Depression is a common illness, affecting approximately 20% of people in developed countries. Her therapy includes an integrated approach, including the use of medications. The new generation tranquilizer Grandaxin for depression is prescribed in case of moderately severe symptoms. It has a gentle effect on the patient’s psycho-emotional background, while exhibiting a minimum of side effects.
Pharmacological group
Grandaxin is classified as an anxiolytic (anti-anxiety) drug or tranquilizer. Most representatives of this group, in addition to anti-anxiety effects, also exhibit others, including:
- sedative – decreased mental and motor activity;
- hypnotic;
- anticonvulsant;
- muscle relaxant - relaxing.
Such effects make it impossible to take such drugs during the day while driving.
Grandaxin is a fundamentally new tranquilizer with a pronounced anxiolytic effect. Its active ingredient is tofisopam, an atypical benzodiazepine derivative. It is synthesized by transforming the molecular structure of diazepam. Thanks to this feature, it is not capable of causing addiction and withdrawal symptoms.
The action of benzodiazepines is based on increasing the sensitivity of receptors to GABA - gamma-aminobutyric acid. This is the main neurotransmitter that causes inhibition in the brain and thereby stops excitement and has a calming effect. However, its excess provokes the opposite reaction - hyperactivity, anxiety, trembling in the arms and legs.
All benzodiazepines are divided into 3 classes, taking into account the predominant effect:
- with anxiolytic;
- with sleeping pills;
- with anticonvulsant effect.
Most representatives have all of the listed properties with one pronounced one. Grandaxin has an anti-anxiety effect, and other manifestations are practically absent.
Considering that the drug does not cause a feeling of drowsiness, relaxation and lethargy, and does not interfere with concentration, it is called a daytime tranquilizer and it is allowed to combine its use with driving, but only after consulting a doctor.
Indications for use
The drug Grandaxin is recommended for the treatment of diseases such as:
- Neurosis-like conditions and neuroses, which are accompanied by emotional stress, disorders of the autonomic system, apathy, anxiety, obsessive feelings and decreased activity;
- Depression with severe symptoms of psychopathology;
- Menopausal syndrome;
- Premenstrual tension in the body;
- Cardialgia;
- Alcohol withdrawal;
- Neurogenic muscular atrophy, myopathy, myasthenia gravis and other pathological conditions with secondary symptoms (in cases of contraindication to anxiolytics with a pronounced muscle relaxant effect on human organs and systems).
How to recognize depression
As already mentioned, the drug helps get rid of depression, but not all of its forms. Grandaxin is taken only for mild to moderate disease with moderately severe symptoms.
During the course of the disease, several syndromes are distinguished:
- Emotional disorders: low mood, melancholy, anxiety and internal tension, pessimistic attitude; self-flagellation, lack of interest in the world around us, inability to have fun.
- Behavioral reactions: solitude, reduced activity; bad habits;
- Cognitive functions: inability to concentrate, slow thinking, decreased memory and perception; pessimistic thoughts, thoughts of suicide, low self-esteem.
- Autonomic disorders: poor sleep, appetite distortion, weakness and malaise, intestinal dysfunction; discomfort in the heart and other organs, headaches.
A specific indication for the use of the drug is reactive depression. It develops in response to the action of some traumatic factor. The condition is characterized by a consistently reduced emotional background and fixation on the problem.
The patient reproaches and blames himself for what happened, his conversations are aimed only at the problem. And, constantly analyzing it, he seeks support from those around him.
A person is worried about insomnia. And he is fully aware of his condition.
Attacks of despair and demonstrative hysterics are possible. Excitement reaches a state called “melancholic raptus.” At the same time, the person rushes about aimlessly, sobs, screams, and suicide attempts are not ruled out.
This state can be replaced by a depressive stupor, when the patient “freezes” in one position, not reacting to what is happening.
Compound
Tofisopam is the active ingredient of the drug - a benzodiazepine derivative. Its properties differ from other representatives of the group, therefore it is considered atypical. The drug "Grandaxin" 50 contains 50 mg of the main component. Additional substances include lactose, potato starch, gelatin, MCC, talc, stearic acid and magnesium stearate.
Impact of Grandaxin
The main effect of the drug is manifested in the anxiolytic effect. It helps eliminate feelings of anxiety and fear, reduce emotional stress, anxiety and agitation, both mental and motor.
Tofizopam exhibits vegetative stabilizing properties to a high degree. With him it is expressed to the greatest extent compared to other tranquilizers:
- normalizes sleep - eliminates insomnia, promotes rapid falling asleep;
- restores blood pressure;
- stabilizes heart rate;
- reduces sweating;
- improves the functioning of the gastrointestinal tract, eliminates constipation.
The vegetative stabilizing effect is achieved by establishing a balance between the sympathetic and parasympathetic systems.
The stress-protective effect of Grandaxin protects the central nervous system from the effects of a destructive factor. It gives the patient a state of psychological comfort and provides an adequate assessment of what is happening. Protects against the development of unwanted vegetative-vascular reactions: tachycardia, vascular spasms, destruction of the gastrointestinal mucosa. Eliminates excitement.
Tofizopam has a coronary effect to some extent:
- improves coronary circulation;
- reduces the need for oxygen in the heart muscle;
- normalizes metabolism in cardiac tissues;
- increases the amount of oxygen delivered to the heart.
This ability of Tofizopam is widely used in the treatment of coronary heart disease. The drug stabilizes the functioning of both parts of the autonomic nervous system, and thereby improves the electrical conductivity of the heart muscle.
The psychostimulating effect of the drug helps restore the patient’s mental and physical activity. Helps improve cognitive functions, restores thinking abilities, improves mood. Strengthens the ability to resist the effects of unwanted environmental factors.
Grandaxin is recommended to be included in complex therapy as:
- enhancing the effect of antidepressants;
- to eliminate anxiety and panic attacks that can be triggered by starting to take antidepressant medications;
- in cases where the dosage of antidepressants is insufficient, and increasing it is impossible due to the risk of adverse reactions.
The use of the drug as monotherapy is undesirable.
special instructions
Like other medications, Grandaxin has its own characteristics. They must be taken into account when using drugs. Experts have compiled a list of rules that must be followed during the treatment process:
When diagnosing reactive psychosis, the tablets should be taken together with antidepressants.- It is worth remembering that the metabolic process slows down with age, so it is necessary to adjust the dosage. For liver or kidney dysfunction, you should also choose the optimal amount so as not to provoke a worsening of the condition.
- The manifestation of depression or increased anxiety also does not allow the use of this tranquilizer, since central nervous system depression may develop and the risk of suicide attempts will increase.
- Patients with lactose intolerance should take into account that the drug contains this substance. In people with epilepsy, while taking pills, the seizure threshold may increase.
- The drug does not affect the ability to drive vehicles in any way. After taking it, you can drive a car or begin work that requires increased concentration. The speed of physical or mental reaction is not slowed down by the influence of this drug.
Grandaxin and other tranquilizers
Due to its mild and selective effect, the drug has a minimum of side effects, unlike other anxiolytics. It does not cause the negative consequences inherent in most representatives of this group. The main ones are:
- "Behavioral Toxicity." Manifested by increased sleepiness during the day, weakness and malaise. Characterized by decreased reaction speed and inability to concentrate. Coordination of movements is impaired, and confusion may occur.
- Addiction. A common problem when taking tranquilizers. There is a possibility that it will worsen even to substance abuse. But more often, addiction develops with long-term treatment with such drugs, with an unauthorized increase in dose or concurrent use of alcohol.
- Withdrawal syndrome occurs when you suddenly stop using a tranquilizer. In this case, the symptoms of the disease return to the patient in a more pronounced or even complicated form.
Grandaxin does not exhibit such complications. It is low-toxic and resistance to it is not developed upon repeated use. Therefore, it is taken during the daytime.
The drug does not reduce physical and mental activity and does not lead to drowsiness. It does not suppress the efficiency of perception, the speed of reactions, and does not interfere with professional activities.
Clinical trials
Grandaxin is a unique CNS-active drug that has undergone many clinical trials. The drug does not have a sedative or muscle relaxant effect, and does not impair intellectual and psychomotor activity, unlike other benzodiazepines.
The drug has a mild cognitive-stimulating effect, a powerful drug that is prescribed to reduce autonomic disorders that accompany psychotic and nervous conditions.
Tofisopam does not have an anticonvulsant effect and even in a subtoxic dose does not cause sedation. Subtoxic dosages are potentiated only by barbiturates and ethanol.
The use of a dosage of the active substance in excess of 200 mg/kg in animals caused an effect similar to antipsychotics. When a dose of 10 mg/kg was administered, a normalizing effect on the temporary organization of animal behavior and the prevention of stress dysrhythmia was revealed.
The effectiveness of the drug in neurological practice was revealed during a multicenter study in which clinics from 11 Russian cities took part. The results of the study were based on observation data of 220 patients aged 18-55 years with psychovegetative syndrome (PVS).
The main group of patients (140 people) took Grandaxin tablets in addition to traditional treatment. The control group (80 people) was prescribed standard treatment with vascular and metabolic drugs without the participation of drugs. By the second week of treatment, personal and reactive anxiety decreased in both groups, but significant changes were noted specifically in the first group (they took Tofisopam).
Similar dynamics were observed in the fourth week of therapy. If at the beginning of the course both groups did not differ in the level of anxiety, then by the end of the second and especially the fourth week the degree of anxiety decreased much more than in the control group (they did not take Tofisopam).
The degree of vegetative-vascular dystonia was assessed through a questionnaire, during which subjective and objective disorders in patients were identified. The average indicators of the severity of autonomic disorders in both groups at the beginning of treatment did not differ.
By the end of the second and especially the fourth week, the scores in the first group were much lower than in the control group.
Thus, the use of Grandaxin has significantly improved the condition of patients, normalized autonomic imbalance and improved the quality of life.
To study the sedative and hypnotic properties of the drug, a study was conducted in which 60 conscripts aged 19-25 years with a minimum driving experience of one year participated. The first group of participants took Tofisopam, the second took pills with a placebo effect of a similar appearance, then the groups changed.
During the entire study period, not a single minor accident or incident occurred. Twelve individuals noted that while driving a truck they did not feel any stress and were able to cope with difficulties much more easily. 5 people indicated a similar effect when taking placebo, but these positive effects were also attributed to the period of taking Grandaxin.
Limitations and adverse reactions
Contraindications to the use of the drug are:
- severe forms of depression - with them there is a high probability of suicidal thoughts and actions;
- phobias, obsessions - possible increase in aggression;
- allergic reactions;
- uncompensated respiratory failure.
The drug is prescribed with caution to elderly people due to their increased susceptibility to it. It is not recommended to use it at this age for too long a time.
The drug is contraindicated for children under 18 years of age. It can be taken only in rare cases after carefully weighing the need and risks. In this case, therapy should be short-term.
Taking the drug in the 1st trimester of pregnancy is contraindicated. It easily crosses the placental barrier and can cause developmental defects in the child. Grandaxin can pass into breast milk, so you should avoid breastfeeding while treating with the drug.
Otherwise, when it enters the child’s body, it accumulates and causes a sedative effect. The newborn's sucking reflex decreases, he cannot suck out milk fully, and loses weight.
Despite the mild effect of the drug, it still exhibits some side effects:
- headaches, agitation and aggressiveness;
- sleep problems;
- confusion;
- increased frequency of seizures in epileptic patients;
- breathing disorders;
- poor appetite, thirst, digestive problems;
- jaundice;
- muscle hypertonicity, muscle pain;
- allergic manifestations.
In such cases, taking the drug is canceled.
Contraindications for use
The use of Grandaxin is contraindicated in patients suffering from psychomotor agitation, deep depression, aggressiveness, respiratory failure, and sleep apnea syndrome.
This drug is not recommended for people with galactose intolerance, congenital lactase deficiency, galactose and glucose malabsorption syndrome.
Grandaxin therapy should not be combined with sirolimus, tacrolimus and cyclosporine.
Women during pregnancy and lactation are also not recommended to take this medication.
How to take it correctly
Grandaxin is a small, round, disc-shaped tablet with the GRANDAX logo. They are white or gray in color and have virtually no odor. Located on a blister of 10 pieces.
The dosage of 1 tablet is 50 mg. The package contains 20 or 60 tablets.
Once in the digestive tract, Grandaxin is quickly absorbed into it. Undergoing transformation in the liver, it enters the blood. Here it reaches its maximum concentration 2 hours after administration. It is excreted by the kidneys and does not accumulate in the body.
The dose of the drug depends on the severity of the condition. It is calculated and prescribed only by a doctor. Self-medication is unacceptable. Usually the scheme is as follows: 1–2 tablets. from 1 to 3 times a day.
The maximum dose per day is 300 mg, in children – 200 mg.
Due to the fact that the drug accumulates in the liver and is evacuated through the kidneys, the drug is prescribed to patients with renal and liver failure with caution. In such patients, the severity and duration of the effect may change, as well as the development of side effects. In this regard, their dose is reduced by half. The same scheme is used for elderly people.
In case of an overdose of the drug, complications such as vomiting, changes in consciousness, coma, seizures and impaired respiratory function are possible.
Grandaxin is not used in parallel with cyclosporine and immunosuppressants such as tacrolimus, sirolimus.
Tablets can intensify the effect of drugs that depress the activity of the central nervous system: analgesics, sedatives and hypnotics, etc.
The use of Grandaxin along with alcohol, smoking, barbiturates, along with antiepileptic therapy reduces its activity.
It is strongly recommended to take Grandaxin before 17.00 to avoid insomnia.
The drug is available with a doctor's prescription. The average cost of 20 tablets is 400 rubles, 60 tablets - 900 rubles.
Drug interactions with other medications
The simultaneous use of several drugs from the same or different pharmacotherapeutic groups can lead to a number of unpleasant consequences. If the patient took medications before or during the prescription of Grandaxin, he should inform his doctor about this. The fact is that drugs can both weaken and strengthen each other’s effects.
Interaction of drugs with other drugs:
When combined with Metoclopramide, the rate of absorption of Grandaxin components increases. As a result, the therapeutic effect occurs much faster.- The main substance of the drug enhances the effect of medications that are intended to suppress the functions of the central nervous system. This may lead to respiratory depression.
- Barabiturates and antiepileptic drugs reduce the concentration of the active component of the drug, which leads to a weakening of its effectiveness.
- Under the influence of antifungal drugs, the metabolic rate in the liver slows down and the amount of tofisopam in the blood increases. A similar phenomenon is observed when combining drugs with antifungal medications.
- Clonidine and various calcium channel antagonists reduce the effectiveness of tofisopam.
- When taken in combination with Digoxin, an increase in its concentration is observed.
- Oral contraceptives, Cimetidine and Omeprazole lead to a decrease in the intensity of metabolism of the main substance Grandaxin.
When receiving your first consultation with a specialist, it is necessary to discuss the possible consequences of taking different drugs simultaneously.
Overdose
The presence of only one dosage form of the drug in a unique concentration, as well as a simple method of administering the drug, minimize the risk of errors during therapy. Even a significant excess of the permissible one-time or daily volume of the drug rarely threatens an overdose. The danger arises when consuming the product in extremely high doses - 50-150 mg per kg of body weight. In this case, the victim vomits, respiratory function is depressed, signs of clouding of consciousness appear, and convulsive seizures are likely. The patient may fall into a coma due to a sharp drop in blood pressure.
Help with this condition should be provided by professionals. Before doctors arrive or if symptoms are mild, it is recommended to rinse the victim’s stomach and give an absorbent to slow down the absorption of the active component of the product into the blood. Most often, activated carbon is used in a volume of 1 tablet for every 10 kg of body weight. Flumazenil, a benzodiazepine antagonist, is used in extreme cases. Its effect on the body in such situations has not been fully studied.
Treatment for an overdose of Grandaxin is symptomatic. Health care workers monitor the patient’s physiological indicators and respond to emerging symptoms. In case of breathing problems, artificial ventilation is performed. To combat hypotension, the patient is placed in the Trendelenburg position and given fluid resuscitation. If the blood pressure does not rise quickly enough or there is no reaction, Dopamine and norepinephrine are used.
