strange nervousness, quick look, suddenly able to stand still and concentrate on the victim. Tu smooth movement and, at the same time, the power to explode up and make a crazy exercise.

• 2.Leuzea improves memory and learning.

In the 70s of the last century Leuzea conducted a study on the 52 healthy volunteers aged 19-25 years. Conducts proof-test, the test on hold attention. A total of 10 drops of extract of Rhaponticum improved performance by 4 times compared with the control group.

Leuzea acts on the energy processes in the nerve cell, to strengthen the synthesis of energy-rich proteins, eg connecting, nucleic acids. Simply put, Leuzea creates energy reserves in the cells, the best energy efficient and writes in a notebook a new standard energy production through nucleic acid.

Another entertaining study was conducted on rats. Maze was used to test their intellectual abilities. There were three groups where Leuzea used in different doses for 10 days, it turned out that the group, which was the average dose showed the best performance. Unfortunately, it is not known what it means to the average dosage for humans.

• 3.Leuzea improves the immune system, fights stress.

Mechanisms are many, one of them - it is the inhibition of the activation of a protein complex NF-kB. It is present in all animal cells and regulates the response to stimuli as stress, viral infection, inflammation, etc. The better the complex is a protein family in our cells, the more we are exposed to stress and viruses. In general, it is normal practice. Man is not a robot. We are made of organic materials and may conditionally "hurt", but Leuzea makes us a little more healthy.

In mice were amply demonstrated above indicated effects. Overall performance has increased by 88%, and in some indicators in 2 times.

In experiments on humans no precise percentage data. But there is a good sample, 902 people took Leuzea. In the experimental decreased depression, improved neuro-psychological tone and decreased craving for alcohol, probably because so tincture contains 70% alcohol :-) After 15 days of improved overall health. You can also like Cerebrolysin.

Course Leuzea

Contraindications adaptogen Leuzea can be acute heart failure, antidepressants - MAO inhibitors, high blood pressure.

Here it is necessary to say what benefits it Leuzea, compared with other adaptogens. Ginseng, Eleutherococcus and Radiola likely to cause in overdose side effects. In the case of today's difficult to achieve substance overdose. In small and medium doses it will be useful and almost harmless for both men and women and children over 12 years.

Side effects inherent not everyone and not always. Most often they occur in those who have an excessive amount of material. There may be this: distraction, rapid breathing, sweating.
Leuzea sold in a variety of different forms of production. Personally, we classmate took alcohol tincture (extract Leuzea). Not because alcoholics, but because the first available under the arm. I drank 1/4 bottle (13 ml), diluted in 300 ml of water in the morning a couple of times a week. My friend take on the bottle, but it seems to me that it is too straining the heart and the body as a whole. Remember, alcoholate, all of a sudden! It is containing alcohol 70 degrees. Little did drive the car ...

Officially, extract Leuzea course is as follows: 20-30 drops 2-3 times a day for 3 weeks. It is about a teaspoon at a time.

Bottom Line:

- Leuzea undervalued and unacknowledged, for unknown reasons.

- This herb has a wide spectrum of action. Especially worth noting Properties of nootropic, adaptogenic, immunostimulating. Also, there are specific effects: reduction of alcohol dependence, improving muscular endurance, an antidepressant effect.

- To understand its effects, take a teaspoon 3 times a day, if the tincture. It can be even more. For sale in pharmacies.

Development of Creativity

22 Dec 2016

It is no secret that the thought patterns are usually less help in life than the ability to find original and creative ways out of difficult situation. This is what we will talk today how to develop creativity, the example of famous people, find common features and the real practical issues.

Creativity requires some innovative and unusual, but these concepts are constantly intersect with various inventors and people of creative mindset: musicians, writers, artists, etc.
So, what is common between the moon walk Michael Jackson, Steve Jobs and his first with beautiful fonts and the creation of Heart Attack Grill by John Basso.

• 1.The denial of the ordinary, patterns, stereotypes.

You should enrage so routine, annoying imposed the idea that wants to change everything at once. And what is more important, not just to criticize, like some old lady at the entrance, but also offers an alternative. Condemn someone or something - this destructive approach, but also the easiest. But to create, on the site of a new criticism of the idea - it is a manifestation of creativity. Write down somewhere on a piece of paper, that every time I do not agree, what I was furious, I'm looking out, an alternative, and not grumble.

Immediately I would like to talk about Heart Attack Grill, a small chain of fast food restaurants, which are located in the USA, positioning itself as a cafe with the most harmful food. Can you imagine how much it differs from the total. There's action in the style of "take order from 7000 calories, get a pack of cigarettes without filter in the present." Waitress service in the form of honey sisters, and all fried foods Refried.

• 2.Courage

No one will ever know about your super-creative genius idea, if do not take efforts to implement it. Whatever good boxer, his world does not know, spending it just fighting with a shadow.

Creative ideas at an early stage of their implementation is likely to be rejected by an inert society, and it is the majority. However, when 2 conditions, the idea of advance, acting on the principle of Overton Window. The first condition - the bold, resolute man, the 2nd - a promising idea.

Courage is not the fact that pricked his face piercings and not in proving its "correct" point of view, this does not apply to the creative audacity. And soon - to try to release the world's first mobile phone with a touch screen, when around one push-button. The company, which once went on such a step, clearly, daring and creative, and especially its owner.

Awake you brain be Phenylpiracetam, Semax, Cerebrolysin.

By daring can even examples do not cause any known creative people became known for this quality.

• 3.Timeliness.

Part of this item was before, when we talk about the prospects. The line between the absurd idea and ingenious, creative might be the time. If Bill Gates talked about the mass distribution of some computers do not yet exist at the beginning of the 20th century, it would not be creators and crazy. An important feature of creative people - to be ahead of their time, but not too far to the decision were valid. In other words, capture trends, promising areas in the world.

One of the most creative directors of our time - James Cameron, who gave the world such cult films as "Aliens," "The Terminator," "Titanic," "Avatar", many of the projects put off for years due to lack of technical and technological component. Ie he could not fully implement its director's ideas at a time when there was this idea.

Another example of timely creative thinking - is the appearance of the first electronic cigarette in Russia in the mid-2000s. The young guy that name, I have not found, became a millionaire in a few months, when on the counter in one of the stores found in China electronic cigarette. First he bought a small lot and it quickly sold out at the hostel, then began to PR through the Internet, only 2-3 months and the profit amounted to several million rubles. But he did not cope with the increased competition.

This story is indicative, just imagine how many ideas are still waiting for their time.

• 4.Curiosity / activity.
  
  

Sphere is absolutely not important. To find interesting, unusual solutions and ideas you need to make it at least something in my head. Be a man of knowledge, he was able to use them. Be super-brainy in this context does not necessarily. There is a billionaire, Richard Branson, I advise you to read his autobiography "Losing virginity", so he is seriously behind in all subjects in school, but in high school issued student magazine. Who is interested in literature, aeronautics, music, crossed half the world in a balloon, where almost died a few times actually.
Lee Iacocca - the man who with his team, led by Ford, and took one of the most controversial and brilliant solutions in the auto industry, creating and starting to produce the famous Ford Mustang, the Mustang was first way should be called Mongoose. It was a revolution in the automotive industry, and so did the first mass sports car for the American consumer. Iacocca childhood interest in many sciences and excelled in many ways. He was president of the school, had exceptional knowledge in the exact sciences, but was known more as a humanist, led by Ford and Chrysler.

In general, where you do not look, just about any truly creative person has an extraordinary outlook, which enables it to generate ideas. It's like some kind of designer, whether a person has 10 parts, it is unlikely that he is something interesting will gather, and another thing when a person 100 or 1000 pieces.

Summary: Being creative does not mean being immoral, antisocial, behave provocatively or live in Pontus. Original thinking is the result of curiosity, courage, the ability to predict the future, its trends, the ability to identify hidden needs of society and deny the bureaucracy template. Then you can create your Ford Mustang.

Phenibut Discussion. Part-2

22 Dec 2016

Phenibut same - it's a very, very unique product, often repeat, is a good substitute - an alternative to supplements, because its tranquilizing properties are quite within 1500-2000mg / day, but there is no side effects, and memory indicators of intelligence in general only improve. If addicts have nothing to take, they OCCASIONALLY Phenibut abuse, which, of course, at high doses, leads to the formation of dependence is very mild. Often it is not required to facilitate specific drug withdrawal. Phenibut, I repeat again, it is one of the few neuroprotective drugs, has no side effects like Piracetam, etc. (agitation, insomnia, etc.) - so Phenibutum very popular. Adding it to the treatment regimen of mental disorders significantly reduces the dose of antipsychotic drugs, biological supplements and other medicines, and thus eliminates the side effects Phenibutum "heavy drugs". A unique product that has no analogues in the world. And the fact that many doctors do not know how to use it properly, and drug addicts sometimes abuse them - it is clear how to grams peas. And even more clear ignorance of many "Psychiatrists" in relation to Phenibut - they are, I repeat, we must be able to use.

Phenibutum actually promotes rejection of depression since the first dose. It helps to maintain physical activity and overloads, Phenotropil is a littleall the same. But ... in conditions of psychological stress preferred the latter. Several noticeable mood-elevating effect of this nootropic that is not always necessary. Overall, a very decent product - not expecting.

Introduction into the molecule of the fatty GABA phenyl radical Phenibut converts it into a preparation. This radical GABA easily penetrates into the brain and has a strong inhibitory action (which is characteristic of this acid).
GABA also exerts nootropic effect (it is mandatory participant in many metabolic processes in the brain).

What do you think about course combination Phenibut and Pantogam (say Pantogam course lasts, and for 2-3 weeks joins Phenibut)?

To reduce the irritating effect on the mucous membrane of the digestive tract Phenibut had to take gastrofarm, with a clear action Phenibut I have not seen.

Before taking phenibut need a square meal, a good anxiolytic, good support in stressful situations, but slows down response time.

In general, I have absolutely no interest in the use of recreational Phenibut not interested as to develop the use of ad hoc, most want to know is about the use of foreign exchange, as I expressed astenik with a combination of fatigue and at the same time quite strong generalized anxiety.

I know a lot of stimulants, some of them tried Enerion the same way, foreign exchange reception very nice reduces fatigue - BUT! - My whip in the first place - the anxiety, uncertainty, stiffness, severe vegetative reactions sometimes the most innocuous anxiogenic stimuli (call the client at work, resolution of operational problems, etc.) - vega rushing, by leaps and bounds: the pulse quickens 3 sekndy and a half times, sweating, subjective sense of increasing blood pressure.

I want it to get out of it completely. Symptom of a watch for about 7 years (21 years for this day, 28 years), and watch it in the steady development. Shoveled tons of material for nootropics, tranquilizers, psychostimulants, etc. Many have tried, but their main problem - the alarm and a monstrous reflection - to win can not. I think, and fatigue grows from here.

He was engaged not only in self, was the doctors. In addition to the procedures and the regime (by the way, involved in athletics, I love warm baths, etc. - helps only during the procedure, from start to finish: got out of the bath / jumped off the treadmill - Symptoms go into growth again)
doctors prescribed: 1) Pantogam 2) Medazepam.

Medazepam tried (although he knew what the charm) - by itself, Tupelo, and sexual life left in the realm of fantasy. Naturally, from the BDT he refused. By the way, I tried Grandaxinum - about anything.

Pantogam begin to accept and finish, more than 3 months did not take any time - yes, some effect is, again, starting with doses of 2g (8 tablets) per day, but more or less serious anxiogenic environment (and I Manager active sales) effect is somewhere far away, faint background.

You write that your main problem is "anxiety, uncertainty, stiffness, monstrous reflection, and hence fatigue." So I do not see in this case, the indications for admission nootropics. You yourself write that you have tried many things, but the condition is getting worse, "a symptom watch for about 7 years (21 years for this day, 28 years), and watch it in the steady development." Therefore, it may make sense to discuss with your doctor the inclusion in the scheme of treatment of antidepressants and tranquilizers?

I took sertraline (Stimuloton) 200 mg / day. Yes, the mood in general is increased, more energy - but! - Anxiety remained still, fatigue, in principle, too. Thus, in general, antidepressant influenced only general background mood. (NB Before taking Sertraline Fluoxetine 2 months - went to Sertalin because of sedation, which is produced in the fluoxetine me).

I would take Sertraline further, but left (descended gradually decreasing doses of "ladder") due to the negative effect of too, which he made on libido, erection and sensitivity, up to anorgasmia. (By the way, occasionally (3 weeks) tried mono bupropion, yes, of course, in the sexual sphere it acts only positive, but - crazy aggression, impulsivity, anxiety generally passed into paranoia ....)

In general, empirically observed that the most positive impact on the complex I have only nootropics, but in different ways. Of course, Timo-analeptic effect of sertraline is beyond competition.

What's to argue Phenibutum popular among the people and is sold without a prescription. How to love to joke with the reception thereof nootropic becoming give a damn :) hence the root Phenibutum. But seriously Phenibutum suppresses anxiety, relieves asthenia, energizing, acting a little Wegetotropona, enhances the antidepressive effect in TCA - prices were not, would this nootropics, but unlike Phenotropil - reduces attention and slows reaction.

I take Phenibut for week, there is a strong effect, but I just have not tried before. You can draw an analogy to its action of bupropion, only changing the negative to the positive.

Bupropion is also based on phenyl-ethylamine structure (this is just for reference).

However, personally from bupropion I watched the monstrous aggression and destructive thinking.
From Phenibut - quite the opposite, I would call it a strong empathogen.


Phenibut acc. the law should be sold strictly on prescription. It should be noted that for him now follow stricter than many other funds, stricter than fluoxetine (eg., Profluzak). And I readily understand why, because Profluzak (when I took it - the doctor wrote 1.5 years ago) almost makes man God's dandelion. Then the action is much more difficult Phenibut.

I for myself have now understood why the whole attitude towards Nootropil skeptical - as compared to all other Phenibut nootropics (and I have tried almost everything, trying to get out of troubling asthenia) - compared to him they - vitamin C in the degree of impact on the psyche.

Moreover, now I would recommend to treat it much neater. Yes, positive, but very, very strange ... I do not know what will happen, but it seems to me that the first time my personality changes, and much more so than it has been in the treatment of other nootropics, DB, antidepressants (fluoxetine and sertraline (at a time, one had to change to another) - on doctor's advice).

I currently find it difficult to give a general description of this change. Of course, I notice a significant reduction asthenic effects (weakness, fatigue), as well as anxiety, but I think it gives a certain price, though, I repeat, I can not say for sure, strategically change negative or positive.

I can only assure you that the anti-social effects, drug aggression is not exactly in this respect it is safe.

But the fact that it is often prescribed to children ... I was puzzled and confused now that I feel in myself these changes. I would not recommend prescribed the drug during the formation of the central nervous system.

But the fact that the drug is definitely powerful, I can confirm (based on my extensive experience in the treatment of a placebo effect can not be considered - not only admit to the second reception at the beginning of the course I felt no small skepticism with regard to the drug - of course , expected effect, but suggested that it would be slender like Pantogam).

Phenibut Discussion. Part-1

22 Dec 2016

The most interesting IMHO nootrop today, however, and the corresponding price

By way of introduction - information from the radar:
Gamma-amino-beta-phenylbutyric acid hydrochloride. Description of the active substance

Therapeutic - anxiolytics
Nootropic (neurometabolic stimulants)

The nosological classification (ICD-10)

F10.3 abstinence
F11 Mental and behavioral disorders due to use of opioids
F40.2 Specific
F41.0 Panic disorder [episodic paroxysmal anxiety]
F41.1 Generalized anxiety disorder
F41.2 Mixed anxiety and depressive disorder
F48.0 Neurasthenia
F51.1 Drowsiness [hypersomnia] inorganic etiology
F63 Disorders habits and instincts
F95 Teaks
F98.0 Enuresis inorganic nature
F98.5 Stuttering [hesitation]
G47.0 Disorders of falling asleep and maintaining sleep [insomnia]
H81.0 Ménière's Disease
H81.9 Violation of vestibular function, unspecified
H83.0 Labyrinthitis
R32 Urinary incontinence unspecified
R42 Dizziness and disturbance stability
R45.1 Restlessness and agitation
R53 Malaise and fatigue
Z100 CLASS XXII Surgical practice
Latin name
Gamma-amino-beta-phenylbutirate hydrochloride
chemical name
gamma-beta-Amino-phenylbutyric acid hydrochloride
Gross - C10H14ClNO2.HCl
Characteristic
The white crystalline powder. It is very easily soluble in water, soluble in alcohol, pH water (2.5%) solution was 2.3-2.7.

The chemical structure can be seen as a phenyl derivative of GABA, as well as a phenylethylamine derivative.
Pharmacology
Mode of action - nootropic, anxiolytic. Influences on GABA receptors in the central nervous system, facilitate GABAergic neurotransmission, improves the bioenergetic processes in the brain. It eliminates tension, restlessness, anxiety, fear, and improves sleep; It extends and enhances the action of hypnotics and antipsychotics, narcotic analgesics. Reduces the symptoms of fatigue and vasovegetative symptoms (including headache, a feeling of heaviness in the head, insomnia, irritability, emotional lability), enhances mental performance; improves attention, memory, speed and accuracy of sensorimotor reactions. When fatigue improves mood, increases interest and motivation activities. Extends latency and reduces the duration and severity of nystagmus.

Absorption from the gastrointestinal tract - a tall, well into all tissues, and the BBB (in brain tissue found around 0.1% of the administered dose, people young and old - much more). It is metabolized primarily in the liver (80-95%) to pharmacologically inactive metabolites. Approximately 5% is excreted in the urine in unchanged form. Not accumulates.
Application
Asthenic syndrome, anxiety and neurotic states (worry, anxiety, fear), obsessive-compulsive disorder, sleep disorder, psychopathy, premedication before surgery, otogenny labyrinthitis, vestibular disorders infectious, traumatic and vascular genesis, including Meniere's disease, vertigo, alcohol withdrawal syndrome (in the complex therapy), the prevention of motion sickness when kinetoses; children - stuttering, tics, enuresis.
Contraindications
Hypersensitivity.
Restrictions apply
Erosive and ulcerative gastrointestinal damage, pregnancy, lactation.
Pregnancy and breast-feeding
The caution (not enough clinical experience). In experimental studies found no mutagenic, teratogenic and embryotoxic action.
Side effects
Drowsiness, nausea (with the first receptions), allergic reactions, hepatotoxicity (with prolonged high doses - 7-14 g).
Interaction
Enhance and prolong the effect of hypnotic and antiparkinsonian agents, neuroleptics and narcotic analgesics.
Overdose
Symptoms: drowsiness, nausea, vomiting, hepatic steatosis (receiving more than 7 g), eosinophilia, hypotension, renal dysfunction.

The most unusual drug for pharmacological effects - it is a tranquilizer with elements of nootropic activity, it nootrop with elements of anxiolytic action. That Phenibut has muscle relaxant action - it is not, etc. Particularly interesting effects that cause the drug in a mixture of stimulants and drugs, CNS depressants.

When the Soviet Union I was in the medical library read enough volumetric book called "nootropics," if I am not mistaken - VERY long been the case, but if there is "old" in this forum on Nootropics in particular, I ask you to respond about this book - I did then studied the surface, and there were a lot of interesting things. I beg you to give a link to download it! In this book the basic "classic" nootropics (Aminalon, vinpocetine, piracetam, Phenibutum, Pantogamum), describes the differences in the effects of certain medications, and more.

Phenibut is interesting and extremely chemically and medically - is very interesting drug, which is worth special attention.

Action phenibut and its para-chloro-derivative - baclofen, bind, as I have already written to competitive blocking of enzymes, regulating the concentration of GABA as a neurotransmitter in the central nervous system - the underlying mechanisms at most explains the muscle relaxant properties of both drugs (while baclofen being a strong agonist of GABA B receptors expressed exhibits properties of the central muscle relaxant, keeping, however, the properties of a tranquilizer, and some nootropic, Phenibutum something quite different in this respect from baclofen).
Phenibut chemically can be regarded as a derivative of GABA, with the phenyl radical in the beta position, and as a phenethylamine derivative containing beta position carboxymethyl group. It explains how the "bipolarity action, and many other aspects.

If we have the average person with an average weight, health, etc., and if he drink away the course phenibut in moderate doses, you get the following picture - in the first two or three days will be relaxed, sleepy night (not at all), along with rapid reduction of headaches caused stress and the disappearance of fatigue, apathy, against the backdrop of improving the overall mood; on the fourth or fifth day is usually felt energizing effect of the drug, and in the evening is not always possible to sleep (!), at the end of a two-week course will be an active person, easily carrying a stressful situation and in a good mood. This dose range 0.25 g to 2.3 p / d and 0.5 g. overnight. I exaggerate, but I hope that the basic idea don¸s - first goes up to the sedation sleepiness, and then it is replaced by activating and actually neuroprotective effect. And the point here is this: pharm action of phenibut is dose-dependent, that is, if you plan to use the drug as a nootropic, the necessary dosage of about 0.25g three times a day, and literally in the first days of this nootropic, special for phenibut, the effect is noticeable, however, there may be problems with falling asleep - a few days later, the body adapts to the drug, and clearly traced antiastenicheskoe, psycho-energizing, nootropic effect with some blood pressure effect. Note that Phenibut characterized dopamine-positive properties (as derived PEA), and in some cases it can be used in parkinsonism; nootropic and antiastenic action of phenibut at these doses is very pronounced, it has served as IMHO the impetus for the creation of a substituted lactam phenibut - phenotropil that demonstrates Inog effects phenibut in a more expanded form: wink: Often, at the end of the first and the second week of reception phenotropil can observe increased activity and in some cases - insomnia. This is Phenibutum-nootrop, and now we'll see what Phenibutum tranquilizer.

At doses of 0.25 and three times per day at night before 0,75g 0,5 g three times a day and at night 0,5-0,75g formulation exhibits properties quite good tranquilizer weak muscle relaxant properties (phenibut anticonvulsant activity manifested at higher doses and relieving seizures caused by some drugs, but not for epilepsy), but at the same time without muscle relaxation and the deterioration of cognitive functions, and to improve them, which is important. You can see some effects similar to GHB - pronounced anti-hypoxic, relaxing and enhancing libido. Phenibut tranquilizing effect is a distinct dose-dependent, and many doctors and patients is unknown, they often complain about the stimulating effect of the drug. Tranquilizing properties Phenibutum shows a dose 1500-2000 mg or more per day, and in addition, it should be noted that this action quickly develop a tolerance, that is, if the treatment gave positive results in small doses, and then replaced by an activating effect, the dosage during the testimony should be enhanced - if Phenibutum again becomes tranquillizer.

But in Psychiatry and Addiction Phenibutum - very valuable but expensive tool.

Phenibutum - it is a tranquilizer with elements of nootropic activity, and in recent years, due to its pronounced antiastenicheskimi, antihypoxic, anti-oxidant, etc. properties svoysvennymi neuroprotective drugs, it is regarded as nootrop with anxiolytic effects. The drug is taken shortly before the meal three times a day, but the dosage will vary depending on what drug is assigned: a tranquilizer for complex treatment of alcohol withdrawal Phenibutum taken at 0.5 grams before meals thrice daily, followed reception bedtime 0 75 grams of the drug. The course in this case is no more than two or three weeks. Like its a substituted lactam Phenotropil, Phenibutum should be strictly specified time, and under the control of liver function and peripheral blood. What is a "positive effect" in your understanding? On the drug often react as anti-asthenic means with anxiolytic activity when taking the drug for a long time, at doses which pleases, etc. With adequate appointment, and if this necessity ect, doctor may prescribe this drug as an antianxiety drug with nootropic activity course in two weeks. Since the drug is not apt to cause a pronounced euphoria and act differently from the database, of course, "perfect," as people sometimes want healthy, it will not function as well as blood pressure and many other PLC. Here we are talking about the treatment, and if your sluchpe there asthenia, then Phenibutum will provide anti-asthenic action with a trigger action. When the drug is given doctor, the history is taken into account, the previous reaction to various drugs, condition, etc. of today, and on the basis of the received data assigned agent. Phenibut - it's not BAD per day, and its mechanism of action is quite complicated - if there is some pathology, etc., he can do things differently. Healthy people drug is given as an adaptogen, and in smaller doses - whereas in the early days can be tranquilization, and after a couple of days - psycho-energizing effect.

Typically, as a tranquilizer OTC and day, appointed mebicar - a drug that affects many structures, but often "patients", ie people who are looking at the pharmacy for something such, that here gave such effect that they want, do not prefer any mebicar sometimes abused Phenibut, not realizing that even at a dose of 5 grams of the drug does not give effect database.

If the drug is taken as an anti-asthenic means, it is the action had, just like poknige - the early days - a tranquilizing pronounced effect sleepiness sometimes, and then - develop animastenic and nootropic effects, and dose escalation may temporarily give strengthening tranquillisation, but then It acts as psihoenergizator. What YOU want? OTC tranquilizer? Mebicar and Phenibutum - they, but many anxiolytic effects of these drugs can not subjectively marked, although there are.

Phenibutum and Phenotropil - a special PLC? the first is a substituted in the beta position Namco and Phenotropil - its a substituted lactam. These PLC should be used as needed, even if subjectively felt all the processes that occur in the body when taking these drugs: Phenotropil most active at single reception after eating before the upcoming difficult task, and is effective the first three days, then his profile completely changes, It appears marked anorectic effect similar to that of amphetamines and irritating, adversely affecting the psyche, so to use it you need to, respectively, but no increase in dose, or else do not turn Phenotropil to amphetamine, the "perfect" psychostimulant with narcogene potential. Phenibut - means a much safer, but has a very clear tranquilizing effect, and I know people who have abused them, and which need then to treatment. That class of drugs, prop that you can often hear a variety of responses: Hidazepam, Grandaxinum, Mebicar, Phenibutum - partly because tranquilizing effect he expressed quite strongly, and Phenibutum is drunk short two-week course, sometimes longer, and often the attending physician determines the course, and dosage per day, and, in fact, a doctor sees whether there is a need for Phenibut, or another person, or not. I repeat that Phenibutum - is not Sibazon and "perfect" can not be as a tranquilizer, it's nosology indispensable part of medicine in old age and in psychiatry and addiction if used, is in the final stages in combination with more effective drugs - it potentiates PLC action of many, particularly the database and can be used together with them, thus decreasing the dosing regimen, not only often without loss of activity, but along with its increase. This drug is not for nothing that is worth so much, and I would not want it to become again "a tranquilizer on which they sit." I have studied some of the mechanisms of its action and is often seen different reactions to monotherapy - one missing 2 pills a day, while others do not even feel the effect, at a time when there were objectively perceivable change. Some were looking for in tianeptine "cure-all", and we know to what it led to, while others do not spare money for sibutramine in different dosage forms to enhance the mood and eliminate alleged depression (sibutramine - it's SIOZSiN), and this led to the fact that in Russia is now easy with the drug - it is by losing weight.

How to treat Phenibut you? I do not know, I did not see much in the WHOLE time you accept already, and what is the exchange rate on the account, although very often hear the same thing from many: "I started to take as read. The effect has been a good, used a week but suddenly the action not what it became, "when in practice it turns out that quite healthy (or not quite healthy) people accept everything, read what it is for them simply, and took, and blood pressure, and the funds and other and did not say that there is in practice. Then the answer is simple: Your individual response to Phenibutum longer as activating the drug and consult a doctor who needs to know everything, and that will determine what you need to PLC, and whether it is necessary. It's easy! PLC appoint a doctor, based on the examination of the patient.

If there is a hedonic effect, even analginum abuse - there is such a word. Phenibut - it is an expensive drug, so not everything is terrible, as you write - "indiscriminate abuse" No PLC is sold without a prescription. And the reaction of each individual, especially in drug addicts - it Phenibutum - a tranquilizer in the USSR! Later we realized that there is no especially terrible and became Phenibutum nootropic component with a tranquilizing - some really reinforce their action of amphetamine, but it is a unit - the drug can impair the action of both stimulants and opioids, eg. Then, the effect from the drug dose-dependent - if you drink one tablet three times a day - it will first tranquilizer, and will soon stimulate and can cause insomnia, so as a tranquilizer Phenibutum administered with a gradual increase in dose - maximum can be 2 tablets three times a day and three tablets at night. At these doses prevails tranquilizing effect, and against the background of this would be strengthening CNS depressants but strengthen amphetamines, etc. it will not be - only a few have resorted to this method, and drug addicts as "withdrawal" that can take Phenibutum equine doses - then there will be addiction, though weak, but will be - to treat her fairly easily replaced for a while by another PLC and performing adequate psychotherapy. This is not "strongly narcogene preparation", and the list does not even - it's just become extreme now - with no database, drug addicts resort to this tranquilizer, and there are a lot of similarities with GHB, which is now controlled, and less PE than in the database. I am 12 years saw alcoholics, neurotics, and even drug addicts drank Phenibutum in tranquilizing dose, and then gradually reduce the dose, and did without problems. Never seen depending on Phenibut FOR 20 YEARS, but I know that they now have, but not all "sitting" on it - a lot of "pure minds" them, because he is the most quiet of all nootropics, though as nootrop not very active - I remind you that its a substituted lactam Phenotropil (carphedon) - it is something similar to the "progenitor" Phenibut, means, but is much more powerful in terms of simulation and is an adaptogen-psycho-energizer instead of a nootropic, as they say - nootropnye elements he expressed in early action, and after a while there comes the excitement and other PE - nobody did not say that it is a drug carphedon. And now he is in the world already " Phenotropil " began. Upon graduation reception Phenotropil nootropic effects disappear very quickly, and he carphedon - a powerful dopamine-positive drug, and even moved in his time as the blood pressure, but many PE not let it happen, and it is the replacement meclofenoxate etc. Stimulants-nootropics mixed type.

Phenibut same - this is a very old medicine, and he devoted a lot of work, and the ICD-10, it is capable of much. It is not narcogene drug - it will be abused in some cases as an effective tranquilizer, and an excellent alternative to the DB. Doses tranquilizer for phenibut lie within 1500mg, 2000mg. At therapeutic doses, it is indispensable medicine and one of the nootropics that does not give hyperstimulation if the right dose is chosen. A misuse - is pure medicine craze - like fluoxetine and other pharmaceutical preparations "sit" many fans to be far from reality. It has always been and always find your. A more alarming fact depending on Prozac, and paroxetine - there's really scary. Phenibut, many doctors do not know how to use and prescribe the wrong dose very often, not having studied the drug, and in the hands of a drug addict any medication would become abused, but there is more good than harm, but spoils the digestive tract, liver and blood - do not know "Phenibutors" , they do not know what the drug as a tranquilizer very active and had once been used for sedation, but most addicts just take Phenibutum as "calm nootrop". With long-term consumption of high doses and abrupt cessation quickly manifest fatigue, bad mood, etc. effects - if you reduce the dose gradually, it will be no problems, but then again - this is a very rare case and narcogene Phenibutum drug is not, can not be said about some of the blood pressure.

Alas, Phenotropil aka carphedon - banned worldwide doping - it's not nootrop and adaptogen-neurometabolic stimulant, has a mild narcotic effect. Once the connection has been received, "nootropic" effect is greater in the stimulating effect during the first days of taking the drug, and therefore the powerful drug of its kind was embedded in military medicine and space exploration to people in difficult conditions to adapt to stress more quickly. But even there he did not catch on, and "down to earth", becoming a fixture in addicts who use it to "restore the brain after drugs" - the first few days is very strongly felt euphoria, stimulation and elements of nootropic activity, but after a week there are PE , which beats any real nootrop - anorexia, aggression, insomnia, dysphoria, and mental disorders - a constant companions "phenotropil course", so it is used as doping during exams, and as a means of facilitating the "comedown" from all kinds of surfactant. Nootropic effects are in the early days of admission, and soon turned into PE and carphedon addicts nicknamed "Animalin" as those who drank it for a long time (30 or more pills)), were shocked by the condition that occurs when taking carphedon. "Phenotropil" is replaced Acephenam etc. psychostimulants with elements of nootropic activity. For the drug addicts will give all the money when you need to recover quickly after taking a heavy, genuine drugs.