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.
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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
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.
Allergic reactions are possible.
Rarely - a headache that usually resolves on its own and does not require discontinuation of the drug.
- lactation period (breastfeeding);
- age up to 18 years;
- hypersensitivity to the components of Afobazole.
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).
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.
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.
- Brand name: Afobazole
- Active ingredient: Morpholinoethylthioethoxybenzimidazole
- Dosage form: Pills
- Manufacturer: Pharmstandard
- Country of Origin: Russia
Studies and clinical trials of Afobazole (Click to expand)
- Allergic contact dermatitis from alclomethasone dipropionate
- Tissue availability of afobazole and its major metabolites in rats
- Neuroprotective effect of afobazole on rats with bilateral local photothrombosis of vessels in the prefrontal cortex
- Effect of afobazole on teratogenic activity of cyclophosphamide in rats
- Excretion of afobazole and its metabolites with urine and feces in rats
- Interaction of Afobazole with σ1-Receptors
- Effect of Afobazole on Mitochondrial Monoamine Oxidase A ActivityIn Vitro
- Effect of Afobazole on DNA Damage in Patients with Systemic Lupus Erythematosus
- Effects of Selective Anxiolytic Afobazole on Active Caspase-3
- Neuroprotective Properties of Afobazole in Repeated Hemorrhagic Stroke Modeling in Aged Rats
- cEffect of Afobazole on Genotoxic Effects of Tobacco Smoke in the Placenta and Embryonic Tissues of Rats
- On the Mechanism of Antifibrillatory Effect of Afobazole
- Comparative Analysis of Tissue Availability for Afobazole and Compound M-11
- Study of Anti-Ischemic Effect of Afobazole in Experimental Myocardial Infarction
- Effects of Afobazole on Cognitive Behavior of the Offspring of Rats Exposed to Tobacco Smoke during Gestation Period
- Effects of Afobazole on the Content of Neurotransmitter Amino Acids in the Striatum in Global Transient Ischemia
- Analysis and standardization of the new anxiolytic drug afobazole
- Developing analytical methods for afobazole in injection forms
- Pharmaceutical analysis and standardization of afobazole in solid dosage form (tablets)
- Synthesis and pharmacological activity of the main metabolite of afobazole and its analogs
- Development of a method for assessing the stability of afobazole by HPLC
- Development of synthesis technology for the selective anxiolytic drug afobazole
- Antimutagenic Activity of Afobazole in Various Regimens of Treatment
- Effect of Noopept and Afobazole on the Development of Neurosis of Learned Helplessness in Rats
- P.3.008 Ex vivo investigation of afobazole effect on H3-diazepam binding by synaptoneurosomal membranes of inbred mice and rats