Afobazol

Aphobazole (sometimes also called fabomotisol) is a medication that belongs to the class of anxiolytics, or drugs used to reduce symptoms of anxiety and stress. It contains the active ingredient fabomotisol.

Fabomotisol is used for treatment of various anxiety states, including generalized anxiety, states associated with anxiety (e.g. Anxiety states in neuroses, neuroses of hysterical origin, adaptation disorders, somatic disorders with symptoms of anxiety, neurasthenic states, anxiety states in menopausal period in women, etc.).

The action of Afobazole is to modulate the functioning of gamma-aminobutyric acid (GABA) in the brain, which helps to reduce anxiety without significant sedation or central nervous system depression. It can also improve mood and help patients reduce anxiety and restore psycho-emotional balance.

It is important to note that before you start taking Afobazol or any other medication, it is important to consult with your doctor for advice on dosage, contraindications, and possible side effects.

Indications Aphobazole

1. General Anxiety: Aphobazole is often used to treat various forms of generalized anxiety such as restlessness, nervousness, anxious thoughts, and physical tension.
2. Anxiety disorders: The drug may be effective in treating anxiety disorders such as panic disorder, social anxiety disorder, generalized anxiety disorder and others.
3. Anxiety symptoms during menopause: In premenopausal and menopausal women, Afobazole may help manage anxiety, nervousness, and other menopause-related symptoms.
4. Adaptation to stressful situations: The drug may be used to improve adaptation to stressful situations such as exams, moving, job changes and other significant life events.
5. Neurasthenia: Aphobazole may help with neurasthenia characterized by increased fatigue, irritability, low mood and other neurasthenic symptoms.
6. Anxiety symptoms in somatic diseases: In patients with somatic diseases such as coronary heart disease, asthma, peptic ulcer disease and others, Afobazol may help manage anxiety associated with their condition.

Release form

Aphobazol is usually available in the form of tablets for oral administration.

Pharmacodynamics

1. Modulation of the GABA-ergic system:

   • Aphobazole enhances the action of GABA, the main inhibitory neurotransmitter in the central nervous system.
   • GABA reduces neuronal excitability and decreases nerve impulse transmission, resulting in sedative and anxiolytic effects.

2. Increased sensitivity of GABA-A receptors:

   • Aphobazole increases the sensitivity of GABA-A receptors to GABA.
   • This leads to more effective neuronal inhibition and reduced anxiety.

3. Interaction with the serotonin system:

   • Aphobazole enhances serotoninergic transmission in certain parts of the brain.
   • Increased activity of the serotonin system is associated with antidepressant and anxiolytic effects.

4. Lackof muscle relaxation and sedation:

   • Unlike benzodiazepines, Aphobazole does not cause muscle relaxation or sedation, making it preferable for patients who need to treat anxiety but remain active and alert.

5. Normalization of neuronal membrane function:

   • Aphobazole promotes normalization of neuronal membrane function and elimination of GABA-ergic transmission dysfunction, which is important for the control of anxiety states.

Pharmacokinetics

1. Absorption: Afobazol is well absorbed from the gastrointestinal tract after oral administration. The maximum concentration (Cmax) is usually reached 1-2 hours after administration.
2. Distribution: The drug has high affinity to plasma proteins (about 99%), which means that most of the drug binds to plasma proteins in the blood. It is distributed in organs and tissues of the body, including the brain.
3. Metabolism: Aphobazol is metabolized in the liver with formation of inactive metabolites. The main metabolite is 2-ethyl-3-hydroxypyridine.
4. Excretion: The drug is excreted mainly through the kidneys as metabolites. It may also be partially excreted with bile.
5. Half-life: The half-life of Aphobazole is about 1-2 hours.
6. Concentration in blood: Establishment of stable concentration of the drug in the blood is usually achieved after several days of regular administration of the drug.
7. Pharmacokinetics in elderly patients: In elderly patients, the pharmacokinetics of Aphobazole are not altered, so no additional dose adjustment is usually required.
8. Pharmacokinetics in children: Data on the pharmacokinetics of Aphobazole in children are limited, and use in patients under 18 years of age is not recommended.

Dosing and administration

Aphobazol is usually taken orally by swallowing the tablet completely, with a small amount of water, regardless of food intake. The dosage and dosage recommendations are usually determined by the doctor depending on the individual characteristics of the patient and the nature of the anxiety symptoms. However, general dosage recommendations may be as follows:

1. For adults:

   • It is usually recommended to take 1 tablet (10 mg) 3 times a day.
   • The maximum daily dose is 30 mg.

2. For kids and teens:

   • Data on the safety and efficacy of Aphobazole in children and adolescents are limited, so it is generally not recommended for use in this age group without medical advice.

Use Aphobazole during pregnancy

Although to date we do not have sufficient clinical data on the safety of using Aphobazole during pregnancy, it is important to note that its use during this period requires special caution. Any drug, especially in the first trimester of pregnancy, may affect the development of the fetus.

It is recommended that you consult your doctor or gynecologist before using Aphobazole or any other medication during pregnancy.

Contraindications

1. Individual intoleranceor allergy: People with known individual intolerance to fabomotisol or any other component of the drug should avoid its use.
2. Pregnancy and lactation: Safety of Afobazol use during pregnancy and lactation has not been established. Therefore, its use should be coordinated with a doctor to avoid negative consequences.
3. Under 18 years of age: The efficacy and safety of Afobazol in persons under 18 years of age have not been established, therefore its use in this age group is not recommended.
4. Liver and kidney condition: In the presence of serious liver or kidney disease, dosage adjustment or complete withdrawal from the drug may be required.
5. Myasthenia gravis: Aphobazole should be used with caution in patients with myasthenia gravis because of its ability to increase muscle weakness.
6. Acute intoxication with alcohol or drugs, impaired cerebral circulation: In these cases, the use of Afobazol may not be appropriate or requires special attention and supervision by a doctor.

Side effects Aphobazole

1. Drowsiness: Drowsiness may occur in some patients, especially at the beginning of treatment. In such cases, it is recommended to avoid driving motor vehicles and performing tasks requiring increased attention.
2. Fatigue: Some patients may experience fatigue or feelings of weakness while taking Aphobazole.
3. Dizziness: In rare cases, the drug may cause dizziness or unsteadiness when moving.
4. Decreased concentration: Some patients may have difficulty concentrating or remembering while taking Aphobazole.
5. Allergic reactions: In rare cases, allergic reactions such as skin rash, itching, swelling or redness of the skin may occur.
6. Other rare side effects: These may include changes in taste, decreased libido, and others.

Overdose

Information on overdose of Aphobazole (Fabomotisol) is limited, as this drug is usually well tolerated and has low toxicity. However, if the recommended dose is significantly exceeded or if undesirable effects occur, medical attention should be sought.

Since Aphobazol does not have a pronounced sedative effect and does not cause muscle relaxation, the likelihood of serious consequences of overdose is low. However, possible symptoms of overdose may include increased drowsiness, dizziness, headache, nausea and vomiting.

Interactions with other drugs

1. Sedatives and anti-anxiety drugs: Aphobazole has anxiolytic effect, therefore its combination with other anti-anxiety drugs, such as benzodiazepines (e.g. Diazepam) or sedative antidepressants (e.g. Mirtazapine), may increase the sedative effect. This may lead to increased drowsiness and central nervous system depression.
2. Alcohol: Although there are no direct data on the interaction between Afobazol and alcohol, it is recommended to avoid alcohol consumption during treatment with Afobazol. This is due to the possibility of increased sedation and increased risk of undesirable effects.
3. Centrally acting drugs: Aphobazole may increase the effect of some centrally acting drugs, such as antidepressants or antipsychotics. This may result in increased sedation and risk of adverse effects.
4. Drugs affecting the liver: There are no known data on the interaction of Afobazol with drugs that may affect liver function. However, in the presence of hepatic pathology or concomitant use of other drugs affecting the liver, regular monitoring of liver function is recommended.