What are anxiolytics?
Anxiolytics are a group of drugs, of different structure and nature, but which have the same function in common: they serve to reduce anguish and anxiety in patients.
From this point of view, the ideal anxiolytic would be the one that achieves the greatest reduction in anxiety and at the same time produces the least sedation possible. The use of anxiolytics will be indicated in processes or disorders where symptoms of anxiety appear .
The anxiolytic in principle were called minor tranquillizers , as opposed to neuroleptics (used in the treatment of schizophrenia and other psychoses) are known as major tranquilizers.
Anxiolytics are very effective drugs for treating anxiety symptoms.
When to treat anxiety?
As we have already commented in other articles, a certain level of anxiety is not bad for the person, but can be beneficial, it protects us from external dangers, increases our concentration, protects us and encourages us to progress.
Now when anxiety levels become pathological and symptoms appear, whether physical or psychological, it is necessary to start a treatment that can be with psychotherapy and / or drugs. The pharmacological substances used in the treatment of anxiety are called anxiolytics.
History of anxiolytics.
Mental illness, anxiety, anguish and “madness” are as old as man himself, and man has tried to find a remedy for these ills. In the Middle Ages, the mentally ill, the “crazy” were considered to be true outcasts and were socially marginalized as if they carried the devil inside their body.
The remedies most used by the “doctors of the time”, the healers or witches were the most varied. It should be noted the use of alcoholic beverages and mandrake-based compounds that sought to sedate or sleep the patient.
Later, laudanum and some hallucinogenic substances began to be used . The first drugs, used as such are coral hydrate and bromides, used during the nineteenth century.
The true history of anxiolytics begins in 1902 with the appearance of the Barbital or Veronal that years later would become famous for being the cause of death by overdose (among many others) of the Hollywood actress, Marilyn Monroe.
Barbital belongs to the barbiturate family and was used for many years as a first-choice drug for treating anxiety disorders. Barbituric acid is the original substance that later gave rise to all barbiturates, which have been used for decades.
Barbituric acid was discovered by the German Nobel Prize winner in Chemistry Von Baeyer in 1864 and apparently owes its name to the fact that the celebration of the discovery was held in a tavern on Santa Barbara’s Day .
The main effect of barbiturates is to produce a deep depression of the central nervous system , which is why they can produce effects ranging from sedation to anesthesia. It is also known for its use as an antiepileptic and as a hypnotic.
Barbituric acid was a substance of low pharmacological activity and it was not until 1902 that two researchers (Von Mering and the Nobel laureate Emil Fischer) from the German laboratory Bayer discovered Veronal. History is full of anecdotes, of which we will never know if they are entirely true.
In the case of Veronal, it seems that it owes its name to the fact that one of its discoverers, Von Mering, while traveling on a train, tried his own medicine and fell fast asleep, waking up when the train arrived in the Italian city. from Verona.
All barbiturates, when consumed for some time, end up producing drug addiction, and their overdose can be fatal, in fact the two discoverers of Veronal ended up being addicted to its use and years later died of an overdose.
In 1904 Emil Fischer synthesized other products derived from barbituric acid, among which the phenobarbital that was marketed in 1912 under the name Luminal stands out . Until the advent of benzodiazepines, it was used as a sedative.
The Luminal also has a black history behind its name, as it was used in Nazi Germany to exterminate children born with malformations in the 1935-1945 decade.
Luminal was the first known anticonvulsant, is included by the WHO in its Essential Medicines List and is still used today as an antiepileptic drug, especially in developing countries.
The Secobarbital , trade name Seconal was another barbiturate used as an anxiolytic and hypnotic
For many years barbiturates were considered the first choice anxiolytics. Its side effects are numerous . Among them, the sedation induced by a depression of the central nervous system stands out .
Cases of overdose are very frequent due to the small safety margin that its dosage allows (small increases in the dose of barbiturate can have very harmful and even fatal effects). This leads to the frequent appearance of occupational accidents due to sedation and drowsiness.
When the overdose is voluntary, due to a suicide attempt, mortality is very high. The emergence of benzodiazepines with far fewer side effects led to barbiturates from being used as anxiolytic drugs.
Meprobamate and other drugs.
In the middle of the 20th century, reserpine was used to treat anxiety, as it was considered a “tranquilizer”. Chlorpromazine was also used as a “major tranquilizer” in the treatment of psychoses. The Meprobamate was synthesized in 1950 by pharmacologist Czech Frank A. Berger and was considered a “minor tranquilizer.”
Meprobamate is a drug that has anxiolytic, anticonvulsant and muscle relaxant action. In 1955 it was approved by the American FDA and marketed under the names of Miltown and Ecuanil. Meprobamate should be considered the first anxiolytic drug, although its use was severely hampered by psychoanalytic theories so entrenched in the 1950s.
Finally, it became widely consumed and was considered the “wonder drug” of the time, even becoming the object of jokes and comedy shows, as it was used to treat diarrhea and although it did not improve the symptoms, it made the patient more bearable. , for its sedative action, his frequent visits to the bathroom.
Meprobamate produces tolerance, abuse, overdose and dependence. Therefore, in 1960 with the appearance of benzodiazepines, it was losing pharmacological prominence and was relegated to the background.
In 1960 , the first benzodiazepine, chlordiacephoxide , synthesized by Leo Henryck Sternbach , a Polish chemist at the University of Krakow , was marketed under the name Librium .
This same researcher, a few years later, discovered the drug, which was to become the most prescribed drug in history: Diazepam , which was marketed in 1963 by Roche laboratories, under the name Valium .
After the appearance of Valium, sales soared around the world, the substance was consumed indiscriminately by stressed housewives and executives. There was no lack of a lunatic, who advocated putting diazepam in the water tanks of the cities to calm and keep the children calm.
Valium became the fashionable “legal” drug in society. In the following decades, with massive consumption worldwide, its adverse effects of dependence and a tolerance effect began to be observed, producing withdrawal syndromes when the medication was withdrawn.
Massive use of benzodiazepines.
Benzodiazepines are the most widely used anxiolytic drugs today . They are used, in the short term, as drugs of first choice when a rapid reduction of the patient’s anxiety is required or a depressant action of the central nervous system is sought.
Long-term use may be indicated in severe anxiety disorders. All benzodiazepines have a withdrawal syndrome when the drug is withdrawn, if it is used continuously for more than two weeks.
In patients who take it for a long time, a dependence on the drug and a tolerance effect are created (each time higher doses are necessary to achieve the same effects).
Action of benzodiazepines.
Benzodiazepines in general can have several actions:
- Anxiolytic : reduces anxiety.
- Hypnotic : Induce sleep.
- Muscle relaxant : It acts as a muscle relaxant.
- Anticonvulsant : Effective in epileptic seizures. For example, Valium in rectal microenemas (Stesolid) is used in cases of seizures, especially in children.
Some benzodiazepines, such as diazepan ( Valium ) have all of these actions. In others, the predominant action is anxiolytic, as in dipotassium chlorazepate ( Tranxilium ). In some the most important action is muscle relaxant, such as Tetrazepam ( Myolastan ). Finally, there are those where the hypnotic and sedative effect is the most important, such as Lormetazepan ( Noctamid ).
According to the duration of their effect, benzodiazepines are classified as:
- Short half-life (with an activity between 2 and 8 hours)
- Long half-life (with an activity greater than 12 hours).
The speed with which they act in the body is important:
- For example, in a patient with difficulty initiating sleep, a benzodiazepine that acts quickly , but lasts for a short time, will be more useful to avoid drowsiness when getting up.
- If the patient, on the other hand, does not have difficulty initiating sleep, but wakes up at dawn and can no longer sleep, a benzodiazepine that acts more slowly but with a longer effect, which ensures sleep throughout the entire duration , will be more indicated. evening.
It is the doctor or psychiatrist who, in view of the patient’s pathology, must decide the type of benzodiazepine to use . If a patient has an acute picture of low back pain, a benzodiazepine with a muscle relaxant effect may be useful, especially when taken at night and helps them sleep.
If the patient has a picture of anxiety, but performs work where he must be as alert as possible, we will use a benzodiazepine with an anxiolytic effect as pure as possible. For cases of insomnia, we will mainly look for the hypnotic effect.
In patients with long-standing anxiety disorders, we can use predominantly anxiolytic benzodiazepines with a long-lasting effect, while in a panic attack we will seek an anxiolytic effect as quickly as possible.
It is clear that benzodiazepines are an important part of the medical arsenal today. The benefits for treating a wide variety of disorders cannot be denied, but they also have some drawbacks :
- The hypnotic or sedative effect can be detrimental when driving vehicles or operating dangerous machinery due to the drowsiness they produce.
- In older people , with impaired kidney function, they produce a cumulative effect and this leads to an increase in sedative effects, causing confusion, disorientation or accidental falls .
- Its prolonged use, as we have commented previously, can cause both physical and psychological dependence . For this reason, benzodiazepines should be used for short periods of time and always under strict medical criteria.
- Abrupt discontinuation of treatment can lead to withdrawal symptoms .
- When combined with alcohol it can produce undesirable side effects.
The use of benzodiazepines is so common that many of these substances or brands have become part of the colloquial language: “Take a Valium that I see you nervous”, “I have taken an Orfidal to sleep”, and so on.
Among the best known drugs for years are: diazepam ( Valium ) and dipotassium clorazepate ( Tranxilium ). We also have the capsule to approve the driving license: Bromazepan ( Lexatin ) which has a mild anxiolytic effect and produces little drowsiness.
A classic is Lorazepam ( Orfidal ), sometimes used sublingually to achieve a faster effect. It is part of the arsenal of medicines of many elderly people with difficulty sleeping. Alprazolam ( Trankimazin ) is another of the most well-known anxiolytics at street level.
The main problem with these “superstar” anxiolytics is that they are often consumed without a prescription and indiscriminately . Not surprisingly, Spain is the second European country in consumption of anxiolytic drugs. Only our neighbors in Portugal beat us in this regard.
In recent years the pharmaceutical industry has taken great interest in the development of other anxiolytic drugs. Some, even though they are from different families, such as antidepressants , have a powerful anxiolytic effect. They provide the advantage of minimizing the most common side effects of benzodiazepines.
In this sense, it is worth highlighting the group of SSRIs (selective serotonin reuptake inhibitors). The best known are sertraline, paroxetine, fluoxetine, citalopram or escitalopram.
All of these drugs that began to appear in the late 1980s have a primary antidepressant action . At the same time, they have been shown to be very effective in the treatment of symptoms of anguish and anxiety .
For this reason, its use in anxiety disorders is becoming more frequent every day. Due to their increasing importance, I think it appropriate to separate them from the anxiolytics and study them in a separate chapter.
Many people have a certain aversion to taking drugs. Sometimes because your symptoms are not overly severe. At other times out of genuine repulsion towards pharmacology. These people blindly trust natural remedies.
There is nothing wrong with natural medicine when you know how to use it. After all, most drugs come from medicinal plants. Mother Nature has a wide variety of plant species. There are herbs and medicinal plants, which can be used to treat a vast variety of human disorders.
For hundreds of years, natural medicine has been the only resource our ancestors had to cure their illnesses. Anxiety disorders have been treated over the centuries with a wide variety of medicinal plants.
Among the most used natural anxiolytics we can highlight the following: Chamomile, linden, lemon balm, lavender and passionflower. Let’s see some details of these anxiolytics of a plant nature:
Chamomile has been used for centuries as a medicinal herb. It has a recognized power to calm digestive problems, gastric discomfort and bloating or excess gas. It also has a certain anxiolytic power. It is indicated in those people who have mild anxiety symptoms with a tendency to somatization in the digestive system.
Who has not ever heard our mothers or our grandmothers recommend us to take a linden tea in a situation of anxiety? Like the previous one, it also has a sedative effect on the digestive system. Its effects are broader than chamomile. It can be given to anyone who is nervous, as long as the degree of anxiety is not excessive.
Melissa is another medicinal plant with anxiolytic effects, although it is less known than the previous two. However, it is quite effective in stressful situations and especially in cases of mild insomnia.
For years it has been an effective remedy for insomnia. It can help people who have difficulty “catching sleep” and spend the night “counting sheep” to sleep. In some areas of Spain Melissa is usually called by the name of Melissa.
It is a very common plant in many gardens and houses in Spain. This is due not only to its healing aspect, but to the excellent decorative aspect it provides for its beauty. Taken as an infusion, it calms down stress. It also relieves nervous tension. Like Lavender, taken after dinner, it helps you sleep better.
It is a very suitable plant to reduce all mild anxiety states. It is not as popularly known as the previous ones although perhaps its anxiolytic effect is more powerful. It is also quite effective in treating insomnia.
Most of the mentioned medicinal plants are used as natural anxiolytics in the form of infusions or herbal teas. Simply boil a cup of water and add the medicinal herb in its natural form. There are also sachets with the plant already marketed.
The curative effect of medicinal plants is difficult to quantify, in relation to anxiolytic drugs. The action will depend on the type of herb, its quantity and its concentration. The pharmacy anxiolytic is dosed. In this way we can increase or decrease the dose, knowing at all times the amount that we ingest of the active principle.
Mild anxiolytics. Anxiolytics without a prescription.
Many pharmaceutical laboratories make pharmacological products from medicinal herbs. It is not uncommon to see a great variety of these products in herbal shops and parapharmacies.
In most cases they usually carry a mixture of different medicinal plants. They are usually presented in the form of capsules, drops, solutions or tablets. Since they are parapharmacy products, it is not necessary to provide a prescription for their purchase.
Alexa Clark specializes in Cognitive Behavioral Therapy. She has experience in listening and welcoming in Individual Therapy and Couples Therapy. It meets demands such as generalized anxiety, professional, love and family conflicts, stress, depression, sexual dysfunction, grief, and adolescents from 15 years of age. Over the years, She felt the need to conduct the psychotherapy sessions with subtlety since She understands that the psychologist acts as a facilitator of self-understanding and self-acceptance, valuing each person's respect, uniqueness, and acceptance.