Afobazol, tablets 10 mg 60 pcs

Pharmacotherapeutic group: anxiolytic medicine (tranquilizer).

ATX code: N05BX.

Pharmacodynamics.

Aphobazole is a selective non-benzodiazepine anxiolytic.

Acting on sigma-1 receptors in nerve cells in the brain, Aphobasol stabilizes GABA/ benzodiazepine receptors and restores their sensitivity to endogenous mediators of inhibition. Aphobazole also increases the bioenergetic potential of neurons and has a neuroprotective effect: it restores and protects nerve cells.

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

Aphobazole reduces or eliminates feelings of anxiety (anxiety, misgivings, apprehension), irritability, tension (jitteriness, tearfulness, anxiety, inability to relax, insomnia, fear), depressed mood, somatic anxiety manifestations (muscular, sensory, cardiovascular, respiratory, gastrointestinal symptoms), autonomic disturbances (dry mouth, sweating, dizziness), cognitive disturbances (difficulty concentrating, impaired memory), including those resulting from stressors.including those arising from stress disorders (adaptation disorders).

The drug is especially indicated for people with predominantly asthenic personality traits such as anxious mistrust, insecurity, increased vulnerability and emotional lability, propensity to have emotional stress reactions.

The effect of the drug develops on the 5th-7th day of treatment. The maximum effect is reached by the end of the 4th week of treatment and lasts for an average of 1-2 weeks after the end of treatment.

Aphobazole does not cause muscle weakness, drowsiness and has no negative effect on concentration and memory. Its use is not addictive, does not cause drug dependence and does not lead to withdrawal syndrome.

Pharmacokinetics.

Aphobazole is well and quickly absorbed from the gastrointestinal tract after oral administration.

The maximum plasma concentration of the drug (C_max) is 0.130+0.073 µg/mL; time to reach maximum concentration (T_max) is 0.85+0.13 h.

Metabolism: Afobazole is subject to a “first pass effect” through the liver; the main directions of metabolism are hydroxylation by the aromatic ring of the benzimidazole cycle and oxidation by the morpholine fragment.

Aphobazole is intensely distributed to well vascularized organs and is characterized by rapid transfer from the central pool (blood plasma) to the peripheral pool (highly vascularized organs and tissues).

The half-life of Aphobazole when taken orally is 0.82+0.54 hours. Short half-life is due to intensive biotransformation of the drug and rapid distribution from plasma to organs and tissues. The drug is excreted mainly as metabolites and partially unchanged in the urine and feces.

Indications

Anxiety, Stress

Aphobazole is used in adults for anxiety conditions:

• generalized anxiety disorders,
• neurasthenia,
• adaptation disorders,
patients with various somatic diseases (bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, coronary heart disease, hypertension, arrhythmias),
• dermatological, oncological and other

The treatment of sleep disorders associated with anxiety, neurocirculatory dystonia, premenstrual syndrome, alcohol withdrawal syndrome, to relieve withdrawal symptoms after quitting smoking.

Active ingredient

Fabomotisol

Composition

Active ingredient:

• fabomotisole (phabomotisole dihydrochloride) – 10 mg.

Excipients:

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

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How to take, the dosage

It is administered orally, after meals.

The optimal single dose is 10 mg; the daily dose is 30 mg distributed in 3 doses during the day. The duration of course of using the drug is 2-4 weeks.

If necessary, upon the recommendation of the physician, the daily dose of the drug can be increased up to 60 mg, and the duration of treatment can be up to 3 months.

Interaction

Aphobazole does not interact with ethanol and has no effect on the hypnotic effect of thiopental.

It enhances the anticonvulsant effect of carbamazepine.

Causes an increase in the anxiolytic effects of diazepam.

Special Instructions

The drug does not adversely affect driving and performance of potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

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

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Side effects

Allergic reactions are possible.

Rarely, headache, which usually goes away on its own and does not require withdrawal of the drug.

Overdose

In case of significant overdose and intoxication development of sedation and increased somnolence without myorelaxation is possible.

Caffeine 20% solution in ampoules 1.0 ml 2-3 times a day subcutaneously is used as an emergency treatment.

Pregnancy use

Administration of the drug Aphobazole® is contraindicated in pregnancy. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Similarities

Aphobasol, Aphobasol