What are the most commonly prescribed tranquilizers in the United States. How do minor tranquilizers affect brain activity. What are the long-term effects of tranquilizer abuse. How is tranquilizer addiction treated effectively.

Understanding Tranquilizers: Types and Prevalence

Tranquilizers are a class of medications widely prescribed in the United States, with approximately 60 million people receiving prescriptions annually. These drugs are primarily used to treat anxiety, depression, and sleep disorders. Tranquilizers fall under the broader category of sedatives and central nervous system depressants.

There are three main classifications of tranquilizers:

1. Major tranquilizers (antipsychotics)
2. Minor tranquilizers
3. Other medications

Major tranquilizers, or antipsychotics, are primarily used to treat severe mental illnesses such as schizophrenia and mania. These drugs are generally non-addictive and rarely habit-forming. On the other hand, minor tranquilizers, which include benzodiazepines, barbiturates, and sleep aids, have a high potential for abuse and addiction.

Commonly Abused Prescription Tranquilizers

• Benzodiazepines: Xanax, Valium, Ativan, Halcion, Librium
• Barbiturates: Amytal, Nembutal, Tuinal, Seconal
• Sleeping aids: Lunesta, Ambien, Sonata

According to the National Institute on Drug Abuse (NIDA), 2.6 million Americans used tranquilizers and sedatives for non-medical purposes in 2010. A study by the University of Michigan revealed that prescription medications, including tranquilizers, are the second most commonly abused substances among teenagers, following marijuana.

The Mechanism of Action: How Tranquilizers Affect the Brain

Minor tranquilizers exert their effects by slowing down brain activity. This results in various physiological and psychological changes, including:

• Drowsiness
• Slowed breathing
• General sense of relaxation
• Euphoria (in some cases)

When consumed in large doses or combined with other medications, tranquilizers can lead to more severe effects such as blurred vision, muscle weakness, and in extreme cases, coma. It’s crucial to understand that tranquilizers do not provide a cure for any condition; they only offer temporary relief or control for specific symptoms.

Recognizing Tranquilizer Addiction Symptoms

Long-term use of tranquilizers can lead to tolerance, where individuals require higher doses to achieve the same effects. This can ultimately result in addiction. Some common symptoms of tranquilizer addiction include:

• Uncontrollable cravings for tranquilizers
• Surreptitious drug use
• Inability to control drug intake
• Loss of appetite
• Nausea and headaches
• Hallucinations and confusion
• Paranoia
• Persistent coughing and runny nose
• Glazed or red eyes
• Memory lapses
• Lowered inhibitions
• Rapid speech
• Mood swings
• Neglect of personal hygiene and social responsibilities

Can tranquilizer addiction lead to severe health complications? Yes, prolonged abuse of tranquilizers can result in various physical and mental health issues, including respiratory problems, cognitive impairment, and increased risk of accidents due to impaired coordination.

The Dangers of Tranquilizer Abuse and Overdose

Tranquilizer abuse poses significant risks to individuals’ health and well-being. These medications are involved in many suicide attempts and accidental overdoses, highlighting the importance of proper use and monitoring.

Are there immediate steps to take in case of tranquilizer overdose? If you suspect a tranquilizer overdose or poisoning, it’s crucial to seek immediate medical attention. Call emergency services (911 in the United States) or contact the National Poison Control Center at 1-800-222-1222 for guidance.

Signs of Tranquilizer Overdose

• Extreme drowsiness or loss of consciousness
• Slowed or stopped breathing
• Bluish lips or fingernails
• Confusion or disorientation
• Slurred speech
• Unresponsiveness to stimuli

Recognizing these signs early can be life-saving, as prompt medical intervention is crucial in cases of tranquilizer overdose.

Tranquilizer Addiction Treatment Options

Treating tranquilizer addiction requires a comprehensive approach, often involving medical supervision, especially for individuals addicted to benzodiazepines and barbiturates. Abrupt cessation of these drugs can lead to severe withdrawal symptoms, making professional help essential.

Detoxification Process

How is the detoxification process managed for tranquilizer addiction? The detox process typically involves a carefully supervised tapering of the drug dosage. Medical professionals may use short-acting drugs to gradually reduce the patient’s dependence on tranquilizers. This approach helps minimize withdrawal symptoms and reduces the risk of complications.

Inpatient and Outpatient Treatment Options

Long-term abusers of tranquilizers may benefit from inpatient detox and rehabilitation programs. These programs offer:

• 24/7 medical supervision
• Structured environment conducive to recovery
• Therapy sessions (individual and group)
• Holistic treatment approaches

Luxury treatment centers provide private treatment sessions and advanced facilities for a more personalized recovery experience. These centers often cater to patients with co-occurring physical and mental health conditions.

Outpatient programs, on the other hand, allow individuals to receive treatment while maintaining their daily routines. These programs are suitable for those with less severe addictions or as a step-down option after completing an inpatient program.

Cognitive Behavioral Therapy (CBT)

Cognitive Behavioral Therapy (CBT) is a widely used treatment modality for tranquilizer addiction. How does CBT help in addiction recovery? CBT focuses on:

• Modifying the patient’s expectations and behaviors related to drug use
• Developing coping strategies for dealing with cravings and triggers
• Addressing underlying mental health issues that may contribute to addiction
• Improving problem-solving skills and stress management techniques

This therapeutic approach helps patients develop healthier thought patterns and behaviors, reducing the likelihood of relapse.

The Role of Support Groups in Recovery

Support groups play a crucial role in the long-term recovery process for individuals overcoming tranquilizer addiction. These groups offer:

• Peer support and understanding
• Opportunities to share experiences and coping strategies
• Accountability and motivation to maintain sobriety
• Access to resources and information about addiction recovery

Many top inpatient and outpatient recovery centers facilitate access to support groups as part of their aftercare programs. These groups can be instrumental in helping individuals maintain their recovery and prevent relapse.

The Journey to Recovery: Timeline and Challenges

How long does it take to recover from tranquilizer addiction? The recovery timeline varies depending on several factors, including:

• The severity and duration of the addiction
• The specific tranquilizer(s) used
• The presence of co-occurring mental health disorders
• The individual’s overall health and support system

Generally, it may take several weeks to months before tranquilizer addiction symptoms can be effectively managed. However, it’s important to note that recovery is an ongoing process, and preventing relapse can be a lifelong endeavor.

Challenges in Recovery

Individuals in recovery from tranquilizer addiction may face various challenges, including:

• Post-acute withdrawal symptoms
• Cravings and triggers
• Adapting to life without the medication
• Addressing underlying mental health issues
• Rebuilding relationships and social connections

Overcoming these challenges requires dedication, support, and often ongoing therapy or counseling. However, with the right treatment approach and support system, full recovery from tranquilizer addiction is achievable.

Prevention and Education: Key to Reducing Tranquilizer Abuse

Preventing tranquilizer abuse and addiction starts with education and awareness. Healthcare providers play a crucial role in this process by:

• Carefully assessing patients before prescribing tranquilizers
• Educating patients about the potential risks and proper use of these medications
• Monitoring patients for signs of dependence or abuse
• Exploring alternative treatments for anxiety and sleep disorders when appropriate

How can individuals reduce their risk of developing tranquilizer addiction? Some strategies include:

• Taking medications exactly as prescribed
• Avoiding alcohol and other drugs while using tranquilizers
• Regularly communicating with healthcare providers about the medication’s effects
• Exploring non-pharmacological approaches to managing anxiety and sleep issues, such as therapy, meditation, and lifestyle changes

By implementing these preventive measures and increasing public awareness about the risks associated with tranquilizer use, we can work towards reducing the prevalence of tranquilizer addiction and its associated health and social consequences.

In conclusion, while tranquilizers serve an important role in managing various mental health conditions, their potential for abuse and addiction cannot be overlooked. Understanding the effects, recognizing the signs of addiction, and knowing the available treatment options are crucial steps in addressing this growing public health concern. With proper education, prevention strategies, and access to comprehensive treatment programs, individuals struggling with tranquilizer addiction can find their path to recovery and regain control of their lives.

Tranquilizer Addiction – Effects, Symptoms and Treatment Options

Edited By: Editorial Staff

Last updated on September 2, 2021

Tranquilizers are some of the most commonly prescribed medications in the United States, with an estimated 60 million people receiving tranquilizer prescriptions every year. These drugs are indicated for the treatment and control of anxiety, depression and sleep problems. Tranquilizers are called sedatives and central nervous system depressants. Tranquilizer addiction symptoms are also common among prescription and non-prescription users.
“Tranquilizers are some of the most commonly prescribed medications in the United States.”
There are three classification groups of tranquilizers: major tranquilizers, minor tranquilizers, and other medications. Major tranquilizers, or antipsychotics, are mainly used to treat mental illnesses like schizophrenia, mania and other serious issues. Antipsychotics are rarely habit-forming and are non-addictive. Minor tranquilizers, on the other hand, are classified as sedatives and depressants. Drugs that fall in this category are benzodiazepines, barbiturates, and sleep aids. These drugs are habit-forming and have high potential for abuse.

Did You Know?

Tranquilizers are the most prescribed psychotherapeutic drug in the world, and they are involved in many suicide attempts and accidental overdoses.

Tranquilizer Effects and Addiction Symptoms

Minor tranquilizers work by slowing brain activity, leading to drowsiness, slowed breathing, and a general sense of relaxation or euphoria. When taken in large doses or mixed with other medications, they can cause blurred vision or muscle weakness and can even put an addict into a state of coma. Long-term users of the drug can develop tolerance to the drug and may show tranquilizer addiction symptoms, including:

• Uncontrollable cravings for tranquilizers
• Using the drug surreptitiously
• Inability to control drug intake
• Loss of appetite
• Nausea
• Headache
• Hallucinations
• Confusion
• Paranoia
• Persistent coughing
• Runny nose
• Glazed or red eyes
• Memory lapses
• Lowered inhibitions
• Rapid speech
• Mood swings
• Neglect of personal hygiene
• Neglect of family or social responsibilities

According to a survey released by the National Institute on Drug Abuse (NIDA), 2. 6 million Americans used tranquilizers and sedatives for non-medical reasons in 2010. Commonly abused prescription tranquilizers include:

• Xanax, Valium, Ativan, Halcion, Librium (benzodiazepines)
• Amytal, Nembutal, Tuinal, Seconal (barbiturates)
• Lunesta, Ambien, Sonata (sleeping aids)

In 2010, a study done by the University of Michigan showed that after marijuana, prescription medications are the most commonly used drug for non-medical and recreational use among teenagers.

In case of tranquilizer addiction symptoms, poisoning, or overdose, call 911 or 1-800-222-1222 to seek help from the National Poison Control Center.

Did You Know?

Tranquilizers do not provide a cure for any condition; they only offer temporary relief or control for certain conditions.

Tranquilizer Addiction Treatment

Many of the drugs that are classified as tranquilizers need careful supervision during treatment for addiction. If a person is addicted to benzodiazepines and barbiturates, he or she must be treated medically, as these drugs can induce acute withdrawal symptoms when stopped immediately. Tranquilizer addiction symptoms can be treated with a carefully supervised detoxification process using short-acting drugs for gradual dosage reduction.

Long-term abusers of tranquilizers may need to enter an inpatient detox and rehab center for full recovery. Luxury centers offer private treatment sessions and use advanced facilities to treat addiction. The best tranquilizer addiction recovery centers also cater to addicted patients with existing physical and mental conditions.

Another type of treatment used for tranquilizer addiction is cognitive behavioral therapy (CBT). CBT focuses on modifying the patient’s expectations, behavior, and thinking towards these drugs while helping him or her cope with various temptations and life stressors. After the detox and rehabilitation program, the patient can choose to join a local support group. The top inpatient and outpatient drug recovery centers offer one-on-one or group therapy and counseling to help their patients continue to work towards full recovery.

Depending on the severity of the addiction, it may take several weeks to months before tranquilizer addiction symptoms can be treated completely. Prevention of a relapse can be a lifelong battle. It is not impossible to recover from addiction completely with the help of the best detox centers and medical experts, and with the support of family and friends. If you or a loved one is suffering from tranquilizer addiction symptoms and wants to seek treatment, it is best to consult a specialist. Call to discuss treatment options.

Did You Know?

Tranquilizers are also used in non-lethal guns. Tranquilizer guns use sedatives, paralytic agents, or anesthetic to temporarily sedate animals and humans without causing injury.

Unsure where to start? Take Our Substance Abuse Self-Assessment

Take our free, 5-minute substance abuse self-assessment below if you think you or someone you love might be struggling with substance abuse. This evaluation consists of 11 yes or no questions that are designed to be used as an informational tool to assess the severity and probability of a substance use disorder. The test is free, confidential, and no personal information is needed to receive the result. Please be aware that this evaluation is not a substitute for advice from a medical doctor.

Tranquilizers Addiction, Side Effects, Withdrawal, and Treatment Options

January 4, 2020 Drug Addiction

Over 39 million Americans struggle with a tranquilizer addiction. Tranquilizer dependency can be emotionally, physically, and mentally devastating. It can also lead to overdose-related fatality if not treated effectively and immediately. If you believe that you or someone you love has been abusing prescription tranquilizers, it is wise to seek professional help as quickly as possible. 

What Are Tranquilizers?

Tranquilizers classify a chemical substance that is typically professionally prescribed and act as central nervous system depressants. They include medications such as barbiturates and benzodiazepines. Generally, these medications treat conditions such as tension, sleep disorders, panic attacks, acute stress reactions, and acute anxiety disorders. 

Some common brands of tranquilizers include Xanax, Valium, Ativan, Klonopin, and Quaaludes. These are mostly prescription sedatives prescribed to treat anxiety on a short-term basis. Unfortunately, tranquilizers have a high likelihood of abuse, and many who use the medications will begin abusing them at one point or another.

The neurological pathways within the brain begin to shift and alter with continued use, leaving those who consistently take barbiturates and benzodiazepines for extended periods with lasting psychological changes that could increase the risk of eventual dependency. 

As the reward pathways within the brain begin to shift, users start mentally and physically depending on the drugs to keep their minds and bodies in normal functioning order.  

Side Effects 

Unlike other drugs, it’s easy to notice side effects and signs of tranquilizer addiction. Initially, symptoms might be as simple as shaky hands and difficulty sleeping. Over time, side effects can lead to memory loss and even death.

Short-Term Effects

Most prescription sedatives and tranquilizers cause feelings of euphoria in users when taken in large doses. Additionally, tranquilizers have significant impacts on proper cognitive functioning.

Slurred speech, impaired reaction time, and decreased heart rate are all common short-term side effects of tranquilizer abuse. When one initially begins taking a prescribed tranquilizer, it is normal to feel sleepy, sluggish, fatigued, and relatively disoriented for several days. 

As the brain becomes used to this specific chemical, these symptoms are likely to disappear completely. However, abuse of this chemical substance entails that an amount far greater than initially prescribed is consumed.  

If an individual consumes tranquilizers in conjunction with another chemical substance, namely alcohol, they risk respiratory failure and even death.

Long-Term Effects

Prolonged abuse of prescription tranquilizers will often lead to physical and mental dependence. Consuming large quantities of barbiturates or benzodiazepines can lead to impaired judgment, memory loss, feelings of irritability, paranoia, and even suicidal ideations in some cases. Benzodiazepine withdrawal can be fatal, as many individuals experience life-threatening symptoms like seizures, heart attack, stroke, or coma. 

Withdrawal Symptoms to Expect

Once dependence occurs, it will be impossible for an individual to abruptly cease use without experiencing severe and potentially lethal withdrawal symptoms. Tranquilizer withdrawal symptoms can be dangerous as the body is already accustomed to the drug. Symptoms vary from person to person, and they depend on the severity of the abuse. Withdrawal symptoms can start to be noticeable within 6-36 hours and include:

• Seizures
• Convulsions
• Chills
• Psychotic episodes
• Altered reality
• Rage
• Confusion

By the end of the second day of withdrawal, it’s common for symptoms to worsen. Since many of these withdrawal episodes can be life-threatening, attempting to stop any tranquilizer alone might be dangerous. As a result, various addiction treatment options incorporate medical supervision to manage these symptoms. 

Addiction Treatment Options Available

With adequate support, recovery from a tranquilizer addiction is possible. If you or someone you love is struggling with tranquilizer addiction, know that there are treatment options. Though it might feel impossible at the time, take hope in knowing that there are specialists in helping those with tranquilizer addictions.

At Lighthouse Recovery Institute, our team of medical therapists can help those struggling with tranquilizer addiction find purpose in life again. Slowly and steadily, together, we reduce the habit, find ways to stay healthy and look forward to the future.

Tagged benzo’s, benzodiazepines, drug addiction, tranquilizers

Tranquilizers

Tranquilizers (from Latin tranquilo-are – to make calm, serene) are psychotropic drugs that eliminate fear, anxiety, affective tension in neuroses and neurosis-like states. Synonyms of the term are the expressions “anxiolytic drugs” (from English anxiety – fear), “anti-anxiety agents” (antianxiety agents), “ataracts” (from the Greek ataraxia – calmness, equanimity), “antiphobic drugs”, “general sedatives”. Most tranquilizers have practically no antipsychotic effect and the ability to eliminate psychotic fear and anxiety. There are, however, powerful tranquilizers with transient to antipsychotic properties (for example, phenazepam). Tranquilizers do not have a pronounced antidepressant effect, but there are some exceptions in this regard. The main properties of this group of drugs are:

• anxiolytic, eliminating anxiety, fear, tension. To a certain extent, tranquilizers can significantly alleviate the emotional state of psychiatric patients, since their depression, fears, and anxiety are not always directly related to the primary damage to neuropsychic processes, but arise as a reaction to a situation or consciousness of an illness;

• soothing and only in this sense hypnotic, that is, facilitating the onset of sleep, so they are not prescribed if the patient performs work that requires a quick mental and motor reaction. Tranquilizers do not have a direct hypnotic effect, although many of them significantly improve the quality of sleep, in particular, relieve patients from painful dreams. The exception is, perhaps, only such drugs as natrazepam, flunitracepam and triazolam;

• central muscle relaxant, reducing the tonic tension of the striated muscles;

• anticonvulsant; tranquilizers can also be effective for mental seizures;

• the ability to potentiate the effect of alcohol, sedatives, sleeping pills, narcotic and analgesic drugs;

• the ability to cause addiction and side effects, in particular an increase in intraocular pressure;

• stress-protective action, that is, resistance to the effects of stress;

• less antidepressant effect; First of all, we mean not endogenous depressions, but situational and arising as a reaction to the impact of psychotraumatic factors.

The mechanisms of action of tranquilizers are not fully known to date. It has been established that tranquilizers have a very weak effect on the noradrenergic, dopaminergic and serotonergic systems of the brain. However, it was found that benzodiazepine tranquilizers actively affect GABAergic structures and potentiate the central inhibitory effect of gamma-aminobutyric acid. In CNS cells, specific “benzodiazepine” receptors (and their subgroups) have been identified, for which benzodiazepines are exogenous ligands (from Latin ligo – I bind). Diphenylmethane derivatives (amizil, etc.) actively influence the cholinergic systems of the brain, which is why such drugs are called central anticholinergics. Derivatives of propanediol do not have a pronounced effect on benzodiazepine and cholinergic receptors.

This is a group of drugs, the representatives of which differ significantly in the profile of psychotropic activity from each other. So, a pronounced anxiolytic effect is especially characteristic of phenazepam, diazepam, nozepam, lorzepam, alprazolam (described in the section “Other antidepressants”). Sedative-hypnotic action is more represented in nitrazepam, alprazolam, flunitrazepam, triazolam. The anticonvulsant effect is especially pronounced in clonazepam, to a lesser extent in phenazepam, sibazon and nitrazepam. Muscle relaxant action is more characteristic of phenazepam, sibazon, lorazepam. In “daytime” tranquilizers, the anti-anxiety effect prevails. Benzodiazepines are generally well tolerated.

1. Chlozepid (Chlozepidum). Synonyms: Librium, Napoton, Chlordiazepoxide, Elenium, Ansiacal, Droxol, Labiton and more. etc. Until now, it has not lost its significance in the treatment of neurotic conditions with fears, anxiety, affective tension, irritability, impressionability, obsessions, as well as shallow hypochondriacal depression, epilepsy, and alcohol withdrawal.

It is administered orally up to 3-4 times a day, regardless of food intake. Treatment of adults begins with 5-10 mg per day. If necessary, the daily dose is gradually (5-10 mg) increased to 30-50 mg. Reduce the dose also gradually, as there is the possibility of developing a withdrawal syndrome. Weakened and elderly patients are prescribed smaller doses (up to 20 mg / day). Children, depending on age, are prescribed 2.5–5 mg per dose.

Side effects: dry mouth, drowsiness, slight dizziness, unsteady gait, skin itching, nausea, constipation, dysmenorrhea, increased appetite, decreased libido, headache, arterial hypotension, impaired concentration, mental and motor reactions slowdown, memory loss , excitement, aggressiveness, fear, muscle weakness. In some cases, at the beginning of treatment, arousal occurs. Hallucinations, ataxia, changes in the picture of peripheral blood are also described. Sometimes there are paradoxical reactions. The drug potentiates the action of hypnotics and analgesics, in the first 3-5 days of continuous treatment it has a moderate hypnotic effect.

Contraindications for use: hypersensitivity, acute liver and kidney disease, myasthenia gravis, first trimester of pregnancy, drug and alcohol dependence. The drug is not combined with MAO inhibitors and phenothiazine derivatives. During treatment it is not recommended to drink alcohol. Persons whose work requires a quick mental and physical reaction should not take chlosepid on the eve of the working day.

These complications and contraindications to the use of chlosepid are common to other benzodiazepine derivatives.

Presentation: 5 mg tablets in a pack of 50 pieces.

2. Sibazon (Sibazonum). Synonyms: Apourin, Bensedin, Valium, Oxazepam, Relanium, Relium, Seduxen, Apozepam, Bensedin, Diazepam, Saromet, Serensin, Vatran, etc. One of the main benzodiazepine tranquilizers. Indicated for use in the treatment of various neuropsychiatric diseases: neurosis, psychopathy, as well as neurosis-like and psychopathic conditions (with schizophrenia, organic brain lesions, including cerebrovascular pathology and somatic pathology), accompanied by symptoms of emotional stress, anxiety, fear, irritability, senestohypochondriac , obsessive-phobic disorder, sleep disorders. It is also used to relieve psychomotor agitation, anxious agitation in these diseases, status epilepticus, treatment of convulsive paroxysms and mental equivalents in epilepsy, spastic conditions, withdrawal symptoms in alcoholism (together with other drugs). In children’s psychoneurological practice, it is used in the treatment of neurotic and neurosis-like conditions with the indicated symptoms, as well as headaches, enuresis, mood and behavior disorders. In somatic medicine, it is used in the treatment of itching dermatosis, gastric ulcer, cardiac arrhythmia, in preparation for operations.

It is administered orally, intramuscularly and intravenously. For adults, when taken orally, the drug is prescribed starting from 2.5-5 mg / day 1-2 times, regardless of food intake. If necessary, a single dose is gradually increased to 5-10 mg, and in some cases – up to 20 mg. The daily dose for inpatient treatment can reach 45 mg, for outpatient treatment – 25 mg. The maximum daily dose is 60 mg (in 2-3 doses). Dose reduction is also gradual. Weakened and elderly patients are prescribed 2.5 mg 1-2 times a day. Single and daily doses for children aged 1 to 3 years are 1 mg and 2 mg, respectively, from 3 to 7 years – 2 mg and 6 mg, from 7 years and older – 3-5 mg and 8-10 mg. For older children, if necessary, the daily dose can be increased to 14-16 mg. The duration of the course of treatment should not exceed 2 months (danger of developing addiction to the drug!).

In / in (drip or jet) and / m sibazon is administered to adults in the treatment of diseases that are accompanied by excitation, convulsions; in the relief of status epilepticus, acute anxiety-depressive and anxiety-phobic conditions of various origins, including withdrawal and psychosis in alcoholism. The average single dose in this case is 10 mg (2 ml of a 0.5% solution), the daily dose is 30 mg, and the maximum dose is 30 mg and 70 mg, respectively. A sedative effect is observed a few minutes after i / v and 30-40 minutes after i / m administration of the drug. Actually therapeutic effect is detected after 3-10 days.

Status epilepticus is stopped by intravenous (slow!) infusion of 10–40 mg of sibazon. Its repeated introduction is done in / in or / m every 3-4 hours. This technique is especially effective if the status of generalized seizures begins to be stopped in the first 3 hours after its onset.

Possible complications, contraindications to the appointment of sibazon are basically the same as in the treatment of chlosepid. When administered intravenously and intramuscularly, the drug should not be mixed with others (to avoid precipitation).

Presentation: 5 mg tablets in a pack of 20; tablets for children 1 mg and 2 mg in a package of 20 pieces; 0.5% solution in ampoules (Solutio Sibazoni pro injectionibus) 2 ml per pack of 10 ampoules. Sibazon is an integral part of the sleeping pill Reladorm.

3. Phenazepam (Phenazepamum). surpasses other tranquilizers in terms of the strength of the tranquilizing effect, it also has a pronounced anticonvulsant, muscle relaxant and hypnotic effect. In terms of anti-anxiety activity, it is not inferior to some antipsychotics. When used together with sleeping pills and narcotic drugs, their mutual potentiation occurs. It is indicated for use in the treatment of neurosis, neurosis-like, psychopathic, psychopathic and reactive conditions, in which anxiety, fear, affective tension, emotional excitability are presented, as well as obsessive-phobic, hypochondriacal phenomena and panic attacks. Used in the treatment of alcohol withdrawal, epilepsy, sleep deprivation.

It is administered orally, regardless of food intake, 2-3 times a day. The daily dose for adults in the hospital can reach 3-5 mg, in outpatient practice – 1.5 mg. In the treatment of epilepsy, it is prescribed in a dose of 2 to 10 mg / day, as a sleeping pill – up to 2.5 mg per dose (20-30 minutes before bedtime). The relief of alcohol withdrawal requires the appointment of 2.5 to 5 mg / day. The maximum daily dose should not exceed 10 mg.

Possible side effects and contraindications for use are the same as in the treatment with chlosepid and sibazon. More often observed, however, ataxia, drowsiness, muscle weakness, dizziness.

Presentation: 0.5 mg and 1 mg tablets in a pack of 50 pieces; tablets of 2.5 mg in a package of 20 pieces.

4. Nozepam (Nozepamum). Synonyms: Apo-oxazepam, Medazepam, Rudotel, Tazepam, Oxazepam, Oxazepam, Rondar, Serax, etc. Its properties are similar to chlozepid and diazepam, but inferior to them in terms of strength. Somewhat less toxic than them, in some cases better tolerated, especially by elderly and somatically debilitated patients. Indications for use, side effects, contraindications for use are similar to those in the treatment with chlosepid.

It is administered orally, regardless of food intake, 2-3 times a day. The initial single dose for adults is 5–10 mg, the average therapeutic dose per dose is 20–30 mg.

Presentation: 10 mg tablets in a pack of 50 pieces.

5. Lorazepam. Synonyms: Apo-lorazepam, Ativan, Lorafen, Merlit, Trapeks, etc. Similar to triazolam (see below). It has a pronounced tranquilizing activity, can be used in the treatment of mental disorders (panic attacks, reactive psychoses, subpsychotic phenomena). Indications for use, side effects, contraindications to the appointment are similar to those in the treatment of Chlosepid.

It is administered orally, regardless of food intake, 2-3 times a day. In neurotic conditions, it is prescribed at a dose of 1.25-5 mg / day, in the treatment of psychosis – up to 15 mg / day.

Presentation: 2.5 mg tablets in a pack of 50 pieces.

6. Bromazepam. Synonyms: Bromazep, Lexotan, Bartul, Deptran, Pascalium and more. other Anxiolytic with sedative-hypnotic, anticonvulsant and muscle relaxant effects. By action, indications for use, side effects and contraindications to the appointment is close to other benzodiazepines. With a single dose, it has a short-term effect.

It is prescribed orally, regardless of food intake, 2-3 times a day at a dose of up to 36 mg / day (in a hospital setting), in outpatient practice – 1. 5-3 mg per dose.

Composition: 1.5 mg, 3 mg and 6 mg tablets.

7. Mezapam (Mezapamum). Synonyms: Nobrium, Rudotel, Anxitol, Imazepam, Merlit, Stratium and more. other Features of the action of the drug are less pronounced muscle relaxant and general inhibitory effect, the presence of some stimulating radical. It is considered a “daytime” tranquilizer, suitable for the treatment of children, the elderly and somatically debilitated patients. Indications, contraindications for use, side effects are generally similar to those in the treatment of other benzodiazepines, excluding acute states of fear and anxiety, reactive psychosis, status epilepticus.

Administered orally 2-3 times a day, regardless of food intake. The average daily dose for adults is 30-40 mg, the highest – 60-70 mg. The elderly and adolescents are prescribed up to 20-30 mg / day, children aged 1-2 years – 2-2.5 mg / day, from 3 to 6 years – 3-6 mg / day, from 7 to 10 years – 6-24 mg / day.

Presentation: 10 mg tablets; granules (20 pieces, contain 40 mg of mezapam) for the preparation of a suspension for children in jars labeled 100 ml. The suspension is prepared in freshly boiled chilled water.

8. Gidazepam (Gidazepamum). Interacts with benzodiazepine receptors in the limbic system, in the intercalary neurons of the lateral horns of the spinal cord. It has an anxiolytic, anticonvulsant and weak muscle relaxant effect. Refers to the “daytime” tranquilizers, does not have a hypnotic effect. Unlike many tranquilizers, it has a psychoactivating effect. Indications and contraindications for use, side effects are generally the same as in the treatment with chlosepid. Gidazepam is also prescribed in the treatment of migraine.

Administered orally with or without food 3 times a day, starting at 6–15 mg/day. The dose is gradually increased to 60-200 mg / day. With migraine and logoneurosis, the therapeutic dose is 40-60 mg / day. The duration of the course of therapy is from several days to 3-4 months.

9. Clobazam. Synonyms: Frizium, Clarmyl, Frizin, Sentil, Urbanil, etc. Anxiolytic with anticonvulsant action. Indicated for the treatment of painful conditions with acute and chronic fear, as well as an additional remedy – epilepsy, dysphoria, aggressiveness.

It is administered orally, regardless of food intake, 2-3 times a day. The dose for adults with neurotic conditions is 10-20 mg / day, with a feeling of fear – from 20 to 30 mg / day. Children under the age of 3 years, the drug is not prescribed, older than 3 years, as well as older patients, reduced doses are recommended. In the treatment of epilepsy, the initial dose of the drug is 5-15 mg / day, it can be increased to 80 mg / day (maximum daily dose). Increasing and decreasing doses should be gradual; as with other tranquilizers, withdrawal symptoms may occur.

Side effects, contraindications for use are the same as in the treatment of other benzodiazepines. In the treatment of high doses and for a long time, there may be articulation disorders, diplopia, nystagmus, in elderly patients – impaired consciousness.

Composition: 5 mg and 10 mg tablets.

10. Alprazolam – see “Other antidepressants”.

11. Tetrazepam. Synonyms: Myolastan, Myolastan. Anxiolytic with a pronounced muscle relaxant effect. It is indicated for the treatment of mainly muscle contractures, tendovaginitis, myositis, accompanied by muscle pain.

Administered orally with or without food 2-3 times a day at adult doses of 50 to 150 mg/day.

Side effects, contraindications for use are the same as in the treatment of other benzodiazepines.

Presentation: 50 mg tablets in a pack of 20.

12. Signopam. Synonyms: Temazepam, Euhuphos, Levanxene, Normison, Planum, Texapan, Veroqual, etc. Anxiolytic with mild antidepressant effect. It is indicated for the treatment of neurosis and neurosis-like conditions, especially those accompanied by depressed mood and hypochondriacal phenomena; shallow depressions, increased neuropsychic excitability in thyrotoxicosis. It has a pronounced anticonvulsant and antidysphoric effect.

Assigned orally, regardless of food intake, 10 mg 2-3 times a day (adults). The dose can be increased to 40 mg / day (in 2-3 doses). The increase and decrease in doses is gradual, within 7-10 days.

Side effects: may be (rarely) drowsiness, fatigue, dizziness, allergic skin reactions, decreased libido, dysmenorrhea, in some cases – disorientation. Drinking alcohol, driving a vehicle is prohibited.

Contraindications for use: hypersensitivity, drug and alcohol dependence.

13. Tranxene. Synonyms: Anxidin, Belseren, Tranex, Tranxilen. Anxiolytic with sedative, muscle relaxant and anticonvulsant action. Can be used to relieve psychomotor agitation when administered parenterally. Assigned inside, in / m and / in. The average therapeutic dose when taking the drug by adults inside is 10-30 mg / day. The dose may be increased to 50–100 mg/day. For elderly and senile patients, the drug is prescribed in reduced doses. To stop psychomotor agitation, attacks of aggressiveness, the drug is administered intramuscularly or intravenously at a dose of 20 to 200 mg / day.

Side effects: drowsiness, muscle weakness, anterograde amnesia, euphoria, paradoxical mental reactions (increased fear, aggressiveness, etc.). With a sharp decrease in dosages, the development of a withdrawal syndrome is possible.

Contraindications for use: hypersensitivity, respiratory and heart failure, pregnancy, breastfeeding, children’s age.

14. Nitrazepam. Synonyms: Berlidorm, Neozepam, Radedorm, Eunoctine, Apodorm, Benzalin, HinpaxInsomin, Magadon, Nitrodiazepam, Senerex and more. etc. It increases the sensitivity of benzodiazepine receptors to the mediator, enhances the inhibitory effect of GABA in the central nervous system, reduces the excitability of cells in the cortex and subcortical areas of the brain, inhibits cells of the reticular formation. It has a tranquilizing, muscle relaxant, anticonvulsant effect, inhibits conditioned reflexes, suppresses polysynaptic spinal reflexes. A distinctive feature is its hypnotic, hypnotic effect, it lengthens sleep and improves its quality. Indicated for the treatment of various sleep disorders, neuroses and psychopathies with symptoms of anxiety, fear, affective tension. In combination with other drugs, it is used in the treatment of schizophrenia, affective and schizoaffective psychoses, some organic and toxic damage to the central nervous system, in particular cerebrovascular disorders and chronic alcoholism. In combination with anticonvulsants, it is used in the treatment of epilepsy.

Assigned orally, regardless of food intake. As a hypnotic, it is used once half an hour before bedtime at a dose of 5-10 mg for adults, 2.5-5 mg for elderly patients. For this purpose, the drug is also prescribed to children at a lower dose: under the age of 1 year – 1.25-2.5 mg; from 1 year to 5 years – 2.5-5 mg; from 6 to 14 years – 5 mg. The maximum single dose as a hypnotic for adults is 20 mg.

As a tranquilizer and anticonvulsant, nitrazepam is used 2-3 times a day, 5-10 mg (adults). If necessary, the dose in the treatment of epilepsy may be increased. The highest daily dose of the drug is 30 mg. The course of treatment averages 4-6 weeks.

Side effects: daytime sleepiness, feeling of lethargy, ataxia, impaired coordination of movements, headache, stupor, dizziness, less often nausea, tachycardia, hyperhidrosis, skin-allergic reactions. In most cases, these phenomena are observed in elderly and somatically debilitated patients. The dose of the drug should be reduced or treatment should be stopped.

Contraindications for use: first trimester of pregnancy, myasthenia gravis, liver and kidney disease with dysfunction, work of patients, if they require a quick mental and physical reaction. The consumption of alcoholic beverages is prohibited. It should be borne in mind the possibility of enhancing the action of analgesics and other neurotropic drugs.

Presentation: 5 mg tablets in a package of 20 pieces.

15. Flunitrazepam. Synonyms: Rohypnol, Somnubene, Hypnodorm, Narcozep, Primum, Sedex, etc. Close to nitrazepam. It has a sedative, hypnotic, anticonvulsant effect. Indicated for the treatment of insomnia. In anesthesiology practice, they are used for premedication and immersion in anesthesia.

Administered orally half an hour before bedtime at a dose of 1–2 mg for adults, 0.5 mg for elderly patients; children under the age of 14 are prescribed extremely rarely and only 0.5-1 mg. Parenterally used for sedation (IM 1-2 mg), for anesthesia – IV 1 mg (injected slowly).

Side effects and contraindications for use are the same as for nitrazepam treatment. There is a possibility of developing a withdrawal syndrome.

Presentation: 2 mg tablets in packs of 10, 30 and 100 pieces; in ampoules of 2 mg of the drug and with the application of ampoules with 1 ml of sterile water for injection, in a package of 25 ampoules (it is impossible to administer the drug without a solvent).

16. Triazolam (Triazonam). Synonyms: Somneton, Halcyon, Apo-Triazo, Clorazolam, Nuctan, Somneton, Songar, etc. Close in structure to alprazolam. Short acting hypnotic, other aspects of action not well understood.

Administered orally 20-30 minutes before bedtime at a dose of 0.25-0.5 mg (adults).

Presentation: 0.25 mg (blue) and 0.5 mg (white) tablets. Foreign analogues of triazolam: Flurazepam (Flurazepam), synonyms – Benozil,

Fluzepam, Waldorm and others; Lorazepam (Lorazepam), synonyms – Almazin, Ansilor, Ativan, Durazolam, Sedatival, etc.; Tomazepam (Tomazepam), synonyms – Cerepax, Levaxol, Temazepam, Temazin, etc.

17. Zopiclone (Zopiclone). Synonyms: Piklodorm, Relaxon, Somnol. Activates GABAergic mechanisms of synaptic transmission in the brain. It has a sedative and hypnotic effect. It is prescribed mainly for the treatment of deficiency and deterioration in the quality of sleep of various origins, including depression, as well as in the treatment of nocturnal asthma (in combination with theophylline).

It is administered orally half an hour before bedtime as a single tablet of 7. 5 mg (adults), for elderly patients – ½ tablet. The course of treatment is no more than 1 month. The maximum dose is 15 mg.

Side effects: lethargy, drowsiness, bitter and metallic taste in the mouth, nausea, irritability, depressed mood, withdrawal syndrome, allergic skin reactions, impaired consciousness. The drug reduces the concentration of trimipramine in the blood, reduces its effect. Enhances the effect of sedatives and alcohol.

Contraindications for use: hypersensitivity, severe respiratory failure, pregnancy, breastfeeding, under 15 years of age.

Release form: 7.5 mg tablets.

18. Estazolam. Excites benzodiazepine receptors, enhances GABAergic transmission and its inhibitory effect. Anxiolytic with sedative, hypnotic and central muscle relaxant action. Indicated for the treatment of neurosis and neurosis-like conditions with depressive-phobic symptoms, anxiety, affective tension, sleep disorders, and epilepsy (as an adjuvant).

It is administered orally, regardless of food intake, several times a day. The average therapeutic dose for adults is 4-6 mg / day. Tablets should be swallowed whole with a small amount of water. As a hypnotic, 2-4 mg are prescribed (elderly patients – 1 mg each) half an hour before bedtime. The increase and decrease in dosages is gradual, with prolonged treatment there may be a withdrawal syndrome with anxiety, anxiety, fears. The use of alcohol is prohibited.

Side effects: daytime sleepiness, fatigue, weakness, irritability, headache, dizziness, ataxia, disorientation, impaired memory and thinking, addiction, dependence. The drug enhances the effect of sedatives. It should be used with caution in persons whose work requires a quick physical and mental reaction. A paradoxical reaction to the drug is possible.

Contraindications for use: hypersensitivity, myasthenia gravis, ataxia, severe respiratory failure, impaired consciousness, angle-closure glaucoma, dependence on alcohol and drugs, pregnancy, breastfeeding, age under 18 years.

Presentation: 1 mg tablets.

19. Clonazepam (Clonazepame). Synonyms: Antelepsin, Rivotril, Clonopin, Ictorivil, Rivatril, etc. Interacts with benzodiazepine receptors, has a GABAergic effect in the limbic system, reticular formation, intercalary neurons of the spinal cord. Reduces the excitability of the subcortical structures of the brain and disrupts their interaction with the cerebral cortex. Anxiolytic with anticonvulsant, antiepileptic and sedative activity, has a hypnotic and central muscle relaxant effect. It is used mainly for the treatment of epilepsy with grand, temporal, focal and small seizures, paroxysmal fear syndromes, phobias (in patients over 18 years of age) and manic states, especially in epilepsy; psychomotor agitation in reactive psychoses, as well as insomnia and muscle hypertension.

It is administered orally, regardless of food intake, 3 times a day. The initial dose for adults is 4.5 mg / day. The dose can be gradually, every 3 days, increased by 0. 5-1 mg to 4-8 mg / day. The maximum dose is 20 mg / day. In the syndrome of paroxysmal fear in adults, 1 mg / day is prescribed, a maximum of up to 4 mg / day. The dose for children is 0.01-0.03 mg / kg / day for 3 doses. Children under the age of 1 year are given 0.1-1 mg / day, from 1 year to 5 years – 1.5-3 mg / day, from 6 to 16 years – 3-6 mg / day. The maximum dose for children is 0.05 mg / kg / day for 3 doses.

Side effects: drowsiness, dizziness, ataxia, choreic hyperkinesis, dysarthria, weakness, fatigue, nervousness, insomnia, visual disturbances, memory and speech disorders, emotional lability, hypersalivation or xerostomia, constipation, abdominal pain, muscle pain, dysmenorrhea , increased urination or urinary retention, decreased appetite and libido, depression, disorientation, paradoxical reactions to the drug, allergic skin reactions, alopecia, hirsutism, erythro-, leuko- and thrombocytopenia, increased blood levels of transaminases and alkaline phosphatase, withdrawal syndrome, addiction, dependence etc. The drug enhances the effect of barbiturates, neuroleptics, antidepressants, anticonvulsants, narcotic analgesics, alcohol and drugs that lower the tone of skeletal muscles. When drinking alcohol, cases of pathological intoxication were noted.

Contraindications for use: hypersensitivity, impaired liver and kidney function, myasthenia gravis, pregnancy, impaired consciousness, central respiratory failure, respiratory failure, glaucoma.

Presentation: 0.5 mg and 2 mg tablets.

Back to content

Tranquilizers in obstetric and gynecological practice | Serov V.N., Baranov I.I.

Tranquilizers (from the Latin tranquillium – “calm”) are one of the most important groups of psychotropic drugs. Recently, they are increasingly called anxiolytics (from Latin anxius – “anxious” game. lysis – “dissolution”). Tranquilizers have been known for more than half a century, the development of the first drugs of this group dates back to the 50s of the twentieth century – the period of the birth of scientific psychopharmacology. Today, the group of tranquilizers has more than 100 drugs, active work continues to create new and improve existing drugs.

The mechanisms of action of anxiolytics are still not fully understood. The action of anxiolytics is manifested by reducing the excitability of the subcortical areas of the brain (limbic system, thalamus, hypothalamus) responsible for the implementation of emotional reactions, inhibition of the interaction of these structures with the cerebral cortex, as well as inhibition of polysynaptic spinal reflexes.
The most important property of tranquilizers is the elimination of anxiety, feelings of anxiety and fear, a decrease in internal tension, increased irritability, insomnia and other manifestations of neurotic, neurosis-like, psychopathic and psychopathic states, autonomic dysfunctions. In addition to the anxiolytic proper, the main clinical and pharmacological effects of tranquilizers include sedative, muscle relaxant, anticonvulsant, hypnotic, vegetative stabilizing, and amnestic. Many anxiolytics are capable of causing drug dependence. These properties are expressed to varying degrees, which must be taken into account when choosing a drug for a particular patient. The improvement of the group under consideration is carried out in the direction of creating drugs with isolated anxiolytic properties, which leads to minimization of side effects.
Among psychotropic drugs, tranquilizers are the most widely used in both inpatient and outpatient settings. The scope of their use goes far beyond psychiatry, covering somatic diseases, neurology, surgery, anesthesiology, oncology, dermatology, gerontology, pediatrics, narcology and, of course, obstetrics and gynecology.
There are several classifications of tranquilizers in the literature. Earlier classifications are based on the features of their chemical structure, duration of action, clinical use. So, in terms of the number of drugs, benzodiazepine derivatives are in the lead, among which there are long-acting, intermediate-acting and short-acting drugs. Derivatives of diphenylmethane, 3-methoxybenzoic acid, quinuclidine, azaspirodecanedione, and esters of substituted propanediol are presented separately. Traditionally, the so-called “daytime tranquilizers” are distinguished, in which the anxiolytic effect proper predominates and sedative, hypnotic, and muscle relaxant effects are minimally expressed. These drugs can be prescribed on an outpatient basis during the day.
Later classifications take into account the mechanism of action of tranquilizers, which is especially important both for understanding the pharmacodynamics and the essence of side effects, and for determining the main directions for the development of a new generation of drugs. In particular, D.A. Kharkevich [6] classifies the most important tranquilizers into benzodiazepine receptor agonists, serotonin receptor agonists and drugs of various types of action, including membrane modulators of the GABA-benzodiazepine receptor complex, primarily Afobazole, which will be given special attention in the future.
Along with the peculiarities of the mechanism of action, the dose and duration of use, the effect of tranquilizers is also influenced by the pharmacogenetic factor – a genetically determined type of the body’s response to emotional stress [3]. According to S.B. Seredenin [5], in clinical studies it was found that in asthenic patients with neurosis, a tranquilizing-activating effect is observed, and in sthenic patients, a tranquilizing-sedative effect of benzodiazepines is observed. In healthy volunteers with high performance in an emotionally stressful environment, benzodiazepines cause sedation, and in the case of a disorganizing effect of stress, an increase in performance. The dependence of the effect on the phenotype of the emotional-stress reaction also takes place in Afobazole.
The change in the action of tranquilizers can also be influenced by such a factor as the mineral composition of the diet (in particular, an increased level of dietary intake of sodium chloride). The decrease in the effectiveness of anxiolytics is obviously due to the fact that increased consumption of sodium chloride contributes to the weakening of GABAergic inhibitory processes [7].
In general, tranquilizers, unlike other psychotropic drugs (neuroleptics, antidepressants), are characterized by the absence of severe side effects and good tolerance. IN AND. Borodin [2] identifies the following main side effects that occur when using tranquilizers:
• hypersedation – dose-dependent daytime sleepiness, decreased wakefulness, impaired coordination of attention, forgetfulness, etc.;
• muscle relaxation – relaxation of the skeletal muscles, manifested by general weakness, weakness in individual muscle groups;
• “behavioral toxicity” – a mild impairment of cognitive functions and psychomotor skills, manifested even in small doses and detected during neuropsychological testing;
• “paradoxical” reactions – increased aggressiveness and agitation (excited state), sleep disturbances, usually disappearing spontaneously or after a dose reduction;
• mental and physical dependence that occurs with prolonged use (6-12 months continuously), the manifestations of which resemble neurotic anxiety.
These manifestations of side effects are most characteristic of benzodiazepines, which can also cause arterial hypotension (especially when administered parenterally), dry mouth, dyspepsia (nausea, vomiting, diarrhea or constipation), increased appetite and food intake, dysuria, impaired sexual desire and potency.
In terms of frequency, lethargy and drowsiness are leading, occurring in about 10% of cases, including the next day as part of “residual effects” after taking the drug in the evening the day before. Dizziness and incoordination associated with muscle relaxation are 5–10 times less common. However, in old age, the side effects in question become more frequent.
Due to the adverse effect on the fetus, anxiolytics are contraindicated during pregnancy. Tranquilizers, especially benzodiazepines, easily cross the placenta. Thus, the concentration of diazepam in the blood of the umbilical cord exceeds its concentration in maternal blood. The level of diazepam and oxazepam in the child’s blood increases slowly due to the high degree of connection of these drugs with the blood proteins of a pregnant woman, but subsequently they create a higher concentration in the child’s blood serum, firmly binding to its proteins [4]. Elimination of these drugs and their metabolites occurs several times slower than in adults. Children, especially in the prenatal and early postnatal period, have an increased sensitivity to depressant effects on the central nervous system, and tranquilizers easily accumulate in their bodies.
When prescribing benzodiazepines during pregnancy to women with epilepsy, it should be taken into account that there are reports of an increased incidence of birth defects in children whose mothers took anticonvulsants during pregnancy, but a causal relationship between these facts has not yet been established. On the other hand, in women taking anticonvulsants, their withdrawal before or during pregnancy is possible only in cases where epileptic seizures are mild and rare in the absence of treatment and if the likelihood of an epileptic state and withdrawal symptoms is assessed as low.
The use of benzodiazepine derivatives in the third trimester of pregnancy (especially in the last weeks) can lead to accumulation of the drug in the tissues of the fetus and, as a result, to CNS depression in newborns. At the same time, newborns may experience muscle weakness, hypothermia, respiratory depression, and a violation of the sucking reflex. Long-term use of benzodiazepines during pregnancy, incl. in later stages, may lead to physical dependence and withdrawal symptoms in the newborn. In newborns, the metabolism of benzodiazepines is slower than in adults, as a result of which these drugs and their metabolites can accumulate in the body and cause sedation. In this case, feeding difficulties and weight loss in newborns are possible.
As for the safety of a single use of diazepam during childbirth for anesthetic purposes, it does not lead to significant deviations in the condition of the newborn. Tranquilizers pass into breast milk. In particular, diazepam creates a 10 times lower concentration in it than in the blood. If it is necessary to use tranquilizers by a nursing woman, breastfeeding should be stopped. Speaking about the teratogenicity of tranquilizers, one cannot help but recall thalidomide, which in the 60s of the twentieth century caused the massive appearance of severe limb anomalies in children in Western Europe.
The problem of drug dependence on tranquilizers is interpreted by experts ambiguously. Most authors agree that its risk is directly proportional to the duration of treatment with tranquilizers. Dependence on benzodiazepines is especially likely.
Withdrawal syndrome indicates the occurrence of physical dependence. Its manifestations are gastrointestinal disorders, sweating, tremor, drowsiness, dizziness, headache, intolerance to sharp sounds and smells, tinnitus, irritability, anxiety, insomnia, depersonalization. As a rule, it runs smoothly. The severity and duration of withdrawal disorders can be underestimated and mistaken for neurotic manifestations of the patient’s illness. At the same time, there are frequent examples of long-term (months and even years) use of benzodiazepines without the difficulties of subsequent withdrawal, which is facilitated by a certain tactic of treatment and withdrawal of the drug. To prevent withdrawal in long-term treatment, use lower doses, fractional short courses of therapy, and withdrawal within 1-2 months against the background of psychotherapy or placebo.
In the origin of addiction, the role of psychological mechanisms is great. The likelihood of its occurrence is highest in individuals with cognitive and behavioral disorders, excessive fixation on somatic symptoms, an irrational belief in the power of drugs and the expectation of severe withdrawal symptoms [1].
Regarding drug interactions of tranquilizers, it should be noted that any (even anxioselective) drugs of this group should not be combined with alcohol. Severe drowsiness, psychomotor retardation, and even respiratory depression are possible. Due to the potentiation of the inhibitory effect on the central nervous system, benzodiazepines should not be combined with phenothiazine antipsychotics. Accounting for side effects, contraindications, drug interactions of tranquilizers is necessary to improve the safety of the use of these most widely used psychotropic drugs.
Thus, the main disadvantage of benzodiazepine tranquilizers is that all their effects appear simultaneously. Therefore, the world’s leading pharmacological laboratories are constantly searching for tranquilizers that would not be inferior to benzodiazepine drugs in their activity, but would not show hypnosedative, muscle relaxant and amnesic effects.
It has been proven that, depending on the characteristics of the nervous system, genetically determined, some people behave actively, looking for a rational way out of an unfavorable situation, while others act passively, stress paralyzes them morally. Benzodiazepines eliminate manifestations of anxiety and fear in those who are unstable to stress, but in people with active behavior under these conditions they cause drowsiness, lethargy and disorganize their behavior. So, the task was to create a drug that would have the desired effect on passive individuals, but would not negatively affect the behavior of active ones.
As a result of a long experimental search, such a compound was found among mercaptobenzimidazole derivatives and named Afobazol. This compound prevents the development of disorders in the GABA-benzodiazepine receptor that occurs in “passive” animals during the formation of an emotional-stress reaction. Most likely, this action of Afobazole is due to its antiradical properties, which prevent membrane-dependent changes in the receptor site of the nerve cell.
Conducted experimental studies convincingly proved the dependence of the action of tranquilizers on the phenotype of emotional stress reactions in both animals and humans. The fundamental significance of this phenomenon is the pharmacological confirmation of the genetic heterogeneity of emotional stress reactions, which makes it obvious that it is necessary to develop pharmacological preparations specific for a particular phenotype of reactions to stress. The data obtained also open up the possibility of individual typing of emotional stress reactions using a benzodiazepine test. The development and testing of the test seems promising for solving the problems of professional selection and other issues when it is important to predict the hereditary form of the reaction to stress.
Afobazole has a positive effect on patients with anxiety disorders and passive reactions to stress, without causing them sedative and muscle relaxant effects. With its use, drug dependence is not formed and withdrawal syndrome does not develop. The action of the drug is realized mainly in the form of a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effect. Reduction or elimination of anxiety (concern, apprehension, apprehension, irritability), tension (shyness, tearfulness, anxiety, inability to relax, insomnia, fear), and therefore somatic (muscular, sensory, cardiovascular, respiratory, gastrointestinal symptoms), vegetative (dry mouth, sweating, dizziness), cognitive (difficulties in concentrating, impaired memory) disorders are observed on the 5-7th day of treatment with Afobazole. The maximum effect is achieved by the end of the 4th week of treatment and persists in the post-therapeutic period (average 1-2 weeks). The use of the drug is especially indicated in patients with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, a tendency to emotional and stressful reactions.
The results of clinical trials have shown that Afobazole has a combination of anti-anxiety, vegetative-stabilizing and moderately pronounced activating effects, eliminates painful bodily sensations associated with anxiety and anxiety-depressive disorders, is well tolerated, does not cause daytime sleepiness, muscle relaxation, does not worsen, and in some cases restores impaired cognitive functions, while taking the drug does not develop addiction and “withdrawal syndrome”.
In gynecological practice, the use of Afobazole is promising in such pathological conditions as menstrual, menopausal and post-castration syndromes.
Premenstrual syndrome (PMS) is a complex pathological symptom complex that occurs during premenstrual days and is manifested by neuropsychic, vegetative-vascular and metabolic-endocrine disorders. The frequency of PMS varies widely in different age periods and after the age of 30 occurs in almost every second gynecological patient.
The pathogenesis of PMS is complex and poorly understood, as evidenced by the emergence of many theories to explain it. Disturbance of the balance of vegetative influences during the menstrual cycle largely determines the nature and severity of the clinical manifestations of PMS.
In the treatment of patients with PMS, along with psychotropic drugs, vegetotropic drugs are widely used, since the clinical manifestations of the disease are realized through vegetative segmental apparatuses. We carried out a comprehensive study of autonomic disorders in patients with premenstrual syndrome and an assessment of the therapeutic efficacy of Afobazole, as a drug with pronounced vegetotropic activity for their correction.
In order to identify the effectiveness of Afobazole for the correction of autonomic disorders in all patients with PMS, the drug was prescribed as monotherapy for a 4-week course (10 mg 3 times a day).
Analysis of the results of the study showed that in patients with PMS, as the severity of the disease increased, the state of the initial vegetative tone in the 1st phase of the menstrual cycle in most cases was represented by its extreme variants – severe parasympathicotonia and sympathicotonia, which are responsible for many clinical manifestations of this disease.
With initial normotonia, sympathicotonia or mixed vegetative tone, treatment with Afobazole was quite effective without prior preparation with sympathomimetics. With sympathicotonia, the mechanisms of increased activity of the sympathetic-adrenal system and the sensitivity of adrenergic receptors predominate, therefore, the most positive positive clinical effect was observed during treatment with Afobazol. Therefore, in order to optimize the treatment process, it is necessary to take into account the functional state of the ANS for the individual selection of combinations of vegetative correctors.
The long history of the existence of the problem of pathological menopause, its unresolved reflect a typical example of the discrepancy between theoretical knowledge and practical results. For several decades, there has been an accurate scientific understanding of the mechanisms of occurrence, formation and transformation of menopausal disorders. However, the effectiveness of therapeutic interventions remains insufficiently high.
The most pronounced neurosis-like (organic genesis) symptoms are expressed in the asthenic variant, and neurotic (psychogenic) in the hysterical, while in senesto-hypochondriacal the proportion of neurosis-like is greater than neurotic, and in anxiety-depressive, on the contrary, neurotic disorders predominate.
The distribution of clinical variants of climacteric syndrome revealed in the clinic reflects the mechanisms of their formation, knowledge of which is essential in choosing a therapy strategy. The effectiveness of the treatment of patients with menopausal syndrome, including mental and vegetative manifestations, depends on how correctly the drugs are chosen.
Taking into account the mechanisms of development of clinical manifestations of climacteric syndrome, at present it seems appropriate to choose the following strategies for the treatment of climacteric disorders: hormonal, replacement, psychopharmacological and psychotherapeutic. The first two should be classified as pathogenetically oriented. With the help of hormonal preparations containing estrogens and androgens in various proportions, as well as antipsychotics and tranquilizers that have an effect on the hypothalamic structures, it is possible to prevent or stop vegetative-vascular and borderline mental menopausal disorders.
We have conducted studies to evaluate the effectiveness of Afobazole in various types of psychopathological climacteric disorders in comparison with other psychotropic drugs previously used and used in the treatment of climacteric syndrome. Afobazole proved to be a highly effective drug in the relief of asthenic and, to a lesser extent, anxiety-depressive variants. It significantly more often than diazepam stopped or significantly weakened the psychopathological manifestations of climacteric syndrome within the asthenic variant and more often than mebicar stopped the manifestations of anxiety-depressive variant of menopausal mental disorders proper. With the help of Afobazole, it was possible to stop or significantly reduce the vegetative-vascular manifestations of menopausal syndrome and asthenic manifestations within one and a half to two weeks. It was noted that Afobazole had a greater effect on hyposthenic compared to hypersthenic symptoms. In the course of therapy, the rapid fatigue, lethargy, and pathological drowsiness of the patients disappeared. In the majority, night sleep was restored, agryptic disorders were stopped due to a decrease in “hot flashes” at night and the actual tranquilizing effect. Along with this, there was a restoration of comfortable relationships with others, a decrease in conflicts. When using Afobazole in patients with anxiety-depressive variant of menopausal syndrome, after 5-6 days there were signs of normalization of mood, the disappearance of emotional lability and anxiety disorders (from generalized to panic attacks), the disappearance or mitigation of depressive phenomena.
Therefore, it can be argued that the choice of an adequate therapeutic strategy contributes to the prevention of the disharmonious course of the menopause in a woman in the form of menopausal autonomic and borderline mental disorders. Afobazole can be attributed to drugs that can significantly improve the mental state of patients.
In recent years, there has been an increase in surgical interventions on the genitals, the volume of which includes the removal of the ovaries. After a total ovariectomy, an extensive complex of neuropsychic, vegetative-vascular and metabolic-endocrine disorders develops due to a sharp shutdown of the hormonal function of the ovaries. In response to a decrease in the level of sex steroids, a natural increase in the secretion of gonadotropic hormones develops. After ovariectomy, the concentration of follicle-stimulating and luteinizing hormones in the blood serum increases on days 5–7 after surgery, and after 20–30 days, the level of these hormones becomes 7–10 times higher than in women of childbearing age, and is likened to the level characteristic of menopause. Removal of the ovaries, carried out during the period of natural age-related involution, aggravates the biological transformation of the body and leads to the breakdown of protective and adaptive mechanisms.
Vegetative-vascular and neuropsychic symptoms usually occur 2-3 weeks after oophorectomy and reach full development after 2-3 months. The reverse development of post-castration syndrome occurs in the first year after surgery, but in 25% of women, pathological symptoms persist for 2-5 years or more. In the first 2 years, neurovegetative disorders predominate in 73% of women, psycho-emotional disorders in 16%, and metabolic endocrine disorders in 11%. In subsequent years, the frequency of metabolic-endocrine disorders increases, psycho-emotional disorders persist for a long time and the frequency of neurovegetative disorders decreases. The removal of the ovaries is especially difficult for women operated on at a transitional age (45–50 years). A protracted and severe course has a post-castration syndrome in women with extragenital pathology.
Removal of the ovaries turns off the cyclic function, followed by a violation of the hypothalamic-pituitary-gonadal relationship with the development of psychovegetative syndrome. The ambiguity of shifts in the mechanisms of hormonal feedback determines the specifics of autonomic and psycho-emotional disorders after castration. The emerging clinical symptom-complex is similar to that in patients with menopausal syndrome.
Among the drugs prescribed in the complex therapy of post-castration syndrome, tranquilizers occupy a worthy place. We evaluated the effect of Afobazole on vegetative-vascular and neuropsychic symptoms of post-castration syndrome according to the survey, control of blood pressure and pulse rate over time.
Patients were prescribed Afobazole at a daily dose of 20 mg in two doses in the morning and afternoon for three weeks as monotherapy. While taking the drug, the patients kept an observation diary, where they recorded the subjective severity of the existing disorders, the pulse rate every three hours 5 times a day and blood pressure at noon.
As a result of the use of Afobazole in patients with post-castration syndrome, the state of health and mood improved in all cases, but the degree of severity was different. Headaches were before treatment in 73% of patients, during treatment they persisted in 32% of observed women. Gastrointestinal disorders decreased by 43%. The best results were obtained in relation to vasomotor reactions, respiratory disorders, gastrointestinal tract, reduced fatigue, headaches, where the frequency of manifestations decreased by 2.5 times. Side effects from the use of the drug were not registered by us.
The results obtained in the treatment of vegetative-vascular disorders in patients with premenstrual, menopausal and post-castration syndromes confirmed the vegetative-stabilizing properties of the drug and allow us to consider it appropriate to include Afobazole in the complex therapy of these pathological conditions.

Literature
1. Avedisova A.S. To the question of dependence on benzodiazepines// Psychiatr. and psychopharmacol. – 1999. – No. 1. – S. 24-25.
2. Borodin V.I. Side effects of tranquilizers and their role in borderline psychiatry// Psychiatrist.