Afobazol 10mg №60 pills
CompositionActive substance: morpholinoethylthioethoxybenzimidazole dihydrochloride (afobazole) (calculated on the dry matter) - 5 mg or 10 mg. Auxiliary substances: potato starch - 48 mg, microcrystalline cellulose - 40 mg (for 5 mg dosage) and 35 mg (for dosage 10 mg), lactose monohydrate - 48.5 mg, povidone (medical polyvinylpyrrolidone, Kollidon 25) - 7 mg, magnesium stearate - 1.5 mg.
Mode of applicationIt is applied inside, after food. Optimum single doses - 10 mg; daily allowance - 30 mg, divided into 3 doses during the day. The duration of the course of the drug is 2-4 weeks. If necessary, according to the recommendation of the doctor, the daily dose of the drug can be increased to 60 mg, and the duration of treatment up to 3 months.
Anxiety in adults:
- generalized anxiety disorders, neurasthenia, adjustment disorders;
- in patients with various somatic (bronchial asthma, irritable bowel syndrome, SLE, ischemic heart disease, arterial hypertension, arrhythmias), dermatological, oncological and other diseases;
- sleep disorders associated with anxiety;
- premenstrual tension syndrome;
- alcohol withdrawal syndrome;
- to relieve withdrawal symptoms when quitting smoking.
Contraindications- pregnancy; - lactation period (breastfeeding); - age up to 18 years; - hypersensitivity to the drug; - individual intolerance to the drug; - intolerance to galactose; - Lactase deficiency or glucose-galactose malabsorption
Pharmacological propertiesAfobazole is a derivative of 2-mercaptobenzimidazole, a selective anxiolytic that is not in the benzodiazepine receptor agonist class. Interferes with the development of membrane-dependent changes in the GABA receptor.
The drug has an anxiolytic action with an activating component that is not accompanied by hypno-sedative effects (a sedative effect is detected in doses 40-50 times higher than the ED50 for anxiolytic action). The drug has no muscle relaxant properties, a negative effect on memory and attention.When using the drug is not formed drug dependence and does not develop withdrawal syndrome.
The action of the drug is realized mainly in the form of a combination of anxiolytic (anti-anxiety) and easily stimulating (activating) effects. Reduction or elimination of anxiety (preoccupation, misgivings, fears, irritability), tensions (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear) and, therefore, somatic (muscular, sensory, cardiovascular, respiratory, gastrointestinal) intestinal symptoms), vegetative (dry mouth, sweating, dizziness), cognitive (concentration difficulties, impaired memory) disorders observed on days 5-7 of treatment with Afobazole. The maximum effect is achieved by the end of 4 weeks of treatment and lasts an average of 1-2 weeks in the post-therapeutic period.
Especially shown is the use of the drug in individuals with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, a tendency to emotional and stressful reactions. Afobazole is non-toxic (LD50 in rats is 1.1 g with an ED50 of 1 mg).
PharmacodynamicsAfobazole is a selective non-benzodiazepine anxiolytic. By acting on sigma-1 receptors in the nerve cells of the brain, Afobazole stabilizes GABA / benzodiazepine receptors and restores their sensitivity to endogenous inhibition 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 mainly in the form of a combination of anxiolytic (anti-anxiety) and light stimulating (activating) effects. Afobazol reduces or eliminates the feeling of anxiety (anxiety, bad feelings, apprehension, irritability), tension (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear), somatic anxiety (muscle, sensory, cardiovascular, respiratory, gastrointestinal intestinal symptoms), autonomic disorders (dry mouth, sweating, dizziness), cognitive disorders (concentration difficulties, impaired memory).Especially shown is the use of the drug in individuals with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, a tendency to emotional and stressful reactions. The effect of the drug develops for 5-7 days of treatment. The maximum effect is achieved by the end of 4 weeks of treatment and persists after the end of treatment on average 1-2 weeks. Afobazol does not cause muscle weakness, drowsiness and does not have a negative effect on concentration and memory. When used, drug dependence is not formed and the syndrome of "cancellation" does not develop.
PharmacokineticsAfter oral administration, Afobazol is well and quickly absorbed from the gastrointestinal tract. The maximum concentration of the drug in plasma (Cmax) is 0.130 &№177; 0.073 μg / ml; the time to reach the maximum concentration (Tmax) is 0.85 &№177; 0.13 h. Metabolism: Afobazole undergoes the “first pass effect” through the liver, hydroxylation in the aromatic ring of the benzimidazole cycle and oxidation in the morpholine fragment are the main directions of metabolism. 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 taking e inside is 0.82 &№177; 0.54 hours. The short half-life is due to the intensive biotransformation of the drug and the rapid distribution from blood plasma to organs and tissues. The drug is excreted mainly in the form of metabolites and partially unchanged with urine and feces. With long-term use does not accumulate in the body.
Pregnancy and lactation periodThe drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Side effectsAllergic reactions are possible. A rare headache that usually resolves on its own and does not require discontinuation of the drug.
With a significant overdose and intoxication, it is possible to develop a sedative effect and increased drowsiness without manifestations of muscle relaxation. As an emergency, caffeine 20% solution is used in ampoules of 1.0 ml 2-3 times a day subcutaneously.
Interaction with other drugsWith the simultaneous use of Afobazol does not affect the narcotic effect of ethanol and the hypnotic effect of thiopental.
With simultaneous use of Afobazol potentiates the anticonvulsant effect of carbamazepine.
With simultaneous use of Afobazol increases the anxiolytic effect of diazepam.
special instructionsThe drug does not adversely affect the driving of motor vehicles and the performance of potentially hazardous activities that require high concentration of attention and speed of psychomotor reactions.
Storage conditionsStore at a temperature not higher than 25 ° С. Keep out of the reach of children.
It is a pharmaceutical drug. Use only as directed by your doctor.