With prolonged use of barbiturates may occur. Barbiturates - what are they and treatment of dependence on them. Center Polinar

Depressants- a variety of sedatives, hypnotics, tranquilizers and similar substances, the main effect of which is the inhibition of certain processes in the central nervous system.

Depressants are barbiturates, benzodiazepines and even alcohol- this alone indicates the danger and ambiguity of this group of psychoactive substances.

Almost all depressants are addictive (both physical and psychological dependence), which is especially facilitated by any regularity of use.

The vast majority of depressants are extremely harmful to health, with their use, the likelihood of an overdose is very high (which, for example, made modern doctors almost stop prescribing barbiturates). The likelihood of an overdose increases dramatically when depressants are mixed with any other drugs (alcohol is the most dangerous).

Means for inhalation anesthesia(which includes volatile solvents and glue) are also classified as depressants.

Many sedatives weaken self-control, which often pushes people into antisocial acts.

Alcohol By pharmacological properties ethanol ( ethanol, the main component of all alcoholic beverages) can be attributed to drugs for anesthesia. The cells of the central nervous system, especially the cerebral cortex, are most sensitive to it, acting on which it causes a characteristic alcoholic excitation associated with a weakening of the processes of inhibition. Then the processes of excitation are also weakened, depression of the spinal and medulla oblongata with activity suppression respiratory center.

Alcohol can cause strong psychological dependence, physical dependence is not noted. Alcohol addiction called alcoholism. Female alcoholism much more serious illness than male alcoholism. Dependence can develop with excessive and regular use of strong alcoholic beverages or pure alcohol. Alcohol is toxic in high doses. Throughout the existence of alcohol, there have been countless cases of poisoning, including high percent deaths (especially when the victim turned out to be a child).

Alcoholism- a very serious disease leading to personality degradation, where a person constantly has a desire to drink an alcohol-containing drink (usually vodka). At late stages alcoholism, various mental disorders can occur, including " delirium tremens"- hallucinations, mostly with devils as the main characters (perhaps one of the few cases when hallucinations are hallucinations from a psychotherapeutic point of view after taking any substances) But it should be noted that alcohol can be useful in SMALL doses, strengthening immune systems organism. Red wine is considered good drink to meat.

Barbiturates is a group of drugs, derivatives of barbituric acid, which have hypnotic, anticonvulsant and narcotic effect, due to the depressing effect on the central nervous system. The duration of action of various barbiturates is not the same, which is associated with the peculiarities of their transformation in the body and excretion from it (long-acting barbiturates are excreted mainly by the kidneys; barbiturates with short term actions are destroyed mainly in the liver). For sleeping pills or sedatives (1/3-1/4 doses, inducing sleep) effect, drugs with a long (barbital, phenobarbital, barbitap sodium), medium duration (cyclobarbital, barbamyl, etaminal sodium) and short (hexobarbitap) action, depending on the nature of sleep disturbance. Barbiturates are administered orally in powders and tablets, as well as intramuscularly, intravenously (mainly for anesthesia) and through the rectum.

Phenobarbital and benzonal taken in powders and tablets as anticonvulsants (for epilepsy). Hexenal, thiobutal and thiopental sodium used for anesthesia. Barbiturates are often combined with other sedatives, antispasmodics, anticholinergics and other drugs. Barbiturates are used in anesthesiology to prepare the patient for anesthesia - the preliminary administration of barbiturates enhances the effect of narcotic, local anesthetics and painkillers. With prolonged use of barbiturates, addiction and addiction to them can occur. The use of barbiturates sometimes causes allergic, as well as perverse reactions - anxiety, arousal.

Barbiturates entered medical practice at the beginning of the twentieth century. More than 2,500 barbiturates have been synthesized and, at their peak, about 50 types were sold for consumption. Today, only about a dozen of them are accepted.

Barbiturate manufactures wide range disorders of the central nervous system, starting with mild sedation and reaching coma and is used as a sedative, hypnotic, analgesic or anti-convulsant. initial hallmarks between types of barbiturates are the following parameters: how quickly they act and how long the effects of this exposure last.

Barbiturates are classified into the following types: ultra-short and short-acting, as well as medium-long and long-acting. Barbiturates Ultra short action exercise analgesic effects within about one minute after intravenous administration. Examples are those used in medicine: methohexital (brevital), thiamilap (surital), and thiopental (pentotap).

Barbiturate abusers tend to prefer short- or moderate-acting barbiturates, namely pentobarbitap (Nembutal) and scobarbital (Amytal). Other barbiturates with short and medium duration of exposure include bugalbital (fioripal, fioricet), butabarbital (butizol), talbugal (lotusate), and aprobarbital (alurate). After using any of these medicines by mouth, the action begins within 15-40 minutes, and the effects last up to 6 hours.

These substances are mainly used to calm and induce sleep. Veterinarians use pentobarbital as an anesthetic and a means for euthanasia (painless death).

Long-acting barbiturates include phenobarbital (Luminal) and mephobarbital (Mebarap). The effects of these barbiturates appear after about one hour and last for 12 hours. In addition, they are used for sedation daytime and treatment of seizures or mild anxiety.

Barbiturates are sleeping pills that long-term use addiction occurs. AT last years have become the subject of increased interest of drug addicts. Barbiturates are structurally similar to barbituric acid. In medicine, the following are the most widely used: barbital, barbamyl, fepobarbital (also called luminal), and etaminal sodium. Abuse of barbiturates is typical for patients with alcoholism and opiomania. This may be due to the fact that the propensity to take barbiturates is inherited by the same mechanism as the propensity to consume alcohol and opiates. In addition to its main medicinal effect, barbiturates cause mild euphoria. This property of them attracts more and more people who abuse sleeping pills, and eventually become an end in itself for them. Unaware for the most part of the danger of uncontrolled intake of barbiturates, they can get into physical addiction from them. And this dependence can be expressed in the form of a tenacious withdrawal syndrome. With a severe overdose of barbiturates (more than 4-6 g per dose), deaths are possible due to paralysis of the respiratory center and the development of coma. It should be taken into account that if too frequent use barbiturates, their doses are summed up, which creates a serious threat to health even when taking relatively low single doses.

Prolonged use of sleeping pills leads to a complete psychological shift, because. there is no way for the mind to realize itself. Barbiturates cause suicidal tendencies. And here, as always with drugs, you need to know what you are doing.
The action of barbiturates is opposite to that of amphetamines.: They depress the central nervous system. In small doses, they act as tranquilizers, and in large doses, they are sleeping pills. Sleeping with barbiturates is not normal sleep, because. they inhibit all kinds of normal activity during sleep.

“The consumer of barbiturates makes a repulsive impression. He lacks coordination, staggers and falls off bar stools, falls asleep in the middle of a conversation, food spills out of his mouth. He is shy, grouchy and stupid." William Burroughs. During the seventies, barbiturists were perhaps the most frequent clients of drug agencies such as Lifeline. This is because they tend to be those drug users who are least able to take care of themselves. Even the most desperate drug addicts treat barbiters with contempt because of the trouble they invariably get themselves into.

Barbiturates are a sedative drug. Usually prescribed as sleeping pills, their use for this purpose has now almost completely disappeared, although weaker members of this group, such as phenobarbital, may still be used to treat epilepsy. And yet, barbiturates appear from time to time. Usually in the form of: sodium amytal - usually bright blue capsules containing 60 mg of the drug, seconal - orange capsules of 50 mg, and finally tuinal, which is a mixture of 50 mg of amytal and 50 mg of seconal, which, unsurprisingly, is available in half orange, half blue capsules. Whoever was responsible for the design of these capsules certainly had a knack for selling drugs to opiates and hypochondriacs.

The first thing to understand about barbiturates is that these things are dangerous. In the seventies, a lot of people died every year from barbiturate poisoning. Many of these people died simply by taking them as sleeping pills.

Usually everything happens as follows. Drink a little to sleep. Then you take a couple of Nembutap (barbiturate) capsules and pour yourself another while waiting for the medicine to work. After a while, you don't remember if you took the capsules or not, so it's better to take a couple more to be sure. In the morning they find your body. Even if you didn't choke on your own vomit, your breathing would gradually slow down until it stopped altogether.

Like opiates, barbiturates are addictive, only to a greater extent. Taking them to better fall asleep, after a few days it becomes impossible to fall asleep without them. Like opiates, barbiturates are addictive, so you have to constantly increase the dose to get the same effect, but withdrawal is the most remarkable. If opiate withdrawal is a cold turkey, then barbiturate withdrawal is like a dead crow. In addition to the compulsive need, discomfort, and inability to sleep, barbiturate withdrawal also causes severe epileptic seizures.

No one dies from opiate withdrawal, but it is very possible with barbiturates, and it is worth even thinking about them only under the supervision of doctors, preferably in a hospital setting.

The possibility of overdose is greatly increased if barbiturates are taken intravenously rather than orally. In general, barbiturates are only used by people who have their switches set to automatic self-destruct mode, because the drug is not pleasurable at all. Barbiturates lack the euphoric potential of opiates and the social smoothing properties associated with alcohol. They just call black and empty oblivion and, as such, will always be popular with people who hate themselves and their lives so much that their behavior is driven by the need to destroy the very possibility of thought and self-esteem. Do yourself a favor. Just say no.

CLINICAL PICTURE OF POISONING

The main signs of barbiturate poisoning are drowsiness, confusion, hallucinations, difficulty speaking and stuttering, shallow breathing and weak pulse.

There is an imbalance, and a person under the influence of barbiturates gives the impression of being intoxicated with alcohol. His movements are uncontrolled and uncoordinated. Precise movements are almost impossible.

Unlike opiate poisoning, the patient's pupils retain normal width. Recall that in opiomaniacs they are maximally narrowed. With a severe overdose, the addict can go into a state of deep shock and even die.

Barbiturate addicts differ greatly from opioid addicts, including in appearance and behavior. chronic poisoning always accompanied by barbiturates mental disorders or personality changes.

characteristic behavior and appearance drug addicts taking barbiturates. They demonstrate slow mental reactions, difficulty in the thought process and speed of making a logical decision, which manifests itself, first of all, in unexpected situations, when it is necessary to quickly draw the right conclusion and adequately respond to circumstances. For this reason, it is barbiturates that are considered very an important factor in the growing number of traffic accidents and accidents at work.

WITHDRAWAL SYMPTOMS

In the event of a sudden cessation of the intake of barbiturates in an organism accustomed to these drugs, a crisis develops already within the first twenty-four hours, reaching its peak on the second or third day and beginning to decline in the following days.

To the most severe complications include: sudden fall blood pressure accompanied by loss of consciousness; convulsions resembling epilepsy. During an attack, the patient turns blue, and bloody foam appears on the lips as a result of biting the tongue. Very often there are disturbances of consciousness in the form of attacks of delirium and hallucinations.

It must be remembered that epileptic convulsions and delirium ns appear simultaneously. Typically, during a barbiturate withdrawal crisis, the patient will have one or two seizures within the first forty-eight hours, and on the third day he will become psychotic or depressed. Such periods of psychosis may be extremely serious and may be accompanied by persecutory delusions, which cause the patient to panic and become a danger to others and to himself. Therefore, an addict who is in a state of barbiturate withdrawal crisis should be taken to the hospital as soon as possible.

Barbiturates are a class of drugs that have a sedative effect. They depress the nervous system, and do not cause excitation, like amphetamines. Therefore, they are the opposite of the latter.

All barbiturates are made on the basis of barbituric acid. They cannot be treated unequivocally and called them drugs.

One-time treatments do not lead to pathological changes in the body and do an excellent job of their purpose: they calm, relieve insomnia.

However, patients do not always adhere to the doctor's recommendations and often begin to use barbiturates permanently. Of course, as a medicine. So there is an addiction to the drug. In terms of intensity, such dependence is no weaker than any other narcotic variety. That's why uncontrolled use these funds can have negative consequences.

Medical record: the history of barbiturates

For the first time, these drugs were discussed in medical circles at the end of the 19th century. This happened after the German chemist Adolf von Bayer synthesized barbituric acid in 1863. Since the discovery took place on the feast of St. Barbara (Barbara), the scientist decided to name the new substance after her. Second root compound word he borrowed from the English (urea is translated from English as urine). So the word "barbituric" appeared, and after it the barbiturates.

Veronal - the first released barbiturate

In 1903, barbiturates were released to the pharmaceutical market. The discoverer was barbital, known to many patients as veronal. By the 20s of the 20th century, about 2,500 barbiturates had already been synthesized. Of these, about 50 varieties were used in medical practice as sleeping pills and sedatives.

The popularity of drugs grew, because many people complained of stress, and these medical supplies could act as antidepressants. However, in the 60s, doctors found themselves face to face with a disappointing fact: along with positive effects negative effects of barbiturate use have also been found. For example, the emergence of drug dependence on drugs.

The production of medicines has declined. There are no more than a dozen in use today. Yes, and permitted drugs are increasingly being replaced by safer varieties - benzodiazepines.

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Medical use of barbiturates

Despite the dangers of using these drugs, modern medicine until she finally gave up on them. The point is that this fast-acting drugs, and sometimes their use is justified in medicinal purposes.

So, today barbiturates are used:

As an anesthetic before surgery.
To prevent epileptic seizures.
As an anticonvulsant.

Experts do not forget about their calming and hypnotic effect.

Barbiturates (such as pentobarbital) are also used in veterinary medicine. These drugs act as pain relievers. They can also be used for euthanasia (that is, if the animal is decided to be euthanized).

Types of barbiturates

In modern pharmacology, these drugs are classified into groups depending on the duration of action. There are 3 major varieties:

Short acting drugs. These include hexenal. It is used for anesthesia. The solution is injected into a vein. The effect occurs almost immediately and can last up to half an hour.
Intermediate drugs. Barbamil can be called a well-known representative of this group. It is used when various types insomnia and for the treatment of sleep. Moreover, the duration of sleep can be from 6 to 8 hours. Barbamil is also effective in atherosclerosis. It lowers cholesterol and saves from angina attacks.
Preparations prolonged exposure. For example, phenobarbital. Medication, which is used to treat epilepsy and relieve seizures. Usually the drug is injected into a vein once. But, if the convulsions continue, then repeated doses are possible every half an hour until the convulsions pass. However daily dose should not exceed 30 mg.

Dependent people prefer to use means of average and long influence. Phenobarbital is considered an addict's dream. The action of the drug begins after 15 (in rare cases 40 minutes), and the effect lasts up to 6, and sometimes 12 hours.

How do barbiturates work in the body?

Statistics say that these funds are usually chosen by people prone to suicide. Barbiturates came to taste and those who have low self-esteem. They do not cause euphoria like opiates. On the contrary, they are characterized by pseudo-healthy sleep. Often they are used precisely because of this.

The effect of the use of these drugs largely depends on the dose. So, a small amount of the drug is almost harmless. It promotes relaxation and calms the nervous system.

One problem - even small dose barbiturates with constant use is addictive.

Average doses are similar to the effects of alcohol on the body. The addict's reflexes slow down, an unsteady gait occurs. He begins to slur words. But the use of barbiturates in large doses can easily lead to lethal outcome. Often the addict in such cases falls into a coma.

How to define addiction?

People who begin using barbiturates for medicinal purposes are usually unaware of the fact that they have become addicted to the drug. Meanwhile, it is necessary to pay attention to the symptoms that eloquently indicate the addiction of the body. So, signs of addiction can be considered:

Decrease in physical activity, working capacity, difficult mental activity, indifference to others under the influence of the drug.
Nervousness and distraction, irritability, and even in mild form aggressiveness after the action of the barbiturates has ended.
Poor health, anxiety and fast fatiguability, weight loss long-term use drug.
Nausea and vomiting, abdominal pain, bad dream loss of interest in life and the world around abrupt refusal from drugs.

In some cases, seizures may occur approximately 5 days after a dose.

In general, with barbituratomania, the withdrawal syndrome is much more difficult than with the use of opiates. It can cause signs of epilepsy, coma, and in some cases death. That is why when you refuse drugs, it is better to contact medical clinic. There this period will pass less painful, because often the first stage of treatment is not a refusal of the drug, but a gradual decrease in the dose of the drug taken earlier.

Fatigue, bad feeling, irritability? These are signs showing barbiturate dependence when trying to withdraw

Barbiturates and overdose

Exceeding the maximum allowable daily allowance leads to overdose. It is fraught with many negative consequences. So, there were cases when a person fell asleep and did not wake up. Another danger is that during sleep, the addict can choke on vomit. After all, one of the signs of an overdose is vomiting.

If the dose is exceeded, it is necessary first of all to clear the stomach of drugs. Can handle this very well Activated carbon. If breathing gradually slows down, it is necessary to do an artificial one until an ambulance arrives.

Overdose may be indicated by clammy skin, rapid pulse, and dilated pupils.

Quitting drug use is difficult. However, if dependent person made such a decision, it must be constantly supported in this. For treatment, different programs are used, taking into account many factors: the age of the addict, the presence concomitant diseases, the degree of poisoning of the organism.

Treatment is designed for a long period, but cases of healing are quite common.

Butyrate. Documentary

Very often the term "barbiturates" is applied to all existing sedative medications. In fact, it is relevant only for a certain group of funds. The list of barbiturates is long enough. Despite the fact that this group of drugs has many contraindications and side effects sometimes it is almost impossible to do without their help.

Mechanism of action of barbiturates

Barbiturates are made from barbituric acid. They were invented at the beginning of the last century. To date, out of more than two thousand known drugs you can meet on sale no more than a dozen. This is explained by the too heavy effect of medicines.

Barbiturates have a powerful sedative, analgesic and effect. Surely many drugs of the barbiturate group are associated with drugs - quite rightly so. The fact is that drugs depress the nervous system, and too frequent use of them threatens with addiction.

The action of barbiturates can be safely compared with the body's reaction to alcohol: first, a period of euphoria and excitement sets in (depending on the physique and state of health of a person, this stage can last from several minutes to two or three hours), after which there is heavy sleep, after which depression and depression remain. broken state.

The pharmacokinetics of almost all barbiturates is the same. Active ingredients drugs are very quickly and almost completely absorbed in the organs gastrointestinal tract. In other organs, adsorption practically does not occur. Basically, barbiturates are excreted from the body by the kidneys, but when taking certain types of drugs, the main burden falls on the liver.

Medicines vary in how long they last. Appropriate ones are selected depending on the problem. So, for example, a drug with a short (up to six hours) action will help calm down one patient, while another will be able to feel the effect only from the strongest medication.

Most of the drugs on the list of barbiturates are prescribed in the following cases:

with convulsions and convulsions;
to deal with stress;
at nervous disorders;
in preparation for anesthesia;
at .

Preliminary use of barbiturates enhances the effect of local anesthesia and painkillers. You can take drugs in the form of tablets or powders, or intravenously or intramuscularly. Some of the drugs are allowed to be administered rectally. But most often, barbiturates are injected into the body intravenously.

Barbiturates are a fairly large group of barbituric acid derivatives. Penetrate the nervous system and have a depressing effect on nerve centers blocking their work. At the time received wide application in medicine because healing effect proven for many years: barbiturates can have a sedative and hypnotic effect, and each representative has different duration and power.

In addition, drugs containing barbituric acid or its derivatives have anticonvulsant and analgesic effects.

However, to date, barbiturates are legal only in a number of countries, and their use is carried out under the strict supervision of the attending physician, since, in addition to all positive sides, negative effect also well known. At long-term and unlimited intake of these funds, a person develops dependence - not only physical, but also psychological.

In addition, all drugs of the group have a large number of contraindications and side effects.

Thus, barbiturates not only treat, but can also cause severe poisoning at the slightest excess of the dosage, so safer analogues were found.

The history of discovery and the formation of the term

Barbituric acid was first obtained by the German scientist Adolf von Bayer in 1864 by the condensation of urea and dialkylmalonic acids, which, in turn, were obtained from malic acid. There is still controversy over the name of the new substance.

According to one version, Adolf named him after the girl Barbara, whom he was fond of at that moment. And according to another, barbituric acid owes its name to Saint Barbara, whose name was combined with Latin name urea - "urea".

Medical practice use

For the first time preparations of barbituric acid and its derivatives were used in medical practice in 1903, that is, half a century after their discovery.

At that time they were prescribed as a sedative and hypnotic. By the 60s of the 20th century, the use of barbiturates greatly increased and reached its peak. There were reasons for that. In that century, people were constantly exposed to and. And any drug that has even the slightest similar action, enjoyed popularity, and consequently, commercial success.

Mechanism of action

The so-called GABA receptors are present in the neurons of the central nervous system. And barbiturates have a certain effect on them, thanks to which the mechanism for opening chloride ion channels is launched and accelerated.

Due to this, there is a faster penetration of chlorine through the membrane of the nerve cell, which, in turn, hyperpolarizes. As a result, inhibitory processes occur in neurons, on which the speed of the reaction of the central nervous system to a nerve impulse depends.

Effect

Barbituric acid and all its derivatives have a powerful effect, which allowed them to be actively used in medical practice for some time.

People suffering from insomnia or were prescribed barbiturates as sleeping pills. Relying on the pronounced sedative effect of this group of medicines they were prescribed for aggression and excessive excitation of the nervous system.

Due to the fact that barbiturates block communication between nerve cells, they are still sometimes used as, appointing people suffering.

For anesthesia - both local and full, they are also well suited. And in combination with the means used for anesthesia, they increase its duration. Among other things, they also have some analgesic effect.

Scope of application

Barbiturates have been (rarely still are) prescribed to patients who are susceptible to certain mental disorders as well as insomnia.

Very often used in initial phase if anesthesia is required.

As shown when, as they are able to stop an epileptic seizure.

Barbiturates have also found their way into veterinary medicine because of their ability to painlessly carry out euthanasia. For these purposes, Pentobarbital is used.

Modern representatives

Add to list modern barbiturates, which can still be found on sale, included the following drugs:

Reasons for not using

Currently, barbiturates are practically not used in medicine. This is due to their ability to cause microsomal induction in the liver. As a result, the use of any drugs after barbiturates is undesirable, since their increased penetration into the blood occurs, which means that a more pronounced uncontrolled effect similar to drug poisoning.

This also applies to repeated use of barbituric acid derivatives themselves. In addition, they have a number of side effects and a long aftereffect.

The elderly, pregnant and lactating is strictly prohibited!

A side effect of the use of barbiturates is expressed primarily in their ability to inhibit myocardial contractions. As a result, drugs with barbituric acid are not recommended for use by the elderly. The body may simply not withstand their strong pharmacological effect.

Barbiturates also cross the placenta from the pregnant mother to the fetus and through the mother's milk to the child during lactation, which is fraught with serious consequences, up to asphyxia and suffocation.

One step from peace to eternal rest

Barbiturates are strong toxic drugs. Most often they are used by opium addicts, but there are those who use only barbituric derivatives.

Small doses cause a condition similar to alcohol intoxication. The person feels happiness, in some cases even euphoria.

Like others toxic substances, barbiturates cause great harm to the liver, since the cleansing of the body occurs precisely through it.

However, barbiturate addicts most often do not survive to cirrhosis of the liver, but die due to cardiac arrest or accidents that occur under the influence of drugs.

Emergency care for poisoning

From healthy body barbiturates in therapeutic amounts are easily excreted naturally, however, their absence causes a condition similar to alcohol syndrome.

The patient develops nausea, drowsiness, depression of consciousness, in some cases even vomiting.

However, if taken too large dose barbiturates, they must be removed from the body as soon as possible, since the outcome of poisoning can be very difficult - from coma to death.

As with any poisoning, you should start with gastric lavage. This will help to get rid of substances that have not yet had time to get into the blood.

The antidote for barbiturate poisoning is sodium thiosulfate. In addition, to prevent and prevent oxygen starvation brain tissues are injected with Bemegrid or Corazole.

Barbituric acid derivatives (barbiturates) have been used in medicine for a long time. Barbituric acid itself was synthesized as early as 1864.

In small doses, barbituric acid derivatives simultaneously cause hypnotic, anti-anxiety, amnestic, anticonvulsant and central muscle relaxant effects. Barbiturate-induced sleep is characterized as compelled. According to the nature of the effect on the central nervous system (CNS) and the lack of selective action, barbiturates are narcotic-type substances.

The preparations of this drug group survived the peak of their popularity and with the advent of benzodiazepine derivatives, they began to be used much less frequently as hypnotics. AT recent times Barbiturates are mainly used as anticonvulsants.

Mechanism of action of barbiturates

There are so-called GABA A-benzodiazepine-barbiturate receptor macromolecular complexes in CNS neurons (see Figure ⭣). Barbituric acid derivatives have a GABA-mimetic mechanism of action, that is, they stimulate barbiturate receptors of macromolecular complexes in CNS neurons, which leads to an increase in the affinity of GABA for GABA A receptors. As a result, there is a faster opening of chlorine ionophores (specific channels), through which chlorine rushes into the cell, the charge of the membrane changes and its hyperpolarization occurs, which leads to inhibitory processes in neurons.

It is believed, however, that the action of barbiturates is not limited to their effect on the GABA A-benzodiazepine-6 arbiturate receptor complex. Barbituric acid derivatives inhibit the release of excitatory CNS mediators (acetylcholine, glutamate, asparaginate), block AMPA receptors for glutamic acid, an excitatory CNS mediator. It is also believed that, interacting with the neuron membrane, they cause changes in its permeability for other ions (sodium, potassium, calcium).

The drug deserves special attention. phenobarbital (luminal), which has a phenyl radical in its structure. In connection with this, this drug increases molecular mass, which leads to an increase in the strength and duration of the drug. In addition, the presence of a phenyl radical allows phenobarbital to influence the permeability of ion channels (for sodium, chloride and calcium) more than other barbiturates and to have an anticonvulsant effect. Due to this property, phenobarbital is widely used to treat epilepsy.

Phenobarbital has a number of dose-dependent pharmacological effects. So, at a dose of 0.1-0.2, the drug has a hypnotic effect. At a dose of 0.05-0.1, the antiepileptic effect prevails. And when taking 0.01-0.02 phenobarbital, only sedative and hypotensive action. It should be noted that the decrease in blood pressure when taking phenobarbital is a consequence of the inhibition of the vasomotor center of the medulla oblongata.

In addition, phenobarbital has a myotropic antispasmodic effect on blood vessels. At this dosage, phenobarbital, together with sedative drugs (see Calming agents), is part of various combined drugs, such as valocordin and corvalol, which have antispasmodic, vasodilating, sedative and mild hypnotic effects. These drugs are prescribed in the form of drops for functional disorders of cardio-vascular system, vegetative dystonia, neurotic states, irritability, sleep disturbances.

Barbiturate poisoning

Barbiturate poisoning occurs with an accidental or intentional overdose (barbituric acid derivatives - drugs with a low latitude therapeutic action). The lethal dose is about 10 therapeutic doses: for short-acting barbiturates - 2.0-3.0, for barbiturates long-acting - 4,0-5,0.

Clinical picture intoxication is characterized by a pronounced depression of the central nervous system. There is a dream that turns into a coma such as anesthesia, hypothermia, inhibition of reflexes, respiration, hypoxia, anuria. There is a weakening of cardiac activity, collapse (which is associated with inhibition of the vasomotor center, blockade of H-cholinergic receptors of sympathetic ganglia and myotropic antispasmodic effect on blood vessels). Death occurs from paralysis of the respiratory center.

Treatment of poisoning is to accelerate the excretion of the drug from the body and to maintain vital important functions. If the introduced barbiturate is not completely absorbed from the gastrointestinal tract, then gastric lavage is done, absorbent agents, saline laxatives are given. To speed up the excretion of an already absorbed substance, large quantities electrolyte solutions and osmotic diuretics (mannitol) or furosemide, causing a rapid and significant increase in diuresis (so-called forced diuresis). Introduction alkaline solutions may also promote the elimination of barbiturates. At very high concentrations barbiturates in the blood carry out hemosorption, as well as peritoneal dialysis and hemodialysis.

One of the main objectives of the treatment of barbiturate poisoning is to establish adequate respiration and eliminate or prevent hypoxia. AT severe cases carry out artificial respiration. Analeptics (bemegrid, nikethamide) are prescribed only for mild forms of poisoning; in severe cases, they not only do not contribute to the restoration of breathing, but can even worsen the patient's condition, because they cause convulsions and inadequately increase the brain's need for oxygen. If hypotension, collapse occurs, then blood, blood substitutes, and norepinephrine are administered.

Undesirable effects of taking barbiturates

It must be taken into account that barbiturates (especially phenobarbital) cause the induction of microsomal oxidation in the liver. Therefore, when repeated injections barbiturates, their metabolic rate, like other medicines, increases. Obviously, this is one of the causes of addiction to barbituric acid derivatives. When using barbiturates (even once) after waking up, there may be an aftereffect in the form of drowsiness, depression, weakness, impaired coordination of movements, headache, memory impairment, vomiting, which persist throughout the day. In addition, with repeated use, material cumulation is characteristic, since these medications able to be deposited in adipose tissue (especially phenobarbital).

This group of hypnotics dramatically changes the structure of sleep, there is a shortening of the phase REM sleep(BDG), so after the change of drugs there is a pronounced recoil phenomenon- overproduction of REM sleep with frequent awakenings, nightmares, a feeling of incessant mental activity. Instead of 4-5 episodes of REM sleep per night, there are 10-15 and even 25-30 episodes. To avoid this phenomenon sleeping pills should be phased out gradually.

It has been established that when taking barbiturates for 5-7 days, the restoration of the physiological structure of sleep occurs only after 5-7 weeks. Prolonged use of barbituric acid derivatives leads to the development of physical and mental dependence with severe syndrome abstinence after stopping the drug (severe mental and somatic disorders - anxiety, irritability, fear, vomiting, blurred vision, convulsions, orthostatic hypotension).

Sources:
1. Lectures on pharmacology for higher medical and pharmaceutical education / V.M. Bryukhanov, Ya.F. Zverev, V.V. Lampatov, A.Yu. Zharikov, O.S. Talalaeva - Barnaul: Spektr Publishing House, 2014.
2. Pharmacology with the formulation / Gaevy M.D., Petrov V.I., Gaevaya L.M., Davydov V.S., - M.: ICC March, 2007.