Афобазол

Quick links to important sections

Афобазол

Selected form

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Афобазол

Quick Facts

Property Description
Active ingredient Fabomotizole mesylate
Form Tablet
Pharmacological class Selective Non-Benzodiazepine Anxiolytic (N05BX)
General purpose Alleviating anxiety and tension
Origin Synthetic (Benzimidazole derivative)
Status Typically Over-The-Counter (OTC) in its primary markets

Defining Афобазол: A Selective Non-Benzodiazepine Anxiolytic

Афобазол is a medicinal preparation containing the active substance Fabomotizole (INN), a synthetic compound derived from the benzimidazole chemical class. It is classified by the World Health Organization's Anatomical Therapeutic Chemical (ATC) system as a component of the Other Anxiolytics group (N05BX04). This preparation is clinically recognized as a selective non-benzodiazepine anxiolytic due to its mechanism of action, which differs fundamentally from traditional tranquilizers. Fabomotizole possesses distinct anxiolytic activity through modulation of the sigma-1 receptor, providing a therapeutic benefit unlike that of classical GABA-agonists.

Composition, Form, and General Purpose

The drug is a single active ingredient product, formulated as Fabomotizole mesylate and presented in a solid oral tablet form. This presentation allows for convenient oral administration. Unlike many prescription anxiolytics, Афобазол is often available as an Over-The-Counter (OTC) product in its primary markets, reflecting its lower potential for strong immediate psychotropic effects. Its general purpose is to stabilize the nervous system, helping individuals manage chronic states of anxiety, tension, and irritability stemming from conditions like neurasthenia or adjustment difficulties. This function includes the exertion of neuroprotective effects, contributing to the overall goal of restoring emotional balance.

What side effects are possible with Афобазол?

Possible Side Effects and Safety Information

The safety profile of Fabomotizole (Афобазол) is based on regulatory information and clinical data, which characterize the drug by generally mild and transient adverse reactions. These effects are categorized by frequency and system involvement as documented in official prescribing information.

Frequency-Classified Adverse Reactions

Classification Examples of Documented Effects
Common Mild gastrointestinal disturbances, such as nausea, dyspepsia, or diarrhea.
Uncommon Nervous system effects (drowsiness, dizziness) and hypersensitivity reactions (skin rash, itching).

These effects are typically classified within the Gastrointestinal Disorders and Nervous System Disorders System-Organ Classes. Official summaries note the absence of explicitly listed serious adverse reactions and clinical data confirms the lack of withdrawal syndrome manifestations upon cessation, a key regulatory distinction from certain classic anxiolytics.

Population-Specific Safety Constraints

The regulatory label for Fabomotizole includes specific constraints regarding its use in certain populations:

  • Pediatric Patients: Use is not indicated in individuals under the age of 18 due to insufficient safety data in this age group.
  • Pregnancy and Lactation: The medication is not recommended for use in pregnant or breastfeeding women as safety data for these populations are lacking.
  • Severe Impairment: Use requires caution in patients with severe hepatic or renal impairment.

Safety-Related Restrictions

Fabomotizole is contraindicated in individuals with known hypersensitivity to the active substance or any excipients. Furthermore, the label notes that co-administration with other Central Nervous System (CNS) depressants, such as alcohol, may lead to an enhancement of sedative effects.

Overdose and Emergency Response

Overdose and When to Seek Help

Documented Clinical Manifestations The official regulatory prescribing information documents the clinical signs of significant intoxication with Афобазол. The primary presentation involves the development of a sedative effect and increased sleepiness or drowsiness. It is explicitly noted that this overdose presentation occurs without manifestations of muscle relaxation (myorelaxation). No severe systemic or life-threatening outcomes are explicitly documented in the official overdose instructions.

Required Emergency Actions The regulatory documents mandate a specific action: upon the appearance of any overdose symptoms, the patient must cease use of the preparation and immediately contact a physician. This requirement establishes the condition under which urgent medical help must be sought, strictly as defined by the label.

Pharmacological Intervention A specific intervention is documented in the official labeling as the required immediate assistance. This involves the administration of a 20% solution of caffeine-sodium benzoate, typically given subcutaneously. This measure is documented to counteract the excessive central nervous system depressant effects.

Official Overdose Profile The regulatory profile establishes that the primary risk associated with overdose is excessive central nervous system sedation. This defines the required help-seeking conditions, which are addressed by the mandated use of a specific pharmacological antagonist to counteract the documented depressant effects.

Therapeutic Uses of Афобазол

What Афобазол Treats: Main Uses and Benefits

The therapeutic focus of Афобазол is rooted in the management of specific anxiety and stress-related symptomatic domains. As an anxiolytic, its use is applied across domains where additional symptomatic support is needed. It is commonly used when symptoms create noticeable physiological strain.

The medication is generally used to help manage symptoms of Generalized Anxiety Disorder (GAD), neurasthenia, and emotional distress arising from adjustment difficulties. It is relevant for easing symptom clusters that include persistent worry, inner restlessness, emotional exhaustion, and somatic manifestations like muscle tension.

“The primary goal is providing supportive relief that may assist with managing the patient's symptomatic discomfort, especially across chronic states of tension.”

By helping to address these symptom clusters, the treatment may contribute to general well-being and assist with maintaining a sense of stability. It is applied in situations where patients experience symptoms that may interfere with daily functioning, and is relevant for managing both psychological and physical signs of tension.


Quick Fact: Supportive Management for Asthenic Symptoms Domain Symptom Group Benefit
Asthenic Anxiety Irritability, low concentration, fatigue Assists with maintaining functional stability
Somatic Manifestations Muscle tension, cardiovascular discomfort Contributes to improved day-to-day comfort
Chronic Stress Pervasive tension, worry, apprehension Offers symptomatic relief for emotional burden

Eligibility and Restrictions for Use

The eligibility for using Афобазол (Fabomotizole mesylate) is strictly defined by its official regulatory labeling. Use of the medicine is permitted only for adults who are 18 years of age and older.

Eligibility Status Population Group Regulatory Basis
Contraindicated Children and Adolescents (Under 18) Safety and efficacy not established.
Contraindicated Pregnant or Lactating Individuals Prohibited due to insufficient safety data.

The medicine is subject to several absolute contraindications. Use is prohibited due to the presence of excipients in the tablet formulation for individuals with specific hereditary metabolic conditions, including lactose intolerance, lactase deficiency, and glucose-galactose malabsorption. Additionally, individuals with a known hypersensitivity to Fabomotizole mesylate or any excipient must not use the medicine.

For patients with severe hepatic (liver) or severe renal (kidney) impairment, regulatory documents specify that use should be approached with caution. The official labeling mandates the exclusion of vulnerable and specified population groups.

What should I know about interactions with other medicines?

Interactions with other medicines and products

This section summarizes the officially documented interaction patterns for Fabomotizole mesylate (Афобазол), based strictly on regulatory prescribing information.

Pharmacodynamic Interactions

The primary documented interactions are pharmacodynamic, meaning they relate to the combined effects of substances in the body. Co-administration with the benzodiazepine Diazepam is officially documented to potentiate the anxiolytic effect of Fabomotizole. Conversely, the regulatory profile notes that co-administration with Carbamazepine does not affect the anxiolytic effect of Fabomotizole.

Interactions with Alcohol

Official labeling states that Ethanol (alcohol) is documented to enhance the effect of Fabomotizole.

Absence of Pharmacokinetic and Contraindication Statements

Regulatory documents do not list any interactions involving metabolic pathways, such as Cytochrome P450 (CYP) enzymes, or drug transporters. Consequently, there are no explicit prohibitions or formal contraindications of medicinal products based solely on an interaction risk documented in the regulatory texts. Furthermore, official labeling does not specify any mandatory time separation requirements for the administration of Fabomotizole relative to other medicines, food, or supplements, nor does it contain explicit population-specific interaction warnings.

Mechanism of Action

How Афобазол Works

Афобазол's mechanism of action is defined by the modulation of the Sigma-1 Receptor (sigma1R) and subsequent functional stabilization of the GABAergic system, defining its distinct mechanism of action.


Modulating the Sigma-1 Receptor for Cellular Protection

This domain covers the drug's core molecular target: the sigma1R, a chaperone protein that acts at the junction of the endoplasmic reticulum and mitochondria. Fabomotizole's agonism at the sigma1R stabilizes the internal environment of nerve cells by regulating calcium flux and reducing molecular damage. This action provides a neuroprotective effect by modulating biochemical processes that contribute to cellular damage.


Indirect Stabilization of the GABA A Inhibitory System

This mechanism focuses on how the drug influences the brain's main inhibitory system, the GABA A receptor. The drug does not directly potentiate GABA but instead prevents the GABA A receptor complex from exhibiting functional impairment. This action maintains inhibitory balance by modulating excessive neural signaling.

Dosage and Administration Information

The administration of Afobazol (Fabomotizole mesylate) is strictly defined by the regulatory documents of the primary markets where it is approved. The usage protocol establishes precise rules for dosage, frequency, and course duration, designed to ensure standardized application.

Administration Scope

Instruction Official Guideline
Route of Administration The medicine is intended solely for oral administration.
Official Dosage The standard single dose is 10 mg, utilizing the tablet form. The typical daily intake is 30 mg in divided doses, though the maximum recommended daily dose may be increased up to 60 mg under specialized guidance.
Frequency Pattern The standard regimen requires the tablet to be taken thrice daily (three times per day).
Timing Administration is specified to occur after a meal (post-prandial use).
Course Duration The standard treatment course is defined as 2 to 4 weeks. Official prescribing information permits the treatment duration to be extended for up to 3 months.

Special Procedural Conditions

The protocol specifies that the 10 mg tablet must be swallowed whole with a small amount of water; it is not to be crushed, dissolved, or chewed. This method is required to preserve the tablet's integrity and ensure proper administration. The standard dosing schedule applies to adults 18 years and older.

Connection to the overall use protocol: The official instructions establish a precise, time-bound protocol for the use of Fabomotizole mesylate, requiring adherence to the fixed 10 mg strength, strict post-meal timing, and defined limits for both daily intake and the overall duration of the treatment course. This structure defines the consistent, label-based approach for its administration.

Recent Clinical Evidence

Research evidence / Overview of studies for Афобазол

Evidence for use in Anxiety and Anxious-Asthenic Disorders

Research exploring whether Афобазол has an association with changes in anxiety symptoms has primarily focused on conditions characterized by anxiety and associated asthenic (fatigue or exhaustion) manifestations. Studies conducted during periods of increased symptom activity have included short-term randomized controlled trials (RCTs) and other comparative clinical studies. Researchers monitored measured outcomes, primarily using standardized assessment tools like the Hamilton Anxiety Rating Scale (HAMA) to monitor symptom intensity.

In these trials, patients diagnosed with anxiety disorders were evaluated against a placebo or an active comparator drug. Researchers monitored and documented measured changes in anxiety scale scores over the study period. Some trials described patterns observed in the studies related to changes in both the anxiety and fatigue components. The research highlights changes measured during the study period, and the evidence contributes to understanding symptom patterns in the study populations.

Research on Investigational and Preclinical Applications

Studies have also explored the actions of Афобазол in laboratory settings, examining outcomes related to cell damage and changes in physiological function in animal models. These investigations are currently restricted to basic science, primarily involving in vitro (cell culture) experiments and various animal models simulating conditions like cerebral ischemia (restricted blood flow to the brain).

Preclinical reports describe measurements observed in the studies, such as the monitoring of neuronal cell counts and specific biochemical markers of cell damage. This research provides insight into short-term changes within these experimental models. It is important to understand that this research explores temporary physiological imbalance and contributes to the broader evidence landscape, but evidence is limited to laboratory environments.

What is Still Uncertain About Афобазол Research

Evidence highlights what is known—and what is still uncertain—about Афобазол. A key limitation is that sample sizes were modest in several initial studies, and follow-up durations were limited, making it difficult to draw broad conclusions about long-term use. Data on the persistence or durability of the observed changes beyond the short-term study duration are not widely characterized. Comparative evidence against the full range of modern anxiety treatments is lacking. The research provides context but not individual predictions, and the findings describe group patterns, not guaranteed personal outcomes.

Frequently Asked Questions (FAQ)

Common questions about Афобазол (FAQ)


Q: Does Афобазол cause drowsiness during the day?

A: According to official product information, drowsiness is listed as an uncommon side effect. Use of the medicine may be associated with nervous system effects, including dizziness and drowsiness. This is typically classified as a mild and transient adverse reaction.


Q: Are there any common interactions between Афобазол and alcohol?

A: Official labeling specifically documents that the co-administration of alcohol (ethanol) is known to enhance the effect of this medicine. Regulatory information advises awareness of this documented effect.


Q: What happens if I stop taking Афобазол suddenly?

A: Clinical data and regulatory information confirm the lack of withdrawal syndrome manifestations upon cessation of use. This finding contributes to the drug’s overall safety profile.


Q: Are there any studies on the long-term safety of Афобазол?

A: Studies and official information indicate that the available evidence primarily consists of trials with limited follow-up durations. The follow-up durations for many studies have been limited, meaning data on the long-term safety and effects beyond the short-term course are not widely characterized.


Q: Does Афобазол interact with common pain relievers?

A: Regulatory documents do not list any specific interactions involving metabolic pathways (like CYP enzymes) or drug transporters relevant to common pain relievers. There are also no explicit prohibitions or formal contraindications based solely on an interaction risk with this type of medicine documented in official labeling.


Q: What kind of anxiety is Афобазол typically used for?

A: The medicine is generally used to help manage chronic states of anxiety, tension, and irritability. This includes conditions like neurasthenia or adjustment difficulties, which are characterized by anxiety and associated asthenic (fatigue or exhaustion) manifestations.


Q: Do I need to take Афобазол every day to see a benefit?

A: The standard regimen specifies that the medicine should be taken thrice daily for the duration of the treatment course. The standard regimen of continuous, daily use is the official administration protocol.


Q: Is it possible to develop a tolerance to the effects of Афобазол?

A: Official clinical data notes the lack of withdrawal syndrome manifestations when treatment is stopped. The lack of documented withdrawal syndrome upon cessation is a key feature of its safety profile.


Q: Does taking Афобазол affect your ability to drive?

A: The medicine is associated with uncommon nervous system effects such as dizziness and drowsiness. Additionally, co-administration with other Central Nervous System (CNS) depressants, including alcohol, may lead to an enhancement of sedative effects, which could potentially impact the ability to perform tasks requiring focus.


Q: Are there any specific foods to avoid while on Афобазол?

A: Official labeling states the medicine is administered after a meal. The regulatory information does not list mandatory restrictions on specific foods or supplements that need to be avoided during the course of treatment.


Q: Can Афобазол be taken with coffee or energy drinks?

A: Official labeling does not specify any mandatory time separation requirements relative to other supplements or food. Furthermore, regulatory documents do not list any known interactions with caffeine or stimulants.


Q: Is there research comparing Афобазол to SSRIs for anxiety?

A: Research summaries indicate that comparative evidence against the full range of modern anxiety treatments, including SSRIs (Selective Serotonin Reuptake Inhibitors), is not widely available.


Q: Does Афобазол interact with oral contraceptives?

A: Regulatory documents do not list any interactions involving metabolic pathways, such as Cytochrome P450 (CYP) enzymes. No specific interaction or prohibition with oral contraceptives is noted in the official prescribing information.


Q: Is there a maximum time frame for taking Афобазол continuously?

A: The standard treatment course is defined as 2 to 4 weeks. However, official prescribing information permits the treatment duration to be extended for a continuous period of up to 3 months.

How should Афобазол be stored and disposed of?

Storage Conditions

Official labeling mandates that Афобазол tablets must be stored at a temperature not exceeding 25 C to maintain product stability. The medicine requires environmental protection and must be kept in a dry place and protected from light. The packaging instructions state that the tablets should remain in their original container until use.

Condition Type Requirement
Temperature Limit Do not store above 25 C
Environmental Control Store in a dry place, protect from light
Shelf-Life Do not use after the expiration date
Child Safety Keep out of the sight and reach of children

Disposal Instructions

Regulatory documents specify that the expired or unused product must not be discarded into household waste or wastewater to prevent environmental contamination. Disposal should be carried out according to local regulations or by consulting a pharmacist for guidance on approved drug take-back programs.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Афобазол found in:

A-Z Index: