Afobazole®

Afobazole is a novel anti-anxiety drug developed in russia. Afobazole does not cause sedation and is not addictive, unlike commonly used anxiety drugs. Besides having an anxiolytic action, afobazole is also shown to possess nootropic properties.

Brand Pharmstandard

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Available since: 2019-09-19

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Afobazole, also known as Fabomotizole, is a novel, non-benzodiazepine anxiolytic drug. It is approved for medical use in Russia to treat anxiety disorders.

The drug was discovered in 2000’s in Zakusov institute of pharmacology (Russia), the same institute that discovered nootropic drug Noopept and long-acting benzodiazepine tranquilizer Phenazepam.

Afobazole has a wide spectrum of clinical application as it has both anxiolytic and nootropic properties. Besides its main use for anxiety management, Afobazole also can be used in conjunction therapy for various somatic diseases. The official indications for use are:

Anxiety disorders
Irritable bowel syndrome
Anxiety-induced sleep disorders
Premenstrual syndrome
Alcohol withdrawal syndrome
Bronchial asthma
Systemic lupus erythematosus
Ischemic heart disease
Hypertension
Arrhythmia

Afobazole does not cause sedation and lacks hypnotic activity and abuse potential, unlike most drugs used for anxiety purposes. The dosage at which hypnosedative effects are observed is about 50 times higher than the effective therapeutic dose.

The relief of emotional as well as the physical symptoms of anxiety usually observed within a week after starting a treatment with Afobazole, with a peak effect at week 4.

The mechanism of action of Fabomotizole based on its ability to antagonize stress-induced changes of GABA/benzodiazepine receptor complex, and restore its sensitivity to the endogenous ligands. The drug does not binds to the benzodiazepine receptors and has no myorelaxant effects. According to the radioligand binding assay, Afobazol also have affinity with dopamine d1 and melatonin MT1/MT3 receptors, and is shown to inhibit MAO-A.

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Dosage and Administration

Afobazole is prescribed by mouth, after eating. A single dose is 10 mg; daily dose - 30 mg, divided into 3 doses during the day. The duration of the course of the drug is 2-4 weeks. If necessary, the daily dose of the drug can be increased to 60 mg, and the duration of treatment up to 3 months.

Adverse reactions

Allergic reactions are possible.

Rarely - a headache that usually resolves on its own and does not require discontinuation of the drug.

Contraindications

pregnancy;
lactation period (breastfeeding);
age up to 18 years;
hypersensitivity to the components of Afobazole.

Drug interactions

With the simultaneous use of Afobazole does not affect the narcotic effect of ethanol and the hypnotic effect of thiopental. With the simultaneous use of Afobazole potentiates the anticonvulsant effect of carbamazepine. With simultaneous use of Afobazole increases the anxiolytic effect of diazepam.

Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Special instructions

The drug does not adversely affect the driving of motor vehicles and the performance of potentially hazardous activities that require high concentration of attention and speed of psychomotor reactions.

Overdosage

Symptoms: with a significant overdose and intoxication may develop a sedative effect and increased drowsiness without manifestations of muscle relaxation.
Treatment: as an emergency, n / a caffeine sodium benzoate 20% is prescribed, a solution of 1 ml 2-3 times / day.