Atrevozol^® (Tablets) Instructions for Use

Marketing Authorization Holder

Tsitera LLC (Russia)

Manufactured By

Grotex, LLC (Russia)

ATC Code

N05BX04 (Fabomotizole)

Active Substance

Fabomotizole (Rec.INN registered by WHO)

Dosage Form

Atrevozol®

Tablets 10 mg

Dosage Form, Packaging, and Composition

Tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – Over-the-Counter
10 pcs. – blister packs (10 pcs.) – cardboard packs (100 pcs.) – Over-the-Counter
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – Over-the-Counter
10 pcs. – blister packs (3 pcs.) – cardboard packs (30 pcs.) – Over-the-Counter
10 pcs. – blister packs (4 pcs.) – cardboard packs (40 pcs.) – Over-the-Counter
10 pcs. – blister packs (5 pcs.) – cardboard packs (50 pcs.) – Over-the-Counter
10 pcs. – blister packs (6 pcs.) – cardboard packs (60 pcs.) – Over-the-Counter
10 pcs. – blister packs (7 pcs.) – cardboard packs (70 pcs.) – Over-the-Counter
10 pcs. – blister packs (8 pcs.) – cardboard packs (80 pcs.) – Over-the-Counter
10 pcs. – blister packs (9 pcs.) – cardboard packs (90 pcs.) – Over-the-Counter
100 pcs. – bottles – cardboard packs (100 pcs.) – Over-the-Counter
120 pcs. – bottles – cardboard packs (120 pcs.) – Over-the-Counter
14 pcs. – blister packs – cardboard packs (14 pcs.) – Over-the-Counter
14 pcs. – blister packs (10 pcs.) – cardboard packs (140 pcs.) – Over-the-Counter
14 pcs. – blister packs (2 pcs.) – cardboard packs (28 pcs.) – Over-the-Counter
14 pcs. – blister packs (3 pcs.) – cardboard packs (42 pcs.) – Over-the-Counter
14 pcs. – blister packs (4 pcs.) – cardboard packs (56 pcs.) – Over-the-Counter
14 pcs. – blister packs (5 pcs.) – cardboard packs (70 pcs.) – Over-the-Counter
14 pcs. – blister packs (6 pcs.) – cardboard packs (84 pcs.) – Over-the-Counter
14 pcs. – blister packs (7 pcs.) – cardboard packs (98 pcs.) – Over-the-Counter
14 pcs. – blister packs (8 pcs.) – cardboard packs (112 pcs.) – Over-the-Counter
14 pcs. – blister packs (9 pcs.) – cardboard packs (126 pcs.) – Over-the-Counter
20 pcs. – bottles – cardboard packs (20 pcs.) – Over-the-Counter
30 pcs. – bottles – cardboard packs (30 pcs.) – Over-the-Counter
40 pcs. – bottles – cardboard packs (40 pcs.) – Over-the-Counter
42 pcs. – bottles – cardboard packs (42 pcs.) – Over-the-Counter
50 pcs. – bottles – cardboard packs (50 pcs.) – Over-the-Counter
60 pcs. – bottles – cardboard packs (60 pcs.) – Over-the-Counter
7 pcs. – blister packs – cardboard packs (7 pcs.) – Over-the-Counter
7 pcs. – blister packs (10 pcs.) – cardboard packs (70 pcs.) – Over-the-Counter
7 pcs. – blister packs (2 pcs.) – cardboard packs (14 pcs.) – Over-the-Counter
7 pcs. – blister packs (3 pcs.) – cardboard packs (21 pcs.) – Over-the-Counter
7 pcs. – blister packs (4 pcs.) – cardboard packs (28 pcs.) – Over-the-Counter
7 pcs. – blister packs (5 pcs.) – cardboard packs (35 pcs.) – Over-the-Counter
7 pcs. – blister packs (6 pcs.) – cardboard packs (42 pcs.) – Over-the-Counter
7 pcs. – blister packs (7 pcs.) – cardboard packs (49 pcs.) – Over-the-Counter
7 pcs. – blister packs (8 pcs.) – cardboard packs (56 pcs.) – Over-the-Counter
7 pcs. – blister packs (9 pcs.) – cardboard packs (63 pcs.) – Over-the-Counter
80 pcs. – bottles – cardboard packs (80 pcs.) – Over-the-Counter
84 pcs. – bottles – cardboard packs (84 pcs.) – Over-the-Counter
90 pcs. – bottles – cardboard packs (90 pcs.) – Over-the-Counter

Clinical-Pharmacological Group

Anxiolytic (tranquilizer)

Pharmacotherapeutic Group

Psycholeptics; anxiolytics; other anxiolytics

Pharmacological Action

Selective non-benzodiazepine anxiolytic. By acting on σ₁-receptors in the nerve cells of the brain, Fabomotizole stabilizes GABA/benzodiazepine receptors and restores their sensitivity to endogenous inhibitory mediators. It also increases the bioenergetic potential of neurons and has a neuroprotective effect: it restores and protects nerve cells.

The effect is manifested primarily as a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects. It reduces or eliminates feelings of anxiety (worry, bad premonitions, apprehensions), irritability, tension (fearfulness, tearfulness, restlessness, inability to relax, insomnia, fear), depressed mood, somatic manifestations of anxiety (muscular, sensory, cardiovascular, respiratory, gastrointestinal symptoms), autonomic disorders (dry mouth, sweating, dizziness), cognitive disorders (difficulty concentrating, impaired memory), including those arising from stress disorders (adjustment disorders).

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

It does not cause muscle weakness, drowsiness and has no negative impact on concentration and memory. Its use does not lead to the development of tolerance, drug dependence, or withdrawal syndrome.

Pharmacokinetics

After oral administration, it is well and rapidly absorbed from the gastrointestinal tract. C_max – 0.130±0.073 µg/ml; T_max – 0.85±0.13 h. It undergoes a first-pass effect through the liver; the main metabolic pathways are hydroxylation of the aromatic ring of the benzimidazole cycle and oxidation of the morpholine fragment. It is intensively distributed to well-vascularized organs, characterized by rapid transfer from the central pool (blood plasma) to the peripheral pool (highly vascularized organs and tissues).

After oral administration, the T_1/2 of fabomotizole is 0.82±0.54 h. The short T_1/2 is due to the intensive biotransformation of fabomotizole and its rapid distribution from blood plasma to organs and tissues. It is excreted mainly as metabolites and partially unchanged in urine and feces. With prolonged use, it does not accumulate in the body.

Indications

Used in adults for anxiety disorders: generalized anxiety disorders; neurasthenia; adjustment disorders.

In patients with various somatic diseases: bronchial asthma; irritable bowel syndrome; systemic lupus erythematosus; ischemic heart disease; arterial 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 withdrawal syndrome when quitting smoking.

ICD codes

Dosage Regimen

Take orally, after meals.

The standard single dose is 10 mg.

The standard daily dose is 30 mg, divided into three doses.

Administer for a course of 2 to 4 weeks.

For insufficient clinical effect, increase the daily dose to 60 mg on physician’s recommendation.

For severe or persistent conditions, extend the treatment duration to 3 months as directed.

Do not exceed the maximum recommended daily dose of 60 mg.

Swallow the tablet whole with water; do not crush or chew.

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose.

Do not double the dose to make up for a missed one.

Discontinue use and consult a physician if no improvement is observed after 4 weeks of therapy.

Adverse Reactions

Possible allergic reactions.

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

Contraindications

Pregnancy, lactation (breastfeeding), children under 18 years of age, hypersensitivity to fabomotizole.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Pediatric Use

The drug is contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

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

Drug Interactions

It enhances the anticonvulsant effect of carbamazepine.

It causes an enhancement of the anxiolytic effect of diazepam.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.