- fabomotizole (fabomotizole dihydrochloride) - 10 mg
- potato starch - 48 mg,
- microcrystalline cellulose - 35 mg,
- lactose monohydrate - 48.5 mg,
- medium molecular weight povidone (medical medium molecular polyvinylpyrrolidone, kollidone 25) - 7 mg, magnesium stearate - 1.5 mg.
Pharmacotherapeutic group: anxiolytic agent (tranquilizer).
ATX code: N05BX.Pharmacodynamics.
Afobazole is a selective non-benzodiazepine anxiolytic.
Acting on sigma-1 receptors in the nerve cells of the brain, Afobazol stabilizes GABA / benzodiazepine receptors and restores their sensitivity to endogenous mediators of inhibition. Afobazole 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 mainly in the form of a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects.
Afobazole 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 (muscle, sensory, cardiovascular, respiratory , gastrointestinal symptoms), autonomic disorders (dry mouth, sweating, dizziness), cognitive disorders (difficulty concentrating, impaired memory), incl. arising from stress disorders (adjustment disorders).
The use of the drug is especially shown in persons with predominantly asthenic personality traits in the form of anxious suspiciousness, uncertainty, increased vulnerability and emotional lability, a tendency to emotional stress reactions.
The effect of the drug develops on the 5-7th day of treatment. The maximum effect is achieved by the end of 4 weeks of treatment and remains 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, addiction, drug dependence and withdrawal syndrome do not develop.Pharmacokinetics.
After oral administration, Afobazol is well and quickly absorbed from the gastrointestinal tract.
The maximum concentration of the drug in plasma (C max ) - 0.130 + 0.073 μg / ml; the time to reach the maximum concentration (T max ) - 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 cycle and oxidation at the morpholine fragment.
Afobazole is intensively distributed over 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 when taken orally is 0.82 + 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 in the urine and feces.
Afobazole is used in adults with anxiety conditions:
- generalized anxiety disorders,
- adjustment disorders,
- in patients with various somatic diseases (bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, ischemic 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 in smoking cessation.
Application during pregnancy and lactation
- Individual intolerance to the drug Afobazol.
- Galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
- Pregnancy, lactation period.
- Children under the age of 18.
Allergic reactions are possible.
Rarely - headache, which usually goes away on its own and does not require discontinuation of the drug.
Afobazol does not interact with ethanol and does not affect the hypnotic effect of thiopental.
Enhances the anticonvulsant effect of carbamazepine.
It enhances the anxiolytic effect of diazepam.
How to take, course and dosage
It is applied orally, after meals.
The optimal single dose is 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, 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.
With a significant overdose and intoxication, the development of a sedative effect and increased drowsiness is possible 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.