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

Afobazole is used in adults for anxiety conditions:

generalized anxiety disorders,
neurasthenia,
adjustment 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.

Pharmacological effect

Pharmacotherapeutic group: anxiolytic agent (tranquilizer).

ATX code: N05BX.

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. 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 primarily as a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects.

Afobazole reduces or eliminates feelings of anxiety (preoccupation, 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.

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, addiction does not form, drug dependence does not develop, and “withdrawal” syndrome does not develop.

Pharmacokinetics.

After oral administration, Afobazole 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.

Special instructions

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.

Active ingredient

Fabomotizol

Composition

Active ingredient:

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.

Pregnancy

Use of the drug Afobazol®
contraindicated during pregnancy. If necessary
use of the drug during lactation, breastfeeding should
stop.

Contraindications

Individual intolerance to the drug Afobazole.
Galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Pregnancy, lactation period.
Children under 18 years of age.

Side Effects

Allergic reactions are possible.

Rarely – headache, which usually goes away 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.

Enhances the anticonvulsant effect of carbamazepine.

Causes an increase in the anxiolytic effect of diazepam.

Overdose

With significant overdose and intoxication, the development of sedation and increased drowsiness without manifestations of muscle relaxation is possible.

As an emergency solution, caffeine 20% solution in 1.0 ml ampoules is used 2-3 times a day subcutaneously.

Storage conditions

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

Shelf life

3 years.

Do not use after expiration date,
indicated on the packaging.

Manufacturer

Pharmstandard-Leksredstva, Russia