Anxiolytic psychoactive drugs: their characteristics and effects

Anxiolytic psychotropic drugs are medications that have contributed greatly to treating anxiety and sleep problems, in addition to pain associated with chronic diseases such as fibromyalgia or accidents.

These drugs, as with all the others, have their advantages and risks, working very well if they are consumed as prescribed by a psychiatrist and are genuinely dangerous if abused.

Next we will see this extensive family of drugs, some examples of them, their main mechanisms of action and what happens when they are abused.

• Related article: "Psychopharmaceuticals: drugs that act on the brain"

What are anxiolytics?

Throughout history, all kinds of natural substances have been used to try to calm and reassure, especially in the form of infusions such as chamomile, valerian, linden or lemon verbena. However, thanks to chemical and pharmacological advances since the mid-nineteenth century, all kinds of psychoactive drugs have been introduced that serve as treatments for anxiety and sleep disorders, replacing both infusions and other treatments such as alcohol and derivatives of opium.

As with the rest of psychoactive drugs, anxiolytics are medications whose main function is to affect certain neurons of the central nervous system, in this case those that induce anxiety and insomnia. Anxiolytics calm nervousness by directly or indirectly influencing the way in which these nerve cells release and reuptake certain neurotransmitters.

The main effect of anxiolytics, along with sedatives, is act on the central nervous system, depressing it, that is, they reduce brain activity that is associated with the origin of symptoms of anxiety. In the case of anxiolytics, they reduce the signs of anxiety and agitation without actually producing numbness, while sedatives do have a clear hypnotic effect, reducing the level of conscience. Likewise, both types of drugs can be used as painkillers.

Because anxiolytics are relatively easy drugs to obtain, their use has been increasing in recent decades, making them one of the most prescribed medications in psychiatric practice. Today its consumption is present in all social sectors, many times seen as a cheaper, faster and easier option to solve anxiety problems that psychological therapy, although, really, do not eliminate the cause, but the symptom.

Classification

The family of anxiolytics does not correspond to a group of drugs that share chemical characteristics, but rather their effects. Among the anxiolytics we can find drugs as diverse as benzodiazepines, barbiturates and analogues of barbiturates

Benzodiazepines

Benzodiazepines are prescribed for the short-term relief of highly disabling anxiety, at pathological levels. These drugs produce a sedative-hypnotic effect.

Benzodiazepines are typically prescribed for the short-term relief of highly disabling anxiety. They are drugs that, despite being quite safe, have a very high capacity to generate tolerance and dependence, resulting in more possibilities of addiction.

All benzodiazepines work by increasing the action of the neurotransmitter GABA (gamma-aminobutyric acid). This neurotransmitter is responsible for transmitting inhibition messages from one neuron to another, that is, making the nerve cells slow down or stop transmitting.

Depending on the duration of its half-life we ​​can speak of up to four types of benzodiazepines:

1. Ultra-short-acting benzodiazepines

Its half-life is less than 6 hours. Among them we can find the Brotizolam. N-fidazolain.

2. Short-acting benzodiazepines

Its half-life is between 6 and 12 hours. They have few residual effects if taken before bed at night, although too frequent use can lead to rebound insomnia and anxiety upon waking. Among them we can find: Loprazolam, Oxazepam and Temazepam.

3. Benzodiazepines of intermediate duration

Its half-life is between 12 and 24 hours. Some residual effects may arise during the first half of the day. Rebound insomnia tends to be more frequent when use is stopped abruptly and without adequate medical supervision. Because of this, some withdrawal symptoms may occur during the day, especially if they have been consumed for a long time.

Among the intermediate-acting benzodiazepines we find: Alprazolam and Bromazepam, Lorazepam.

4. Long-acting benzodiazepines

Its half-life is greater than 24 hours. They have very powerful sedative effects, which tend to last through the next day if used to treat insomnia.

Its half-life is greater than 24 hours. Its sedative effects are very powerful, so they tend to last during the day after consuming them to treat insomnia.

Among these benzodiazepines we find: Clonazepam, Clobazepam, Clorazepate, Diazepam and Ketazolam.

• You may be interested in: "Benzodiazepines (psychoactive drug): uses, effects and risks"

Drugs Z

Z drugs, also called benzodiazepine analogs, are drugs whose chemical structure is different from that of benzodiazepines but have a similar pharmacological action. It is for this reason that they usually have the same therapeutic indications as their analogues, and curiously they have the same side effects and involve the same risks. These peculiar drugs are three: Zolpidem, Zopiclone and Zaleplon.

Barbiturates

The barbiturates They are drugs that reduce anxiety due to their powerful sedative effect.

They have quite a bad reputation since they are known for their high risk of abuse and addiction, so their use to treat anxiety is currently discouraged. Among them we find Amobarbital, Butalbital, Phenobarbital, Secobarbital and Pentobarbital.

Pharmacologically speaking, behave as GABA-A receptor agonists, although they also act at other levels, such as antagonizing the excitatory effect of glutamic acid and in high doses interfering with the transport of calcium, sodium and potassium ions across the neuronal membrane, which has been related to their greater intensity compared to benzodiazepines.

Azapirones

Among the azapirones we find buspirone, gepirone, ipsapirone and tandospirone, drugs with moderate anxiolytic capacity that only manifests itself when they are administered chronically. They have also been used as antidepressants.

They are partial agonists of 5-HT receptors, with which its action is focused on the regulation of serotonergic neurotransmission, without affecting GABAergic neurotransmission. They cannot be used as hypnotics since they lack a direct sedative effect.

Effects of anxiolytics

As the name suggests, anxiolytics are prescribed to treat anxiety. The effects and intensity depend on the type of drug that has been consumed, the dose and the characteristics of the person, especially their ability to eliminate the drug.

In the case of benzodiazepines, at low doses they reduce restlessness, emotional tension and anxiety, without significantly altering sensory perception or alertness. At medium doses they produce calm and drowsiness and can even cause some momentary difficulties in speech. At high doses, benzodiazepines cause unconsciousness, which is why they are used as surgical anesthesia.

Side effects

Each anxiolytic drug has its own side effects, directly linked to the dose, mechanism of action and time in which they take to be eliminated from the body. However, we can find that many adverse effects of these drugs coincide, especially those effects that are related to anxiety and the state of consciousness, either increasing them or reducing them to problematic levels. The most common side effects of these drugs are.

• Dry mouth and nose
• Dysgeusia: metallic taste sensation
• Mydriasis: dilation of the pupil
• Constipation
• Blurry vision
• Dizziness
• Sickness
• Restlessness
• Tremors
• Loss of sexual desire
• Erection problems in men

In the specific case of benzodiazepines, their long-term side effects are very worrying since they can cause permanent physical and psychological alterations. Its long-term consumption causes sexual dysfunction, damage to the cerebellum, skin rashes, joint pain, headaches, blood pressure drops, heart attacks, liver and kidney poisoning, tremors, vertigo and deterioration serious psychological

Mixing anxiolytic psychotropic drugs with other drugs, both anxiolytics and non-anxiolytics, and drugs can be very dangerous. It is true that in clinical practice all types of drugs are combined, but these combinations are controlled and studied by psychiatrists, who know how these drugs interact and what benefits they will bring to the patient.

It is especially inadvisable to mix benzodiazepines with alcohol since its effects do not add up, but multiply so uncontrollably that life can be endangered. Among the symptoms that may appear from this explosive combination are cardiorespiratory arrest and loss of breath. consciousness, although, ironically, anxious symptoms such as high excitability, hostile reactions and aggressiveness.

Anxiolytic withdrawal syndrome

A little-known effect of anxiolytic psychotropic drugs is a picture that resembles that of an alcohol hangover. East It appears especially if the medication has been abused, consuming it in large doses.

Benzodiazepines usually cause a high tolerance and great dependence, making the person go consuming more and more doses, since the therapeutic effects are reduced with the passage of weather. When the treatment is stopped abruptly, anxious symptoms and excitement appear even more intense than when the treatment began. treatment, which makes the person, in case they get new drugs, take them again and fall into a addiction.

The degree of dependence on anxiolytics it will depend on the type of drug that has been taken, the dose consumed and the length of time it has been used. Withdrawal syndrome manifests itself with the following symptoms.

• Perception disturbances
• Fainting
• Restlessness
• Constant nervousness
• Tremors
• Weakness
• Sickness
• Vomiting
• Headache
• Hyperactivity to external stimuli
• Nystagmus: rapid movements of the eyes without being able to control them

In most cases, people who become addicted to anxiolytics and sedatives started taking them for medical reasons, such as having anxiety symptoms, insomnia or pain associated with an accident or chronic disease such as fibromyalgia. Dependence can develop in a very short time, in just two weeks of constant use.

Taking into account the severity of the withdrawal syndrome related to anxiolytic psychotropic drugs it is very important that, when starting treatment with them, you are under the supervision of a doctor. He will dose the drug, prescribe how to consume it and, if the two weeks are exceeded, he will initiate the cessation by gradually reducing the dose, never suddenly.

Overdose and treatment

Anxiolytic psychotropic drug overdose gives rise to a picture with the following symptoms, in addition to presenting a risk of death.

• Drowsiness
• Confusion
• Respiratory depression
• Dragging the words when speaking
• Stupor: difficulty being awakened.
• Poor coordination
• Confusion

In the elderly, symptoms can be more severe and can include:

• Dizziness
• Disorientation,
• Delirium
• Loss of balance: causes bone breakdown, especially in the hips.

If you have overdosed on benzodiazepines, you are facing a truly dangerous picture. The person can go into a coma, have a serious alteration of the respiratory and cardiac function and, in addition, can end up dying. It should be said that although this is relatively difficult to happen, since the therapeutic dose is usually much lower than the life-threatening dose in the case of benzodiazepines this must be taken into account, especially in practice surgical

Severe or life-threatening symptoms of benzodiazepines are unlikely compared to barbiturates, due to that benzodiazepines are usually prescribed at doses farther away from dangerous doses, with a significant margin of safety. People can take relatively large amounts of benzodiazepines on their own and not die.

Another different matter is in surgical practice, where the amounts are much higher than those prescribed in psychiatry.

In the event of an overdose due to benzodiazepine, the antidote drug used is flumazenil, which can reverse a severe overdose. However, this drug can trigger benzodiazepine withdrawal and cause seizures in people who have taken benzodiazepines for a long time. Therefore, flumazenil is not usually administered routinely for an overdose. In barbiturate overdoses, doctors may give sodium bicarbonate intravenously to help the person excrete the barbiturate in the urine.

Bibliographic references:

• Adam, A. and Prat, G. (2016). Psychopharmacology: Mechanism of action, effect and therapeutic management. Barcelona, ​​Spain. Marge Medica Books.
• Gómez-Jarabo, G. (1999). Behavioral Pharmacology. Basic manual for psychotherapists and clinicians. Madrid: Synthesis psychology.
• Morón, F.G.; Borroto, R.; Calvo, D.M.; Cires, M.; Cruz, M.A. and Fernández, A. (2009). Clinical pharmacology. Havana: Medical Sciences Editorial; 1-30.
• 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