Grandaxin for VSD: a new generation tranquilizer

Therapy of vegetative-vascular dystonia is a complex and lengthy process.
It is sometimes difficult for such patients to choose a truly effective remedy. Grandaxin for VSD helps eliminate the alarming symptoms of this complex, as well as other neurological disorders. The medicine is a relatively new product on the pharmaceutical market, but has already managed to prove itself on the positive side.

Description

Grandaxin is an anxiolytic drug or tranquilizer. Produced in 50 mg tablets. They have a round and flat shape, the color range varies from white to grayish. On one side there is a dividing line, on the other there is the Grandax logo.

The tablets are placed on a blister that holds 10 tablets. There are 2 or 6 pieces in a package.

The active substance of Grandaxin is represented by tofisopam. It is obtained by an atypical chemical modification of the diazepam molecule. Tofisopam belongs to the group of benzodiazepines and exhibits the properties of tranquilizers, but has some peculiarities.

Grandaxin (tofisopam): mechanism of action and range of application

Grandaxin (tofisopam), produced by , has been actively used all over the world for more than 20 years and is well known in Russia.

The main feature of the group of drugs to which Grandaxin (tofisopam) belongs is the location of the nitrogen group. If in traditional benzodiazepines the nitrogen group is located in position 1-4, then in Grandaxin and similar drugs it is located in position 2-3, and therefore they are usually designated as 2-3-benzodiazepines.

Due to the specifics of its structure, the drug’s properties differ significantly from “classical” benzodiazepines. Its vegetative-corrective and anxiolytic effects, not accompanied by sedatives and muscle relaxants, have made it possible to find widespread use in clinically pronounced manifestations of anxiety within the framework of well-studied psychogenic mental illnesses, psychopathy, and pathocharacterological personality developments.

Grandaxin (tofisopam) is used for menopausal syndromeiii, PMS, alcoholism, adaptation disorders, PTSD, ADHD and other conditions accompanied by anxiety, emotional stress, mild depression, autonomic dysfunction, apathy, decreased activityiv.

Grandaxin (tofisopam) today is included in a number of standards of primary health care and specialized care, for example, for withdrawal, amnestic conditions and acute intoxication caused by the use of psychoactive substances.

Tranquilizers and Grandaxin

Tranquilizers are identical to the concept of anxiolytics. Translated from Latin, anxietas means fear or anxiety, and litikoc from ancient Greek means weakening. Thus, tranquilizers are designed to relieve anxiety.

Anxiolytics are called minor tranquilizers, while antipsychotics are classified as major tranquilizers. Most of them exhibit 5 main effects:

• anxiolytic - elimination of emotional stress, obsessive thoughts and fears, reduction of anxiety;
• sedative - removal of psychomotor excitability, slowing down activity, speed of reactions, both mental and motor. Decreased concentration;
• sleeping pills - normalization of sleep, increasing its depth;
• muscle relaxant - muscle relaxation. May be accompanied by lethargy, weakness, slow reaction, excessive relaxation;
• anticonvulsant - reduction of excitation in epileptoid foci of the brain.

Grandaxin is also a representative of tranquilizers. However, it does not exhibit a pronounced sedative, muscle relaxant and anticonvulsant effect, but has mainly an anti-anxiety effect.

“Physiological” or “mental” depression: how to determine the cause of the disease

The first thing to remember is that panic attacks do not appear out of the blue; there is always a reason for their “awakening”. If a person does not have an innate predisposition to a depressive state, there have been no significant events in life that “knocked him out of the rut”, in 90% of cases we are talking about problems with the physical state of vital systems - cardiovascular and circulatory. The cause of uncontrollable panic and reluctance to enjoy life in the case of osteochondrosis is degeneration of vertebral cartilage in one form or another, which leads to disruption of the functioning of surrounding nerve roots and blood vessels. The resulting protrusions, hernias or other damage to the intervertebral disc lead to compression of the vessels providing blood supply to the brain. In 60% of cases, “advanced” osteochondrosis leads to oxygen starvation of the brain. Trying to normalize its condition, the “main organ” gives alarming signals, including those of a psychological nature.

How the drug works

When treated with Grandaxin, there is no drowsiness or lethargy. Moreover, it moderately increases mental and motor activity, stimulates mental activity, and provides a surge of strength and energy.

The drug does not cause muscle relaxation, eliminates the feeling of fatigue and increases performance. It returns sound and healthy sleep, but there is no lethargy or drowsiness during the day. In general, this drug does not have the side effects that are inherent in many tranquilizers.

Taking Grandaxin for VSD provides a vegetative stabilizing effect.

Our autonomic system regulates the activity of internal organs, as well as blood vessels. It consists of the sympathetic and parasympathetic divisions. If the balance in their work is disturbed, there is, accordingly, a failure in the regulation of the work of those systems for which they are responsible. Such violations can manifest themselves in different ways:

• tachycardia, pain and compression in the heart area;
• difficulty breathing, shortness of breath, feeling of lack of air;
• feeling of a lump in the throat;
• sweating, low-grade fever;
• redness of the skin, feeling of heat;
• headache, dizziness;
• asthenia, malaise;
• fear of death or concerns about one's health.

A similar symptom complex is a manifestation of vegetative-vascular dystonia.

Grandaxin helps to establish a synergistic effect of both parts of the autonomic nervous system, eliminates most symptoms of VSD, relieves apathy, anxiety, phobias and obsessive thoughts.

Panic attack symptoms

People with panic disorder very often do not see a doctor for a long time and do not tell their loved ones about the existing problem. As a rule, a person either thinks that there is no problem, and he himself will be able to cope with his poor health, forcibly overcoming all the signs of a panic attack, or he is embarrassed by his “weakness,” or is completely afraid that he will be “sent to a mental hospital.” This is completely unnecessary. However, it is necessary to treat sudden and regular panic fear.

“When I first had a panic attack, I had to call an ambulance. They just gave me glycine and didn't tell me anything else. After that, I went through the entire cardiology center and passed all the tests. I was told that I was absolutely healthy. My family and friends thought I was faking it. I tried not to pay attention to the attacks, reassuring myself that when I came home everything would be fine. Sometimes he deliberately drove himself into a traffic jam in order to overcome his fear. Such a nightmare was happening that you could at least abandon the car and leave. Sometimes I did just that. I would drop my car off at the metro station and come and pick it up the next day. Although before this illness I generally tolerated traffic jams calmly,” patient Pavel (41 years old).

First, let’s look at the symptoms with which you can probably come to the doctor and say: “Doctor, I’m having panic attacks. What to do?"

Psycho-emotional component of a panic attack. Symptoms and signs:

- Sudden, unreasonable attacks of fear/anxiety/panic, lasting from several minutes to several hours

- Waiting for sudden death, waiting for an attack

- Intrusive thoughts (usually related to death)

— Blurred consciousness

- Feeling of derealization (“I am separate, the world is separate”, “the world through cellophane”, “like in an aquarium”)

- Constant feeling of anxiety

— Various phobias (agoraphobia, social phobia, etc.)

— Insomnia, “nightmare” dreams

— Decreased mood, tearfulness

- Irritability, aggressiveness

“In the summer of 2014, I realized that I regularly could not fall asleep until 5-6 o’clock in the morning. The stuffy summer aggravated my condition, I constantly experienced a feeling of lack of air, my heartbeat quickened, obsessive thoughts arose in my head: “What if I’m dying?” - panic grew, but I had no strength to move or call an ambulance. I lay there like that until the morning, when my eyes closed on their own from fatigue and constant tension. This happened several times a week,” patient Elena (28 years old, manager).

Physiological component of a panic attack. Symptoms and signs:

— Dizziness, headache, heaviness in the head, noise in the head/tinnitus

- Lack of air, suffocation, shortness of breath

— Rapid heartbeat, feeling of interruptions in the heart, pain in the heart

- Nausea, abdominal discomfort

- Chills, fever, sweating

- Trembling in the arms, legs, body

- Muscle tension, numbness in limbs

— Gastrointestinal tract disorder

- Feeling tired, weak, lack of strength

“5 years ago I was unsuccessfully treated with antibiotics and after that I started having stomach problems. All these years I suffered from constant diarrhea. I contacted a parasitologist, gastroenterologist, immunologist and other specialists. Tests and clinical studies did not reveal any diseases. I tried to be treated with probiotics and prebiotics, but to no avail. Other symptoms also began to bother me: heaviness in the head, tension in the back and neck, anxiety for no reason, fear for one’s health, sometimes the heart was pounding wildly, in the morning after sleep there was slight dizziness and, of course, constant fatigue and weakness,” patient, Andrey (31 years old).

Important symptoms of panic attacks are also their systematicity and regularity. The interval between panic attacks can vary from a few minutes to several days or months, but their regular occurrence indicates that you are suffering from a panic disorder.

Other indications

Grandaxin is effective not only for VSD, but also for neuroses, as well as other similar conditions. Indications include:

• alcohol withdrawal;
• premenstrual, menopausal period;
• mental maladjustment;
• mild depression;
• conditions accompanied by muscle asthenia and atrophy, when muscle relaxant anxiolytics are unacceptable for use.

The drug is a daytime tranquilizer. It does not cause addiction or withdrawal symptoms.

An important property of Grandaxin is the relief of panic attacks. This is a feeling that occurs suddenly or under the influence of a stressful situation. Accompanied by a strong feeling of fear and vegetative disorders.

The concepts of VSD and panic attack are closely related: the attack is a kind of exacerbation of neurocirculatory dystonia. Therefore, therapy for these conditions follows a similar plan.

How can a specialist help with depression?

Depression, especially spontaneous depression, is not a reason to make an appointment with a psychiatrist. Start with something simple - a visit to a therapist. A thorough visual inspection will tell a good specialist a lot. The doctor’s goal is to make a correct diagnosis, on which 90% of the effectiveness of treatment depends. If there is a suspicion of osteochondrosis and the symptoms are associated specifically with this pathology, a laboratory study of blood biochemistry and ultrasound of the vessels of the cervical spine are recommended. After studying the results, it will be possible to decide what caused the panic attack and depression. Treatment is prescribed in accordance with the physical and psychological condition of the patient and is carried out comprehensively. The goal is to simultaneously normalize blood flow in narrowed vessels and relieve a person from emotional exhaustion. Therapeutic measures can be different: taking medications to improve brain function, physiotherapy, prescribing sedatives or antidepressants.

Features of use

Grandaxin is taken 1-2 tablets 1 to 3 times a day. The course of treatment is based on the severity of the manifestations and is prescribed exclusively by a doctor. A maximum of 300 mg of the drug per day is allowed.

Like any medicinal component, Grandaxin can lead to adverse reactions and intolerance by the body. They are manifested by the following violations:

• allergic rash and itching;
• pain and increased muscle tone;
• labored breathing;
• irritability and agitation, sleep disturbance, clouding of consciousness, headaches, exacerbation of epilepsy.

In case of an overdose of the drug, the development of a coma and breathing problems, depression of the central nervous system is possible.

Grandaxin should not be used for obsessive states and persistent psychoses. This will lead to a suicide attempt and increased aggression.

If you are allergic to lactose, the drug is also contraindicated, since each tablet contains about 90 mg of this substance.

The drug is not prescribed for respiratory disorders.

The drug should not be prescribed in the first 3 months of pregnancy and during breastfeeding.

The drug is prescribed with caution to patients with epilepsy, personality disorders and organic damage to the central nervous system, as well as elderly people, patients with mental retardation and decreased kidney function.

When the drug enters the intestines, it is quickly absorbed. Its highest concentration in the blood appears after a few hours. The active ingredient is not concentrated in the body. Most of it is excreted in urine, and a small amount is excreted in feces.

Grandaxin has some peculiarities of contact with other drugs. Its combination together with certain immunosuppressants (tacrolimus), as well as with cyclosporine, increases their accumulation in the blood.

Grandaxin enhances the intensity of the action of psychotropic drugs: sedatives, hypnotics and antidepressants.

In turn, its intensity of impact is increased by antihypertensive drugs, and accumulation in the blood is intensified by antimycotic drugs.

The combined use of Grandaxin and antacids reduces its absorption.

Anxiolytic mitigates the toxic effects of alcohol-containing drinks on the central nervous system. But its parallel use with these liquids, barbiturates, antiepileptic drugs, nicotine reduces its effectiveness.

Why does panic disorder develop?

Many experts believe that at least once in their life everyone experiences symptoms similar to a panic attack. But the majority do not focus on them; a pathological reaction is not triggered.

Panic attacks can also occur against the background of various somatic and functional disorders and psychopathologies.

The causes vary as much as the severity of the symptoms. If we summarize all the available data, we can identify several main triggers:

1. A long stay in a psychotraumatic situation is stress at work or study, which the body expresses with the help of psychosomatics.
2. Secondary benefit - often a panic attack carries some benefit: by feeling unwell, the patient avoids any tasks or responsibilities. Sometimes the presence of such a benefit is itself the cause of the disorder.
3. Somatic diseases. Often the symptoms of the disorder are caused by diseases of the endocrine system.

Treatment is aimed at both relieving symptoms and eliminating the underlying cause. Therefore, first of all, the specialist will try to find out what led to the unpleasant symptoms.

Clinical practice and evidence of effectiveness

Use of Grandaxin (tofisopam) for anxiety disorders

Permanent anxiety disorders are often accompanied by various types of psychovegetative symptoms. Grandaxin (tofisopam), thanks to its vegetative-corrective effect, quickly relieves anxiety and its vegetative accompaniment, significantly improves the patient’s quality of life and helps restore optimism regarding the prognosis of the disease.

In case of paroxysmal anxiety, panic attacks, the use of Grandaxin (tofizopam) is advisable for: • accelerating the clinical effect, since the anti-panic effect of antidepressants is delayed; • for the correction of anxiety and panic disorders, the intensification of which is provoked by the start of taking antidepressants; • enhancing the effect of an antidepressant when increasing its dose is impossible due to the risk of side effects.

The absence of sedative and muscle relaxant effects allows treatment to be carried out on an outpatient basis, without disturbing the patient’s usual routine and without adding reasons for stress.

In addition, the dopaminergic effect of Grandaxin (tofisopam) determines its activating effect and contributes to a certain behavioral correction. It is no coincidence that 2-3-benzodiazepine drugs are sometimes referred to as atypical antipsychotics. In the case of panic disorders, these properties of Grandaxin (tofisopam) may be useful for relieving secondary disorders, in particular agoraphobic, hysterical and hypochondriacal syndromes.

Use of Grandaxin (tofisopam) for psychovegetative disorders

Autonomic disorders are one of the pressing problems of modern medicine. In the population, autonomic disorders of varying severity. starting from puberty, they occur in 25-80%ixx. Psychovegetative symptoms are encountered by specialists of various profiles, and patients are often referred to see a psychologist, psychotherapist or psychiatrist.

Psychovegetative syndrome develops with pathology of the suprasegmental autonomic systems of the brain of any etiology, more often psychogenic than organic.

The main manifestations, as the name suggests, unfold in the mental and autonomic spheres in the form of permanent and paroxysmal disorders.

In the work carried out by Artemenko A.R. et al.xi studied the effectiveness of Grandaxin (tofisopam) in patients with psychovegetative disorders (asthenic manifestations, emotional disorders, sleep disorders, headaches, blood pressure lability, hyperhidrosis, cardialgia, hyperventilation disorders, etc.).

After 4 weeks of treatment, fatigue significantly decreased in patients; the severity of emotional disorders, sleep disturbances and appetite decreased; manifestations of Raynaud's phenomenon and sweating have decreased; non-infectious low-grade fever completely regressed; headaches, hyperventilation symptoms, fluctuations in blood pressure, cardialgia and gastrointestinal dysfunction decreased.

As a result of treatment, indicators of emotional tension significantly decreased, quality of life improved, and the indicator of subjective assessment of health impairment (according to VAS) decreased.

Thus, the authors showed that Grandaxin (tofisopam) can be used as monotherapy for mild to moderate manifestations of PVS. Therapeutic doses of Grandaxin (tofisopam) are well tolerated by patients and lead to virtually no side effects. Grandaxin (tofisopam) deserves wider use in clinical practice, not only as a well-known daytime tranquilizer, but also as a highly effective vegetative correctorxii.

The use of Grandaxin (tofisopam) for psychoemotional and neurovegetative disorders during menopause

Menopausal syndrome is an interdisciplinary problem, and often the therapy of patients experiencing menopause is carried out not only and not so much by gynecologists, but by endocrinologists, cardiologists, neurologists, psychologists and psychotherapists.

In addition to the physiological decline of ovarian function, an important medical and social problem is the rehabilitation of women after gynecological operations (adnexectomy, hysterectomy). The most common psycho-emotional consequences of hysterectomy are depression and anxiety, which can contribute to a decrease in quality of life and a worse prognosis.

Thus, depression accompanies menopause, both physiological and postoperative, and its therapy is extremely important for complete comprehensive rehabilitation.

A study of the use of Grandaxin (tofisopam) in patients with psychoemotional and neurovegetative disorders during menopause showed a significant improvement in their well-beingxiii. The maximum effect was achieved in relation to psycho-emotional disorders. An excellent correction of both depression and anxiety (not only severity, but also frequency), especially situational anxiety in operated patients, was noted.

The data obtained indicate an undoubted positive effect of therapy with Grandaxin (tofizopam) for the purpose of correcting psychoemotional and neurovegetative disorders, and therefore Grandaxin (tofizopam) can be recommended for use as part of the complex therapy of menopausal disorders.

Use of Grandaxin (tofisopam) for premenstrual syndrome

The deterioration of a woman’s mental and physical condition before menstruation has been described since the time of Hippocrates. And today, PMS is often the cause of exacerbation of the serious condition of women who are regularly observed by psychiatrists and psychologists.

“Premenstrual dysphoric disorder” in a pronounced form occurs in 8-25% of women of reproductive age. Hormonal therapy (in particular with GRF agonists) may not always be used - due to the high risk of somatic complications, as well as due to the psychological resistance of women who prefer to suffer from recurrent PMS symptoms rather than take hormones.

Therefore, recently, in the treatment of PMS, drugs have been actively used that reduce emotional, affective and motivational disorders and have a secondary effect on the occurrence of autonomic and metabolic endocrine-metabolic disorders.

Solovyova A.D. et al. in 2001 xiv studied the effectiveness of Grandaxin (tofisopam) in women with PMS, using it for 8 weeks at a dose of 100 mg. After treatment, the patients' sleep significantly improved, personal anxiety and depression decreased, and their quality of life improved. It should also be noted that Grandaxin (tofisopam) also turned out to be effective against specific hormonally caused symptoms of PMS, such as swelling, engorgement and tenderness of the mammary glands and pain in the lower abdomen, which once again confirms the close connection between brain structures and sex hormones.

Use of Grandaxin (tofisopam) for stress

Stress is an inevitable accompaniment of an active social life, and in most cases a person has the reserves to cope with stress on his own. However, in some cases, the body's response to stress becomes disproportionately strong compared to the external influence that causes it. This disrupts the body’s adaptive capabilities and can sometimes even provoke the development of psychosomatic diseases.

Therefore, the optimal help for a patient in a state of chronic stress is outpatient treatment with drugs from the group of daytime tranquilizers.

A group of Moscow scientists summarized the experience of using Grandaxin (tofisopam) to correct pre-exam stress in university studentsxv. Experts came to the conclusion that the drug was highly clinically effective: 94% of students had a very good or good effect when using it. According to the students themselves, this therapy helped them cope more successfully and much easier with the tasks posed during the exam session.

Students who are under severe psycho-emotional stress caused by chronic stress most often exhibit anxiety disorders of a non-psychotic level with pronounced PVA of a psychophysiological nature (sweating, lability of temperature, pulse, blood pressure, gastrointestinal disorders, etc.). The drug Grandaxin (tofisopam) affects the level of anxiety and vegetative manifestations, resulting in significantly improved indicators of stress resistance, and therefore adaptation in situations of psycho-emotional stress.

Use of Grandaxin (tofisopam) for attention disorder with hyperactivity disorder in adolescents

ADHD is a major social problem, as it occurs in 5-30% of children and adolescents in the general populationxvixviixviiixix. Children who are characterized by restlessness, distractibility, hyperactivity, impulsiveness, low academic performance, short temper, and low self-esteem are seen by psychiatrists and psychologists xx xxi. At older ages, children, especially adolescents with ADHD, often experience anxiety and depressive disordersxxiixxiii.

Psychostimulants, recommended for the treatment of ADHD and showing high effectiveness in the Western world, are not approved in our country. In the Russian Federation, in such cases, Cerebrolysin, piracetam, and instenon are prescribed xxiv. However, these drugs do not affect impulsivity and anxiety-depressive disorders. Thus, the development of new treatments for ADHD is an important medical and social problem. The drug Grandaxin (tofisopam) has found widespread use in clinical psychopharmacology.

A study xxv conducted on 36 adolescents with ADHD aged 14 to 17 years showed a significant improvement of 63.9%. Parents noted improvements in behavior, attention, and memory in their children. In 80% of adolescents who complained of headaches, treatment reduced their frequency and intensity.

A psychological study conducted using the TOVA test revealed a statistically significant increase in attention indicators, a decrease in reaction time, a decrease in impulsivity and hyperactivity (70%), and anxiety.

After 30 days of using Grandaxin (tofisopam) at a dose of 50 mg, 1 tablet 2 times a day, pronounced positive changes in the clinical condition were observed, the behavior and academic performance of children improved.

The effectiveness of using Grandaxin (tofisopam) in the treatment of ADHD is approximately equal to the results of using psychostimulants in the absence of their typical side effects.

Use of Grandaxin (tofisopam) for adaptation disorders

Mental trauma and mental stress, associated, in particular, with a forced change of place of residence, economic difficulties, unsettlement for a long time in a new place, uncertainty of the future, in the vast majority of cases lead to the development of neurotic disorders of various levels and social maladjustmentxxvi.

Despite the fact that adaptation disorders, in principle, are conditions with a favorable prognosis and are successfully amenable to psychotherapeutic influencexxviixxviii, the risk of developing more complex psychopathological disorders (for example, generalized anxiety disorders, pathological personality development, etc.) with long-term and currently unresolvable stress situations is quite high. This requires psychopharmacotherapy using tranquilizers that best meet the safety criterion.

The study of Grandaxin (tofisopam) for adaptation disordersxxix allows us to classify it as one of the main, so-called “drugs for the population.” Their use minimizes the risk of developing adverse events, so they can be prescribed on an outpatient basis to a wide range of people with unexpressed anxiety disorders who are in a chronic stressful situation, to prevent the development of more severe psychopathological disorders in them. The drug can be recommended for use in a comprehensive program of therapy and rehabilitation of refugees and forced migrants with adaptation disorders with alarming symptoms, in medical and psychological rehabilitation centers.

The use of Grandaxin (tofisopam) for post-traumatic stress disorders

The problem of post-traumatic stress disorder (PTSD) has become increasingly relevant in recent years: all over the world and, in particular, in Russia, there are many hotbeds of tension where active hostilities are taking place. The search for a drug for adequate treatment of anxiety, repeated repeated experiences of a traumatic situation, constant tense anticipation of the return of a traumatic event, is the subject of work of many specialists.

The effectiveness of Grandaxin (tofisopam) for the treatment of PTSD was tested in a studyxxx, which involved military personnel who participated in combat operations in Chechnya in 1994-1996. and 1999-2000 All patients were diagnosed with borderline mental disorders. Syndromatically, these conditions were regarded as anxious, depressive, and hypochondriacal.

After taking Grandaxin (tofisopam) at a dose of 50 mg 3 times a day for 2-3 weeks, subjective improvement was noted in almost all patients. Sleep indicators significantly improved: presomnia disorders were relieved in 72% of patients, intrasomnia disorders in 50%, nightmares stopped bothering 78.6% of patients. A decrease in anxiety symptoms correlates with normalization of sleep. The total score on the anxiety scale changed 7 times, on the depression scale - 2 times, on the asthenia scale - 1.5 times towards improvement. The data of A.M. were also confirmed. Vein (2000) about the positive effect of Grandaxin (tofisopam) on cephalgic syndrome.

It can be assumed that the reduction of the alarming radical will entail a decrease in craving for alcohol; relief of cephalalgia will reduce the dose of consumed analgesics; Normalizing sleep will reduce the need for hypnotics. Rehabilitation of patients with PTSD, of course, cannot at this stage be reduced to one, albeit effective, drug. Of course, it is necessary to use a set of measures, including psychological and social assistance. However, Grandaxin (tofisopam) should take its rightful place in the treatment of patients suffering from post-traumatic stress disorder. Thus, Grandaxin (tofisopam) is an effective drug in the arsenal of psychiatrists and psychologists, which is able to effectively protect against stress, combat psycho-emotional and autonomic disorders that accompany both normal physiological processes and somatic, neurological and mental diseases.