Как правильно пишется фенибут или фенибут

Форма выпуска, упаковка и состав
препарата Фенибут

From Wikipedia, the free encyclopedia

Phenibut

Clinical data
Trade names	Anvifen, Fenibut, Noofen, others[1]
Other names	Aminophenylbutyric acid; Fenibut; Fenigam; Phenigam; Phenybut; Phenygam; Phenylgamma; Phenigama; PHG; PhGABA; β-Phenyl-γ-aminobutyric acid; β-Phenyl-GABA[2]
Routes of administration	Common: By mouth[3] Uncommon: Rectal[3]
Drug class	GABA receptor agonist; Gabapentinoid
ATC code	N06BX22 (WHO)
Legal status
Legal status	AU: S9 (Prohibited substance) US: Unapproved «New Drug» (as defined by 21 U.S. Code § 321). Use in dietary supplements, food, or medicine is unlawful; otherwise uncontrolled. RU: Rx-only
Pharmacokinetic data
Bioavailability	Well-absorbed[4] ≥63% (250 mg)[5]
Metabolism	Liver (minimal)[4][5]
Metabolites	Inactive[4]
Onset of action	Oral: 2–4 hours[3] Rectal: 20–30 minutes[3]
Elimination half-life	5.3 hours (250 mg)[5]
Duration of action	15–24 hours (1–3 g)[3]
Excretion	Urine: 63% (unchanged)[5]
Identifiers
IUPAC name 4-Amino-3-phenylbutanoic acid
CAS Number	1078-21-3  3060-41-1 (hydrochloride)
PubChem CID	14113
ChemSpider	13491
UNII	T2M58D6LA8
KEGG	D10509
ChEMBL	ChEMBL315818
CompTox Dashboard (EPA)	DTXSID70870838
ECHA InfoCard	100.012.800
Chemical and physical data
Formula	C10H13NO2
Molar mass	179.219 g·mol−1
3D model (JSmol)	Interactive image
Melting point	253 °C (487 °F)
SMILES O=C(O)CC(c1ccccc1)CN
InChI InChI=1S/C10H13NO2/c11-7-9(6-10(12)13)8-4-2-1-3-5-8/h1-5,9H,6-7,11H2,(H,12,13)  Key:DAFOCGYVTAOKAJ-UHFFFAOYSA-N
(verify)

Phenibut, sold under the brand names Anvifen, Fenibut, and Noofen among others,^[1] is a central nervous system depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications.^[5] It is usually taken by mouth as a tablet, but may be given intravenously.^[4][5]

Side effects of phenibut include sedation, sleepiness, nausea, irritability, agitation, dizziness, and headache, among others.^[4][6] Overdose of phenibut can produce marked central nervous system depression including unconsciousness.^[4][6] The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue.^[5] Phenibut is thought to act as a GABA_B receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB).^[5] However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing stimulatory effects in addition to the anxiolysis.^[7]

Phenibut was developed in the Soviet Union and was introduced for medical use in the 1960s.^[5] Today, it is marketed for medical use in Russia, Ukraine, Belarus, Kazakhstan, and Latvia.^[5] The medication is not approved for clinical use in the United States and most of Europe, but it is also sold on the Internet as a supplement and purported nootropic.^[3][8] Phenibut has been used recreationally and can produce euphoria as well as addiction, dependence, and withdrawal.^[3] It is a controlled substance in Australia, and it has been suggested that its legal status should be reconsidered in Europe as well.^[3]

Medical uses[edit]

Phenibut is used in Russia, Ukraine, Belarus and Latvia as a pharmaceutical drug to treat anxiety and to improve sleep (e.g., in the treatment of insomnia).^[5][4] It is also used for various other indications, including the treatment of asthenia, depression, alcoholism, alcohol withdrawal syndrome, post-traumatic stress disorder, stuttering, tics, vestibular disorders, Ménière’s disease, dizziness, for the prevention of motion sickness, and for the prevention of anxiety before or after surgical procedures or painful diagnostic tests.^[4][5]

Available forms[edit]

Phenibut is available as a medication in the form of 250 mg or 500 mg tablets for oral administration and as a solution at a concentration of 10 mg/mL for infusion.^[4][6][9] In the US, dietary supplements labeled as containing phenibut have been found to contain zero to greater than 1,100 mg of phenibut per serving.^[8]

Contraindications[edit]

Contraindications of phenibut include:^[4][6]

• Intolerance to phenibut
• Pregnancy and breastfeeding
• Children who are younger than two years of age
• Liver insufficiency or failure
• Ulcerative lesions of the gastrointestinal tract

Phenibut should not be combined with alcohol.^[6]

Side effects[edit]

Phenibut is generally well-tolerated.^[5][6] Possible side effects may include sedation, somnolence, nausea, irritability, agitation, anxiety, dizziness, headache, and allergic reactions such as skin rash and itching.^[4][6] At high doses, motor incoordination, loss of balance, and hangovers may occur.^[3] Due to its central nervous system depressant effects, people taking phenibut should refrain from potentially dangerous activities such as operating heavy machinery.^[4][6] With prolonged use of phenibut, particularly at high doses, the liver and blood should be monitored, due to risk of fatty liver disease and eosinophilia.^[4][6]

Overdose[edit]

In overdose, phenibut can cause severe drowsiness, nausea, vomiting, eosinophilia, lowered blood pressure, renal impairment, and, above 7 grams, fatty liver degeneration.^[4][6] There are no specific antidotes for phenibut overdose.^[6] Lethargy, somnolence, agitation, delirium, tonic–clonic seizures, reduced consciousness or unconsciousness, and unresponsiveness have been reported in recreational users who have overdosed.^[3] Management of phenibut overdose includes activated charcoal, gastric lavage, induction of vomiting, and symptom-based treatment.^[4][6] There have been several cases of lethal overdose.^[10]

Dependency and withdrawal[edit]

Tolerance to phenibut easily develops with repeated use leading to dependency.^[5] Withdrawal symptoms may occur upon discontinuation, and, in recreational users taking high doses, have been reported to include severe rebound anxiety, insomnia, anger, irritability, agitation, visual and auditory hallucinations, and acute psychosis.^[3] Baclofen has successfully been used for treatment of phenibut dependence.^[11]

Interactions[edit]

Phenibut may mutually potentiate and extend the duration of the effects of other central nervous system depressants including anxiolytics, antipsychotics, sedatives, opioids, anticonvulsants, and alcohol.^[4][6]

Pharmacology[edit]

Pharmacodynamics[edit]

GABA and analogues
at biological targets^[12]

Compound	GABAB	GABAA
GABA	0.08	0.12
GHB	>100	>100
GABOB	1.10	1.38
Phenibut	9.6	>100
4-F-phenibut	1.70	>100
Baclofen	0.13	>100
(R)-Baclofen	0.13	>100
(S)-Baclofen	74.0	>100
Values are IC50 (μM) in rat brain.

Phenibut acts as a full agonist of the GABA_B receptor, similarly to baclofen.^[13][14] It has between 30- to 68-fold lower affinity for the GABA_B receptor than baclofen, and, in accordance, is used at far higher doses in comparison.^[13] (R)-Phenibut has more than 100-fold higher affinity for the GABA_B receptor than does (S)-phenibut; hence, (R)-phenibut is the active enantiomer at the GABA_B receptor.^[15]

Phenibut and analogues
at biological targets^[16]

Compound	α2δ	GABAB
Phenibut	ND	177
(R)-Phenibut	23	92
(S)-Phenibut	39	>1,000
Baclofen	156	6
Gabapentin	0.05	>1,000
Values are Ki (μM) in rat brain.

Phenibut also binds to and blocks α₂δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.^[16][17] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (K_i = 23 and 39 μM, respectively).^[16]

Pharmacokinetics[edit]

Little information thus far has been published on the clinical pharmacokinetics of phenibut.^[5] The drug is reported to be well-absorbed.^[4] It distributes widely throughout the body and across the blood–brain barrier.^[4] Approximately 0.1% of an administered dose of phenibut reportedly penetrates into the brain, with this said to occur to a much greater extent in young people and the elderly.^[4] Following a single 250 mg dose in healthy volunteers, its elimination half-life was approximately 5.3 hours and the drug was largely (63%) excreted in the urine unchanged.^[5]

Some limited information has been described on the pharmacokinetics of phenibut in recreational users taking much higher doses (e.g., 1–3 grams) than typical clinical doses.^[3][18] In these individuals, the onset of action of phenibut has been reported to be 2 to 4 hours orally and 20 to 30 minutes rectally, the peak effects are described as occurring 4 to 6 hours following oral ingestion, and the total duration for the oral route has been reported to be 15 to 24 hours (or about 3 to 5 terminal half-lives).^[3]

Chemistry[edit]

Phenibut is a synthetic aromatic amino acid. It is a chiral molecule and thus has two potential configurations, as (R)- and (S)-enantiomers.^[14]

Structure and analogues[edit]

Phenibut is a derivative of the inhibitory neurotransmitter GABA.^[5] Hence, it is a GABA analogue.^[5] Phenibut is specifically the analogue of GABA with a phenyl ring substituted in at the β-position.^[5] As such, its chemical name is β-phenyl-γ-aminobutyric acid, which can be abbreviated as β-phenyl-GABA.^[5] The presence of the phenyl ring allows phenibut to cross the blood–brain barrier significantly, unlike the case of GABA.^[5] Phenibut also contains the trace amine β-phenethylamine in its structure.^[5]

Phenibut is closely related to a variety of other GABA analogues including baclofen (β-(4-chlorophenyl)-GABA), 4-fluorophenibut (β-(4-fluorophenyl)-GABA), tolibut (β-(4-methylphenyl)-GABA), pregabalin ((S)-β-isobutyl-GABA), gabapentin (1-(aminomethyl)cyclohexane acetic acid), and GABOB (β-hydroxy-GABA).^[5][16] It has almost the same chemical structure as baclofen, differing from it only in having a hydrogen atom instead of a chlorine atom at the para position of the phenyl ring.^[5] Phenibut is also close in structure to pregabalin, which has an isobutyl group at the β position instead of phenibut’s phenyl ring.^[16]

A glutamate-derivative analogue of phenibut is glufimet (dimethyl 3-phenylglutamate hydrochloride).^[19]

Synthesis[edit]

A chemical synthesis of phenibut has been published.^[9]

History[edit]

Phenibut was synthesized at the A. I. Herzen Leningrad Pedagogical Institute (USSR) by Professor Vsevolod Perekalin’s team and tested at the Institute of Experimental Medicine, USSR Academy of Medical Sciences.^[5] It was introduced into clinical use in Russia in the 1960s.^[5]

Society and culture[edit]

Other names[edit]

Alternate spellings include fenibut and phenybut.^[2] It is also sometimes referred to as aminophenylbutyric acid.^[1] The word phenibut is a contraction of the chemical name of the drug, β-phenyl-γ-aminobutyric acid.^[5] In early publications, phenibut was referred to as fenigam and phenigama.^[5][20] The drug has not been assigned an INN.^[2][4]

Brand names[edit]

Phenibut is marketed in Russia, Ukraine, Belarus and Latvia under the brand names Anvifen, Fenibut, Bifren and Noofen (Russian: Анвифен, Фенибут, Бифрен and Ноофен, respectively).^[1]

Availability[edit]

Phenibut is approved in Russia, Ukraine, Belarus and Latvia for medical use.^[3] It is not approved or available as a medication in other countries in the European Union, the United States, or Australia.^[3] In countries where phenibut is not a licensed pharmaceutical drug, it is sold online without a prescription as a «nutritional supplement».^[3][8] It is often used as a form of self-medication for social anxiety.^[3]

Recreational use[edit]

Phenibut is used recreationally due to its ability to produce euphoria, anxiolysis, and increased sociability,^[3] as well as remaining undetected in routine urinalysis. Because of its delayed onset of effects, first-time users often mistakenly take an additional dose of phenibut in the belief that the initial dose did not work.^[3] Recreational users usually take the drug orally; there are a few case reports of rectal administration and one report of insufflation, which was described as «very painful» and causing swollen nostrils.^[3]

Legal status[edit]

As of 2021, phenibut is a controlled substance in Australia,^[3] France,^[21] Hungary,^[22] Italy,^[23] and Lithuania.^[24][25] In 2015, it was suggested that the legal status of phenibut in Europe should be reconsidered due to its recreational potential.^[3] In February 2018, the Australian Therapeutic Goods Administration declared it a prohibited (schedule 9) substance, citing health concerns due to withdrawal and overdose.^[26][27]

As of 14 November 2018, Hungary added phenibut and 10 other items to its New Psychoactive Substances ban list.^[28]

As of 26 August 2020, Italy added phenibut to its New Psychoactive Substances ban list.^[23]

As of 18 September 2020, France added phenibut to the controlled psychoactive substances list, prohibiting production, sale, storage and use.^[29]

In the United States, Phenibut is not a Controlled Substance. However, Dietary supplements that contain Phenibut are unlawful to introduce into interstate commerce, because Phenibut is considered a «New Drug» and any food, supplement, cosmetic, or drug that contains Phenibut is therefore adulterated. Alabama scheduled Phenibut and Tianeptine in 2021 first by action of the Alabama Department of Public Health and then followed by the state legislature.^[30]

References[edit]

From Wikipedia, the free encyclopedia

Phenibut

Clinical data
Trade names	Anvifen, Fenibut, Noofen, others[1]
Other names	Aminophenylbutyric acid; Fenibut; Fenigam; Phenigam; Phenybut; Phenygam; Phenylgamma; Phenigama; PHG; PhGABA; β-Phenyl-γ-aminobutyric acid; β-Phenyl-GABA[2]
Routes of administration	Common: By mouth[3] Uncommon: Rectal[3]
Drug class	GABA receptor agonist; Gabapentinoid
ATC code	N06BX22 (WHO)
Legal status
Legal status	AU: S9 (Prohibited substance) US: Unapproved «New Drug» (as defined by 21 U.S. Code § 321). Use in dietary supplements, food, or medicine is unlawful; otherwise uncontrolled. RU: Rx-only
Pharmacokinetic data
Bioavailability	Well-absorbed[4] ≥63% (250 mg)[5]
Metabolism	Liver (minimal)[4][5]
Metabolites	Inactive[4]
Onset of action	Oral: 2–4 hours[3] Rectal: 20–30 minutes[3]
Elimination half-life	5.3 hours (250 mg)[5]
Duration of action	15–24 hours (1–3 g)[3]
Excretion	Urine: 63% (unchanged)[5]
Identifiers
IUPAC name 4-Amino-3-phenylbutanoic acid
CAS Number	1078-21-3  3060-41-1 (hydrochloride)
PubChem CID	14113
ChemSpider	13491
UNII	T2M58D6LA8
KEGG	D10509
ChEMBL	ChEMBL315818
CompTox Dashboard (EPA)	DTXSID70870838
ECHA InfoCard	100.012.800
Chemical and physical data
Formula	C10H13NO2
Molar mass	179.219 g·mol−1
3D model (JSmol)	Interactive image
Melting point	253 °C (487 °F)
SMILES O=C(O)CC(c1ccccc1)CN
InChI InChI=1S/C10H13NO2/c11-7-9(6-10(12)13)8-4-2-1-3-5-8/h1-5,9H,6-7,11H2,(H,12,13)  Key:DAFOCGYVTAOKAJ-UHFFFAOYSA-N
(verify)

Phenibut, sold under the brand names Anvifen, Fenibut, and Noofen among others,^[1] is a central nervous system depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications.^[5] It is usually taken by mouth as a tablet, but may be given intravenously.^[4][5]

Side effects of phenibut include sedation, sleepiness, nausea, irritability, agitation, dizziness, and headache, among others.^[4][6] Overdose of phenibut can produce marked central nervous system depression including unconsciousness.^[4][6] The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue.^[5] Phenibut is thought to act as a GABA_B receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB).^[5] However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing stimulatory effects in addition to the anxiolysis.^[7]

Phenibut was developed in the Soviet Union and was introduced for medical use in the 1960s.^[5] Today, it is marketed for medical use in Russia, Ukraine, Belarus, Kazakhstan, and Latvia.^[5] The medication is not approved for clinical use in the United States and most of Europe, but it is also sold on the Internet as a supplement and purported nootropic.^[3][8] Phenibut has been used recreationally and can produce euphoria as well as addiction, dependence, and withdrawal.^[3] It is a controlled substance in Australia, and it has been suggested that its legal status should be reconsidered in Europe as well.^[3]

Medical uses[edit]

Phenibut is used in Russia, Ukraine, Belarus and Latvia as a pharmaceutical drug to treat anxiety and to improve sleep (e.g., in the treatment of insomnia).^[5][4] It is also used for various other indications, including the treatment of asthenia, depression, alcoholism, alcohol withdrawal syndrome, post-traumatic stress disorder, stuttering, tics, vestibular disorders, Ménière’s disease, dizziness, for the prevention of motion sickness, and for the prevention of anxiety before or after surgical procedures or painful diagnostic tests.^[4][5]

Available forms[edit]

Phenibut is available as a medication in the form of 250 mg or 500 mg tablets for oral administration and as a solution at a concentration of 10 mg/mL for infusion.^[4][6][9] In the US, dietary supplements labeled as containing phenibut have been found to contain zero to greater than 1,100 mg of phenibut per serving.^[8]

Contraindications[edit]

Contraindications of phenibut include:^[4][6]

• Intolerance to phenibut
• Pregnancy and breastfeeding
• Children who are younger than two years of age
• Liver insufficiency or failure
• Ulcerative lesions of the gastrointestinal tract

Phenibut should not be combined with alcohol.^[6]

Side effects[edit]

Phenibut is generally well-tolerated.^[5][6] Possible side effects may include sedation, somnolence, nausea, irritability, agitation, anxiety, dizziness, headache, and allergic reactions such as skin rash and itching.^[4][6] At high doses, motor incoordination, loss of balance, and hangovers may occur.^[3] Due to its central nervous system depressant effects, people taking phenibut should refrain from potentially dangerous activities such as operating heavy machinery.^[4][6] With prolonged use of phenibut, particularly at high doses, the liver and blood should be monitored, due to risk of fatty liver disease and eosinophilia.^[4][6]

Overdose[edit]

In overdose, phenibut can cause severe drowsiness, nausea, vomiting, eosinophilia, lowered blood pressure, renal impairment, and, above 7 grams, fatty liver degeneration.^[4][6] There are no specific antidotes for phenibut overdose.^[6] Lethargy, somnolence, agitation, delirium, tonic–clonic seizures, reduced consciousness or unconsciousness, and unresponsiveness have been reported in recreational users who have overdosed.^[3] Management of phenibut overdose includes activated charcoal, gastric lavage, induction of vomiting, and symptom-based treatment.^[4][6] There have been several cases of lethal overdose.^[10]

Dependency and withdrawal[edit]

Tolerance to phenibut easily develops with repeated use leading to dependency.^[5] Withdrawal symptoms may occur upon discontinuation, and, in recreational users taking high doses, have been reported to include severe rebound anxiety, insomnia, anger, irritability, agitation, visual and auditory hallucinations, and acute psychosis.^[3] Baclofen has successfully been used for treatment of phenibut dependence.^[11]

Interactions[edit]

Phenibut may mutually potentiate and extend the duration of the effects of other central nervous system depressants including anxiolytics, antipsychotics, sedatives, opioids, anticonvulsants, and alcohol.^[4][6]

Pharmacology[edit]

Pharmacodynamics[edit]

GABA and analogues
at biological targets^[12]

Compound	GABAB	GABAA
GABA	0.08	0.12
GHB	>100	>100
GABOB	1.10	1.38
Phenibut	9.6	>100
4-F-phenibut	1.70	>100
Baclofen	0.13	>100
(R)-Baclofen	0.13	>100
(S)-Baclofen	74.0	>100
Values are IC50 (μM) in rat brain.

Phenibut acts as a full agonist of the GABA_B receptor, similarly to baclofen.^[13][14] It has between 30- to 68-fold lower affinity for the GABA_B receptor than baclofen, and, in accordance, is used at far higher doses in comparison.^[13] (R)-Phenibut has more than 100-fold higher affinity for the GABA_B receptor than does (S)-phenibut; hence, (R)-phenibut is the active enantiomer at the GABA_B receptor.^[15]

Phenibut and analogues
at biological targets^[16]

Compound	α2δ	GABAB
Phenibut	ND	177
(R)-Phenibut	23	92
(S)-Phenibut	39	>1,000
Baclofen	156	6
Gabapentin	0.05	>1,000
Values are Ki (μM) in rat brain.

Phenibut also binds to and blocks α₂δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.^[16][17] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (K_i = 23 and 39 μM, respectively).^[16]

Pharmacokinetics[edit]

Little information thus far has been published on the clinical pharmacokinetics of phenibut.^[5] The drug is reported to be well-absorbed.^[4] It distributes widely throughout the body and across the blood–brain barrier.^[4] Approximately 0.1% of an administered dose of phenibut reportedly penetrates into the brain, with this said to occur to a much greater extent in young people and the elderly.^[4] Following a single 250 mg dose in healthy volunteers, its elimination half-life was approximately 5.3 hours and the drug was largely (63%) excreted in the urine unchanged.^[5]

Some limited information has been described on the pharmacokinetics of phenibut in recreational users taking much higher doses (e.g., 1–3 grams) than typical clinical doses.^[3][18] In these individuals, the onset of action of phenibut has been reported to be 2 to 4 hours orally and 20 to 30 minutes rectally, the peak effects are described as occurring 4 to 6 hours following oral ingestion, and the total duration for the oral route has been reported to be 15 to 24 hours (or about 3 to 5 terminal half-lives).^[3]

Chemistry[edit]

Phenibut is a synthetic aromatic amino acid. It is a chiral molecule and thus has two potential configurations, as (R)- and (S)-enantiomers.^[14]

Structure and analogues[edit]

Phenibut is a derivative of the inhibitory neurotransmitter GABA.^[5] Hence, it is a GABA analogue.^[5] Phenibut is specifically the analogue of GABA with a phenyl ring substituted in at the β-position.^[5] As such, its chemical name is β-phenyl-γ-aminobutyric acid, which can be abbreviated as β-phenyl-GABA.^[5] The presence of the phenyl ring allows phenibut to cross the blood–brain barrier significantly, unlike the case of GABA.^[5] Phenibut also contains the trace amine β-phenethylamine in its structure.^[5]

Phenibut is closely related to a variety of other GABA analogues including baclofen (β-(4-chlorophenyl)-GABA), 4-fluorophenibut (β-(4-fluorophenyl)-GABA), tolibut (β-(4-methylphenyl)-GABA), pregabalin ((S)-β-isobutyl-GABA), gabapentin (1-(aminomethyl)cyclohexane acetic acid), and GABOB (β-hydroxy-GABA).^[5][16] It has almost the same chemical structure as baclofen, differing from it only in having a hydrogen atom instead of a chlorine atom at the para position of the phenyl ring.^[5] Phenibut is also close in structure to pregabalin, which has an isobutyl group at the β position instead of phenibut’s phenyl ring.^[16]

A glutamate-derivative analogue of phenibut is glufimet (dimethyl 3-phenylglutamate hydrochloride).^[19]

Synthesis[edit]

A chemical synthesis of phenibut has been published.^[9]

History[edit]

Phenibut was synthesized at the A. I. Herzen Leningrad Pedagogical Institute (USSR) by Professor Vsevolod Perekalin’s team and tested at the Institute of Experimental Medicine, USSR Academy of Medical Sciences.^[5] It was introduced into clinical use in Russia in the 1960s.^[5]

Society and culture[edit]

Other names[edit]

Alternate spellings include fenibut and phenybut.^[2] It is also sometimes referred to as aminophenylbutyric acid.^[1] The word phenibut is a contraction of the chemical name of the drug, β-phenyl-γ-aminobutyric acid.^[5] In early publications, phenibut was referred to as fenigam and phenigama.^[5][20] The drug has not been assigned an INN.^[2][4]

Brand names[edit]

Phenibut is marketed in Russia, Ukraine, Belarus and Latvia under the brand names Anvifen, Fenibut, Bifren and Noofen (Russian: Анвифен, Фенибут, Бифрен and Ноофен, respectively).^[1]

Availability[edit]

Phenibut is approved in Russia, Ukraine, Belarus and Latvia for medical use.^[3] It is not approved or available as a medication in other countries in the European Union, the United States, or Australia.^[3] In countries where phenibut is not a licensed pharmaceutical drug, it is sold online without a prescription as a «nutritional supplement».^[3][8] It is often used as a form of self-medication for social anxiety.^[3]

Recreational use[edit]

Phenibut is used recreationally due to its ability to produce euphoria, anxiolysis, and increased sociability,^[3] as well as remaining undetected in routine urinalysis. Because of its delayed onset of effects, first-time users often mistakenly take an additional dose of phenibut in the belief that the initial dose did not work.^[3] Recreational users usually take the drug orally; there are a few case reports of rectal administration and one report of insufflation, which was described as «very painful» and causing swollen nostrils.^[3]

Legal status[edit]

As of 2021, phenibut is a controlled substance in Australia,^[3] France,^[21] Hungary,^[22] Italy,^[23] and Lithuania.^[24][25] In 2015, it was suggested that the legal status of phenibut in Europe should be reconsidered due to its recreational potential.^[3] In February 2018, the Australian Therapeutic Goods Administration declared it a prohibited (schedule 9) substance, citing health concerns due to withdrawal and overdose.^[26][27]

As of 14 November 2018, Hungary added phenibut and 10 other items to its New Psychoactive Substances ban list.^[28]

As of 26 August 2020, Italy added phenibut to its New Psychoactive Substances ban list.^[23]

As of 18 September 2020, France added phenibut to the controlled psychoactive substances list, prohibiting production, sale, storage and use.^[29]

In the United States, Phenibut is not a Controlled Substance. However, Dietary supplements that contain Phenibut are unlawful to introduce into interstate commerce, because Phenibut is considered a «New Drug» and any food, supplement, cosmetic, or drug that contains Phenibut is therefore adulterated. Alabama scheduled Phenibut and Tianeptine in 2021 first by action of the Alabama Department of Public Health and then followed by the state legislature.^[30]

References[edit]

МНН: Аминофенилмасляной кислоты гидрохлорид (фенибут)

Производитель: Московский эндокринный завод ФГУП

Анатомо-терапевтическо-химическая классификация: Фенибут

Номер регистрации в РК:
РК-ЛС-5№023457

Информация о регистрации в РК:
03.01.2018 — 03.01.2023

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Торговое название

Фенибут

Международное непатентованное название

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Лекарственная форма

Таблетки, 250 мг

Состав

1 таблетка содержит:

активное
вещество
— аминофенилмасляной
кислоты гидрохлорид

(фенибут)
— 250 мг,

вспомогательные
вещества: лактозы
могогидрат, крахмал картофельный,
повидон
(поливинилпирролидон низкомолекулярный медицинский), кальция стеарат.

Описание

Таблетки белого или
белого со слегка желтоватым оттенком цвета плоскоцилиндрической формы
с фаской и риской.

Фармакотерапевтическая группа

Психоаналептики.
Психостимуляторы и ноотропы. Психостимуляторы и ноотропы другие.
Фенибут

Код
АТХ N06ВХ22

Фармакологические свойства

Фармакокинетика

Абсорбция высокая,
препарат хорошо проникает во все ткани организма и через
гематоэнцефалический барьер (в ткани мозга проникает около 0,1 %
введенной дозы препарата, причем у лиц молодого и пожилого возраста в
значительно большей степени). Равномерно распределяется в печени и
почках. Метаболизируется в печени – 80-95 %, метаболиты
фармакологически неактивны. Не кумулирует. Через 3 ч начинает
выводиться почками, при этом концентрация в ткани мозга не снижается,
и его обнаруживают в мозге еще в течение 6 ч. Около 5 % выводится
почками в неизмененном виде, частично выводится с желчью.

Фармакодинамика

Ноотропное средство,
облегчает ГАМК (γ-аминомасляная кислота) — опосредованную
передачу нервных импульсов в центральной нервной системе (прямое
воздействие на ГАМК-ергические рецепторы). Транквилизирующее действие
сочетается с активирующим эффектом. Также обладает антиагрегантным,
антиоксидантным и некоторым противосудорожным действием.

Улучшает
функциональное состояние мозга за счет нормализации его метаболизма и
влияния на мозговой кровоток (увеличивает объемную и линейную
скорость, уменьшает сопротивление сосудов, улучшает микроциркуляцию).

Не
влияет на холино- и адренорецепторы. Удлиняет латентный период и
укорачивает продолжительность и выраженность нистагма. Уменьшает
вазовегетативные симптомы (в т.ч. головную боль, ощущение тяжести в
голове, нарушения сна, раздражительность, эмоциональную лабильность).
При курсовом приеме повышает физическую и умственную
работоспособность (внимание, память, скорость и точность
сенсорно-моторных реакций).

Уменьшает проявления
астении (улучшает самочувствие, повышает интерес и инициативу
(мотивация деятельности)) без седации или возбуждения.

Способствует
снижению чувства тревоги, напряженности и беспокойства, нормализует
сон.

У людей пожилого
возраста не вызывает угнетение центральной нервной системы,
мышечно-расслабляющее последействие чаще всего отсутствует.

Уменьшает угнетающее
влияние этанола на центральную нервную систему.

Показания к применению

— астенические и
тревожно-невротические состояния

— заикание, тики и
энурез у детей

— бессонница и
ночная тревога у людей пожилого возраста

— болезнь Меньера,
головокружения, связанные с дисфункциями вестибулярного анализатора
различного генеза; профилактика укачивания при кинетозах

— в составе
комплексной терапии при лечении алкогольного абстинентного синдрома.

Способ применения и дозы

Внутрь после еды 2-3
недельными курсами.

Взрослым
и детям
с 14 лет назначают по 250-500 мг 3 раза в день (максимальная суточная
доза 1500 мг).

Детям
с 8 до 14 лет
— по 250 мг 3 раза в день.

Однократная
максимальная доза у взрослых и детей с 14 лет составляет 750 мг, у
лиц старше 60 лет — 500 мг, с 8 до 14 лет — 250 мг.

Купирование
алкогольного абстинентного синдрома
в первые дни лечения: днем по 250-500 мг 3 раза в день и на ночь 750
мг, с постепенным понижением суточной дозы до обычной для взрослых.

Профилактика
укачивания:
250-500 мг однократно за 1 час до предполагаемого начала качки или
при появлении первых легких симптомов морской болезни.
Противоукачивающее действие фенибута усиливается при увеличении дозы
препарата. При наступлении выраженных проявлений морской болезни
(рвота и т.д.) назначение фенибута внутрь малоэффективно даже в дозах
750-1000 мг.

Отогенный
лабиринтит и болезнь Меньера
в период обострения: 750 мг 3-4 раза в сутки в течение 5-7 дней, при
снижении выраженности вестибулярных расстройств – по 250-500 мг
3 раза в сутки в течение 5-7 дней и затем – по 250 мг 1 раз в
сутки в течение 5 дней. При легком течении заболеваний – по 250
мг 2 раза в сутки в течение 5-7 дней, с последующим снижением дозы до
250 мг 1 раз в сутки в течение 7-10 дней.

Астенические
состояния:
внутрь, по 40-80 мг/сут, в отдельных случаях – до 200-300
мг/сут в течение 1-1,5 мес.

Депрессивные
состояния
позднего возраста – 2-3 раза в день по 40-200 мг/сут в течение
1,5-3 мес.

Побочные действия

— усиление
раздражительности

— возбуждение

— тревожность

— головокружение

— головная боль

— сонливость

— тошнота (при
первых приемах)

—
аллергические реакции (кожная сыпь, зуд)

Противопоказания

—
гиперчувствительность к компонентам препарата

— пациенты с редкими
наследственными заболеваниями, такими как непереносимость лактозы,
дефицит лактазы или глюкозо-галактозной мальабсорбцией не должны
принимать препарат

— детский возраст до
8 лет

Лекарственные взаимодействия

Удлиняет и усиливает
действие снотворных, наркотических анальгетиков, нейролептиков,
противопаркинсонических и противоэпилептических средств.

Особые указания

Применять
с осторожностью при
эрозивно-язвенных поражениях желудочно-кишечного тракта, печеночной
недостаточности.

При длительном
применении необходимо контролировать показатели функции печени и
периферической крови. Необходимо воздерживаться от потенциально
опасных видов деятельности, требующих повышенного внимания.

Фенибут
следует отменять постепенно. Схему для отмены препарата определяет
лечащий врач в зависимости от состояния пациента и рекомендованных на
курс лечения дозировок. Как правило, отмена Фенибута производится с
постепенным снижением дозировки в течение 1 — 2 недель.

Применение в
педиатрии

Детский возраст с 8
лет.

Применение во
время беременности и период лактации

С осторожностью.
Возможно, если польза для матери превышает потенциальный риск для
ребенка (необходимо проконсультироваться с врачом).

Особенности влияния лекарственного средства на
способность управлять транспортным средством или потенциально
опасными механизмами

Не
выявлены

Передозировка

Симптомы:
выраженная сонливость, тошнота, рвота, жировая дистрофия печени
(прием более 7000 мг), эозинофилия, снижение артериального давления,
нарушение функции почек.

Лечение:
промывание желудка, прием активированного угля и проведение
симптоматической терапии.

Форма выпуска и упаковка

Таблетки
по 250 мг.

По
10 таблеток
в
контурную ячейковую упаковку.

2 контурные
ячейковые упаковки вместе с инструкцией по медицинскому применению на
государственном и русском языках помещают в картонную пачку.

Условия хранения

В защищенном от
света месте при температуре не выше 25 °С.

Хранить в
недоступном для детей месте.

Срок хранения

3 года

Не применять по
истечении срока годности.

Условия отпуска из аптек

По рецепту

Производитель

Федеральное
государственное унитарное предприятие «Московский эндокринный
завод»

Россия, г. Москва,
109052, ул. Новохохловская, д. 25,

тел./факс (495)
678-00-50 / 911-42-10.

e—mail:
mez@endopharm.ru

Адрес
производства:
Россия,
109052,
г. Москва, ул. Новохохловская, д. 25, стр. 1, стр. 2.

Владелец регистрационного удостоверения

Федеральное
государственное унитарное предприятие «Московский эндокринный
завод»

Наименование,
адрес и контактные данные организации
на территории Республики Казахстан, принимающей претензии
(предложения) по качеству лекарственных средств от потребителей и
ответственной
за пострегистрационное наблюдение за безопасностью лекарственного
средства:

ИП
«Нестеренко А.Е.», Республика Казахстан, 050000, г.
Алматы, ул. Муканова, д.104,

тел.: +7 7273271602,
+7 7077862629, +7 7058887587, факс +7 72796659,

e—mail:
pharm_vigilance@mail.ru.,
ip_n_nesterenko@list.ru.

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