Barbiturates are used both as anticonvulsants and are used to intoxicate themselves or to carry out … the death pen alty. In the past, barbiturates were used in medicine quite often, now their role in the medical world has significantly decreased. This was because of the risks associated with their use of barbiturates - they include, inter alia, the risk of becoming addicted to these drugs and the fact that overdosing can occur quite easily.
Barbiturates , actually barbituric acid, was first synthesized in 1864 in Germany by the chemist Adolf von Baeyer.
The discovery of the first barbiturate preparation is related to some interesting facts - there are at least several theories as to why the compound discovered by Baeyer was called barbituric acid. One of them is that the scholar went to celebrate his discovery in a tavern, which was also celebrated in connection with a celebration in honor of Saint Barbara. Ultimately, the name of barbituric acid would be derived from this female name.
Another theory about the origin of the name of barbituric acid is based on what was used to synthesize it. Well, one of the substrates was then urea, which can be found, among others in urine. In the case of the latter theory, its supporters argue that the name barbituric acid comes from the fact that the urea used in Baeyer's laboratory came from the urine of a waitress named Barbara.
Barbituric acid can be treated as a prototype compound from the barbiturate group - since its production, more than two thousand of its derivatives have been synthesized. For many years since the emergence of compounds from this group, they have been widely used and, interestingly, they have been used in medicine, of course, but not only.
Barbiturates: use in medicine
Barbiturates are agents that exert a depressive effect on the activity of the nervous system. For this reason, soon after they appeared on the medical market, preparations from this group began to be used as sleeping pills - now, however, they are used very rarely for this purpose (they have been used).somewhat superseded by benzodiazepines that are safer in terms of use).
Barbiturates have been used in surgical medicine - in this case they were used as an anesthetic.
Another use of these drugs comes from the fact that they have an anticonvulsant effect - for this reason they are sometimes recommended to people suffering from epilepsy (anyway, barbiturates are used primarily as anticonvulsants).
Barbiturates are sometimes also used in and in the case of completely different diseases than those mentioned. Sometimes they are used in people with increased intracranial pressure, sometimes there are also attempts to use them in the treatment of jaundice, migraine headaches or in the treatment of withdrawal syndrome in people addicted to alcohol or benzodiazepines.
Barbiturates: non-medical use
However, not only medics use barbiturates. Preparations belonging to this group were also used by various investigative services as the so-called "truth serum" (i.e. the agent after which the interrogated person would be more willing to answer the questions asked).
In the case of barbiturates, the boundary between the therapeutic dose and the dose that is toxic and can lead to death is relatively small - the existence of such a relationship has led to the fact that drugs belonging to this group are used in some countries of the world for euthanasia or capital punishment.
Barbiturates: Mechanism of Action
Barbiturates have a depressant effect on the nervous system due to the fact that they lead to hyperpolarization of nerve cells (so these agents make neurons less excitable).
Preparations from this group exert such an effect through several mechanisms. Barbiturates bind to GABAergic receptors, which means that GABA, a neurotransmitter that inhibits the activity of nerve cells, more easily binds to these receptors.
The result is an influx of chloride ions inside the neurons and this is what leads to their hyperpolarization. Barbiturates also lead to the opening of chloride channels in the membranes of nerve cells, and they also regulate the inflow of sodium and calcium ions to their interior.
Additionally, preparations from this group can also inhibit the activity of nerve cells belonging to the reticular formation and the cerebral cortex.
Barbiturates: examples
It has already been mentioned that an extremely large amount of barbiturates have been synthesized. All of themmore than two thousand derivatives of barbituric acid could not be mentioned here, therefore we should limit ourselves to giving a few examples of preparations that belong to the group of barbiturates - they are:
- tiopental
- fenobarbital
- cyclobarbital
- pentobarbital
- methylphenobarbital
- barbital
- metoheksital
Barbiturates: interactions and precautions
In a situation where the doctor orders the patient to take barbiturates, the patient should inform him about any other medications he is taking. This necessity arises because barbiturates interact with many different pharmaceuticals.
Drugs from this group may, for example, weaken the effects of other pharmaceuticals - this is what happens in the case of, among others, some HIV medications, ranolazine (a drug sometimes used in ischemic heart disease) or voriconazole (an antifungal drug).
Barbiturates, however, can lead to opposite interactions, i.e., where they can enhance the effects of other drugs. Here we are talking primarily about other preparations that can have a depressive effect on the nervous system - such as benzodiazepines and hypnotics, such as zaleplon or zolpidem.
For these reasons, it is always necessary to take this type of medication extremely carefully together with barbiturates.
Barbiturates: side effects
Today, barbiturates are used in medicine much less frequently than in the past - for good reason. One of these reasons is the aforementioned slight difference between the therapeutic dose and the toxic dose of these drugs, and another reason why barbiturates are used less and less are their side effects.
The problems that may arise during the use of barbiturates include, but are not limited to:
- dizziness
- nausea
- vomiting
- headache
- psychomotor coordination disorders and balance disorders
- memory impairment
- slowing down the pace of thinking
- concentration disorders
- sleepiness
Barbiturates: addiction and overdose
The limited use of barbiturates is not only caused by the risk of side effects, but also by the fact that they can lead to addiction.
Taking barbiturates may lead to the development of both mental and physical dependence, unfortunately even after a relatively short time of taking these preparations.
Riskaddiction to these drugs is due to several different factors. First of all, it appears due to the fact that tolerance develops quite quickly when taking barbiturates - this leads to the fact that in order to achieve the effect of taking the drug, it is necessary to take increasingly higher doses.
The risk of addiction is also caused by the fact that barbiturates not only have a calming effect, but their intake may result in euphoria or a feeling of satisfaction and relaxation.
Addiction to barbiturates is dangerous in itself, but the risk is increasing because of the fact that it is not difficult to overdose on these drugs. Overdosing of such preparations can be very dangerous - if this happens, the patient may have, among others:
- complete lack of motor coordination
- slurred, unintelligible speech
- difficulty assessing the situation
- breathing disorders (e.g. in the form of very shallow breathing)
- a significant decrease in heart rate (bradycardia)
- renal dysfunction (which may lead to renal failure)
- coma
In the most severe cases of poisoning with barbiturates, the patient may die. However, not only a single overdose of barbiturates is dangerous - long use of these drugs can also lead to various difficulties, including persistent memory disorders, difficulties in maintaining concentration and focus, or sexual disorders.
Addiction to barbiturates is a really serious problem - various disorders can appear both during their chronic use and when a person suddenly stops taking them. A withdrawal syndrome may develop then, the symptoms of which may be such ailments as, among others, anxiety, insomnia, muscle pain or nausea, vomiting and an increase in body temperature.
There is also a risk of seizures, hallucinations and delusions associated with withdrawal syndrome from stopping the use of barbiturates.
Barbiturates and pregnancy and breastfeeding
Barbiturates in pregnant and lactating women are recommended only when necessary. This is because in pregnant women these drugs can pass through the placenta to the fetus, and in nursing mothers, drugs from this group can be found in their milk.
When barbiturates enter the child's body, side effects of these drugs may occur. In addition, there is a risk that in the event that the mother took barbiturates during pregnancy, after herresolution - especially when the woman does not breastfeed later - the baby will develop withdrawal syndrome.
These and several other dangers mean that barbiturates are rather avoided in pregnant and breastfeeding women.