Barbiturates: effects, mechanisms of action, and toxicity.

These dangerous psychotropic drugs have been widely used as an anesthetic and as "truth serum".

Anxiety and the various problems it can cause in our lives are widely known today. But although it is considered that our current pace of life facilitates the appearance of this type of problems, the truth is that anxiety has been known since ancient times.

Throughout history, attempts have been made to create different techniques and substances effective against anxiety. One of the most successful types of psychopharmaceuticals until the advent of benzodiazepines have been the barbiturates.

Barbiturates: what are they?

The barbiturates are a type of psycholeptic psychopharmaceuticalsthat is, they have calming and depressant effects on the central nervous system. These drugs are derived from barbituric acid, which was first synthesized by Adolf von Baeyer in 1863. However, the first drugs properly known as barbiturates did not appear until 1903, by Emil Fischer and Josef von Mering. They are considered the first psychotropic drugs with sedative-hypnotic effects.

The action of barbiturates on the nervous system causes a high level of sedation, relaxing and decreasing muscular and mental activity. They have a great hypnotic, anesthetic and analgesic effect.. They are also useful in the treatment of convulsions and other motor symptoms.

On the other hand, barbiturates generate alterations in mood, such as mild feelings of euphoriasuch as mild sensations of euphoria. Due to their effectiveness in reducing anxious symptoms, they were once the treatment of choice for symptoms of anxiety, depression and insomnia.

Risks of their use

Barbiturates, although highly effective in the treatment of certain symptoms and problems, are highly toxic and have a high level of danger.

In spite of their effectiveness, the use of barbiturates pose a high risk to health, generating dependence very easily.. Moreover, the doses that are therapeutic and those that are toxic are very close, which can lead to intoxication and even overdose.

A barbiturate overdose can lead to death in 1 out of 4 cases. In fact, there are many deaths linked to barbiturate overdose, there are many deaths linked to the overdose of these drugssuch as that of Marilyn Monroe.

Today, barbiturates have been have been superseded by benzodiazepines, which enjoy a higher level of safety, while they do not generate as much dependence and do not cause as serious side effects.which enjoy a higher level of safety, while at the same time do not generate as much dependence and do not cause as serious side effects. Despite this, barbiturates continue to be used medically in specific cases in which other substances are not effective, such as anesthesia in surgical interventions or neuropsychological examinations (always with a high level of control).

The risks are multiplied if barbiturates are mixed with other substances. In combination with depressant substances, they can cause respiratory failure. In combination with alcohol, antihistamines and depressant drugs, barbiturates enhance the depressant effects. depressants potentiate the depressant effects, and the result can be fatal. On the other hand, the intake of activating substances in an attempt to counteract the effects of barbiturates may in turn lead to cardiac problems.

Another risk of great importance is related to the cases of pregnant women and nursing mothers.. Barbiturates, which are highly liposoluble, can be transmitted through the placenta and breast milk. Likewise, an overdose can be dangerous for the life of the fetus, which may result in miscarriage.

Some side effects

The consumption of these substances can cause a series of side effects of great relevance, which can even lead to death.which can even lead to death. Some of these effects may be the following.

1. Excessive sedation

Barbiturates have come to be used as an anesthetic because of their powerful sedative effect. While this may sometimes be intended, it can be detrimental to proper functioning and personal performance by causing excessive drowsiness that reduces the individual's physical and mental capacities. They can cause mild paralysis and tingling in different parts of the body. in different parts of the body.

2. Incoordination of different functions

The consumption of barbiturates can cause physical coordination problems, being more complicated to walk or even to speak.. Driving under the effects of this type of medication should be avoided even if there is no drowsiness.

3. Cardiorespiratory problems

Barbiturates are psychotropic drugs of great potency as nervous system depressants, as we have just mentioned. However, this depression can lead to respiratory problems, and even in extreme cases, there is a risk of going into cardiac arrest. there is a risk of cardiorespiratory arrest..

4. Behavioral disinhibition

Although as a general rule barbiturates generate depressant effects on the nervous system that sedate the subject, in some people they can produce a high level of behavioral disinhibition, which can lead to the performance of actions that under normal circumstances would not be carried out. In fact, they have been used as so-called "truth serums".

5. Risk of dependence

The addictive potential of this type of substances is very high, generating dependence very easily.The risk of dependence is very high, generating dependence very easily. It is also easy to abuse their consumption, which is especially dangerous with this medication. The main reason is the high level of tolerance that it tends to provoke, which means that a larger and larger quantity is needed to achieve the same effects as in the first doses.

6. Withdrawal syndrome

When a person with barbiturate dependence stops taking barbiturates abruptly, he or she may suffer withdrawal syndrome. In the case of abstinence to barbiturates, it is frequent that the opposite effects to those of the consumption of the substance are generated.

Specifically, it is easy to find restlessness, anxiety, aggressiveness, gastrointestinal symptoms, insomnia orinsomnia or seizures. Hallucinations and delusions may also occur. It can cause a dangerous drop in Blood Pressure for survival. In fact, in some cases the withdrawal syndrome can be fatal. That is why both the intake and cessation of these drugs must be prescribed with special caution, withdrawing them gradually.

Mechanism of action

The functioning of barbiturates is based mainly on the facilitation of the action of gamma-aminobutyric acid or GABA, which reduces the overload of the nervous system by making it difficult for nerve impulses to be produced and transmitted.

This GABA favoring is carried out through the action of the drug on GABA-sensitive ion channels in the brain. Specifically, hinder the entry of sodium into the neuron, while facilitating the entry of chloride into the cell.while facilitating the entry of chlorine into the cell.

Types of barbiturates

Barbiturates, like other drugs, can be classified into several groups according to how long they take to take effect and how long the effects last. However, even when the effects end, their characteristics mean that they can remain in the organism for a long time. We can identify 4 types of barbiturates.

1. Ultra-short-acting

Barbiturates with ultra-short action are characterized by having a half-life of several minutes, with their effects starting seconds after theTheir effects start seconds after consumption. Within this group we can find thiopental and methohexital.

2. Short-acting

Barbiturates such as hexobarbital, pentobarbital or secobarbital are known as short-acting barbiturates, which begin their effects between ten and fifteen minutes after consumption and last for about 3 or 4 hours. and last for about 3 to 4 hours..

3. Intermediate-acting

Intermediate-acting barbiturates usually take about an hour to take effect, lasting between 6 and 8 hours.. Within this type of barbiturates we find one of the best known and used in various procedures such as the Wada test, amobarbital.

4. Long-acting

Primidone and phenobarbital are some examples of long-acting barbiturates. are some of the examples of long-acting barbiturates, which usually take more than an hour to take effect, but nevertheless tend to last about 12 hours.

Uses and applications

Although they have now been replaced by other substances in the treatment of most conditions, barbiturates are still used in certain cases. The following are some of the current and past uses of these substances.

Neuropsychological examination

Barbiturates are used in some neuropsychological assessment procedures. An example of this is the Wada test, in which amobarbic acid is used to assess the neuropsychological status of the brain.test, in which sodium amobarbital is used to sedate a specific area of the brain and determine the functionality of areas linked to aspects such as laterality, memory or language.

Anesthetic

Some barbiturates are used both to to both initiate and maintain anesthesia in patients during different surgical procedures. during different surgical interventions. This is one of the main current applications.

Seizures

One of the indications for certain types of barbiturates is their use in cases of their use in cases where convulsions occur.They contribute to control motor symptoms thanks to their sedative effect and to the reinforcement of GABA, which helps to inhibit the discharge of nervous impulses.

Trauma and brain accidents

Barbiturates are used to control and diminish the effects of cerebral infarctionsas well as edema produced by different cranioencephalic traumas.

Insomnia

Although other types of sedatives such as benzodiazepines are currently used, barbiturates have been used in the past as a sedative for insomnia. have been used in the past as sleeping pills..

Anxiety

As with insomnia, other types of substances (most commonly benzodiazepines and some antidepressants) are currently used to treat anxiety, but in the past barbiturates were the main substance used as a treatment for anxiety..