Phenibut

One of the most efficient anxiolytics you can buy

One of the most popular Russian nootropic drugs is Aminophenylbutyric acid (Phenibut), known under such trade names as Anvifen, Fenibut, and Noofen. It is considered as supplement outside of Russia, so you can buy Phenibut from a variety of vendors.

Phenibut is considered as a nootropic, tranquilizing, psycho-stimulating, antiaggregant and antioxidant agent. Some experts believe that Phenibut improves the functional state of the brain due to the normalization of tissue metabolism. Accordingly, for adults, the drug is recommended for the treatment of anxiety disorders, asthenic conditions (chronic fatigue), including in patients with schizophrenia.

Phenibut is also used in pediatrics. The drug recommended for the treatment of anxiety disorders, asthenic conditions, tics and stuttering, sensorineural hearing loss, and ADHD in children. Moreover, the possibility of using Phenibut in narcology is discussed. It is shown that Phenibut contributes to the relief of alcohol withdrawal syndrome, as well as the reduction of pathological cravings for alcohol.

Most frequently used anxiolytic drugs are benzodiazepine tranquilizers. However, benzodiazepines may impair cognitive functions, memory, and psychomotor coordination. In search of a replacement for benzodiazepines, on the initiative of Professor I.P. Lapin from the Institute of V.M. Bechterew at the Department of Organic Chemistry of the Pedagogical Institute A.I. Herzen has synthesized a new GABAergic drug – Phenibut.

The molecule of Phenibut was obtained by the addition of a phenyl ring to the gamma-Aminobutyric acid, which adds lipophilic properties to the molecule. As a result, Phenibut easily penetrates the blood-brain barrier. However, because of the change in the structure of the molecule, the Phenibut has its own inhibitory mechanism. And this new variant, perhaps, can be designated as “selective” anxiolytic drug. Unlike benzodiazepines, Phenibut does not enhance the effects of endogenous GABA, but itself performs its role.

Moreover, Phenibut has only one of the two mechanisms of GABA. Thus, Phenibut is able to influence GABA-A receptors located on various neurons. In addition, this influence is less pronounced than that of GABA itself. That is why Phenibut does not have an anticonvulsant effect and does not cause significant sedation. There are also no scientific data showing the effect of Phenibut on the endocrine system and, in particular, the release of growth hormone.

The selective variant of inhibition is associated not only with a decrease in the activity of neurons but also with a more palpable (in comparison with GABA) recovery of dopamine neurons. The above-mentioned differences in the sensitivity of GABAA-receptors, as well as the weaker (in comparison with GABA) effect on them of Phenibut, affect here.

As a result, this drug is able to inhibit dopamine neurons only in very significant doses that go beyond therapeutic ones. Thus, Phenibut has two main components of the mechanism of action that are important for the clinical use of the drug – inhibitory and activating. The first of them can be beneficial in numerous pathological conditions, whose pathogenesis is associated with an increase in the activity of glutamate, norepinephrine, acetylcholine and histamine neurons.

In clinical practice, benzodiazepines are often used to treat these disorders. And this tactic seems quite justified taking into account the mechanism of action of these drugs. However, it has already been mentioned above that there are numerous contingents of patients in whom generalized inhibition, often associated with sedition, will create certain problems in the conduct of pharmacotherapy.

In this situation, it seems preferable to use a moderate inhibitory component of the mechanism of action of the Phenibut. Better tolerability of therapy is in agreement with the fact that Phenibut (unlike benzodiazepines) has an activating component in its mechanism of action.

Meanwhile, dopamine activity is necessary for the realization of the functions of the intellectual and motor spheres of both adults and children. It is the dopamine neurons that are responsible for the development of motivation, the reinforcement system, and therefore, the targeted behavior in the learning process of any new skills. In addition, dopamine neurons are extremely important for switching from one task to another. Finally, they are responsible for emotions, the organization of precise movements and their smoothness, as well as regulation of the endocrine system.