Afobazol, pills 10 mg, 60 pcs.

Composition

Active ingredient: 

• fabomotizol (fabomotizol dihydrochloride) – 10 mg.

Auxiliary substances:

• potato starch-48 mg,
• microcrystalline cellulose-35 mg,
• lactose monohydrate-48.5 mg,
• medium-molecular povidone (polyvinylpyrrolidone medium-molecular medical, collidone 25) – 7 mg, magnesium stearate-1.5 mg

. Pharmacological action

Pharmacotherapy group: anxiolytic agent (tranquilizer).

ATX code: N05BX.

Pharmacodynamics.

Afobazole is a selective non-benzodiazepine anxiolytic.

By acting on sigma-1 receptors in brain nerve cells, Afobazole stabilizes GABA / benzodiazepine receptors and restores their sensitivity to endogenous inhibitory mediators. Afobazole also increases the bioenergetic potential of neurons and has a neuroprotective effect: restores and protects nerve cells.

The action of the drug is realized mainly in the form of a combination of anxiolytic (anti-anxiety) and light stimulating (activating) effects.

Afobazole reduces or eliminates feelings of anxiety (preoccupation, bad feelings, apprehension), irritability, tension (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear), depressive mood, somatic manifestations of anxiety (muscle, sensory, cardiovascular, respiratory, gastrointestinal symptoms), vegetative disorders (dry mouth, sweating, dizziness), cognitive disorders (difficulty concentrating, impaired memory), including those that occur when stress disorders (adaptation disorders).

Especially indicated is the use of the drug in people 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 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 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 it is used, addiction, drug dependence is not formed, and the “withdrawal”syndrome does not develop.

Pharmacokinetics.

After oral administration, Afobazole is well and rapidly absorbed from the gastrointestinal tract.

The maximum concentration of the drug in plasma (cmax) is 0.130+0.073 mcg / ml; the time to reach the maximum concentration (tmax) is 0.85+0.13 hours.

Metabolism: Afobazole undergoes the” first pass effect ” through the liver, the main directions of metabolism are hydroxylation along the aromatic ring of the benzimidazole cycle and oxidation along the morpholine fragment.

Afobazole is intensively distributed to well-vascularized organs, and it is characterized by rapid transfer from the central pool (blood plasma) to the peripheral pool (strongly vascularized organs and tissues).

The oral half-life of Afobazole is 0.82+0.54 hours. The short half-life is due to intensive biotransformation of the drug and rapid distribution from the blood plasma to organs and tissues. The drug is mainly excreted in the form of metabolites and partially unchanged in the urine and feces.

Indications

Afobazole is used in adults with 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 relieve the “withdrawal” syndrome when quitting smoking.

Use during pregnancy and lactation

The use of Afobazol®is contraindicated during pregnancy. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Contraindications

• Individual intolerance to Afobazol.
• Galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.
• Pregnancy and lactation.
• Children under 18 years of age.

Side effects

Possible allergic reactions.

Rarely – headache, which usually resolves on its own and does not require discontinuation of the drug.

Interaction

Afobazole does not interact with ethanol and does not affect the hypnotic effect of thiopental.

Increases the anticonvulsant effect of carbamazepine.

Causes an increase in the anxiolytic effect of diazepam.

How to take, course of administration and dosage

It is applied inside, after eating.

Optimal single doses – 10 mg; daily-30 mg, distributed in 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 can be up to 3 months.

Overdose

With a significant overdose and intoxication, sedation and increased drowsiness may develop 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.

Special instructions

The drug does not have a negative effect on driving vehicles and performing potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf

life is 3 years.

Do not use after the expiration date indicated on the package.

Active ingredient

Fabomotizol

Dosage form

Tablets

Description

For adults

Indications

Neurosis, Stress, Increased nervous excitability

Weight

Weight: 17 gr.