The costs of the modern pace of life and current events are endless lack of sleep, frequent outbursts of aggression and irritability, fatigue and apathy. However, living in the ringing silence of Tibet or a dense forest is not at all a way to avoid the negative factors that accompany our everyday life. It is quite possible to learn to manage your bad mood. Moreover, pharmacology willingly helps with this with a wide variety of means.
Today we are talking about Afobazole, a popular drug for stress and anxiety. When can it be used, what is it good for and what effect to expect.
Medicine Afobazol
It has been on the Russian market of anti-anxiety and sedatives since 2000. The drug was developed at the Research Institute of Pharmacology of the Russian Academy of Medical Sciences, as a result of the search for selectively acting anxiolytics that would be devoid of side effects characteristic of the main group of anti-anxiety drugs. During this time, the drug was noted by consumers as effective in relieving anxiety and stress, and as a drug with the fewest side effects.
Composition of Afobazole
Afobazole is “in the middle”, between simple sedatives (dietary supplements) and serious psychotropic drugs. The drug is over-the-counter, but should be taken as prescribed by a specialist.
The main active ingredient of afobazole, fabomotizole, is a mild and delicate antidepressant (anxiolytic substance), which, acting on certain types of receptors in the brain, restores their sensitivity to inhibitory mediators. That is, it helps to achieve a balance between the processes of excitation and inhibition, normalizing the mental state.
Increases the bioenergetic potential of neurons in general, has a neuroprotective effect: restores and protects nerve cells. The drug is metabolized in the liver and is quickly transferred from the general bloodstream to peripheral areas. The effect of the drug is achieved after 5-7 days of use. A stable result is observed after a month of use and persists for 10-14 days after discontinuation of the drug.
Release form and dosage
Afobazole is available only in tablet form. 1 tablet contains 10 mg of active ingredient. The number of tablets per package is 60 pcs. Among the excipients in afobazole tablets are: potato starch; microcrystalline cellulose; lactose. So, people with lactose intolerance, and any components of the composition, should take afobazole with caution, or consider another drug.
Indications for Afobazole
Taking the drug immediately has a double effect on the body:
- Firstly, it eliminates anxiety or reduces its manifestations - fears, worries and nervousness, bad premonitions and fears about future events and the present, even if there are no visible reasons for anxiety.
- Secondly, it has a mild activating, stimulating effect. The drug helps to balance the mental state, cope with irritability, nervous tension, helps to relax and normalize sleep, reduces nervousness and tearfulness, including during premenstrual syndrome in women. Reduces symptoms of depression and stabilizes mood.
Afobazole is indicated for the treatment of frequent manifestations of anxiety companions: muscle spasms, cardiovascular, respiratory and gastrointestinal. The drug is especially indicated for persons with persistent manifestations of psychosomatics: bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, hypertension and arrhythmia.
Afobazole eliminates disorders of the autonomic system: dry mouth, sweating, dizziness. Copes with cognitive disorders, which are almost constant companions of mental and stress disorders: inability to concentrate when solving even simple problems, weakened memory. It can be prescribed to asthenics with personality traits such as anxious suspiciousness, uncertainty, increased vulnerability and emotional instability, as well as to persons prone to emotional stress reactions.
Helps to survive difficult situations, stressful periods, and periods of adaptation to new living conditions with comfort and minimal emotional and mental losses.
Also provides mental health support during treatment of: sleep disorders of various origins, premenstrual syndrome in women; hangover; to alleviate the “withdrawal” syndrome when quitting smoking. Afobazole does not cause muscle weakness and drowsiness, does not reduce memory and concentration, and therefore does not have a negative effect on driving. While taking the drug, addiction does not develop, and withdrawal syndrome does not occur, which often occurs when taking other types of antidepressants with the development of dependence.
Afobazole treatment regimens
The optimal single dose is 10 mg. The daily dose of the drug is 30 mg (3 doses of 10 mg each). Take the tablets with water. Depending on the severity of symptoms and indications, the course of the drug ranges from 2 to 4 weeks, but after consultation with a specialist, therapy can be extended to 3 months with an increase in the daily dose to 60 mg.
Contraindications
- Individual intolerance and hypersensitivity to the composition;
- galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- During pregnancy and breastfeeding;
- children and adolescents under 18 years of age.
Special recommendations for Afobazole
Despite the fact that Afobazole is maximally free of side effects and does not cause drowsiness or addiction, its use should be taken as seriously as possible, weighing the potential benefits and harms. The drug can be taken when performing potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Afobazole and alcohol
Alcohol is in principle incompatible with the concept of “treatment”. The drug does not interact with ethanol, but despite this, any therapy should be separated from alcohol intake due to the increased load on the liver and gastrointestinal tract. Afobazole can be used during a hangover period, as an aid in getting out of a drunken state. It is very important not to interrupt treatment at this moment, even if relief has occurred.
Afobazole for children
Afobazole is not used in children, because the full formation of the nervous system in children has not yet been completed, and in adolescents it is destabilized due to entering adolescence and hormonal changes. If corrective medications are required during this period, it is best not to consider afobazole as suitable. To select anti-anxiety and sedatives for children and adolescents, it is best to consult a specialist.
Afobazole during pregnancy
The drug has a high ability to penetrate the placenta and breast milk. So it is strictly prohibited for use during pregnancy and lactation due to the possibility of harming the developing fetus.
Afobazole for heart disease
The drug will have a positive effect on cardiovascular pathologies only if the latter are the result of mental disorders and arise against the background of stress and depressive states. If you have confirmed cardiovascular diagnoses, it is best to consult with a specialist and compare the harm and benefit of taking the drug.
Afobazole and smoking
Nicotine does not reduce the effect of taking the drug. But at the same time it helps to get rid of the nervous consequences of quitting smoking, acting on neurons and the nervous system in an inhibitory way. Quitting smoking is a stress for heavy smokers, which Afobazol is designed to cope with.
It is important to remember that no medicine can be taken constantly, relying on it to survive stressful situations.
Monitor your mental state regularly, then the participation of medications in your life will be minimal! Take care of yourself and be healthy!
Afobazol tablets 10 mg No. 20x3
Name
Afobazole tablet 10 mg in container pack No. 20x3
Description
Tablets are white or white with a yellowish tint, flat-cylindrical with a bevel.
Main active ingredient
Morpholinoethylthioethoxybenzimidazole
Release form
pills
Dosage
10mg
Pharmacodynamics
Afobazole® is a selective non-benzodiazepine anxiolytic. Acting on sigma-1 receptors in nerve cells of the brain, Afobazol® stabilizes GABA/benzodiazepine receptors and restores their sensitivity to endogenous inhibitory mediators. Afobazol® also increases the bioenergetic potential of nerve cells and protects them from damage (has a neuroprotective effect). The effect of the drug is realized primarily as a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects. Afobazole® reduces or eliminates feelings of anxiety (preoccupation, apprehension, apprehension, irritability), tension (fearfulness, tearfulness, restlessness, inability to relax, insomnia, fear), somatic manifestations of anxiety (muscular, sensory, cardiovascular, respiratory, gastrointestinal -intestinal symptoms), autonomic disorders (dry mouth, sweating, dizziness), cognitive disorders (difficulty concentrating, impaired memory). The use of the drug is especially indicated in persons with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, and a tendency to emotional stress reactions. The effect of the drug develops on days 5-7 of treatment. The maximum effect is achieved by the end of 4 weeks of treatment and persists after the end of treatment for an average of 1-2 weeks. Afobazole® does not cause muscle weakness, drowsiness and does not have a negative effect on concentration and memory. When using it, drug dependence does not form and “withdrawal” syndrome does not develop.
Pharmacokinetics
After oral administration, Afobazol® is well and quickly absorbed from the gastrointestinal tract. The maximum concentration of the drug in plasma (Cmax) is 0.130±0.073 mcg/ml; time to reach maximum concentration (Tmax) - 0.85±0.13 hours. Metabolism: Afobazole® undergoes a “first pass effect” through the liver, the main directions of metabolism are hydroxylation at the aromatic ring of the benzimidazole ring and oxidation at the morpholine fragment. Afobazole® is intensively distributed throughout well-vascularized organs; it is characterized by rapid transfer from the central pool (blood plasma) to the peripheral (highly vascularized organs and tissues). The half-life of Afobazole® when taken orally is 0.82±0.54 hours. The short half-life is due to intensive biotransformation of the drug and rapid distribution from blood plasma to organs and tissues. The drug is excreted primarily in the form of metabolites and partially unchanged in urine and feces. With long-term use it does not accumulate in the body.
Indications for use
Afobazole® is used in adults for anxiety conditions: generalized anxiety disorders, neurasthenia, adaptation disorders, in patients with various somatic diseases (bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, coronary heart disease, hypertension, arrhythmias), dermatological, oncological and other diseases. In the treatment of sleep disorders associated with anxiety, neurocirculatory dystonia, premenstrual syndrome, alcohol withdrawal syndrome, to alleviate the “withdrawal” syndrome when quitting smoking. The use of the drug Afobazol® for the treatment of generalized anxiety disorder is permissible only as prescribed by the attending physician.
Directions for use and doses
Used internally after meals. Optimal single doses - 10 mg; daily - 30 mg, divided into 3 doses during the day. The duration of the course of use of the drug is 2-4 weeks. If necessary, on the recommendation of a doctor, the daily dose of the drug can be increased to 60 mg, and the duration of treatment up to 3 months.
Use during pregnancy and lactation
The use of the drug during pregnancy and lactation is contraindicated, because The safety of the drug has not been studied in pregnant and lactating women. There was no evidence of reproductive toxicity in experimental studies.
Interaction with other drugs
Afobazol® does not interact with ethanol and does not affect the hypnotic effect of thiopental. Enhances the anticonvulsant effect of carbamazepine. Causes an increase in the anxiolytic effect of diazepam.
Contraindications
Individual intolerance to the drug. Galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Pregnancy, lactation period. Children under 18 years of age.
Compound
For one tablet: Active substance: fabomotizole (fabomotizole dihydrochloride) - 10 mg. Excipients: potato starch - 48 mg, microcrystalline cellulose - 35 mg, lactose monohydrate - 48.5 mg, medium molecular weight povidone (medium molecular weight polyvinylpyrrolidone, Kollidon 25) - 7 mg, magnesium stearate - 1.5 mg.
Overdose
With significant overdose and intoxication, the development of sedation and increased drowsiness without manifestations of muscle relaxation. As an emergency solution, caffeine 20% solution in 1.0 ml ampoules is used 2-3 times a day subcutaneously.
Side effect
Allergic reactions are possible. Rarely - headache, which usually goes away on its own and does not require discontinuation of the drug.
Storage conditions
Store at a temperature not exceeding 25 °C. Keep out of the reach of children. Store the drug in its original packaging to protect it from light and moisture.
Afobazol - instructions for use
Where can I buy?
Registration number : LP-006555 Trade name of the drug: Afobazol® Retard INN or group name: fabomotizol Dosage form: extended-release film-coated tablets
the only* over-the-counter anti-anxiety drug that is used once a day *according to GRLS data as of 04/01/2021
Composition per tablet:
Active substance:
fabomotizole (fabomotizole dihydrochloride) – 30.0 mg.
Excipients:
Kollidon® SR [polyvinyl acetate, povidone, sodium lauryl sulfate, silicon dioxide] - 120.0 mg, hypromellose - 25.0 mg, lactose - 23.0 mg, magnesium stearate - 2.0 mg.
Shell composition:
Opadry II 85 F18422 white [polyvinyl alcohol, partially hydrolyzed, titanium dioxide, macrogol 4000, talc] - 6.0 mg.
Description: round, biconvex, almost white film-coated tablets. On a cross section, the kernel is almost white or white with a yellowish-brownish tint.
Pharmacotherapeutic group: anxiolytic agent (tranquilizer).
ATX code: N05BX.
Pharmacodynamics.
Afobazol® Retard is a selective non-benzodiazepine anxiolytic.
Acting on sigma-1 receptors in nerve cells of the brain, Afobazol® Retard stabilizes GABA/benzodiazepine receptors and restores their sensitivity to endogenous inhibitory mediators. Afobazol® Retard also increases the bioenergetic potential of neurons and has a neuroprotective effect: it restores and protects nerve cells.
The effect of the drug is realized primarily as a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects.
Afobazole® Retard reduces or eliminates feelings of anxiety (concern, bad feelings, fears), irritability, tension (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear), depressive mood, somatic manifestations of anxiety (muscular, sensory, cardiovascular , respiratory, gastrointestinal symptoms), autonomic disorders (dry mouth, sweating, dizziness), cognitive disorders (difficulty concentrating, weakened memory), incl. arising from stress disorders (adaptation disorders). The use of the drug is especially indicated in persons with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, and a tendency to emotional stress reactions.
Afobazole® Retard does not cause muscle weakness, drowsiness and does not have a negative effect on concentration and memory. When using it, addiction does not form, drug dependence does not develop, and “withdrawal” syndrome does not develop.
Pharmacokinetics.
After oral administration, Afobazol® Retard is well and quickly absorbed from the gastrointestinal tract. Food intake does not affect the absorption of the drug and the pharmacokinetic parameters.
The maximum concentration of the drug in plasma (Cmax) after a single dose is 47.740 + 43.252 ng/ml, after multiple doses - 27.668 + 13.770 ng/ml; time to reach maximum concentration (Tmax) – 2.1+1.1 and 2.6+1.0 hours after single and multiple doses, respectively.
Metabolism: Afobazole® Retard undergoes a “first pass effect” through the liver; the main directions of metabolism are hydroxylation at the aromatic ring of the benzimidazole ring and oxidation at the morpholine fragment.
Afobazol® Retard is intensively distributed throughout well-vascularized organs; it is characterized by rapid transfer from the central pool (blood plasma) to the peripheral (highly vascularized organs and tissues).
The half-life of Afobazol® Retard when taken orally is 8.41+5.01 hours after a single dose and 6.05+3.54 hours after multiple doses. The drug is excreted mainly in the form of metabolites and partially unchanged by the kidneys and through the intestines.
Indications for use.
Afobazol® Retard is used in adults for anxiety conditions: generalized anxiety disorders, neurasthenia, adaptation disorders, in patients with various somatic diseases (bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, coronary heart disease, hypertension, arrhythmias), dermatological, oncological and other diseases; in the treatment of sleep disorders associated with anxiety.
Contraindications.
- Hypersensitivity to fabomotizole and/or any excipient in the drug.
- Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.
- Pregnancy, breastfeeding period.
- Children under 18 years of age.
If you have one of the diseases listed above, you should consult your doctor before using the drug.
Use during pregnancy and breastfeeding.
The use of Afobazol® Retard is contraindicated during pregnancy.
If it is necessary to use the drug during lactation, breastfeeding should be discontinued.
Before using Afobazol® Retard, if you are pregnant or think you might be pregnant, or are planning a pregnancy, you should consult your doctor.
Method of administration and dose.
Used internally.
1 tablet 1 time per day, in the morning, regardless of meals.
The duration of the course of use of the drug is 2–4 weeks.
If there is no improvement after treatment, or symptoms worsen, or new symptoms appear, you should consult your doctor.
Use the drug only according to the indications, method of administration and in the doses indicated in the instructions.
Side effects.
Undesirable effects that may develop during treatment with Afobazol® Retard are classified according to the following frequency of occurrence:
very often (> 1/10), often (from > 1/100 to < 1/10), infrequently (from > 1/1,000 to < 1/100), rarely (from > 1/10,000 to < 1/10) 1,000), very rare (< 1/10,000), frequency unknown (cannot be determined from available data).
From the immune system: frequency unknown - allergic reactions.
From the nervous system: rarely - headache, which usually goes away on its own and does not require discontinuation of the drug.
If you experience the side effects listed in the instructions, or they get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
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Overdose.
Symptoms With significant overdose and intoxication, the development of sedation and increased drowsiness without manifestations of muscle relaxation is possible. Treatment. As an emergency solution, caffeine 20% solution in 1.0 ml ampoules is used 2-3 times a day subcutaneously.
If symptoms of overdose appear, stop taking the drug and consult a doctor immediately.
Interaction with other drugs.
Afobazole® Retard does not interact with ethanol and does not affect the hypnotic effect of thiopental. Enhances the anticonvulsant effect of carbamazepine. Causes an increase in the anxiolytic effect of diazepam.
If you are using the above or other medications (including over-the-counter medications), consult your doctor before using Afobazol® Retard.
Influence on the ability to drive vehicles and machinery.
The drug does not have a negative effect on driving vehicles and performing potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form.
Extended-release film-coated tablets, 30 mg.
20 tablets each in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
1 blister pack with instructions for use is placed in a cardboard pack.
Storage conditions.
At a temperature not higher than 25 ºС. Keep out of the reach of children.
Best before date.
2 years. Do not use after the expiration date stated on the packaging.
Vacation conditions.
Over the counter.
Marketing authorization holder/organization receiving consumer complaints
OTCPharm JSC, Russia, 123112, Moscow, st. Testovskaya, 10. Tel., fax. www.otcpharm.ru
