Experience of using Afobazole in the treatment of pathological anxiety in patients with general somatic practice

Update date: 09/17/2020 15:31:12 13968 Share:

Author: Maria Feldshtein

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In modern medicine, neuroses and the consequences of stress are treated not only with psychotherapy. Medications that can relieve anxiety and fear, improve mood, normalize sleep and return a person to normal life come to the rescue. These are drugs from the group of anxiolytics, and today we will compare two such drugs - Adaptol and Afobazol. What is the difference between them, read the article.

The drug and its characteristics Adaptol Afobazole
Pharmacological group Anxiolytic Anxiolytic
Active substance Tetramethyltetraazabicyclooctanedione Fabomotizol
Release form Pills Pills
Manufacturer OlainFarm (Latvia) OTCPharm (Russia)
Price 600-700 rub. 250-350 rub.
Vacation at the pharmacy On prescription Over the counter

Indications for prescribing anxiolytics

According to the official instructions, the drugs Adaptol and Afobazol are prescribed for the treatment of anxiety conditions and neuroses accompanied by irritability, anxiety and fear. These anxiolytics are used only in adult practice. For children under 18 years of age with similar symptoms, other remedies are recommended.

For other indications, anxiolytics differ.

Adaptol is recommended in the following situations:

  1. cardialgia (pain in the heart) not associated with ischemic heart disease and other organic causes;
  2. nicotine addiction – in complex therapy as a means of reducing cravings for tobacco;
  3. when taking antipsychotics and tranquilizers - to improve their tolerability.

Afobazole is prescribed for the following conditions:

  1. in complex therapy of various somatic diseases - for example, bronchial asthma, irritable bowel syndrome, arrhythmia;
  2. dermatological and oncological diseases;
  3. premenstrual syndrome;
  4. alcohol withdrawal;
  5. cardiopsychoneurosis.

Indications for therapy are determined by the doctor after examining the patient.

How do anti-anxiety medications work?

In the medical literature, anxiolytics are also known as tranquilizers. By influencing the central nervous system, they relieve or reduce the severity of anxiety, restlessness, fear and emotional stress.

The mechanism of action of anxiolytics has not been fully elucidated. It is assumed that they reduce the excitability of the subcortical centers of the brain (hypothalamus, thalamus and limbic system). At the cellular level, the effect of different drugs is different, and we will talk about this in more detail.

Adaptol

The drug works through the emotiogenic zones of the hypothalamus. The chemical composition of Adaptol is similar to the body's natural metabolites - its molecule consists of two urea fragments. Once in the body, it affects all major neurotransmitter systems: GABA-, choline-, serotonin- and adrenergic. The drug harmonizes their work and thereby reduces anxiety, worry and fear, and eliminates internal tension.

What you need to know:

  1. The calming effect of Adaptol is not accompanied by side reactions characteristic of other similar drugs, such as muscle weakness and impaired coordination of movements.
  2. It does not reduce mental and motor activity, so it can be prescribed during the day.
  3. Does not cause drowsiness, but enhances the effect of sleeping pills.
  4. Improves mood, but does not lead to euphoria.
  5. It has a nootropic effect: improves attention and memory, stimulates mental performance.

Afobazole

Afobazole binds to sigma-1 receptors in brain cells, stabilizes the functioning of GABA receptors and restores their sensitivity to mediators - special substances that trigger inhibition processes in the nervous system. It also acts as a neuroprotector: it reduces the permeability of nerve cell membranes, increases their stability and accelerates recovery.

Afobazole works both as an anti-anxiety and a stimulant drug. It reduces or completely eliminates anxiety, relieves emotional tension and irritability, and normalizes sleep. The drug also removes somatic manifestations of anxiety (rapid heartbeat, upset bowel movements, muscle weakness, feeling of shortness of breath, etc.). At the same time, it improves attention and memory.

The effect of the drug is observed after 5-7 days from the start of therapy, reaches a maximum in the 4th week and persists after completion of the course for two weeks.

According to the instructions, Afobazole is most effective in people with asthenic character traits, prone to suspiciousness and anxiety, and emotional lability.

Possibilities of using adaptol in clinical practice

  • Doctor of Medical Sciences, Prof. V.R. Mkrtchyan,
  • Doctor of Medical Sciences, Prof., Honored Russian scientist V.A. Orlov,
  • asp. L.Z. Kozhokova

Adaptol (active ingredient tetramethyltetraazabicyclooctanedione, mebicarum, OlinePharm JSC) is positioned as a drug with a wide range of clinical activity, possessing the properties of tranquilizers, nootropics, adaptogens, biocorrectors, antidepressants, lipid-lowering and antianginal agents.
Such a wide spectrum of therapeutic action is not inherent in, perhaps, any of the known drugs. Analysis of the studies conducted allows us to confidently say that adaptol has a clear tranquilizing effect. This effect of the drug is due to its normalizing effect on the balance of activity of various neurotransmitter systems of the brain: activating in relation to the inhibitory neurotransmitter GABA and weakening in relation to the excitatory neurotransmitters - norepinephrine and glutamate, as well as a normalizing effect on the relationship between adrenergic and serotonergic effects. The drug acts on the activity of structures included in the limbic-reticular complex, in particular on the emotiogenic zones of the hypothalamus. It exhibits clear central adrenolytic activity and does not have a peripheral adrenolytic effect. Like antipsychotics, it changes the permeability of the blood-brain barrier. Even in high concentrations it has no effect on isolated smooth muscle organs. Acting on the serotonergic system of the body, in small and medium doses it enhances the effect of the serotonin precursor tryptophan. It was experimentally established that the drug significantly increases the content of serotonin in the brain stem of rats.

Adaptol, being a derivative of bicyclic biureas, is a separate chemical group of tranquilizers; the drug has a pronounced anxiolytic, vegetative stabilizing, and sedative effect. Adaptol does not cause muscle relaxation, impaired coordination of movements, and does not have a hypnotic effect; it only enhances the effect of hypnotics, normalizing sleep phases. The anxiolytic effect of Adaptol consists of suppressing negative emotions, without affecting positive ones, which distinguishes it from diazepam, the use of which enhances positive emotions, which can lead to a kind of “euphoric” effect.

The drug is also used in psychiatry and to improve the tolerability of neuroleptics (reduces the inhibitory effect of chlorpromazine on the speed of reactions without enhancing the hepatotropic negative effects of chlorpromazine, has a reducing effect on neurotic and somatovegetative disorders that have arisen as side effects of neuroleptic therapy, compared with cyclodol and piracetam more intensely affecting vegetative-vascular disorders) and benzodiazepine tranquilizers (causes a decrease in muscle relaxation and an increase in the speed of psychomotor processes), antidepressants, antiepileptic drugs. At the same time, the therapeutic effectiveness of these drugs increases. Thus, adaptol does not cause pronounced behavioral toxicity and is a daytime tranquilizer that allows you to fully maintain performance when taking it.

A high degree of safety is evidenced by the intake of 30 g (100 tablets) of the drug by 2 patients with suicidal goals, which did not cause them any harm. There is a known patient who took 60 or 80 mebicarum tablets per day for 2 months as self-medication. They underwent 2 such courses, and there were no signs of intoxication in the blood, and the patient’s subjective well-being during treatment was impeccable.

The drug does not interact with other drugs and food, no metabolites are formed when it is taken, and it is excreted from the body unchanged in urine and feces. It does not accumulate in the body, and therefore there is no addiction to the drug, therefore 2-3-month courses of continuous therapy with adaptol are allowed.

The properties of adaptol make it possible to prescribe it in childhood. In child psychiatry, it is used for residual organic brain failure with a prevailing neurosis-like syndrome (sleeping, sleepwalking, night terrors), addictive behavior (hashish, heroin in combination with smoking), neuroleptic syndrome (with early dyskinesia). The drug has the most pronounced effect on affective disorders that accompany neurolepsy (anxiety, fear). To relieve neurolepsy, it is combined with benzodiszepine tranquilizers. The drug is used for neurasthenia - irritable weakness (increased excitability and easy exhaustion), anxiety-phobic disorders (anxiety, neurotic phobias, anxiety disorder due to fear of separation in childhood, generalized anxiety disorders, specific phobias, social phobias), obsessive-compulsive disorders (obsessive states). A feature of the listed disorders in children is the insufficiency or absence of personal awareness of existing disorders, the predominance of somatovegetative or movement disorders.

Unlike adults, in whom the maximum single dose of adaptol can reach 3 g, and the daily dose is 10 g, children aged 5-7 years adaptol are prescribed 0.5 g / day, at the age of 7-10 years - 0.75 g / day , at the age of 10-14 years - 1.0 g / day, at the age of 14 years and older - 1.0-1.5 g / day.

The course of continuous treatment is 1-2 months. Improvement can be observed in the 1st week of therapy. Single therapeutic doses are selected individually: from 0.1 to 0.3 g for residual organic failure; from 0.3 to 0.6 for addictive behavior, frequency of administration 2-3 times a day. The effect is observed already on the 2-3rd day of administration. The duration of treatment is 3 months for residual organic failure and 3-4 weeks for addictive behavior.

It should be noted that in pediatrics, adaptol begins to be used from 5-7 years of age. This means the possibility of its use in premenstrual syndrome, as in the literature there is data on the effectiveness of adaptol therapy from the 14th-18th day of the menstrual cycle until the onset of menstrual bleeding, 2-3 courses of treatment. The drug eliminates vegetative-vascular dystonia and emotional manifestations of the disease. However, no studies have been conducted in girls aged 11–14 years.

It can be assumed that the drug has a positive effect in adolescents with psychovegetative disorders of various origins.

In addition, adaptol is recommended for parents when initially contacting a psychiatrist in a state of anxiety, anxious anticipation of a “terrible” diagnosis in a child.

The use of the drug in obstetric practice revealed its affinity for placental membranes; the drug accumulates in the placenta and causes a pronounced dilating effect on the uterine and placental vessels. The use of mebicarum led to the normalization of disorders in all parts of the functional system mother-placenta-fetus. The drug increases the specific activity of the kallikrein-kinin system, which enhances the vasodilator effect. The use of mebicarum normalized the condition of the fetus during hypoxia due to the normalization of uteroplacental blood flow and a direct effect on the functions of fetal centers that regulate homeostasis and activation of the hormonal function of the placenta. The drug was used starting from the 28th week of pregnancy at the rate of 20-25 mg per 1 kg of body weight of the pregnant woman in 4-5 doses per day for 6-7 days. The vasodilating effect of mebicarum occurred on days 2-3 and persisted for a long time.

The nootropic effect of adaptol can also be considered proven. Even in studies on mebicarum, comparison of the nootropic effect of the drug with piracetam and pyriditol made it possible to identify a harmonious spectrum of nootropic action of mebicarum. In elderly patients with organic brain lesions and schizophrenia with a disease duration of more than 10 years, mebicarum monotherapy for 3-4 weeks in doses of 0.3-1.5 g/day was more effective than compared drugs in patients with symptoms of hyperesthesia, emotional and vegetative lability, increased emotional excitability and intense emotional experiences. Clinical manifestations of weakened memory and understanding were subject to greater reduction. At the same time, pyriditol was superior to compared drugs in its effect on abulia, motor retardation, decreased affect, and increased exhaustion, and piracetam was most effective in ideational retardation and was comparable to pyriditol in its effect on apathy. Vasovegetative disorders decreased with treatment with all drugs to the same extent. The authors associate the harmonious nature of the nootropic spectrum of action of mebicarum with its optimizing effect on the thinking of patients. At the same time, the stimulating component in the action of pyriditol and piracetam introduces fussiness and irritability into the behavior of patients, and reduces the active inhibition necessary for targeted volitional and intellectual efforts. In addition, mebicarum had a normalizing effect on deficit thinking disorders in patients with paranoid schizophrenia, reduced symptoms such as paralogy, reasoning, incoherence, and did not stimulate any disorders in this area. Mebicarum contributed to a change in the type of thinking from the “right hemisphere” - emotional, concrete and figurative, to the “left hemisphere” - predominantly verbal, abstract and logical, and piracetam enhanced the “right hemisphere” features of thinking - emotionality, imagery and concreteness. The dose dependence of the nootropic effect of mebicarum has been established. When prescribing small doses of the drug (0.9 g/day), the psychostimulating and antidepressant effect is more pronounced, at medium doses (1.8-2.7 g/day) - antiasthenic and nootropic, at high doses (4.5 g/day) ) - sedative.

According to data obtained by S.A. Zhivolupov et al., adaptol improves neuroplasticity processes by increasing the level of one of the neurotrophic growth factors, brain-derived neurotrophic factor (BDNF), in patients with certain functional and organic diseases of the nervous system. The use of the drug in complex therapy of patients with somatoform dysfunction of the autonomic nervous system and the consequences of closed craniocerebral injury, in addition to regression of clinical symptoms, 30 days after the start of treatment led to a significant increase in the level of BDNF in the blood, and this effect was dose-dependent and more pronounced at a daily dose of adaptol 3000 mg than at a dose of 1500 mg.

Many studies have noted the ability of the drug to normalize the functioning parameters of various, sometimes multidirectional, changes in many body systems. When treated with adaptol, the tolerability of conditions that require tension in adaptation processes improves, which is considered as the adaptogenic activity of this drug. Thus, in patients with long-term consequences of exposure to ionizing radiation, 16 years after the accident at the Chernobyl nuclear power plant, who received against the background of traditional therapy (nootropics, cardiotrophics, vascular drugs, vitamins) mebicarum for 2 weeks on the 1st day - 300 mg, during 2-3 days - 600 mg, then 900 mg (300 mg 3 times a day) until the end of the course, the effectiveness of therapy increased on average 2 times for leading symptoms (irritability, anxiety, sleep disturbances, blood pressure normalized and heart activity, decreased severity of headaches and shortness of breath during emotional experiences) and decreased addiction to smoking. Moreover, positive results were achieved already in the 1st week of treatment.

In case of tobacco addiction, data have been obtained on a decrease in the desire to smoke and alleviation of withdrawal disorders with the use of mebicarum in complex therapy at a dose of 0.6 g 3 times a day for 3-4 weeks.

Mebicarum in doses of 1.5-2.1 g/day for 3-4 weeks eliminates or weakens the severity of borderline mental disorders in patients with alcoholism - asthenia, irritability, emotional lability, dysphoria, craving for alcohol. In addition, mebicarum increases the synthesis of endogenous alcohol in the body of patients by approximately 75% - 2 times more than after taking sodium hydroxybutyrate, and 4 times more than after taking seduxen. It is the increase in the concentration of alcohol in the blood of patients to normal that leads to a decrease and disappearance of the need for alcohol after taking 1.5 g of mebicarum.

In the treatment of chronic alcoholism with the calculation of an individual dosage regimen, based on an assessment of the drug content in the blood plasma during the development of the tranquilizing effect, after taking a single dose, effective elimination of psychopathological disorders was ensured.

According to the data available in the literature, the use of the drug is considered effective for non-coronary cardialgia of various origins, with the exception of cardialgia associated with spinal osteochondrosis. In climacteric syndrome, mebicarum affects the manifestations of cardiac syndrome: eliminates or weakens pain, shortness of breath, palpitations; normalizes repolarization processes in the myocardium and central hemodynamic parameters. Also eliminates or weakens other manifestations of menopausal syndrome: hot flashes, paresthesia, headaches, fatigue; normalizes sleep. It is known that currently, menopausal syndrome is considered largely as a process of adaptation of the body to new conditions of hormonal regulation.

If the listed properties of adaptol can largely be explained by its central mechanism of action, then the remaining described effects of the drug clearly require explanation.

So, according to L.O. Gromova et al., in the mechanisms of action of adaptol there is a direct antioxidant effect, which consists in the ability to inhibit the peroxidation of not only lipids, but also proteins.

When using the drug as a tranquilizer, its hypolipidemic effect was noted.

Mebicarum at a dose of 1.8 g/day for 3 weeks reduced the content of total cholesterol (TC) in the blood plasma by 36%, very low density lipoprotein cholesterol (VLDL) by 28%, low density lipoprotein cholesterol (LDL) by 20.4%, triglycerides (TG) - by 23% and increased the level of high-density lipoproteins (HDL) - by 47% compared to the initial level. At a dose of 1.2 g/day, after 2 weeks of treatment, mebicarum reduced the level of total cholesterol in the blood plasma by 28%, LDL cholesterol by 21% and increased the level of HDL cholesterol by 32%. According to the same authors, the drug corrects the proatherogenic effect of β-blockers. To clarify whether the hypocholesterolemic effect of mebicarum is a consequence of its psychotropic activity or this is its original specific property, a comparative experimental study was conducted on the effect of mebicarum (250 mg/kg) and diazepam (2 mg/kg) on ​​lipid metabolism in rats. Mebicarum, unlike diazepam, reduced the level of LDL cholesterol by 27.4% and increased the level of HDL cholesterol by 48%. This indicates that the antihyperlipidemic effect of mebicarum is not related to its psychotropic activity, but is a specific feature.

In an experiment on rats, hypokinesia for 14 days led to a decrease in animal body weight, an increase in the relative weight of the adrenal glands, an increase in the content of total cholesterol, TG, malondialdehyde and a decrease in the level of HDL cholesterol and phospholipids. The use of mebicarum not only prevented a decrease in the body weight of rats and an increase in the mass of the adrenal glands, but also led to a decrease in total cholesterol, TG and the level of malondialdehyde, as well as an increase in the content of HDL cholesterol and phospholipids, which made it possible to state that mebicarum has a combination of adaptogenic, hypolipidemic and antioxidant properties .

A similar antihyperlipidemic effect of the drug was found when reproducing nutritional hypercholesterolemia in rabbits. Thus, mebicarum also has an antihyperlipidemic effect in models of hypercholesterolemia not associated with stress effects on lipid metabolism.

Unlike benzodiazepine tranquilizers, mebicarum enhances the contractile function of the myocardium, increases systolic and cardiac output, and accelerates blood flow in the aorta. The cardiac stimulating effect of the drug is also manifested in an isolated heart and in conditions of blockade of beta-adrenergic receptors of the heart. Mebicarum increases the volumetric velocity of coronary blood flow, the strength and duration of this effect depends on the dose of the drug and ranges from 15 to 35 minutes. In parallel with the increase in coronary blood flow, the absorption of oxygen by the heart increases, but to a much lesser extent, therefore the content of oxyhemoglobin in the venous blood increases. Experiments on various models of acute coronary insufficiency (ligation of the descending branch of the left coronary artery, dosed narrowing of the coronary artery with simultaneous imposition of a high contraction rhythm on the heart) revealed a positive effect of mebicarum on ischemic myocardium: ST segment elevation decreased, the ratio of lactate and pyruvate in the blood flowing from the heart was normalized. ischemic zones.

At doses of 200-500 mg/kg, mebicarum expanded the peripheral (femoral) arteries, reducing their resistance to blood flow, which was not due to a direct myotropic effect, but was realized through neurogenic sympathetic tone. At the same doses, mebicarum suppressed the bioelectrical activity of the sympathetic nerves of the kidneys and heart.

According to clinical studies, a good and satisfactory antianginal effect was observed in approximately 70% of patients with angina pectoris. Their mood improved, the number of anginal attacks and daily consumption of nitroglycerin decreased by 2-4 times. In patients with angina pectoris of functional class II, tolerance to dosed physical activity increased. The authors believe that for angina of functional class I and II, mebicarum can be considered as an independent antianginal agent; for more severe angina, it is recommended to be used in combination with nitrates and β-adrenergic blockers.

Mebicarum had an analgesic effect in the acute period of myocardial infarction (MI), enhanced the analgesic effect of fentanyl and eliminated its side effects on the cardiovascular system.

The use of mebicarum during the rehabilitation period in patients who had suffered an MI helped to improve their coronary blood flow, expand the range of physical activities, and reduce fear of them. According to I.E. Zimakova et al., improvement of oxygen balance in the heart muscle occurred due to an increase in coronary blood flow, antihypoxic effect, decrease in blood viscosity and intravascular aggregation of erythrocytes.

Patients with post-infarction cardiosclerosis and the presence of psychosomatic pathology (high level of personal anxiety, anxious-asthenic, anxious-phobic states) in addition to standard therapy with nitrates, angiotensin-converting enzyme inhibitors, β-blockers, aldosterone antagonists, disaggregants, statins, trimetazidine in one group were prescribed the anxiolytic adaptol at a dose of 500 mg 2 times a day, on the other - standard therapy and placebo adaptol. Observation continued for 1 month. An assessment of the quality of life showed that the addition of adaptol contributed to an increase in mental resistance to stressful situations and an improvement in the psychological adaptation of patients who had suffered an MI. Indicators of social functioning remained virtually unchanged in both groups. The antianginal effect of adaptol was observed due to a decrease in the frequency of angina attacks that occurred after psycho-emotional stress, with angina pectoris of physical exertion; there were no differences between the groups.

Among the patients included in the study, an analysis of the quality of life in chronic heart failure stages I-IIA was carried out in both groups. In the adaptol group, the quality of life increased in a significantly larger number of patients due to the physical and emotional spheres, in the group receiving standard therapy and placebo, mainly due to improved physical indicators.

In a later study of the therapeutic potential of adaptol in the early post-infarction period (3-4 weeks after MI) in patients with anxiety disorders, the authors concluded that adaptol at a dose of 1500-2000 mg/day after 28-30 days of therapy has an anxiolytic, stress-protective, vegetative-normalizing and anti-asthenic effects, eliminates sleep disturbances by accelerating the process of falling asleep, reducing the number of night and early morning awakenings; reduces the sympathetic effect on the activity of the heart, helping to normalize autonomic reactivity. The authors indicate that the administration of adaptol as part of basic therapy improves the clinical course of the post-infarction period, reduces the number of anginal attacks, while reducing the frequency of taking nitroglycerin tablets, and increases the distance covered during the 6-minute walk test. At the same time, no adverse interaction of adaptol with drugs in the basic therapy of chronic heart failure: nitrates, β-blockers, angiotensin-converting enzyme inhibitors, diuretics was detected.

According to available data, in addition to the work of R.A. Camburg et al. (1986), which indicates the possibility of considering adaptol as an independent antianginal agent, all subsequent work proves an increase in the antianginal effect in patients with angina pectoris and in the post-infarction period only if angina pectoris was caused by stress or the presence of anxiety disorders. Thus, the question of whether adaptol has an independent antianginal effect remains open.

The inclusion of adaptol in addition to antihypertensive therapy in patients with post-infarction cardiosclerosis with hypertension was accompanied by more pronounced positive dynamics in the variability of systolic and diastolic blood pressure during the day and night than in the placebo group.

The inclusion of adaptol in the treatment regimen increased the severity of the lipid-lowering effect of the combination of statins and adaptol compared to statins. According to L.A. Lapshina, P.G. Kravchun, O.S. Shevchenko (2008), correction of psychopathological manifestations and oxidative stress by adaptol in patients who have suffered a myocardial infarction is evidence of the specific effect of adaptol in correcting the lipid composition of the blood and seems especially important in patients who have suffered an acute MI.

Compared with standard therapy for patients with post-infarction cardiosclerosis, the addition of adaptol to it led to a more pronounced positive effect on the processes of free radical oxidation (decrease in pro-oxidant and increase in antioxidant activity). V.N. Kovalenko et al. (2006) showed that the addition of adaptol to the complex therapy of hypertension and neurocirculatory dystonia contributed to the improvement of heart rate variability parameters with a decrease in the activity of the sympathetic division of the autonomic nervous system, restoring its balance with normalization of the regulation of heart activity.

In the work of L.M. Vasilets et al. The structure of heart rhythm disturbances and the features of temporal analysis of heart rate variability in patients with the syndrome and phenomenon of premature excitation of the ventricles were studied. It was shown that the use of adaptol in a dose of 500 mg 2 times a day for 60 days against the background of antiarrhythmic therapy with amiodarone helped to reduce autonomic imbalance and reduced the arrhythmogenic readiness of the myocardium.

The antihyperlipidemic, antioxidant, and anti-ischemic effects of the drug obtained experimentally and clinically cannot in any way be due only to the studied central mechanisms of its action. And if the antioxidant effect of the drug can also be explained by the fact that the drug molecule contains two methylated urea fragments, and urea is considered as a reference antioxidant, then the antihyperlipidemic and antianginal effects of the drug cannot be associated only with its central and antioxidant action. In this regard, it is of particular interest to directly study the mechanisms of the drug’s influence on lipid metabolism, the peroxidation system, and especially coronary blood flow, both experimentally and in clinical practice, especially taking into account the effect of the drug on the chemical activity of water.

There is evidence that extremely high-frequency (EHF; millimeter waves) irradiation stimulates cellular receptors of a protein nature due to the activation of the aqueous component of the extracellular fluid. At the same time, the fraction of mobile, chemically active H2O molecules increases. The introduction into the biological environment of certain low-molecular substances that destabilize the structure of water can simulate the effects of EHF irradiation. This effect is inherent in urea. Under its influence, the generation of a fraction of mobile water molecules in solution and, along with this, the depletion of a fraction of bulk water not included in the fraction of mobile molecules was revealed. Depletion of the bulk water fraction was correlated with the instability of proteins such as chymotrypsinogen and serum albumin (denaturation). The authors believe that since the unfolding of the protein globule is preceded by an increase in intraglobular mobility, the denaturation effect manifests both direct and indirect effects of urea on protein dynamics through the destruction of the water structure.

The structural determinant of the urea fragment, which is responsible for its ability to generate mobile water molecules, has been established: the presence of two close and parallel N–H bonds.

Similar properties were found in mebicarum. Urea and mebicarum activate water as a nucleophilic reagent. An increase in the chemical activity of water is associated with the destruction of the structure of water, i.e. with an increase in the proportion of rotator molecules. Most likely, all this determines the unusually wide range of pharmaceutical activity of the anxiolytic mebicarum without its inclusion in metabolism and in the absence of specific receptors.

The above can largely shed light on the unique, multifaceted spectrum of clinical effectiveness of adaptol and proves the need for a deeper study and detailed mechanisms of action of the drug in such various pathological processes both in the clinic and in experiments.

3.3

23

Assessing the effectiveness of drugs

The effectiveness of drugs is determined based on the results of clinical studies and practical experience of use.

Adaptol

From the perspective of evidence-based medicine, Adaptol remains a controversial drug. The Cochrane Library contains studies confirming the effectiveness and safety of anxiolytics. There are several articles on the drug in the medical database PubMed, but none of them contain information about large placebo-controlled studies. One of them indicated that Adaptol is effective in asthenoneurotic syndrome against the background of muscular dystonia, but the sample of patients was small, and we cannot rely on these data.

In Russian-language literature, Adaptol is treated differently. Review articles indicate that the drug is used for. Clinical trials have shown that in the second week of therapy, patients’ anxiety decreases and concomitant autonomic disorders go away. Adaptol is also used in some other areas of medicine.

Afobazole

Afobazol, like Adaptol, does not have a serious evidence base. There is no mention in PubMed or the Cochrane Library that placebo-controlled studies have been conducted for the drug. And only in Russian-language literature can you find information about the drug:

Afobazole for neuroses associated with anxiety. A clinical study showed that the effect of the drug develops slowly, with improvement observed by the end of the 4th week of treatment. There are practically no side reactions.

Afobazole itself and for generalized anxiety disorders. The review article shows that long-term use does not reduce the effectiveness of the drug and does not increase the risk of adverse reactions.

Comparison of addiction between Afobazol and Adaptol

Like safety, addiction also involves many factors that must be considered when evaluating a drug.

So, the totality of the values ​​of such parameters as “syndrome o” in Afobazole is quite similar to the similar values ​​in Adaptol. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Afobazole has a fairly low “syndrome” value, just like Adaptol.

Application diagram

The treatment regimen for the drugs is similar:

  1. Adaptol is prescribed three times a day. The maximum single dosage is 3 g, daily dosage is 10 g. The drug should be taken orally regardless of food intake. The duration of therapy ranges from several days to three months and depends on the clinical picture.
  2. Afobazole is prescribed three times a day. The maximum daily dosage is 30 mg. The course of therapy is 2-4 weeks. If necessary, you can increase the duration of treatment to three months.

Comparison of side effects of Afobazole and Adaptol

Side effects or adverse events are any adverse medical event that occurs in a subject after administration of a drug.

Afobazol's side effects are almost the same as Adaptol's. They both have few side effects. This implies that the frequency of their occurrence is low, that is, the indicator of how many cases of an undesirable effect of treatment are possible and registered is low. The undesirable effect on the body, the strength of influence and the toxic effect of Afobazole are similar to Adaptol: how quickly the body recovers after taking it and whether it recovers at all.

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