Acute phenibut withdrawal: A comprehensive literature review and illustrative case report

Abstract

Phenibut is a glutamic acid derivative with activity on the γ-aminobutyric acid (GABA)B, A, and B-phenethylamine receptors. It is prescribed in former Communist Bloc countries for anxiolysis and related psychiatric disorders. It can be easily obtained in Western countries and is thought to have abuse potential. Abrupt discontinuation has been reported to precipitate an abstinence syndrome. A review of the literature identified 22 reported cases, many of which were notable for severe psychomotor agitation and requirements for aggressive pharmacologic treatment. Neurologic and autonomic signs and symptoms may mimic serotonin or neuroleptic malignant syndrome. Patients were typically younger and had coexisting substance abuse disorders to other drugs. Also presented is a case of a 23-year-old male with an acute phenibut abstinence syndrome. This patient exhibited severe psychomotor agitation requiring physical restraints, dexmedetomidine, lorazepam, haloperidol, diphenhydramine, cyproheptadine, melatonin, olanzapine, and baclofen for symptom control.

Phenibut Addiction in a Patient with Substance Use Disorder

“…GABA receptors are inhibitory receptors that decrease neuronal excitability and probability of firing. Phenibut is also structurally related to baclofen, another GABA B receptor agonist, which has been used to treat alcohol dependence as well as several cases of phenibut dependence [4, 11-13, 17, 18]. The opposing physiological outcomes of these two GABA B agonists suggest either differences in pharmacological properties of the drug on the receptor or different off-target effects between the two compounds.…”

“…Alcohol use results in impaired central nervous system activity including poor motor coordination and behavioral changes due to altered synthesis, release, and signaling of neurotransmitters including serotonin, glutamate, GABA, and endocannabinoids as well as their corresponding receptors. Furthermore, the symptoms of phenibut withdrawal are similar to those of alcohol withdrawal, which include anxiety, agitation, depression, cognitive deficits, insomnia, hallucinations, and tremors [4, 10-13]. It is unknown whether the use and withdrawal symptoms associated with long-term phenibut use enhance those symptoms associated with concurrent alcohol use.…”

Safety and Tolerability of the Anxiolytic and Nootropic Drug Phenibut: A Systematic Review of Clinical Trials and Case Reports

“…Phenibut (3-phenyl-4-aminobutyric acid) was developed in St. Petersburg, Russia, in 1963 as an anxiolytic and cognitive enhancer for cosmonauts. In clinical practice, phenibut is used as a prescription drug in Eastern European countries, including Latvia, Estonia, Belarus, Kazakhstan, Russia, and Ukraine [1,2]. Phenibut is a nootropic drug that has been used for the treatment of anxiety, tics, stuttering, insomnia, dizziness, and alcohol withdrawal for more than half a century [1].…”

Influence of Pharmacological Correction on the Quality of Life of Children With Functional Dyspepsia

“…The issue of the advisability of long-term administration of drugs to such patients that affect the function of the central nervous system is being constantly debated in the scientific literature [4,7]. Therapy with tricyclic antidepressants (amitriptyline, imipramine) has proven its effectiveness in complex cases, but its common use is limited by a significant number of side effects [4,9]. The advisability of psychotherapeutic correction in case of functional dyspepsia, like other forms of FGID, is considered, which requires active training of relevant specialists in Ukraine and the development of the psychotherapeutic care system in general [10,11].…”

“…Thus, a combination of soothing and mild psychostimulating effects is achieved. In its pure form, exogenously introduced GABA does not penetrate the blood-brain barrier (BBB) [18], which intensified the need for the creation of several complex compounds [9,12]. In our opinion, γ-amino-β-phenylbutyric acid hydrochloride (Phenibut) and calcium hopantenate are of great interest to the FD treatment [11].…”