Aphobazole instructions for use: consider thoroughly

Afobazol ® (Afobazol) instructions for use

Form of manufacture, packaging and composition of the drug Afobazol ®.

White or white tablets with a cream color, flat-cylindrical, beveled.

1 tablet.
fabomotisole (in the form of dihydrochloride)5 mg

Excipients: potato starch – 48 mg, microcrystalline cellulose – 40 mg, lactose monohydrate – 48.5 mg, povidone medium molecular weight (polyvinylpyrrolidone medium molecular weight medical, collidone 25) – 7 mg, magnesium stearate – 1.5 mg.

10 pcs. – Contoured cellular packs (3, 5, 10) – cardboard boxes. 20 pcs. – Contour cell packs (1, 2, 3, 4, 6) – cardboard boxes. 25 pcs. – Contour cell packs (2, 4) – cardboard boxes. 30 pcs. – Contour cell packs (1, 2, 3, 4) – cardboard boxes. 30 ects. – Plastic jars (1) – cardboard boxes. 50 pcs. – Polymeric jars (1) – cardboard boxes. 100 pcs. – Polymeric cans (1) – carton packs. 120 pcs. – Polymeric pots (1) – reams of cardboard.

White or white tablets with a cream color, flat-cylindrical, beveled.

1 tablet.
fabomotisole (in the form of dihydrochloride)10 mg

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

10 pcs. – Contoured cellular packs (3, 5, 10) – cardboard boxes. 20 pcs. – Contour cell packs (1, 2, 3, 4, 6) – cardboard boxes. 25 pcs. – Contour cell packs (2, 4) – cardboard boxes. 30 pcs. – Contour cell packs (1, 2, 3, 4) – cardboard boxes. 30 ects. – Plastic jars (1) – cardboard boxes. 50 pcs. – Polymeric jars (1) – cardboard boxes. 100 pcs. – Polymeric cans (1) – carton packs. 120 pcs. – Polymeric pots (1) – reams of cardboard.

Pharmacological action

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

The action of the drug is realized mainly as a combination of anxiolytic (anti-anxiety) and mild stimulating (activating) effects. Afobazol® 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. cognitive disorders (difficulty concentrating, impaired memory), including those resulting from stress disorders (adaptation disorders). The drug is especially indicated for people with predominantly asthenic personality traits such as anxious mistrustfulness, uncertainty, increased vulnerability and emotional lability, propensity to emotional stress reactions.

The effect of the drug develops on the 5th-7th day of treatment. The maximal effect is reached by the end of the fourth week of treatment and is maintained for an average of 1-2 weeks after the end of the treatment period.

Afobazol® does not cause muscle weakness, drowsiness and has no adverse effect on concentration and memory. During its use there is no formation of addiction, drug dependence and there is no “withdrawal” syndrome.

Pharmacokinetics

After oral administration Aphobazole® is well and quickly absorbed from digestive tract. C max – 0.130±0.073 µg/ml; T max – 0.85±0.13 h.

Aphobazole® undergoes “first pass” effect through liver, main metabolic pathways are hydroxylation by aromatic ring of benzimidazole cycle and oxidation by morpholine fragment. Aphobazole® is intensively distributed in well vascularized organs and is characterized by rapid transfer from the central pool (blood plasma) to the peripheral pool (highly vascularized organs and tissues).

T 1/2 of phabomotisole when administered orally is 0.82±0.54 h. Short T 1/2 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. During long-term use the drug does not accumulate in the body.

Aphobazole® indications

Aphobazol® is used in adults with anxiety disorders:

  • generalized anxiety disorders;
  • neurasthenia;
  • adaptive disorders;
  • In patients with various somatic diseases: bronchial asthma, irritable bowel syndrome, systemic lupus erythematosus, IHD, hypertension, arrhythmias;
  • dermatological, oncological and other diseases.

  • Sleep disorders associated with anxiety;
  • neurocirculatory dystonia;
  • premenstrual syndrome;
  • alcohol withdrawal syndrome;
  • for relieving withdrawal symptoms after quitting smoking.

Open ICD-10 code list
ICD-10 code Indication
F10.3 Withdrawal state
F17.3 Mental and behavioural disorders caused by tobacco use – withdrawal state
F40 Phobic anxiety disorders (incl. agoraphobia, social phobias)
F41.1 Generalised anxiety disorder
F43 Serious stress reactions and adaptation disorders
F45.3 Autonomic nervous system somatoform dysfunction
F48.0 Neurasthenia
F51.2 Sleep and wakefulness disorders of non-organic etiology
I10 Essential [primary] hypertension
I20 Stenocardia [chest pains]
J45 Asthma
K58 Irritable bowel syndrome
M32 Systemic lupus erythematosus
N94.3 Premenstrual syndrome

Dosage regimen

The drug is administered orally, after meals.

Optimal single dose is 10 mg; daily dose is 30 mg, divided into 3 doses during the day.

The duration of the course of application of the drug is 2-4 weeks.

If necessary, according to the doctor’s recommendation, the daily dose of the drug can be increased to 60 mg, and the duration of treatment up to 3 months.

Side effects

Possible: allergic reactions.

Rarely: headache, which usually disappears on its own and does not require cancellation of the drug.

Contraindications to use

  • Hypersensitivity to the drug components;
  • galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
  • pregnancy;
  • Lactation period (breast-feeding);
  • Children under 18 years of age.

Administration during pregnancy and lactation

The use of the drug Aphobazole ® is contraindicated in pregnancy.

If it is necessary to apply the drug during lactation, breastfeeding should be discontinued.

Administration in children

Special precautions

Influence on the ability to drive vehicles and mechanisms

The drug has no adverse effect on driving motor transport and performing potentially dangerous activities, which require increased concentration and quick psychomotor reactions.

Overdose

Symptoms: in case of significant overdose and intoxication, development of sedation and hypersomnia without myorelaxation is possible.

Treatment: caffeine 20% solution in ampoules 1.0 ml 2-3 times a day by p/k is used as an emergency treatment.

Drug interaction

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

Afobazole – instructions for use

Where to buy?

Registration number : LS-000861 Trade name of drug: Aphobazole® INN or grouping name: fabomotisole Dosage form: tablets

Contents per tablet:

Active substance: fabomotisole (fabomotisole dihydrochloride) – 5 mg and 10 mg. Excipients: potato starch – 48 mg, microcrystalline cellulose – 40 mg (for 5 mg dosage) and 35 mg (for 10 mg dosage), lactose monohydrate – 48.5 mg, povidone medium molecular (polyvinylpyrrolidone medium molecular medical, collidone 25) – 7 mg, magnesium stearate – 1.5 mg.

Description: white or white tablets with cream-colored shade, flat-cylindrical with bevel.

Pharmacotherapeutic group: anxiolytic medicine (tranquilizer).

ATX code : N05BX.

Pharmacodynamics:

Aphobazole® is a selective non-benzodiazepine anxiolytic.

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

The action of the drug is realized mainly 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 mistrustfulness, uncertainty, increased vulnerability and emotional lability, propensity to emotional stress reactions.

The effect of the drug develops on the 5th-7th day of treatment. The maximal effect is reached by the end of the fourth week of treatment and is maintained for an average of 1-2 weeks after the end of the treatment period.

Afobazol® does not cause muscle weakness, drowsiness and has no negative influence on concentration and memory. During its use there is no formation of addiction, drug dependence and there is no “withdrawal” syndrome.

Pharmacokinetics:

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

Maximum drug concentration in plasma (Cmax) is 0.130 + 0.073 mcg/ml; time to reach maximum concentration (Tmax) is 0.85 + 0.13 hours.

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

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

Half-life of Aphobazole® when administered orally 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 excreted mainly as metabolites and partially unchanged in urine and feces.

Indications for use:

Aphobazole® is used in adults with anxiety states: 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 withdrawal symptoms after quitting smoking.

Contraindications:

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

Administration during pregnancy and lactation:

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

Dosage and administration method:

It is used orally, after meals.

The optimal single dose is 10 mg; the optimal daily dose is 30 mg, divided into 3 doses during the day. The duration of course of drug administration is 2-4 weeks.

If necessary, according to the doctor’s recommendation, the daily dose of the drug can be increased to 60 mg, and the duration of treatment up to 3 months.

Side effects:

Allergic reactions are possible.

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

Overdose:

With significant overdose and intoxication, the development of sedation and increased somnolence without manifestations of myorelaxation is possible. Caffeine 20% solution in ampoules 1.0 ml 2-3 times a day subcutaneously is used as an emergency treatment.

Interaction with other drugs:

Afobazol® does not interact with ethanol and has no effect on the hypnotic effect of thiopental. It enhances anticonvulsant effect of carbamazepine. Causes enhancement of anxiolytic effect of diazepam.

Effect on the ability to drive vehicles and mechanisms:

The drug has no adverse effect on driving motor transport and performing potentially dangerous activities, which require increased concentration and quick psychomotor reactions.

Form of production:

Tablets of 5 mg or 10 mg.

In a carton pack of 10, 20, 25 or 30 tablets.

30, 50, 100 or 120 tablets in plastic jars.

Each jar or 3, 5 or 10 contour packs of 10 tablets, or 1, 2, 3, 4 or 6 contour packs of 20 tablets, or 2 or 4 contour packs of 25 tablets, or 1, 2, 3 or 4 contour packs of 30 tablets along with instructions for use are placed in a carton pack.

Storage conditions:

Store at a temperature not exceeding 25 ºC. Keep out of reach of children.

Shelf life:

3 years. Do not use after expiration date stated on the package.

Conditions for dispensing from pharmacies:

Holder of the registration certificate / organization accepting consumer claims:

OTCPharm PJSC, Russia, 123317, Moscow, Testovskaya str. 10. Tel.: +7(800) 775-98-19, fax +7(495) 221-18-02. otcpharm.ru

Manufacturer:

Pharmstandard-Leksredstva OJSC, 1a/18 2nd Agregatnaya St, Kursk, 305022, Russia tel./fax: (4712) 34-03-13, www.pharmstd.ru

Where to buy?

Registration number : LP-006555 Trade name of drug: Aphobazole® Retard INN or grouping name: fabomotisole Drug form: sustained-release film-coated tablets

Contents per tablet:

Active ingredient: fabomotisole (fabomotisole dihydrochloride) – 30.0 mg.

Excipients: Collidone® SR [polyvinyl acetate, povidone, sodium lauryl sulfate, silicon dioxide] – 120.0 mg, hypromellose – 25.0 mg, lactose – 23.0 mg, magnesium stearate – 2.0 mg.

Contents of the coating: Opadray II 85 F18422 white [partially hydrolyzed polyvinyl alcohol, titanium dioxide, macrogol 4000, talc] – 6.0 mg.

Description: round biconvex film-coated tablets of almost white color. On cross-section the core is almost white or white with a yellowish-brownish tinge.

Pharmacotherapeutic group: anxiolytic medicine (tranquilizer).

ATX code: N05BX.

Pharmacodynamics.

Aphobazole® Retard is a selective non-benzodiazepine anxiolytic.

Acting on sigma-1 receptors in the nerve cells of the brain, Aphobazole® Retard stabilizes GABA/Benzodiazepine receptors and restores their sensitivity to endogenous mediators of inhibition. Aphobazol® Retard 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 stimulant (activating) effects.

Aphobazole® Retard reduces or eliminates 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). It is especially indicated for individuals with predominantly asthenic personality traits such as anxious hesitancy, insecurity, increased vulnerability and emotional lability, propensity to emotional stress reactions.

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

Pharmacokinetics.

After oral administration, Aphobazole® Retard is well and quickly absorbed from the gastrointestinal tract. Food intake has no effect on the drug absorption and pharmacokinetic parameters.

Maximal concentration of preparation in plasma (Сmax) after single use – 47,740 + 43,252 ng/ml, after multiple use – 27,668 + 13,770 ng/ml; time of maximal concentration achievement (Тmax) – 2.1 + 1.1 and 2.6 + 1.0 hours after single and multiple use, respectively.

Metabolism: Afobazole® Retard undergoes “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 morpholino fragment.

Aphobazole® Retard is intensively distributed in well vascularized organs, it 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® Retard when administered orally is 8.41 + 5.01 hours after single administration and 6.05 + 3.54 hours after multiple administration. The drug is excreted mainly as metabolites and partially unchanged by the kidneys and intestine.

Indications for use.

Aphobazole® Retard is used in adults with anxiety states: generalized anxiety disorder, 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 treatment of sleep disorders associated with anxiety.

Contraindications.

  • Hypersensitivity to fabomotisole and/or any excipient of the drug.
  • Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.
  • Pregnancy, breastfeeding period.
  • Children under 18 years of age.

If you have one of the above mentioned diseases, consult your physician before using the drug.

Use during pregnancy and breast-feeding period.

Administration of Aphobazole® Retard is contraindicated in pregnancy.

If it is necessary to apply the drug during lactation, breastfeeding should be discontinued.

Before application of Aphobazole® Retard, if you are pregnant or think that you might be pregnant or plan to become pregnant, consult your physician.

Dosage and administration.

One tablet once a day, in the morning, regardless of meals.

The duration of the course of application of the drug is 2-4 weeks.

If after treatment no improvement or worsening of symptoms or appearance of new symptoms, consult a physician.

Use the drug only in accordance with the indications, the method of administration and in such doses as directed.

Side effects.

Adverse effects which may develop during treatment with Aphobazole® Retard are classified according to the following frequency of occurrence:

Immune system disorders: frequency unknown – allergic reactions.

Nervous system disorders: rare – headache, which usually resolves on its own and does not require discontinuation of the drug.

If you have side effects mentioned in the instructions or they worsen, or if you notice any other side effects not mentioned in the instructions, inform your doctor.

Overdose.

Symptoms. In case of significant overdose and intoxication, development of sedation and increased somnolence without manifestation of myorelaxation is possible. Treatment. Caffeine 20 % solution in ampoules 1.0 ml 2-3 times daily subcutaneously is used as an emergency treatment.

If symptoms of overdose occur, stop taking the drug and consult a physician immediately.

Interaction with other drugs.

Aphobazole® Retard does not interact with ethanol and has no effect on the hypnotic effect of thiopental. It enhances anticonvulsant effect of carbamazepine. Causes enhancement of anxiolytic effect of diazepam.

If you use the above mentioned drugs or other drugs (including over-the-counter ones), consult your physician before using Aphobazole® Retard.

Effect on ability to drive vehicles, mechanisms.

The drug has no adverse effect on driving motor transport and performing potentially dangerous activities, which require increased concentration and quick psychomotor reactions.

Form of production.

Long-release film-coated tablets, 30 mg.

There are 20 tablets in a polyvinyl chloride film and aluminum foil wrapped in varnish.

One envelope with instructions for use is placed in a carton pack.

Storage conditions.

Keep at the temperature not more than 25 ºС. Keep out of reach of children.

Shelf life.

2 years. Do not use after expiration date stated on the package.

Dispensing conditions.

The holder of the registration certificate / consumer claims authority

OTCPharm JSC, 10 Testovskaya St., Moscow, 123112, Russia Tel.: +7 (800) 775-98-19, fax: +7 (495) 221-18-02. www.otcpharm.ru

Manufacturer:

Pharmstandard-Leksredstva OJSC, 1a/18 2nd Agregatnaya St, Kursk, 305022, Russia tel./fax: (4712) 34-03-13, www.pharmstd.ru

© 2022 OTCPHARM, A.S.

All Rights Reserved

123112, Moscow, 10 Testovskaya St., floor 12, room II, room 29

THERE ARE CONTRAINDICATIONS. IT IS NECESSARY TO CONSULT WITH A SPECIALIST.

THERE ARE CONTRAINDICATIONS. IT IS NECESSARY TO CONSULT WITH A SPECIALIST.

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