Phenibut

Phenibut was synthesized at the Leningrad Pedagogical Institute. Herzen Professor V.V. Perekalin ^[5] . The study of the clinical and pharmacological properties of phenibut was performed in the laboratory of psychopharmacology of the Leningrad Research Institute named after V. M. Bekhterev Senior Researcher R. A. Khaunina ^[6] . In 1982, Honored Worker of Science of the RSFSR V.V. Perekalin, Ph.D. for work "Synthesis, Pharmacology, Clinic and Introduction into Industrial Production, into the Preventive and Treatment Practice of the New Domestic Tranquilizer" Phenibut " honey. Sciences of R. A. Khaunin, as well as Professor M. M. Zobacheva , Honored Inventor of the RSFSR I. P. Neumyvakin and others, were awarded the State Prize of the Latvian SSR ^[7] .

At one time, Phenibut was among the medicines that must be included in the astronaut’s first-aid kit . Conventional tranquilizers poorly lowered the high level of stress of the astronauts, because in addition to the calming effect, they also had a relaxing effect. When taking Phenibut, the performance of the astronauts remained at the same level.

In 1975, the drug phenibut was included in the first-aid kit of astronauts who participated in the Soyuz – Apollo experimental flight ^[6] .

By its chemical structure, phenibut can be considered as a phenyl derivative of gamma-aminobutyric acid and also as a phenylethylamine derivative.

Phenibut has elements of nootropic activity, has a psychostimulating and tranquilizing effect, reduces tension, anxiety, improves sleep ; lengthens and enhances the effect of sleeping pills, drugs, antipsychotics and psychostimulants.

Phenibut is used for asthenic and anxiety-neurotic conditions , anxiety , anxiety , fear , insomnia , and also as a sedative before surgical interventions.

It is also prescribed for Meniere's disease , dizziness associated with dysfunction of the vestibular apparatus, for the prevention of motion sickness.

Children are prescribed for stuttering and tics , and are also prescribed for adults with severe speech impairment .

There is evidence of an increase in the effect of antiparkinsonian drugs under the influence of phenibut (due to the presence of a dopaminopositive component in the drug).

When using Phenibut in children under 10 years of age with stuttering, speech impairment can be observed, and the pattern of the electroencephalogram can also be changed, including the appearance of sharp wave peaks. The specified drug for children should be used with extreme caution.

Asthenic and anxiety-neurotic conditions, anxiety, anxiety, fears, insomnia, logoneurosis, nervous tics, as well as a sedative before surgery. A feature is a pronounced effect in the treatment of dizziness.

Direct exposure to GABAergic receptors facilitates GABA- mediated transmission of nerve impulses to the central nervous system. It improves the functional state of the brain due to normalization of tissue metabolism and effects on cerebral circulation (increases the volumetric and linear velocity of cerebral blood flow, reduces the resistance of cerebral vessels, improves microcirculation, has an antiplatelet effect), and also has a tranquilizing, psychostimulating, antiplatelet and antioxidant effect. It helps to reduce or disappear feelings of anxiety, tension, anxiety and fear, normalizes sleep, does not have an anticonvulsant effect, but enhances the effect of anticonvulsants. Does not affect choline and adrenoreceptors. Extends the latent period and shortens the duration and severity of nystagmus. It reduces the manifestations of asthenia and vasovegetative symptoms (including headache, a feeling of heaviness in the head, sleep disturbance, irritability, emotional lability), and increases mental performance. Improves psychological indicators (attention, memory, speed and accuracy of sensory-motor reactions). With a course admission, it increases physical and mental performance, improves memory, normalizes sleep; improves the condition of patients with motor and speech disorders. Patients with asthenia from the first days of therapy feel better, increase interest and initiative (motivation of activity) without sedation or arousal. When prescribed after severe traumatic brain injury, the number of mitochondria in the perifocal regions increases. With neurogenic lesions of the heart and stomach, it normalizes lipid peroxidation processes. In the elderly, it does not cause congestion and excessive lethargy, a relaxing aftereffect is most often absent. It improves microcirculation in the tissues of the eye, reduces the inhibitory effect of ethanol on the central nervous system. The drug has low toxicity, does not cause allergic effects, does not have teratogenic, embryotoxic and carcinogenic properties.

Absorption is high, it penetrates well into all body tissues and through the BBB (about 0.1% of the administered dose of the drug penetrates into the brain tissue, and to a much greater extent in young and old people). Evenly distributed in the liver and kidneys. It is metabolized in the liver - 80-95%, metabolites are pharmacologically inactive. Does not cumulate. After 3 hours, it begins to be excreted by the kidneys, while the concentration in the brain tissue does not decrease and it is found in the brain for another 6 hours. About 5% is excreted by the kidneys unchanged, partially with bile.

White crystalline powder. The taste is sour. Very soluble in water, soluble in alcohol; The pH of an aqueous (2.5%) solution is 2.3-2.7.

Hypersensitivity to the drug, pregnancy, breastfeeding, children under 8 years old. Caution should be used for erosive and ulcerative lesions of the gastrointestinal tract and liver failure. At the first doses of phenibut or with an overdose, drowsiness may occur.

It is generally well tolerated. At the first receptions drowsiness is possible, with an overdose - severe drowsiness, nausea, diarrhea, vomiting ^[8] ; increased irritability , agitation, anxiety, dizziness , allergic reactions .

Enhances and lengthens the effect of sleeping pills , antiparkinsonian and antiepileptic drugs, antipsychotics , narcotic analgesics ^[8] , amitriptyline .

With prolonged use, it is necessary to monitor liver function indicators and the picture of peripheral blood. It is necessary to refrain from potentially hazardous activities requiring increased attention. It is ineffective with severe motion sickness ("indomitable" vomiting, dizziness, etc.).

Phenibut in the Russian Federation is sold in pharmacies only according to the prescription of the attending neurologist and psychiatrist, or on the recommendation of a doctor in writing, certified by the seal of the medical institution. Selling medicine without a doctor’s prescription, without the recommendation of a doctor, or without the seal of a medical institution is prohibited.

• Lapin, I. Phenibut (beta-phenyl-GABA): A tranquilizer and nootropic drug: [ eng. ] // CNS Neuroscience & Therapeutics: j. - 2001. - Vol. 7, no. 4 (December). - P. 471−481. - DOI : 10.1111 / j.1527-3458.2001.tb00211.x . - PMID 11830761 .
• Synthesis of y-amino-p-phenylbutyric acid (phenibut) / V.V. Sivchik, G. O. Grigoryan, V. L. Survilo, T. V. Trukhacheva; RUE "Belmedpreparaty", Minsk // Medical and social ecology of the individual : status and prospects: Materials of X international. Conf., April 6-7. 2012, Minsk: [ arch. March 5, 2016 ] / Ans. ed. V.A. Prokasheva. - Minsk: Publ. BSU Center, 2012. - P. 448–450. - UDC .
• Sytinsky, I. A. Gamma-aminobutyric acid in the activity of the nervous system. - L .: Science, 1972.
• Mashkovsky, M.D. Medicines. - 16th ed., Rev., Rev. and add. - M .: New Wave, 2012 .-- S. 121. - 1216 p. - ISBN 978-5-7864-0218-7 .

Documents

• Registry entry FS-001655 (Russian) . State register of medicines . Ministry of Health of the Russian Federation (May 29, 2017).
• Registration certificate LP-005076 (Russian) . State register of medicines . Ministry of Health of the Russian Federation (September 26, 2008).
• Kopatko, S. A. Instructions for the medical use of the drug Phenibut : LP-005076-260918 / Vertex JSC. - Ministry of Health of the Russian Federation, 2018 .-- September 26. - 4 p.