Phenibut

Phenibut, sold under the brand name Anvifen among others, is a central nervous system (CNS) depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications. It is usually taken orally (swallowed by mouth), but may be given intravenously. Side effects of phenibut can include sedation, sleepiness, nausea, irritability, agitation, dizziness, euphoria, and sometimes headache, among others. Overdose of phenibut can produce marked central nervous system depression including unconsciousness. The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue. Phenibut is thought to act as a GABA B receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB). However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing stimulatory effects in addition to the anxiolysis. Phenibut was developed in the Soviet Union and was introduced for medical use in the 1960s. Today, it is marketed for medical use in Russia, Ukraine, Belarus, Kazakhstan, and Latvia. The medication is not approved for clinical use in the United States and most of Europe, but it is sold on the Internet as a supplement and purported nootropic. Phenibut has been used recreationally and can produce euphoria as well as addiction, dependence, and withdrawal.…

Phenibut, sold under the brand name Anvifen among others, is a central nervous system (CNS) depressant with anxiolytic effects, and is used to treat anxiety, insomnia, and for a variety of other indications. It is usually taken orally (swallowed by mouth), but may be given intravenously. Side effects of phenibut can include sedation, sleepiness, nausea, irritability, agitation, dizziness, euphoria, and sometimes headache, among others. Overdose of phenibut can produce marked central nervous system depression including unconsciousness. The medication is structurally related to the neurotransmitter γ-aminobutyric acid (GABA), and hence is a GABA analogue. Phenibut is thought to act as a GABA B receptor agonist, similarly to baclofen and γ-hydroxybutyrate (GHB). However, at low concentrations, phenibut mildly increases the concentration of dopamine in the brain, providing stimulatory effects in addition to the anxiolysis. Phenibut was developed in the Soviet Union and was introduced for medical use in the 1960s. Today, it is marketed for medical use in Russia, Ukraine, Belarus, Kazakhstan, and Latvia. The medication is not approved for clinical use in the United States and most of Europe, but it is sold on the Internet as a supplement and purported nootropic. Phenibut has been used recreationally and can produce euphoria as well as addiction, dependence, and withdrawal. It is a controlled substance in Australia, and it has been suggested that its legal status should be reconsidered in Europe as well. In Germany, phenibut is not approved as a drug and, as a food supplement, is controlled under the German New Psychoactive Substances Act. In a 2023 assessment, the U.S. Food and Drug Administration (FDA) determined that phenibut does not meet the definition of a dietary ingredient, thereby making phenibut supplement products misbranded and illegal for marketing. FDA warning letters had been issued to supplement manufacturers marketing phenibut products as adulterated. Phenibut also binds to and blocks α 2 δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid. Both (R)-phenibut and (S)-phenibut display this action with similar affinity (K i = 23 and 39 μM, respectively). It is often claimed on websites about nootropics and elsewhere on the internet that phenibut increases dopamine. Three papers published in Russian by Soviet scientists in 1979¹, 1986, and 1990 report that phenibut increases dopamine in the striatum of rats and in the mouse brain. The mechanism underlying this putative effect is unclear. Structurally, phenibut can also be considered a derivative of phenethylamine, and some research suggests that phenibut antagonizes the action of phenethylamine.

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