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Fabomotizole (brand-name Afobazole) is a novel anxiolytic drug with nootropic properties used in Russia to treat anxiety and some cardiac disorders. One of the most important advantages of fabomotizole over benzodiazepines is that it does not form dependence and has fewer side effects.
Afobazole was discovered in the beginning of 2000s at Zakusov Institute of Pharmacology. This institute is also known for its discoveries of dipeptide nootropic Noopept, adaptogen Ladasten (Bromantane) and anxiolytic peptide Selank.
What makes it special among other anti-anxiety medications is that Afobazol does not have sedative, hypnotic and muscle relaxant action and does not form dependence. Besides that, studies in models of local and global ischemia have revealed neuroprotective effects of the drug.
Afobazol’s mechanism of action is different from that of benzodiazepines. It is not a benzodiazepine receptor site agonist; at the same time, it prevents stress-induced changes of GABA-benzodiazepine receptor complex and restores its sensitivity to endogenous inhibitory mediators. The drug acts on sigma-1 receptors, melatonin MT1, and MT3 receptors and was shown to reversibly inhibit MAO-A. It also has some neurotrophic properties, although they are not as pronounced as in another non-sedative anxiolytic, Stresam. In studies performed on rats, Afobazol prevented stress-induced BDNF decrease and increased NGF and BDNF content in hippocampal HT22 cells culture.
In Russia and other CIS countries, Afobazole is a non-prescription drug. It is one of the few effective OTC anxiolytics available . And because of its effectiveness and the fact that benzodiazepines require a prescription, it rapidly grows in popularity. Sales rose from 100 thousands of packages in 2006 to one million of packages in 2015.
The treatment is usually well-tolerated by the patients. Possible adverse effects as stated by the official instruction are headaches and allergic reactions. The drug is not habit-forming and does not cause withdrawal after cessation.
Fabomotizole is used in Russia to treat the following symptoms:
- Generalized anxiety disorder symptoms, e.g. bad feelings, tensions in the body, irritability, tearfulness, fearfulness, etc.
- Various somatic (psycophysiological) disorders, e.g. asthma, irritable bowel syndrome, systemic lupus erythematosus, ishemic heart diseases, etc.
- Sleep disorders caused by anxiety
- Premenstrual syndrome
- Alcohol and nicotine withdrawal.