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AFOBAZOLE [Fabomotizole]

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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 at the beginning of the 2000s at the Zakusov Institute of Pharmacology. This institute is also known for its discoveries of dipeptide nootropic Noopept, adaptogen Ladasten (Bromantane), and anxiolytic peptide Selank. Now you can buy Afobazole in every Russian pharmacy.

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 a dependence in any dosage. 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 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.

Afobazole | 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 (psychophysiological) disorders, e.g. asthma, irritable bowel syndrome, systemic lupus erythematosus, ischemic heart diseases, etc.
  • Sleep disorders caused by anxiety
  • Premenstrual syndrome
  • Alcohol and nicotine withdrawal

Country of Manufacture: Russia. Produced by Pharmstandard.

Dosage and administration Afobazole ® should be taken following meals. The normal daily dose is 30 mg: 10 mg thrice daily (morning, afternoon and evening). The duration of a course of treatment is 2 - 4 weeks. If needed, the daily dose can be raised to 60 mg and the course length extended to 3 months. Side effects Allergic reactions, occasional headaches. Overdose Sedative effect and sleepiness are possible; they should be treated with caffeine. Country of Manufacture: Russia You can read the full instruction here
  1. Neznamov et al (2001) Clinical study of the selective anxiolytic agent afobazolhttps://www.ncbi.nlm.nih.gov/pubmed/11548440
  2. VS Kudrin (2006) A comparative study of the effect of afobazole on brain monoamine systems in BALB/C and C57BL/6 micehttps://www.ncbi.nlm.nih.gov/pubmed/17153957
  3. A Uyanaev, V Fisenko (2006) Studies of long-term noopept and afobazol treatment in rats with learned helplessness neurosishttps://link.springer.com/article/10.1007/s10517-006-0327-5
  4. Davydova et al (2010) Neurochemical study of effects of the new anxiolytic drugs afobazol and ladasten on the synthesis and metabolism of monoamines and their metabolites in the brain structures of Wistar rat on the model of monoamine synthesis blockade induced by aromatic amino acid decarboxylase inhibitor NSD-1015https://www.ncbi.nlm.nih.gov/pubmed/20408420
  5. Reutova et al (2010) Anxiolytic afobazole action self-evaluated by patients with anxiety-asthenic disordershttps://www.ncbi.nlm.nih.gov/pubmed/21086645
  6. Volkova et al (2010) Comparative study of the interoceptive effects of afobazole and diazepamhttps://www.ncbi.nlm.nih.gov/pubmed/21254504
  7. Kryzhanovskyi et al (2011) Study of anti-ischemic effect of afobazole in experimental myocardial infarctionhttps://www.ncbi.nlm.nih.gov/pubmed/21240343
  8. Cuevas et al (2011) Afobazole modulates microglial function via activation of both sigma-1 and sigma-2 receptorshttps://www.ncbi.nlm.nih.gov/pubmed/21715561
  9. Seredenin et al (2013) On the mechanism of anti-ischemic effects of afobazolehttps://www.ncbi.nlm.nih.gov/pubmed/24288760
  10. Behensky et al (2013) Afobazole activation of σ-1 receptors modulates neuronal responses to amyloid-β25-35https://www.ncbi.nlm.nih.gov/pubmed/24006338
  11. Kadnikov et al (2015) Cytoprotective Effect of Afobazole and Its Main Metabolite M-11https://www.ncbi.nlm.nih.gov/pubmed/26033588
  12. TS Syunyakov, GG Neznamov (2016) Evaluation of the therapeutic efficacy and safety of the selective anxiolytic afobazole in generalized anxiety disorder and adjustment disorders: Results of a multicenter randomized comparative study of diazepamhttps://www.ncbi.nlm.nih.gov/pubmed/27636931
  13. Kryzhanovkii et al (2018) On the Mechanism of the Cardioprotective Action of σ1 Receptor Agonist Anxiolytic Fabomotizole Hydrochloride (Afobazole)https://www.ncbi.nlm.nih.gov/pubmed/30225699
  14. Ostrovkaya et al (2018) Antidiabetic Activity of Afobazole in Wistar Ratshttps://www.ncbi.nlm.nih.gov/pubmed/30225697

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