Phenibut: Clinical uses and Synthesis method

Introduction

Phenibut (β-phenyl-γ-aminobutyric acid, β-phenyl-GABA, PB) was synthesized by Perekalin and his associates at the Department of Organic Chemistry of the Herzen Pedagogic Institute in St. Petersburg, Russia. In initial publications, phenibut was known as phenigamma. Phenibut, a nootropic and anxiolytic drug, belongs to the family of γ-amino butyric acid (GABA) derivatives. While several Eastern European states allow its medical use, it is mostly considered a New Psychoactive Substance (NPS) in the Western world.

Synthesis method

The production of phenibut is a multi-stage process, in which the first gets benzalmalonic acid diethyl ether, which is then converted into cyanobenzylmalonic acid diethyl ether. Reduction of diethyl ether with hydrogen gives 4 phenyl-3-carbethoxypyrrolidone-2. By hydrolysis and decarboxylation of this compound in an acidic medium, phenibut is obtained.

Benefits

The active ingredient of the Noofen® medication is Phenibut (IV), a nootropic drug that improves metabolic processes in the brain. Phenibut has both nootropic and anxiolytic activity. It reduces anxiety and a sense of fear and improves sleep, so this medication can be used to treat neurosis, as well as before surgery. Phenibut prolongs and enhances the effect of sleeping pills, narcotic, antipsychotic and antiparkinsonian drugs. Phenibut significantly reduces the manifestations of asthenia and vasovegetative symptoms, including headaches, a feeling of heaviness in the head, sleep disturbances, irritability, emotional instability, and increased working capacity. Phenibut affects the improvement of psychological indicators - attention, memory, speed of sensorimotor reactions and accuracy. In patients suffering from asthenia and emotional instability, phenibut from the first days of treatment improves subjective well-being and increases interest initiative and labour motivation without having an undesirable sedative or stimulating effect.

Clinical uses

The largest amount of information is available on the clinical use of PB in neuroses (i.e., mental disorders characterized by anxiety). In geriatric patients, PB appears to be superior to tranquillizers or neuroleptics. Like BAC, PB reduces spasticity. It has been successfully used in the treatment of post-traumatic stress disorder, “asthenic-depressive” syndrome, stuttering, and even vestibular disorders. In children, PB has been claimed to be effective in neurotic disorders, “organic brain syndrome,” insomnia and various forms of hyperactivity. PB has been successfully used in preschool-age children for speech disorders, particularly stuttering. Due mainly to its tranquilizing activity, it is helpful in epileptic patients. As a tranquillizer, PB appears to be weaker than BDZs. However, unlike BDZs, PB does not reduce performance and controls irritability and fatigue. No toxic effects of PB have been reported. Somnolence in geriatric patients was occasionally mentioned as a side effect. A drawback of PB therapy is the development of tolerance. In some patients, the dose has to be increased by one-fourth to one-third after two weeks of treatment.  

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