Afobazole

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Afobazole

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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 Afobazole

Quick Facts

Property Description
Active ingredient Fabomotizole (Morpholinoethylthioethoxybenzimidazole)
Form Oral tablets or pills
Pharmacological class Selective non-benzodiazepine anxiolytic
General purpose Alleviates anxiety and promotes neuroprotection
Origin Synthetic (chemically derived)

What is Afobazole and What Class of Drug is it?

Afobazole, whose international nonproprietary name (INN) is Fabomotizole, is a synthetic, single-ingredient medication categorized as a selective non-benzodiazepine anxiolytic drug. This compound, which was developed and launched in Russia, is chemically distinct from older classes of tranquilizers. The World Health Organization classifies this compound within the group of other anxiolytics.

The active substance, Morpholinoethylthioethoxybenzimidazole, has been the subject of pharmacological studies published in scientific literature, which have consistently supported its profile as an agent that achieves anti-anxiety effects without the pronounced sedative or muscle-relaxant actions commonly associated with older anxiolytic classes.

Composition, Form, and General Purpose

As a synthetic preparation, Fabomotizole is primarily provided for the oral route of administration in the dosage form of a tablet or pill. The drug's mechanism is unique for its primary function as a sigma-1 receptor modulator, an action that contributes to its neuroprotective effects. The general purpose of the compound is to offer relief from symptoms of anxiety, tension, and worry, a goal which is clinically recognized for medications in this class. Research has explored its potential benefits for patients managing the anxiety and chronic stress that can arise alongside ongoing medical conditions, indicating a specific therapeutic focus beyond generalized anxiety.

What side effects are possible with Afobazole?

Possible Side Effects and Safety Information

The official safety profile of Fabomotizole (Afobazole) is documented in the prescribing information approved by the national regulatory authority in its country of origin, as the medicine lacks marketing authorization from agencies such as the U.S. Food and Drug Administration (FDA) or the European Medicines Agency (EMA).

Documented Adverse Reactions

The most commonly referenced adverse reactions are classified by system-organ class, including effects on the Immune System, characterized by allergic reactions, and effects on the Nervous System.

Adverse Reaction Frequency Classification System-Organ Class
Headaches Occasional Nervous System
Allergic Reactions Not explicitly classified Immune System

The official labeling notes that headaches are typically transient, or time-limited, and often resolve naturally without requiring the discontinuation of treatment. In the event of significant intoxication or overdose, the regulatory documents indicate the potential for a sedative effect and increased drowsiness; notably, this does not result in the muscle relaxation effects associated with other classes of psychotropic medications.

Safety Constraints and Restrictions

Specific safety considerations, as defined by official regulatory constraints, prohibit the use of Afobazole in certain populations. The drug is contraindicated for patients below 18 years of age and for women who are pregnant or lactating (breastfeeding).

Additional contraindications relate to potential excipient intolerances, including intolerance to galactose, lactase deficiency, and glucose-galactose malabsorption. The official prescribing information also includes statements that the drug does not cause muscle weakness and does not negatively affect the concentration of attention or memory, framing the medicine's specific high-level safety characteristics.

Overdose and Emergency Response

The official regulatory documents for Afobazole (Fabomotizole) define its overdose profile based on manifestations of central nervous system (CNS) depression. Documented presentations following a significant overdose include a sedative effect and increased somnolence or drowsiness. While symptoms are generally classified as non-life-threatening, ingestion of a massive dose carries the potential for severe oversedation that may progress to a loss of consciousness.

Regulatory authorities mandate that immediate medical attention must be sought for any suspected overexposure.

The management approach is officially defined as symptomatic and supportive treatment. The official regulatory statements governing the management and risk are:

  • No specific antidote is known for Afobazole.
  • Procedures such as gastric lavage and the administration of activated charcoal are listed as supportive measures.
  • Hospital monitoring and clinical observation are required to track the progression of CNS status.

Connection to the overall overdose profile: The drug's official overdose profile is defined by manifestations of dose-related CNS depression which, due to the lack of a specific antidote, requires mandatory contact with emergency medical services and reliance on symptomatic supportive care.

Therapeutic Uses of Afobazole

What Afobazole Treats: Main Uses and Benefits

Afobazole (Fabomotizole) is commonly used to help with symptomatic discomfort in conditions involving increased emotional and physical tension, supporting patients during periods of noticeable symptomatic stress. Clinical studies focusing on its efficacy show it is considered relevant for symptomatic management across specific therapeutic domains.

This medication is applied to address symptom clusters that may become intense or disruptive in conditions like Generalized Anxiety Disorder, neurasthenia, and Adjustment Disorders. It supports the relief of symptoms related to heightened physiological activity, including persistent worry, excessive apprehension, and unprovoked muscle tension.

Quick Fact: Relevant for Non-Sedating Symptom Management

The symptomatic assistance provided by this medication may contribute to comfort, as it:

“The support may assist with easing the impact of symptoms that interfere with routine activities.”

This may help patients cope more steadily and supports the maintenance of functional stability during periods of heightened discomfort or prolonged medical strain.

Eligibility and Restrictions for Use

Who can and cannot use Afobazole?

Afobazole (Fabomotizole) is an anxiolytic drug authorized by a national regulatory body outside of the United States and European Union, and it is not approved by the FDA or the EMA. Eligibility for its use is strictly defined by the official prescribing information.


Population Exclusions and Restrictions

Category Official Regulatory Statement
Populations for whom use is allowed Adults aged 18 years and older are the approved population.
Absolute Contraindications Use is contraindicated in patients with a known hypersensitivity to the drug or its components, including individuals with galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.
Age Restriction The medicine is contraindicated for pediatric patients under the age of 18; use is not established in this group.
Reproductive Status Use is contraindicated during pregnancy and lactation due to a lack of sufficient safety data.
Condition-Specific Restrictions Use requires caution in patients with severe hepatic impairment or severe renal impairment.

These official classifications define a limited eligible population: adults (18 and older) who do not possess any of the specified contraindications or organ-function limitations. The drug must be used with caution when severe kidney or liver issues are present.

What should I know about interactions with other medicines?

Official Interaction Profile

The documented interaction profile for Afobazole (Fabomotizole) is established strictly through specific findings stated in authoritative government regulatory documentation, focusing on pharmacodynamic patterns with certain co-administered agents.

Interactions with Medicinal Products

Co-administration is officially documented to result in a clinically significant potentiation of the effects of some co-administered medicines. The regulatory labeling states that this drug increases the anxiolytic effect when taken alongside Diazepam. Similarly, it is officially documented to potentiate the anticonvulsant effect of Carbamazepine. The medicine is also noted for its lack of influence on the hypnotic effect of Thiopental. These findings reflect the specific interaction classifications detailed in the drug's approved profile.

Interactions with Substances

The official regulatory profile specifically addresses the interaction with alcohol. It is documented that Afobazole does not influence the narcotic effect of Ethanol. No formal interactions with food, supplements, or specific herbal products are documented in the official prescribing information.

Administration Constraints

No mandatory requirements for the separation of administration times, such as 'administer X hours apart,' are specified in the official labeling. The profile does not classify any drug combination as a formal contraindication based on interaction risk, nor does it detail specific cautions regarding altered interaction severity in patient populations.

Mechanism of Action

How Afobazole Works

Fabomotizole acts primarily as a selective agonist and modulator of the Sigma-1 receptor (sigma 1R), an internal chaperone protein located in the Endoplasmic Reticulum (ER). This modulation influences critical processes such as Intracellular Calcium ( Ca^2+) Homeostasis and the excitability of the neuronal membrane. This action results in the modulation of central nervous system hyper-excitability through cellular-level regulatory activity.

The sigma 1R modulation cascade indirectly influences GABA A receptor function—the brain's principal inhibitory system—by preventing the stress-induced reduction in receptor availability, thereby maintaining the capacity for inhibitory neurotransmission. Fabomotizole also acts as a reversible inhibitor of Monoamine Oxidase A ( MAO-A), a pathway that affects the catabolism of key monoamine neurotransmitters.

Furthermore, the mechanism involves the modulation of neuronal viability by promoting the expression of neurotrophic factors, including Brain-Derived Neurotrophic Factor (BDNF). This effect is complemented by the inhibition of the enzyme NQO2 (MT3 receptor), a mechanism that reduces the contribution of certain metabolic pathways to cellular oxidative stress. This multi-target approach modulates the mechanisms influencing cellular integrity and stress response.

Dosage and Administration Information

How Afobazole is Used: Official Administration Guidelines

The following information describes the official usage pattern for Afobazole (Fabomotizole). These guidelines define the standardized administration protocol for the medicine.

Administration Feature Regulatory Guideline
Route of Administration The medicine is administered via the oral route.
Standard Dosing Schedule The typical total daily dose is 30 mg, divided across the day. The dosage may be formally increased up to a maximum of 60 mg per day under specialized supervision.
Frequency and Timing Administration is carried out three times daily (t.i.d.). Each dose is scheduled to be taken after a meal.
Preparation Requirements The tablet must be swallowed whole with a small amount of water; it is not intended to be dissolved or chewed.
Course Duration The standard course of administration typically lasts 2 to 4 weeks. Based on clinical assessment, the duration may be formally extended up to a maximum period of 3 months.
Age-Group Rules The established standard dosing regimen is applicable for adult patients between the ages of 18 and 70 years.

The documented instructions establish a precise oral administration protocol. This protocol requires the total daily dosage to be consistently divided into three administrations and specifically timed after meals. This regimen ensures adherence to the recognized pattern of use, defining the frequency and contextual timing necessary for the entire treatment cycle.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Afobazole

Evidence for Use in Anxiety and Adjustment Disorders

The foundation of clinical evidence for Afobazole includes multicenter Randomized Controlled Trials (RCTs). These short-term studies were used in research examining outcomes related to Generalized Anxiety Disorder (GAD) and Adjustment Disorders. The research examined populations consisting primarily of adults (ages 18 to 60) and applied standardized tools, such as the Hamilton Anxiety Rating Scale (HAMA), to monitor the intensity and variability of symptoms.

These studies explored outcomes related to physical discomfort and outcomes reflecting daily functioning or activity level. Findings describe patterns observed in the studies where patient groups, including those receiving Afobazole, recorded changes in their anxiety symptom scores during the specific, defined treatment intervals, sometimes against a standard comparator. The evidence contributes to understanding symptom patterns and how patient-reported outcomes describing perceived discomfort evolved in the observed populations during the short study period.

The quality of the evidence varies across studies. The majority of the key published clinical trials are derived from Russian-led research. A limited number of large-scale international studies have been published to date. Furthermore, follow-up durations were limited, as the core clinical research primarily focused on short-term symptom changes, typically over active treatment periods of about 30 days.


Studies in Patients with Co-occurring Medical Conditions

Afobazole was also evaluated in studies exploring outcomes related to anxiety that occurs alongside chronic somatic or medical conditions, such as cardiovascular disease (CVD). This research scenario involved specialized clinical trials and observational cohorts, rather than large comparative RCTs.

Research highlights outcomes measured during the study period for patients with co-occurring medical illness who participated in the trial. Data for certain groups remain insufficient. The evidence is generally limited, often relying on small populations and non-comparative study designs. Certainty remains low regarding the consistency of reported findings across various medical conditions, and there is limited information for long-term outcomes in this specific group.


Key Research Gaps and Uncertainty

While research describes a framework of evidence for Afobazole, particularly in specific anxiety disorders, several gaps and uncertainties exist. Long-term effects are not fully established, as research exploring short-term symptom changes does not provide sufficient data on outcomes over periods longer than a few months. Research has not widely explored the use of Afobazole in certain groups, such as children or older adults. The majority of the primary evidence base is documented in non-English scientific journals, which means comparative evidence is lacking from large-scale studies outside of Russia. Findings describe group patterns, not personal outcomes, and research does not determine whether an individual will respond similarly.

Key Studies & References Afobazole modulates neuronal response to ischemia and acidosis via activation of sigma-1 receptors

Frequently Asked Questions (FAQ)

Common questions about Afobazole (FAQ)

Q: Are there any common mild side effects that people report when starting Afobazole?

The official prescribing information documents adverse reactions classified as effects on the nervous system, such as headaches, and effects on the immune system, such as allergic reactions. Headaches are often described as being transient, meaning they resolve on their own without needing to stop the treatment. Some reports also mention mild digestive system issues, including nausea or discomfort.

Q: Does Afobazole need time to build up in the system before the effects are noticeable?

Clinical data suggests that the drug has a relatively rapid onset of action compared to older types of anti-anxiety medications. However, clinical trials and administration guidelines define a treatment period of several weeks, which is the timeframe used to evaluate the full therapeutic effect.

Q: How quickly should someone expect to feel the therapeutic effects of Afobazole?

The drug is generally recognized for its relatively rapid onset of action. Clinical trials examine the full benefits over the duration of the defined treatment course, which can be extended up to three months. The official guidelines emphasize that the effects are linked to the completion of the structured treatment course.

Q: Can Afobazole be used by people who have existing liver or kidney conditions?

According to official product information, the drug must be used with caution in patients who have severe hepatic impairment (serious liver issues) or severe renal impairment (serious kidney issues). This caution is based on how the drug is metabolized and excreted.

Q: What types of food or drinks, if any, should be avoided while using Afobazole?

The official regulatory information states that Afobazole does not influence the narcotic effect of ethanol (alcohol). Furthermore, no formal interactions with food, supplements, or specific herbal products are documented in the official prescribing profile.

Q: Can Afobazole affect a person's ability to drive or operate machinery?

Official safety statements note that at standard therapeutic doses, the drug is not documented to negatively affect concentration or memory. Drowsiness and sedative effects are specifically noted as potential consequences only in cases of intoxication or overdose.

Q: Is Afobazole suitable for use by older adults?

The established standard dosing regimen, according to the official administration guidelines, is applicable for adult patients between the ages of 18 and 70 years.

Q: Is it true that Afobazole can cause withdrawal symptoms if stopped suddenly?

The compound is chemically distinct from benzodiazepines, an older class of anxiolytics often associated with a high risk of withdrawal. Literature on the mechanism of action often highlights that the drug is distinct from benzodiazepines and is generally noted to act without the risk of physical dependence commonly associated with that older class.

Q: What are the most serious side effects officially associated with Afobazole?

The official prescribing information primarily documents the occurrence of allergic reactions and headaches as adverse reactions. In the event of intoxication or overdose, the regulatory documents indicate the potential for a sedative effect and increased drowsiness.

Q: Is it normal to feel slightly drowsy when first beginning treatment with Afobazole?

The drug is generally noted for not causing the pronounced sedative effects associated with other anxiolytic classes. Drowsiness or sedation is specifically documented as a potential symptom only of intoxication or overdose, rather than a typical effect at a standard therapeutic dose.

Q: Can Afobazole be taken with or without food?

The official administration protocol is precise regarding the timing of administration. It specifies that each dose must be scheduled to be taken after a meal.

Q: Is Afobazole intended for long-term maintenance or only short-term use?

The standard course of administration is considered short-term, ranging from two to four weeks, with a formal maximum duration of three months. Research has noted that long-term effects beyond the short clinical trial period are not fully established.

Q: How does Afobazole differ from other common anxiety medications (non-comparative claims)?

Afobazole is categorized as a selective non-benzodiazepine anxiolytic drug. Its mechanism is unique, primarily involving the modulation of the Sigma-1 receptor (sigma 1R) and indirectly influencing the GABA A system. This mechanism is noted to achieve anti-anxiety effects without the pronounced sedative or muscle-relaxant actions of older tranquilizer medications.

Q: Is there a risk of dependence or addiction associated with Afobazole?

The drug is chemically distinct from compounds associated with a high risk of dependence. Clinical literature on the mechanism of action often highlights that the drug is distinct from benzodiazepines and is generally noted in clinical literature to be described as acting without the risk of dependence associated with that older class.

Q: Is Afobazole safe to use for an extended period of time?

The maximum established course duration for treatment is three months. Research has noted that long-term effects are not fully established beyond the short clinical trial period, indicating that the long-term safety profile is not fully established beyond this period.

Q: Is it safe to use Afobazole with herbal remedies or dietary supplements?

The official prescribing information states that no formal interactions with supplements or specific herbal products are documented. This indicates that no formal assessment of safety or risk has been documented by the authorizing body regarding combination with these specific products.

Q: Does Afobazole interact with common non-prescription pain relievers or cold medicines?

The official interaction profile only mentions specific interactions with certain prescription medicines. However, general pharmacodynamic patterns suggest caution when combining Afobazole with other medicines that may cause Central Nervous System (CNS) depression, such as certain common cold or pain relievers.

Q: Are there any known interactions between Afobazole and caffeine?

The official prescribing information states that no formal interaction between Afobazole and caffeine is documented.

Q: Where can I find the official regulatory information about Afobazole?

The drug's regulatory authorization and prescribing requirements are based on the national regulatory authority in the Russian Federation, which is the government body that authorized the drug’s use. Official patient information is derived from this source.

Q: Does Afobazole help with both the mental and physical symptoms of anxiety?

Clinical research for Afobazole includes studies that explored outcomes related to both physical discomfort and the mental symptoms of anxiety. The drug is generally used to offer relief from symptoms of anxiety, tension, and worry.

Q: Does Afobazole interact with other prescription psychiatric medicines?

Official documentation states that co-administration is noted to increase the anxiolytic effect when taken alongside the prescription medicine Diazepam. It is also officially noted to potentiate the anticonvulsant effect of Carbamazepine.

Q: Can Afobazole be used for occasional, situational stress?

Clinical research has primarily focused on specific diagnoses, such as Generalized Anxiety Disorder (GAD) and Adjustment Disorders. The official administration guidelines outline a structured course of treatment lasting several weeks, which implies use beyond occasional or as-needed situations.

Q: Is Afobazole primarily used for generalized anxiety or panic? (Factual scope)

The foundation of clinical evidence includes multicenter randomized controlled trials that examined outcomes related to Generalized Anxiety Disorder (GAD) and Adjustment Disorders.

Q: Are there different formulations or strengths of Afobazole available?

The drug is primarily provided in the dosage form of oral tablets. Clinical trial records cite the use of 10 mg tablets, indicating that 10 mg is an available strength.

How should Afobazole be stored and disposed of?

How to Store and Dispose of Afobazole?

Afobazole (Fabomotizole) must be stored strictly according to its official labeling to maintain stability. The container should be kept tightly closed and stored in a dry, cool, and well-ventilated place.


Storage Requirements

Condition Requirement
Environment Dry, cool, and well-ventilated
Protection Keep away from direct sunlight, moisture, and sources of ignition
Child Safety Store out of the sight and reach of children

Disposal

Disposal of unused or expired product must follow all local and federal regulations for pharmaceutical waste. The medication should not be allowed to enter drains or contaminate the environment. Authorized disposal methods, such as removal to a licensed chemical destruction plant or controlled incineration, are required to prevent environmental discharge.

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

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