AFOBAZOLE (AKA FABOMOTIZOLE)

by L F

Afobazole is a novel anxiolytic drug with nootropic properties used in Russia to treat anxiety and some cardiac disorders. According to clinical trials, its efficacy in patients with generalized anxiety disorder and adjustment disorder is comparable to benzodiazepines.  
The active ingredient is Fabomotizole. 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.  
 

MECHANISM OF ACTION

Afobazol mechanism of action is different from 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 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.   
 

INDICATIONS AND USAGE

  
Indications for use are:
  • Generalized anxiety disorder.
  • Neurasthenia.
  • Adjustment disorder.
  • Anxiety related insomnia.
  • Neurocirculatory dystonia.
  • Premenstrual syndrome.
  • Alcohol abstinence syndrome.
  • Nicotine withdrawal.
 
 In Russia and other CIS countries, Afobazole is a non-prescription drug. It is one of the few effective OTC anxiolytics available among with Adaptol (Mebicar) and Phenibut. 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.   
 

SIDE EFFECTS AND CONTRAINDICATIONS

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 do not cause withdrawal after cessation.  
Contraindications for use are pregnancy and lactation, age below 18 years old.  
   

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  References
  1. Seredinin S.B, Voronin M.V "Neuroreceptor mechanisms involved in the action of Afobazole."
  2. Silkina I.V, Aleksandrin V.V, Ganshina T.S, Seredinin S.B, Mirzoyan R.S "Afobazole increases cerebral blood flow in rats with global ischemia."
  3. Ganshina T.S, Kurdymov I.N, Turilova A.I, Mirzoyan R.S, Seredinin S.B "Afobazole effects on cerebral circulation under hemorrhagic stroke model conditions."
  4. Abramova E.V, Voronin M.V, Seredinin S.B "Interaction of afobazole with sigma-1 receptors in mice brain."
  5. Silkina I.V, Zenina T.A, Seredinin S.B, Mirzoyan R.S "Effect of afobazole on the accumulation of free radical oxidation products and the catalase activity in rats with cerebral ischemia."
  6. Seredinin A.B, Melkumyan D.S, Valdman E.A, Yarkova M.A, Seredinina T.S, Voronin M.V, Lapitskaya A.S "Effects of afobazole on the bdnf content in brain structures of inbred mice with different phenotypes of emotional stress reaction."
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