Gamma-aminobutyric acid: instructions for use, analogues, cost, patient reviews. Gamma-aminobutyric acid - instructions for use

More and more information is emerging about the neurotransmitter, which has the complex but proud name of gamma-aminobutyric acid - drugs with this substance are recommended as a sedative. How does this acid actually work, what effect do drugs with GABA have on the body?

GABA (GABA, gamma-aminobutyric acid) is a neurotransmitter that blocks impulses between nerve cells in the brain. Low GABA levels may manifest as:

• Worsening of mood and appearance of signs of anxiety disorder;
• Epilepsy attacks;
• Chronic headaches.

As a result of the studies, it was revealed that increasing the level of gamma-aminobutyric acid can improve mood or have a calming, relaxing effect on the nervous system.

In addition, the neurotransmitter GABA, produced by the body, affects the regulation of muscle tone and the production of hormones necessary for building muscle cells. If you are looking for a supplement that helps increase muscle strength, then you might be interested in GABA supplements. They are popular among weightlifters because of their ability to burn fat and improve athletic performance.

Gamma-aminobutyric acid: when do drugs not work?

• Improved mood
• Reducing anxiety
• Reduce symptoms of depression
• Improved sleep quality
• Relieving PMS symptoms

Although the neurotransmitter GABA (produced by the body) has a great influence on brain function, taking it in the form of dietary supplements may not produce results. Research shows that drugs with gamma-aminobutyric acid do not have the expected effect on brain function, so they should not be used for these purposes.

Let's take a closer look at why this happens and what the effect of gamma-aminobutyric acid actually is when taken additionally in the form of dietary supplements.

How does this not work?

As a result of the studies, it was found that taking GABA drugs to reduce anxiety and depression is not effective. This is due to the blood-brain barrier, which is a system that separates circulating blood from brain tissue. In order for any of the nutrients to get into the brain cells, it must cross the barrier. Only certain types of connections can do this.

If aminobutyric acid is taken in the form of drugs, then the active substances will be absorbed in the intestines and transported to the brain in the blood, but will not be able to cross the blood-brain barrier.

In order for GABA to have an effect on brain function, it must be synthesized by the brain cells themselves from their predecessors. That is, taking a drug with gamma-aminobutyric acid cannot increase the level of the neurotransmitter in the brain.

How to Increase Gamma-Aminobutyric Acid Levels

Scientists have found a way to increase the level of GABA in the human body with the help of drugs. Dietary supplements are intended to reduce anxiety and depression, but do not contain gamma-aminobutyric acid.

Nootropics have been found, precursors of GABA, which supply the human body with the components necessary for the synthesis of the neurotransmitter. An excellent natural substance that stimulates the production of gamma-aminobutyric acid is L-Theanine. This compound is widely known and found in large quantities in green tea.

Phenibut is also a precursor to GABA. It, like L-Theanine, is able to cross the blood-brain barrier. The active substances stimulate brain receptors to produce GABA.

Research has proven that picamilon, which contains GABA and niacin, is able to penetrate the blood-brain barrier. After taking this drug, the activation of brain receptors increases.

Should I buy drugs with GABA as a sedative?

Despite the categorical conclusions of scientists that taking GABA does not reduce attacks of anxiety and depression, many people continue to take these drugs. On the Internet you can find a large number of reviews of real people who felt relaxation and decreased anxiety after taking medications with gamma-aminobutyric acid.

This can be explained both by the placebo effect and by the dosage and composition of the drugs taken. There is information that large doses of drugs with gamma-aminobutyric acid can still slightly increase the level of GABA in the body.

Research on the effect of aminobutyric acid on the human body is still ongoing. It is not fully understood how the dosage of the substance taken affects brain function. Not enough experiments have been conducted to determine the specific conditions that affect the body's absorption of GABA.

Everyone must decide for themselves whether to buy drugs with gamma-aminobutyric acid as a sedative. If you purchase dietary supplements as prescribed by a doctor, then there should be no questions. If you are going (according to the old Russian tradition) to self-medicate, then you should carefully approach the choice of drugs.

When do GABA medications work?

So why are supplements that contain GABA but do not provide the expected nootropic effects so popular? The answer is simple - preparations with gamma-aminobutyric acid are considered strong natural fat burners.

The effect of gamma-aminobutyric acid on weight loss

GABA supports the production of hormones that help build muscle mass. In other words, the effect of taking drugs with gamma-aminobutyric acid is to speed up metabolism (additional muscle mass requires more calories). If you are just starting to work on building your body or are looking for drugs to help you lose weight, then GABA is your choice.

Can you get GABA from foods?

It is impossible to obtain gamma-aminobutyric acid from food. However, various foods contain substances such as flavonoids, which act to increase GABA levels in the brain. These are accessible and known to everyone:

• Fruits;
• Vegetables;
• Red wine.

Side effects from GABA

Side effects may include the following:

• excessive relaxation; it is better not to drive in this state.
• short-term changes in heart rate and breathing intensity, they usually disappear quickly.
• Avoid taking GABA medications together with alcohol and drugs. This can lead to serious problems.

GABA: list of working drugs

When choosing drugs with GABA to obtain a nootropic effect, be sure to study the composition. IHerb has an excellent supplement that contains both GABA and L-Theanine. Those. By purchasing this particular dietary supplement, you are guaranteed to get the expected nootropic effect - reduced anxiety, reduced symptoms of depression, improved mood.

You can buy gamma-aminobutyric acid with L-Theanine at the following link:

• Now Foods, GABA, Chewable

But here is a drug with a rich composition (GABA, L-Theanine, valerian, a lot of microelements and vitamins.):

• Now Foods, Nervous & Mood Support Vitamins, 90 Vegetarian Capsules.

The dietary supplement will also be effective in calming the nervous system.

To lose weight and build a body, you can choose a drug containing only GABA, for example, a dietary supplement at the link:

• Now Foods, GABA, Powder, 6 oz (170 g)

A large selection of drugs with gamma-aminobutyric acid can be found on iHerb by clicking on the link. There you can choose dietary supplements with a suitable composition, both soothing and helping for weight loss.

How to take gamma-aminobutyric acid

The recommended dose range of GABA for weight loss is 2 to 4 g per day. This amount can be taken all at once (less effective) or in portions throughout the day. If GABA is used solely for fat burning, then the best time to take supplements is 2 hours before bed. Do not take gamma-aminobutyric acid supplements with protein foods - it may affect digestion.

Are you familiar with gamma-aminobutyric acid - which GABA preparations do you prefer?

Gamma-aminobutyric acid (GABA)- the main inhibitory transmitter in the human nervous system. But only those of us who have already developed it. And to provide us with truly Olympic peace of mind, she is sometimes helped by a motley group of very well-known substances. We'll take a closer look at GABA and find out that this molecule is not as simple as it seems at first glance.

Resting neurotransmitter

Gamma-aminobutyric acid(GABA; γ-aminobutyric acid, GABA) is synthesized in the brain from glutamic acid, another neurotransmitter, by decarboxylation (removing the carboxyl group from the main chain) (Fig. 1). According to the chemical classification, GABA is an amino acid, but not the usual one, that is, used for the synthesis of protein molecules, an α-amino acid, where the amino group is attached to the first carbon atom in the chain. In GABA, the amino group is bonded to the third atom from the carboxyl group (in glutamate it was the first atom before decarboxylation).

GABA is synthesized directly in the brain and binds to two types of receptors on the surface of neurons - GABA receptors types A and B. Type A receptors were previously divided into receptor types and (found mainly in the retina), but were subsequently united due to their common action. This type of receptor is ionotropic: when GABA binds to them, an ion channel opens in the membrane of the nerve cell, and chloride ions rush into the cell, reducing its reactivity. The nerve cell membrane has resting potential. There are fewer charged ions inside the cell than outside, and this creates a charge difference. On the outside, the superiority is created by chlorine, calcium and sodium, while on the inside, potassium ions and a number of negatively charged organic molecules predominate. In a theoretical sense, membrane potential has two paths: increasing (called depolarization) and decrease ( hyperpolarization) (Fig. 2). At rest, the membrane potential is approximately −70...−90 mV (millivolts), and when the nervous system operates, a “tug of war” begins between two forces - those that excite the cell (depolarizing the membrane) and those that inhibit it (hyperpolarizing).

Figure 2. Scheme of the occurrence of an action potential on the cell membrane. It is necessary to change the content of ions inside and outside the cell of such a force that the value of the charge on the membrane changes and reaches a certain threshold. If this happens, the membrane continues to depolarize further, the neuron becomes excited and transmits a signal to other cells. Overshoot(inversion) - the period when the membrane potential is positive. This is followed by a repolarization phase, and the membrane charge returns to its previous values.

To understand how this works, you need to consider two points. The first is that several oppositely directed forces can act on one neuron at the same time: for example, five excitatory and three inhibitory neurons converge on one cell in this part of the nervous system. At the same time, they can affect the dendrite of this neuron and the axon in the presynaptic part. The second point is that the nerve cell experiencing these influences will work according to the “all or nothing” principle. She cannot send a signal and not send it at the same time. All effects of signals arriving at the cell are summed up, and if the resulting changes in membrane potential exceed a certain value (called excitation threshold), then the signal will be transmitted to another cell through the synapse. If the threshold value is not reached, then sorry - try again, guys. All this is reminiscent of Krylov’s fable about a swan, a crayfish and a pike: everyone is pulling in their own direction, but it is not very clear what will come of it.

So, the GABA molecule has bound to the ion channel receptor. The ion channel, which has a rather complex structure (Fig. 3), opens and begins to let negatively charged chlorine ions into the cell. Under the influence of these ions, the membrane hyperpolarizes, and the cell becomes less susceptible to the excitatory signals of other neurons. This is the first and, perhaps, main function of GABA - inhibition of nerve cell activity in the nervous system.

Figure 3. Ionotropic GABA receptor. The GABA A receptor is a heteropentamer: it consists of 5 protein subunits, which, depending on the homology of amino acid sequences, can belong to eight different families (more often - to α, β, γ; members of the ρ-family homo-oligomerize - the resulting GABA A -ρ receptors, “former » GABA C). This determines the diversity of GABA A receptors. A - Receptor structure diagram. Left: Each of the subunits at the long globular N-terminus, which extends to the surface of the neuron, has a characteristic cysteine ​​loop structure and binding sites for GABA and other ligands. This is followed by 4 α-helical transmembrane domains (between the last of them there is a large cytoplasmic loop responsible for binding to the cytoskeleton and “internal” modulators) and a short C-terminus. On right: Five subunits form an ion channel, oriented by the second transmembrane domain ( orange cylinder) to each other. This is the quaternary structure of the receptor. When binding to two GABA molecules, the receptor changes conformation, opening a pore for anion transport. b - Micrograph of the GABA receptor in the pig brain.

Another aspect of the inhibitory effect of GABA is its effect on emotional processes - in particular anxiety. Anxiety is a very broad concept. It contains both completely healthy human reactions to stressful influences (an exam, a dark alley, a declaration of love) and pathological conditions (anxiety disorders in the medical sense of the word). Based on the provisions of modern psychiatric science, we can say that there is normal anxiety And anxiety is like a disease. Anxiety becomes a disease when it interferes with your daily or professional life, blocking you from making any decisions - even the most necessary ones.

The part of the brain that is responsible for emotional reactions is amygdala- a collection of nerve cells in the depths of our head. It is one of the most ancient and important parts of the nervous system in animals. The amygdala's special specialty is negative emotions—we feel angry, angry, afraid, and anxious through the amygdala. GABA allows the brain to reduce the intensity of these experiences.

Nerve pill

Medicines that are effective in treating anxiety and seizures must bind to the GABA receptor. They are not direct receptor stimulators, i.e. do not bind to the same part of the molecule as GABA. Their role is that they increase the sensitivity of the ion channel to GABA, slightly changing its spatial organization. Such chemicals are called allosteric modulators. Allosteric modulators of GABA receptors include ethanol, benzodiazepines, and barbiturates.

Alcohol is known for its relaxing and anti-anxiety effects. Solutions ethyl alcohol in various concentrations have long been widely used by the population of the Earth to calm the nerves. Ethanol gives people relaxation by binding to the GABA receptor and facilitating its further interaction with the neurotransmitter. It happens that people overestimate their ability to drink alcohol, and this leads to a gradual loss of control over their actions and an increase in inhibition. Alcoholic hyper-relaxation occurs, which, with continued use, can lead to an alcoholic coma - the inhibitory effect of alcohol on the central nervous system is so strong. Potentially, alcohol could be used during surgical operations as an anesthetic (previously, in critical situations - for example, at the front - this was done - Ed.), but the range of concentrations where it turns off pain sensitivity and does not yet “turn off” a person completely is too small.

Figure 7. Veronal box from the company Bayer(in the top left corner).

This and other groups of drugs used in the complex treatment of not anxiety, but depression are described in the “juicy” review “ A Brief History of Antidepressants": with all the ins and outs of this condition, with theories / hypotheses and doubts about them. - Ed.

Figure 8. GABA A receptor and drug binding sites. The most common combination of subunits in the central nervous system (about 40% of GABA A receptors) is two α1, two β2 and one γ2s, located around the chloride pore ( view from above). GABA site (on the surface, junction α and β) - the place where GABA attaches to the receptor; BDZ site (on the surface, junction of α and γ) is the binding site for benzodiazepines, ETF site (on β) is etifoxine, NS site (in the channel) is neurosteroids. The binding sites for barbiturates and ethanol are presumably located deep in the channel (on the transmembrane domains). In the first case, the β subunit probably plays the main role; various subunits, including ρ and δ, interact with ethanol, but their sensitivity differs.

The reason for the dislike of benzodiazepines lies in their side effects, of which there are quite a few, and not all of them are taken into account by official structures. First, benzodiazepines, like all GABAergic drugs, are addictive. Secondly, benzodiazepines impair a person’s memory. The use of drugs in this group enhances the inhibitory effect of GABA on the cells of the hippocampus, the memory center. This can lead to difficulties in remembering new information, which is observed when taking benzodiazepines, especially in older people.

GABA, despite its narrow “specialty,” is an amazing neurotransmitter. In the developing brain, γ-aminobutyric acid excites nerve cells, and in the developed brain, on the contrary, reduces their activity. It is responsible for a feeling of calm, and drugs that activate its receptors give doctors a lot of reasons for concern. This is how gamma-aminobutyric acid appeared before us - a simple molecule responsible for ensuring that our brains do not “burn out.”

? Addiction. 106 , 2086–2109;

Gross formula

C4H9NO2

Pharmacological group of the substance Gamma-aminobutyric acid

Nosological classification (ICD-10)

CAS code

56-12-2

Characteristics of the substance Gamma-aminobutyric acid

White crystalline powder with a slightly bitter taste and specific odor. Easily soluble in water, very slightly soluble in alcohol; pH of a 5% aqueous solution is 6.5-7.5.

Pharmacology

pharmachologic effect- nootropic, stimulating metabolism in the central nervous system.

It is the main mediator involved in the processes of central inhibition. Improves blood supply to the brain, activates energy processes, increases the respiratory activity of tissues, improves glucose utilization and removal of toxic metabolic products. Interacts with specific GABAergic receptors of types A and B. Improves the dynamics of nervous processes in the brain, increases the productivity of thinking, improves memory, and has a moderate psychostimulating, antihypoxic and anticonvulsant effect.

Helps restore speech and motor functions after cerebrovascular accident. It has a moderate hypotensive effect, reduces initially elevated blood pressure and the severity of symptoms caused by hypertension (dizziness, insomnia), and slightly reduces heart rate. In patients with diabetes mellitus, it reduces blood glucose levels; with normal glycemia, it often causes hyperglycemia due to glycogenolysis.

Plasma concentrations reach a maximum after 60 minutes and then decrease rapidly; after 24 hours it is not detected in blood plasma. According to experimental data, it penetrates the BBB poorly. Low toxic.

Application of the substance Gamma-aminobutyric acid

Damage to cerebral vessels (atherosclerosis, hypertension, etc.), cerebrovascular insufficiency and discirculatory encephalopathy, impaired memory, attention, speech, dizziness, headache, consequences of stroke and traumatic brain injury, alcoholic encephalopathy, alcoholic polyneuritis, mental retardation in children , dementia, cerebral palsy, endogenous depression with a predominance of astheno-hypochondriacal phenomena and difficulty in mental activity, motion sickness symptom complex (sea and air sickness).

Contraindications

Hypersensitivity, children's age (up to 1 year), acute renal failure, pregnancy (1st trimester).

It is well known that the most important component of our food is proteins. Although carbohydrates are very important for providing the body with energy, they can be obtained from both fats and amino acids. Fats aren't a problem either. But proteins - muscle proteins, connective tissue proteins, and, most importantly, enzymes - are obtained only from amino acids. Of these, 14 can be synthesized in the body, and 8, like vitamins, must enter the human body from food. If during hunger the body, having depleted its reserves of fat and carbohydrates, turns to proteins to maintain energy processes - disaster. In children, there is a lag in physical and mental development, in adults - hunger edema, a decrease in temperature and a weakening of all types of vital activity.

A person needs only 120 g of proteins per day, but there are not enough of them in plant foods, and plant proteins are poorly absorbed. In my opinion, meat, fish and dairy products should definitely be included in the diet. If the food lacks certain amino acids (even if they are not essential), they can be taken in the form of medications, such as glutamic acid and histidine. Methionine is especially often used, which is absolutely necessary for degenerative processes in the liver and heart, and glycine as a sedative. (But we'll talk about that later.)

Gamma-aminobutyric acid

For a long time it remained unclear how a decrease in overall brain activity is achieved - for example, during sleep. Scientists guessed that there must be a substance, perhaps a transmitter of nerve impulses - a mediator, which would ensure a decrease in the activity of the nervous system not in individual cells or even in the nerve nuclei, but in the brain in general. And such a universal inhibitory mediator was discovered. It turned out to be gamma-aminobutyric acid, which we will henceforth call for short - GABA.

GABA was first discovered in the brain by Yu. Roberts and his colleagues (and independently by Jörg Avapara) in 1950. Since the butyric acid molecule has a chain of three carbon atoms (and the fourth in the COO group), according to systematic nomenclature the acid should be called aminobutanoic acid, but no one calls acetic acid ethanoic acid (Fig. 1).

The building blocks of proteins are alpha amino acids: those in which the amino group is attached to a carbon atom located next to the carboxy group. What can gamma amino acid be useful for?

It is known that when the skin (as well as any other sensory organs) is irritated, electrical potentials called primary responses arise in the corresponding areas of the cerebral cortex. In 1963, the English scientist K. Krnevich brought a pipette filled with a very weak GABA solution to one of the neurons reproducing primary responses. He was the first to establish that the amino acid flowing from the pipette was capable of completely suppressing the occurrence of impulses in the sensitive cells of the cerebral cortex. Japanese researchers made it even simpler: they brought a light electrode to the surface of the brain, and placed a filter paper moistened with a GABA solution “on top” of it. The advantage of such an experiment was not only its simplicity, but also the fact that the amplitude of the recorded potentials, formed not by one, but by several neurons at once, approximately reflects the strength of the impact. In this case, of course, a higher concentration of the substance was required, but the effect turned out to be the same - the potentials were suppressed. Later, similar experiments were reproduced by the author of this article (Fig. 2).

It was further found that GABA can inhibit not only evoked, but also spontaneously occurring potentials, both in the cortex and in other areas of the brain. In this case, GABA is synthesized and released precisely in those brain nuclei that are responsible for its inhibition. It is believed that GABA mediates the transmission of inhibitory impulses in approximately 30–50% of nerve contacts. How does she do it?

Contacts of nerve fibers with cells - synapses functioning with the participation of GABA - are not fundamentally different from others. GABA is synthesized in the cytoplasm of the neuron and, with the arrival of an impulse, is released into the synaptic cleft between the endings of the nerves and the adjacent portion of the neuron sheath (Fig. 3). Specialized receptor proteins (from the Latin recipe - take) that interact with GABA have also been discovered. As a result of this interaction, channels open in the membrane of the receiving neuron, allowing negatively charged chlorine ions, which are contained in excess in the intercellular fluid, to enter the cell. The penetration of chlorine causes a state of hyperpolarization in the cell, that is, inhibition (recall that the transfer of excitation occurs due to the opposite process: depolarization of the neuron membrane). It has now been established that GABA receptors are also found in blood vessels, especially in the brain.

Scientists have compiled maps that indicate exactly where GABA acts as an inhibitory transmitter and how great its significance is in each area. Although the concentration of this acid varies in different parts of the brain, it can be found almost everywhere. We calculated the approximate total number of its molecules - and were surprised. It turned out that the brain contains GABA in much larger quantities than required for mediator functions. Why, one might ask, so much?

It was natural to assume that GABA performs some other functions in the brain. And in fact, it turned out to be an obligatory participant in many exchange processes. It affects the transport and utilization of glucose, the respiration of cells, the formation of energy reserves in them, increases the resistance of cells and the brain as a whole to oxygen starvation, and activates protein synthesis. The variety of physiological and biochemical functions performed by GABA, as well as data on the disruption of its formation in some psychopathological and neurological disorders - all this spoke of its enormous importance. Pharmacologists could not pass by such an amazing molecule.

In the search for new drugs, scientists remembered that plants, millions of years ago, learned to synthesize compounds that successfully block the effects of mediators. In the case of GABA, these are the alkaloids picrotoxin (found in the seeds of tree vines of the genus Anamirta, which grow in tropical Asian countries - Indonesia, India, New Guinea, the Moluccas, as well as in various types of astragalus) and bicuculline (isolated from the leaves of Dicentre cucullaria of the fumaria family ). They tried to use both of these substances to activate the brain, but they turned out to be too dangerous, since even in negligible doses they caused severe convulsions. (The natives once prepared poison from anamirtha for “chemical” fishing and for arrows.) Now, to excite the respiratory center, a synthetic drug bimegride is used, which also blocks the effects of GABA, but more selectively and not so actively.

The first medicine that activated GABA receptors was this acid itself in its pure form. Her drug called “gammalon” was developed in Japan, and later exactly the same domestic product appeared, called “aminalon”. Despite the fact that both drugs have been used for quite some time, their therapeutic effects remain unclear. The fact is that due to low solubility in fats, GABA almost does not enter the brain tissue from the blood - however, its central effects are beyond doubt and are well studied. The explanation of the valuable properties of gammalon-aminalone by the ability of GABA to dilate blood vessels seems unsatisfactory.

Pharmacologists know that in order to increase the permeability of substances into the brain through the blood-brain barrier, which separates the blood (essentially an aqueous solution) from the lipid-rich brain cells, they need to “suspend” a highly fat-soluble radical. Leningrad pharmacologists, including my friend Professor I.P. Lapin, proposed introducing a phenyl radical into the GABA molecule, which turned it into the drug phenibut, which easily overcomes the barrier - and has a pronounced inhibitory effect (Fig. 1)! Today, phenibut is a common daytime tranquilizer, and, what is especially valuable, it does not interfere with driving.

Over time, it was established that in brain tissue GABA loses its amino group, which is replaced by hydroxyl. This substance is called gamma-hydroxybutyric acid. If injected directly into the blood, it not only penetrates the blood-brain barrier, but also has such a strong inhibitory effect on the brain that its sodium salt, sodium hydroxybutyrate, can be used as a means for general anesthesia (more precisely, to turn off consciousness) during operations. Think about it: a person produces a substance in his brain that can cause a state of anesthesia! How can one not remember about operations under hypnosis?

The second way to improve the penetration of a drug molecule into brain tissue is to attach some naturally occurring substance, such as a vitamin, to it. In particular, the drug picamilon is obtained by combining nicotinic acid, also known as PP, with GABA. As expected, picamilon dilates blood vessels in the brain and has a calming effect in cases of anxiety, fear, increased irritability, and also increases resistance to physical and mental stress.

The creation of GABA-like drugs and the study of their effects made it possible to talk about the existence of two main functions of GABA - mediator and metabolic. The mediator function is associated with the participation of GABA in regulating the level of wakefulness, motor activity, vascular tone, maintaining a high seizure threshold and partly improving memory and thinking. Metabolic function is the provision of energy to the brain, resistance to oxygen starvation and other harmful influences.

Nootropics

In 1963, the Belgian company UCB obtained a compound that was a gamma-aminobutyric acid coiled into a ring with some additional radicals. When studying this compound, Professor K. Giurji and his collaborators found that it actively improves memory and facilitates the learning process, that is, it affects the higher intellectual functions of the brain. Since in Greek thinking and reason are noos, and affinity is tropos, the new medicine was called “nootropil”. And in 1972 the term “nootropic drugs” appeared.

According to WHO experts, nootropic drugs activate the ability to learn, improve memory and mental activity, and also increase the brain’s resistance to aggressive influences.

In Russia, nootropil is produced under the name “piracetam”, and around the world under more than 30 names - further evidence of its extraordinary popularity. Indications for its use are memory impairment, decreased concentration, mood changes, behavioral and thinking disorders in vascular diseases, injuries and sclerosis of the brain, as well as mental disorders in chronic alcoholism. The drug is well tolerated, but in some people it causes unexpected reactions: excitement or, conversely, drowsiness, sometimes dizziness, and sometimes increased sexuality.

Today, the group of nootropic drugs does not have strictly defined boundaries. In addition to the already mentioned aminalon, phenibut and picamilon, it also includes deonol (nooclerin), idebenone, meclofenoxate, nicotinoyl-GABA and pantogam. All these drugs are metabolic and, to some extent, antioxidant. Conventionally, nootropic drugs include drugs that have a pronounced ability to cause dilation of cerebral blood vessels: vinpocetine (Cavinton), complamine, trental, cinnarizine, etc. Caffeine and some vitamins can also be considered nootropic: B6, B15, BC, and B12.

If we consider the nootropic effect as such, we can point out that it is based on three characteristic properties (which are expressed to varying degrees in different drugs): firstly, they restore the balance between excitatory and inhibitory processes in the brain, secondly, they activate metabolism and energy processes in nerve cells, thirdly, increase the endurance of neurons during oxygen starvation and membrane toxic effects.

In recent years, the idea of ​​nootropic drugs has changed somewhat. It is expected that the next generation of drugs in this group will not only activate higher integrative functions of the brain, but also restore memory and mental processes, reduce deficits arising from various types of damage to the nervous system and increase the body's resistance. These funds will transform the life of mankind, relieving them of the consequences of brain diseases and ensuring active aging. And perhaps they will allow us to treat congenital or acquired dementia.

GABA receptors have a very interesting feature: they are surrounded by other receptors that also regulate the process of inhibition, both through GABA receptors and independently. Among these “companions,” the receptors for barbiturates, alcohol and, most importantly, benzodiazepines are today some of the most common and valuable drugs with tranquilizer, muscle relaxant, ataractic, anticonvulsant and hypnotic effects. They will have to devote a separate section.

Benzodiazepines are the main tranquilizers

The word “bedlam”, meaning “total disorder,” comes from the name of the largest 14th-century psychiatric hospital in London. Something completely chaotic was really going on there: patients with various forms of psychosis were kept in common rooms. Some of them behaved so violently that they became dangerous to others. Then they were put in a special chair, like an electric chair, to which not only the arms and legs, but also the head of the unfortunate person were tied. The patient, unsuccessfully trying to break free from his bonds, gradually became tired and calmed down, calmed down. Such chairs were called tranquilizers (from the Latin tranquillo - I calm). This is where this now widespread term comes from.

Currently, tranquilizers are used to treat neuroses rather than psychoses - these are drugs from the arsenal of neuropathologists rather than psychiatrists. The most common causes of neuroses are loss of a sense of security and confidence in the future. There is an opinion that neurosis is “no big deal,” that everyone has neuroses, but this “not scary” disease is sometimes followed by depression and suicide.

Tranquilizers replaced sedatives, which were given to people who could not find a place for themselves from excitement, restlessness or anxiety. Unfortunately, they could not relieve anxiety and fear, but they allowed us to somehow calm down, sit down and relax (hence the name: sedere - in Latin “to sit down”). The favorite sedatives were bromine and barbiturates, which caused total inhibition in the brain, which, of course, did not restore health and were far from harmless. Medicinal herbs act in a similar way, only weaker: valerian, peony and passionflower.

In the early 60s, the first benzodiazepine appeared - Librium (Elenium), which immediately interested doctors of all specialties. Particularly attractive were its central muscle relaxant (relaxing skeletal muscle) and anticonvulsant activities. Currently, there are many benzodiazepines. Anti-anxiety tranquilizers include elenium (in the Russian version chlozepid), sibazon (diazepam, relanium, seduxen), nozepam (tazepam) and phenazepam, which have a pronounced anxiolytic (anti-anxiety, from anxius - anxious, fear-ridden) and sedative effect. Benzodiazepines without sedative-hypnotic effects are called daytime tranquilizers. These include mezapam (aka rudatel).

All of these drugs are well tolerated, but many of them have side effects described: headache, drowsiness, impaired potency, decreased reaction speed, the ability to enhance the effect of alcohol, causing pathological intoxication with loss of consciousness. Phenazepam is especially dangerous in this regard, the effect of which can last from one to four days. With long-term use, addiction occurs, less often addiction, worsening mood, a person begins to take new drugs from this group... In short, it is better to start treating insomnia not with phenazepam, but to take a more difficult route - for example, reduce coffee consumption in the afternoon and brew it before bedtime herbal tea: what if you don’t need a pill?

Now Russia is purchasing from abroad a relatively new drug, gidazepam, the tranquilizer effect of which is combined with an activating effect. It is also effective in treating migraines. Alprozalam is interesting for its antidepressant effect. In my opinion, these drugs should be in special demand, but this is not the case. Probably because their names do not appear on colorful posters and are not repeated in advertising videos.

Glycine as a mild tranquilizer

The second nonessential inhibitory amino acid, glycine, has had a quiet but well-deserved success, even though it is only an aminoacetic acid. There is little of it in brain tissue, but this small amount is absolutely necessary. Being an inhibitory transmitter, glycine prevents the spread of an impulse arriving along the sensitive dorsal roots of the spinal cord to its other half and other segments. Natural antagonists of glycine that are unsurpassed in activity and bind to its receptors are tetanus toxin and the alkaloid strychnine, contained in the emetic nuts Nux vomica, also known as the fruits of St. Ignace. (Strychnine is a well-known poison, and emetic nuts are one of the most favorite medicines among homeopaths.) If the action of glycine is blocked, then the slightest irritation causes a tonic contraction of the muscles of the entire body, which takes on the opisthotonus position typical of strychnine or tetanus poisoning: arching with support on back of the head and heels. In modern scientific medicine, strychnine is rarely used. But glycine is gaining more and more popularity

The clinic has confirmed that (when used sublingually) not only enhances the effect of anticonvulsants, but also accelerates sleep, has an antioxidant, anti-stress, tranquilizing and nootropic effect, blocking the pituitary-adrenal system.

According to clinical data, glycine suppresses irritability and makes behavior more reasonable. At the same time, it is similar to tranquilizers only in its sedative effect, and in all other respects it is the opposite of them. Thus, it does not have a muscle relaxant effect, weakens the effect of alcohol, does not cause addiction, increases the speed of reactions, enhances mental performance, and with increasing dose its effect decreases. Glycine not only does not interfere with driving, but is recommended for drivers!

Let's face it, you can't always trust a clinic. But there is also very authoritative experimental data in favor of the fact that in a model of brain hypoxia with the occurrence of a heart attack, glycine prevents it more effectively than piracetam. At the same time, the turnover of GABA increases, the content of the main brain mediators increases or normalizes in many of its parts, especially in the area of ​​ischemia. The journal Human Physiology (2001) reports that after three weeks of taking glycine twice a day, an increase in the speed of thought processes was recorded.

Today, indications for the use of glycine include stressful conditions, psycho-emotional tension, increased excitability, emotional lability, neuroses, vegetative-vascular dystonia, consequences of traumatic brain injury, encephalopathy, including alcoholic, sleep disorders... A real miracle is the effect of an ordinary amino acid that we consume with food and produced in our own body. Perhaps it is precisely such medicines that will open the path to health and longevity for people.

“Chemistry and life - XXI century”

Greetings to all lovers of healthy sports and physical development. Today I will touch on the topic of sports supplements, or more specifically, GABA (more commonly known as GABA). In the sports nutrition industry, there are a lot of additives that are of little use and even ineffective, which are imposed by powerful marketing. But gamma-aminobutyric acid is a pleasant exception. It's not just a component for muscle growth, weight loss or cognitive enhancement - it's a natural substance. It will improve both athletic performance and overall health.

Let me start with the fact that GABA, or Gamma Aminobutyric Acid, to be more precise, is not a new “revolutionary drug” suddenly discovered for you by sports nutrition manufacturers. The substance has been studied for decades, and breakthrough studies showing its effectiveness were carried out back in the 2000s. That is, at the moment GABA has a huge evidence base, which is supported by dozens of authoritative studies.

What kind of miracle is gamma-aminobutyric acid, and why has it been so actively used in most sports disciplines? Its structure is aminobutyric acid, the most important neurotransmitter in the brain. GABA inhibits the transmission of neural impulses between nerve cells in the brain.

At first glance it sounds scary, but in fact this is a real medicine for the nervous system and brain, which allows you to maintain its health. Essentially, it is a fuse that protects the brain and central nervous system from overexcitation, exhaustion and a number of serious diseases. It has been proven that GABA deficiency can lead to:

• Epilepsy.
• Depression.
• Insomnia.
• Sudden mood swings.
• Chronic migraines.
• Feelings of anxiety and other mental disorders.

GABA also regulates sleep and the state of wakefulness/rest, and is involved in regulating energy processes in the brain.

Description and brief history of appearance

In the body, GABU produces glutamic acid, which is its opposite. The process is carried out thanks to the enzyme glutamate decarboxylase. Glutamic acid, unlike GABA, is responsible for arousal.

The first studies that identified gamma-aminobutyric acid were carried out back in 1954-56. Then only its presence in the human central nervous system was determined. It was not until 1963 that the synthesis of GABA was completed. By the end of the decade, scientists had created the first amino acid-based supplement, the use of which gave positive results. In Russia it appeared a little later and was called “Aminalon”.

The main problem with GABA is that the substance does not penetrate the blood-brain barrier well. As a result, high dosages of gamma-aminobutyric acid were needed to obtain the effect, which impaired the body's tolerance of the substance and made GABA production too expensive. It wasn't until the 2000s that scientists were able to improve the GABA molecule by combining it with vitamins B5 and B6, as well as phenyl radicals. This allowed GABA to cross the blood-brain barrier much more efficiently.

There is another route used in modern GABA preparations. They include substances that easily enter the brain and there, under the influence of enzymes, are converted into GABA. Since then, supplements and medications have become truly effective and have become actively used both in sports and in medicine.

Conditions of release/sale

I would like to immediately separate the concepts of a food additive (classified as a dietary supplement) and a medicinal product. In the case of the first, there are no purchase prohibitions; they are freely distributed. The effectiveness of such substances can vary greatly depending on which manufacturer produces them. In medicine, everything is much more complicated. Some drugs are available by prescription only, although others can be purchased without restrictions. Let me give you some examples of popular names:

1. Picamilon is an effective supplement that contains substances that are converted into GABA and niacin after entering the brain. Banned in 2015 in the United States.
2. Gamibetal is a drug containing gamma-aminobutyric acid, available only by prescription.
3. Gopantam and Pantogam– modified supplements that combine beta aminobutyric acid molecules with B vitamins. Available without a prescription and suitable even for children.
4. Phenibut is a popular drug that contains GABA with the addition of a phenyl radical. Often added to pre-workout supplements to enhance focus and attention. In Russia it is distributed by prescription.
5. Nicotinoyl is distributed freely.

In medicines, pay attention to the fact that the formula C4H9NO2 must be indicated in the name. If we talk about sports supplements, Now Gaba is quite popular. The reason is simple - the optimal ratio of the number of GABA servings and price. Although I recommend carefully choosing a brand and studying the composition, dosages, reviews, etc. Among the moderately priced options for gamma-aminobutyric acid, we can highlight Gaba Plus from the Polish brand OstroVit.

GABA supplements are produced by almost all sports companies from Twinlab to domestic brands, which often complicates the choice.

How it affects the body

In the body, GABA is responsible for sleep, regulating the state of rest and arousal. That is, the use of gamma-aminobutyric acid or a medicine based on it can improve the quality of sleep and reduce a number of negative effects from headaches to mood swings during premenstrual syndrome. In sports, GABA has gained enormous popularity for two reasons:

• GABA improves mental focus, mood, and mental clarity.
• Increases the production of growth hormone.

What does the last effect give us? To summarize, that's it. This is one of the main growth factors, it stimulates muscle growth, accelerates fat burning, increases strength, endurance, and restores muscle and other tissues.

Naturally, GABA will not give the same result as GH injections (increasing levels up to 10-15 times), which are used by professional bodybuilders. However, it has been scientifically proven that the use of the supplement will increase the production of growth hormone by 5-6 times. For a natural athlete, this will be more than enough to see a pronounced effect from the use of gamma-aminobutyric acid.

Pharmacokinetics and pharmacodynamics

GABA is classified as a nootropic agent that restores metabolic processes in the brain, accelerates the utilization of glucose and the removal of breakdown products. Gamma-aminobutyric acid normalizes blood pressure, eliminating hypertension, insomnia, and dizziness. GABA has a mild suppressive effect on heart rate and lowers glucose levels for diabetics. The drug is characterized by rapid absorption with a peak of 60 minutes. After this, the concentration decreases with complete elimination from the body within 24 hours.

What products contain

To obtain GABA from foods, you do not need to follow any special diet. Many foods high in gamma-aminobutyric acid are present in the normal diet of residents of the CIS countries, so you won’t have to change your preferences much. GABA is mainly found in foods of plant origin. Among the most common I can highlight the following (in descending order):

• Tomatoes.
• Mackerel.
• Pickled vegetables (especially legumes after fermentation).
• Potato.
• Grapefruits.
• Sprouted rice.
• Broccoli.
• Eggplant.
• Peaches, oranges, pumpkin.
• Carrot.
• Beet.

To understand: tomatoes contain about 60-64 mg of GABA per 100 grams of product, peaches and kiwis - from 11 to 13. Beets - 4 mg. The richest source of gamma-aminobutyric acid is considered to be “gaba tea”, or Gabarone. The concentration of GABA in it can reach from 150 to 400 mg per 100 grams. But I want to note that you cannot get the same amount of GABA from tea as from tomatoes, which you can eat a lot without harm to your health.

Release form

Depends on the manufacturer. If these are medications with gamma-aminobutyric acid in a pharmacy, then 99% of GABA will be available in tablets. GABA comes in three forms:

• In tablets, including chewable ones.
• In capsules.
• In powder form.

It all depends on the components of the supplement and the manufacturer of GABA.

Compound

Medicines use different formulas, so you need to look at the packaging. This may be N-nicotinoyl-g-aminobutyric acid sodium salt, Gamma-amino-beta-phenylbutirate hydrochloride and other substances. Such drugs should be taken only on the recommendation of a doctor. But in the case of a dietary supplement, most manufacturers simply indicate GABA. At best, they add the decoding of the abbreviation.

Benefits and harms

We have already talked a lot about the benefits of gamma butyric acid. Therefore, I will summarize briefly the pros and cons of GABA:

• Improved sleep.
• Elimination of depression, frequent migraines, excessive overexcitation, etc.
• Acceleration of muscle growth and fat burning by stimulating the synthesis of growth hormone.

There is no harm from taking gamma-aminobutyric acid.

Indications and contraindications

Let’s leave the medications because it’s better not to use them yourself. But there are no contraindications to obtain the effect in bodybuilding. The only exceptions can be people with an increased reaction to GABA: it causes drowsiness. In this case, the daily dose should be taken before bedtime. During pregnancy, taking gamma-aminobutyric acid is allowed only after consulting a doctor.

As for the indications for taking GABA, the list is quite wide. These include various psycho-emotional disorders, headaches, and even recovery after a stroke. In sports, GABA is used for two purposes - increasing mental activity (focus, reaction speed, attention, memory, etc.) and the level of growth hormone.

Possible side effects

Side effects can only occur if GABA dosages are exceeded. Most often they are expressed in a slight short-term tingling in the face and neck. But for drugs, possible “side effects” should be looked at in the instructions for use; they may differ for different GABA drugs.

Overdose

Possible only if the recommended dose of GABA is excessively exceeded. Manifested by headache, nausea, skin rashes, emotional overexcitement or irritability.

How long does a package last?

Much depends on the manufacturer. But rarely does a manufacturer produce a package of gamma-aminobutyric acid that lasts for less than 30 days. Usually it is 45-50 days. Therefore, always look at the number of servings, dosage and total cost of GABA. Compare these parameters and look for the best option. Sometimes the most expensive packaging turns out to be the best value due to the large number of servings. This is the benefit of large GABA cups. Among the forms, the powder version turns out to be more profitable (due to the portion/price ratio).

Storage conditions

There are no special conditions that distinguish gamma-aminobutyric acid from other sports nutrition. Do not open the GABA package open; store in dry places away from direct sunlight.

Best before date

For medications, the period usually does not exceed 3 years. For GABA it can range from 2 to 3 years. But one rule is common to all drugs - do not use after the expiration date. In this case, GABA will not give the desired result, plus an expired drug can increase deficiencies and negative reactions.

How to take it correctly

Here I will rely on the results of research that has been conducted over many years. If you want more detailed recommendations, see the instructions. It is almost impossible to cover all medications and supplements and highlight general meanings.

Directions for use and dosage

To maximize all the benefits of GABA, I recommend drinking a serving before bed. According to research, this is the most effective option. You can also divide your daily GABA intake into two servings, taking them after training and before bed. But only if the daily dose of gamma-aminobutyric acid does not cause severe drowsiness.

The optimal dose is from 1.5 to 2 g per day. Manufacturers often lower it to 0.5 or 0.75 g, but this may be a marketing ploy. The substance does not penetrate the BBB well; it all depends on the transport agent. Medicines freely pass the BBB, which is why their dosages are always lower than those of GABA (200-500 mg).

Course duration

The optimal duration of a GABA course in adults is 1-2 months. After this, you should take a break for at least 2-4 weeks, as the effect of taking it gradually decreases. If GABA is used as a medicine, the course is prescribed by a doctor.

Dosage regimens

According to scientific reviews and studies, two schemes are used in sports:

1. Alternating 1 month of admission - 2 weeks of rest.
2. Long course 2-4 months with a break of 6-8 weeks.

How long does it take for it to start working?

The first improvements from gamma-aminobutyric acid can be observed after just a week from taking it. Everything before is a placebo. But GABA reaches its full capacity only by week 3, so short courses simply do not make sense.

What you can and cannot combine with

You can combine it with everything. The only exceptions are strong central nervous system stimulants or those medications that increase excitability and the production of glutamic acid. I can compare this to trying to drive a car backwards and forwards at the same time. In the case of medications, read the instructions for the specific drug.

How not to buy a fake

A very complex and voluminous question even for experienced athletes. I recommend checking based on the following basic criteria:

1. We filter out any dubious drugs with a similar name: Giba, GAMK and others. It is obvious that these are fakes. Palenque is often sold under the name Gabba.
2. Choose well-known manufacturers (less risk of purchasing a fake).
3. Carefully study the packaging and compare it with the photo of GABA on the manufacturer’s website.
4. A good way is to check the price. If the approximate price on the manufacturer’s website is significantly higher than in the store, then it is most likely a fake.

What should the packaging be like?

In 95% of cases, all forms of GABA are stored in plastic jars. The size depends on the number of servings in one package. Occasionally, manufacturers produce GABA in glass jars. Medicines are mainly in blisters.

It is important to understand the difference between a fake and an original. First of all, this is the absence of possible harm. It is unknown what scammers add to tablets or capsules. It could be simple chalk, or it could be something potentially hazardous to health. Therefore, you never know what a local craftsman added to the Gabba packaging and how it will affect your health. Well, it’s a completely obvious fact - the original product will work as stated. “Palenka”, even if it is of high quality and expensive, is not.