The culture and society in which we live is characterized by a high level of dynamism and constant change, along with high demands on the people who are part of it.
We are constantly required to be productive, proactive and forward-thinking, having to adapt both to the changes in current society and to the possible situations that could happen in the future. For this reason, it is common for us to worry about what could come, a worry that can lead us to aversive emotional states due to fear and tension over what could happen.
In this way, we can observe how disorders related to stress and anxiety are becoming more prevalent, with anxious problems being the most prevalent in the general population and in the clinic. In order to treat this type of problems, different types of treatments have been developed and synthesized and, among them, At a pharmacological level, various types of anxiolytics have been synthesized
The different types of anxiolytics that we will talk about in this article have various points in common, but the main one is the type of problem they treat: anxiety.
While most people know what it is and have actually experienced anxiety throughout their lives, it is a phenomenon that is often difficult to define. Anxiety is considered to be that state of emotional discomfort that arises without there being an immediate stimulus or danger that generates it, the forecast of a future phenomenon being what causes this reaction. Subjects who suffer from anxiety have a high level of activation along with high negative affectivity.
Although its origin is usually cognitive, the effects it produces can also be translated to a physiological level, producing reactions such as tachycardia, physical tension or sweating. It also causes effects at a behavioral level, such as the avoidance of situations that could lead to what causes anxiety. For example, fearing that a phenomenon that occurred in the past will occur again may cause us to avoid similar situations in order to ensure that this is not possible.
Thus, taking into account the discomfort it causes and the fact that it can even invalidate important aspects of our lives (such as in cases of individuals with agoraphobia), seeking a treatment that alleviates these problems has motivated the creation of various treatments, as anxiolytics in the case of pharmacological treatments
The general function of anxiolytics is to induce a decrease in activity, through a depressant action on the nervous system. To this end, most types of anxiolytics act on gamma-aminobutyric acid or GABA and its receptors, enhancing the inhibitory action of this neurotransmitter.
Despite this, in recent times An increase has been observed in the use of drugs that act on serotonin, leading to the use of antidepressants such as SSRIs as the drug of choice in some anxiety disorders. Let’s look at some types of anxiolytics below.
1. Barbiturates
Prior to the arrival of benzodiazepines, these derivatives of barbituric acid were the type of anxiolytic that was most used at the time, having a high sedative potential despite the high risk of addiction and fatal overdose that they entail. Its mechanism of action is based on preventing the flow of sodium to neurons
They were discovered by Emil Fischer in 1903, and their use continued until approximately the 1970s, when the search for effective, less dangerous substances for anxiety led to the discovery of benzodiazepines. Despite this, some barbiturates such as amobarbital were and are used in a very controlled manner in surgical medical interventions, such as in the Wada test.
2. Meprobamate
This substance, like barbiturates, enjoyed great fame and prestige during a time due to its action on anxiety. In addition to acting on anxiety processes, it was used in cases of spasms, insomnia, alcohol withdrawal and migraines. It is a drug that acts in different regions of the nervous system, and can also have an effect on the spinal cord.
However, It was discontinued because it was considered that the benefits it could bring did not outweigh the risks causing confusion and loss of consciousness among other problems in addition to being highly addictive.
3. Benzodiazepines
This class of anxiolytic is the best known and used today, acting as indirect GABA agonists at type A receptors. They increase the affinity of GABA for its receptor throughout the brain, but especially in the limbic system. Likewise, in the Rafe nuclei they act by inhibiting the activity of serotonin on the limbic system.
They produce relief of cognitive tension and, depending on the dose, a certain level of sedation, also serving as an anticonvulsant. Within this type of anxiolytics, some of the best known and most consumed are lorazepam, bromazepam (Lexatin), alprazolam, diazepam (Valium) and clorazepate.
There are various types of benzodiazepines, depending on whether their life in the body is short, medium or long, each having different advantages and disadvantages.
A short-lived benzodiazepine is considered one that lasts a few hours, specifically less than twelve. They have a very quick effect and are very useful in cases where anxiety needs to be reduced quickly, such as in the case of an anxiety crisis or conciliation insomnia. On the other hand, it is easier for them to cause addiction as they require more frequent consumption to maintain the effect of the drug, and they are more common to have side effects.
Long-lived benzodiazepines are those that last more than 24 hours in the body. They have the drawback that when their action is prolonged, they can have a cumulative effect with the previous dose, generally producing greater sedation, but on the other hand, fewer doses are necessary to keep the anxious symptoms under control, which makes addiction difficult.
Intermediate-acting benzodiazepines have a life of around 12 to 24 hours, being useful in cases in which the symptoms want to be treated more quickly than with a long-acting substance and without remaining in the body as long but without needing constant taking of the drug to maintain the effect.
4. Buspirone
Buspirone is one of the few psychotropic drugs used in anxiety that acts on a neurotransmitter other than GABA For this same reason, it has the advantage that, unlike other types of anxiolytics, it does not produce the same side effects, with no interactions with depressant substances or addiction, nor does it cause sedation.
This substance acts on serotonin, specifically as a partial agonist. On the other hand, its action takes weeks to take effect, so it is not useful in anxiety crises.
5. Antihistamines
This type of substance has been used on occasion in cases of anxiety due to the sedation they produce, but apart from this effect they do not present any therapeutic advantage against anxiety.
6. Beta-adrenergic blockers
Beta-adrenergic blockers have been occasionally used as adjuvant treatment because they seem to contribute to reducing somatic symptoms
Main risks and adverse effects
The administration of anxiolytics is very common today, but it must be taken into account that, as with all drugs, their consumption can entail a series of unwanted side effects and even some serious risks. These risks and side effects of these drugs are what have motivated the research of new formulas, moving from barbiturates to benzodiazepines and from these (although they continue to be the most used today) to other substances.
Although the adverse effects will depend on the substance and active ingredient of the drug in question.In general, the possible side effects of different types of anxiolytics can be considered to include the following:
Addiction and dependence
The different types of anxiolytics have proven to have a great capacity for addiction among their consumers That is why its consumption must be very scheduled, generally recommending that the administration of this type of drugs be carried out for not very long periods (around two to four weeks).
Likewise, abrupt withdrawal can cause withdrawal syndromes and rebound effects, so when stopping consumption, cessation must be gradual.
Risk of poisoning and overdose
Excessive consumption of some types of anxiolytics can cause an overdose These overdoses can be really dangerous, potentially causing the death of the individual. In the case of barbiturates, the risk of overdose and death is very high, this being one of the main causes of the development of other substances such as benzodiazepines.
In the case of benzodiazepines there is also a certain risk of death, although unless it has been combined with other substances that enhance the depression of the nervous system (including alcohol), if you suffer from an illness or if you have a weakened body as in the case of benzodiazepines, In the case of the elderly, death from this cause is a strange phenomenon.
Sedation and activity reduction
The fact that they produce a depression of the nervous system causes Most anxiolytics (with exceptions such as buspirone) can cause drowsiness and therefore decrease the level of functionality and performance in some vital areas by reducing the concentration and reaction rate.
paradoxical reaction
In rare cases, anxiolytics can cause an effect completely opposite to that expected, causing hyperarousal and irritability. On these occasions you must go to the doctor immediately.
Stevens, J.C. & Pollack, M.H. (2005). Benzodiazepines in clinical practice: consideration of their long-term use and alternative agents. J Clin Psychiatry; 66 (Suppl 2):21-7.
