Phenibut

Phenibut is a compound that has gained increasing attention in recent years, particularly due to its potential anxiolytic and cognition-enhancing properties. In a world where stress and anxiety are ubiquitous, many people are looking for alternative ways to boost their mental health.

What is Phenibut?

Phenibut is a GABA agonist that acts at the GABA-B receptors and possibly also binds to the GABA-A receptors at higher doses. This distinguishes it from benzodiazepines, which work on a different mechanism of action. It is a chiral molecule present as a racemate, with the (R)-enantiomer being pharmacologically active.

Properties and effects:

• Analyte name Phenibut: Hydrochloride CAS number Molecular formula C10 H13
• Neuro- and cardioprotection: Animal studies indicate that phenibut improves interhemispheric transmission and has increased BDNF activity.
• Tolerance and dependence: Regular use can lead to the development of tolerance and withdrawal symptoms, similar to benzodiazepines.

Phenibut is often used for cognitive performance enhancement and as an anti-stress agent. However, it carries risks such as tolerance development and the possibility of dependence if taken regularly.

Mechanism of action of Phenibut

Phenibut is a chemical compound that acts as an agonist at the GABA B receptor. This distinguishes it from benzodiazepines, which act as allosteric ligands at the GABA A receptor. At higher doses, however, phenibut can also bind to GABA A receptors, which indicates its versatility.

A significant aspect of Phenibut's mechanism of action is its ability to cross the blood-brain barrier and show effects for up to 24 hours after ingestion. Animal studies also indicate a dopaminergic mechanism of action, which means that Phenibut may also influence dopamine release in the brain.

Phenibut citrate offers additional benefits by reducing the harmful effects of alcohol by increasing oxidative phosphorylation. These versatile biochemical interactions make phenibut an interesting subject of investigation for cognitive performance enhancement and stress management.

Summary of the mechanisms of action of Phenibut:

• Agonist at the GABA B receptor
• Possible binding to GABA A receptors at higher doses
• Dopaminergic effects
• Reduction of the harmful effects of alcohol through increased oxidative phosphorylation

Clinical applications of Phenibut

Phenibut, a compound developed in Russia, has proven to be effective in various clinical applications. Originally developed by the Academy of Medical Sciences in Russia, it is primarily used to treat anxiety and agitation. Phenibut's versatile action makes it an important drug in neuropharmacology.

Use in medicine

1. Anxiety and restlessness: In Russia and other Eastern European countries, Phenibut is often used to help patients with anxiety and restlessness. Its calming effect calms the nervous system and promotes a sense of calm and serenity.
2. Sleep disorders in the elderly: Phenibut is approved to support elderly patients who suffer from sleep disorders. It helps to regulate the natural sleep cycle without too much of the sedation that can be observed with many other sleep aids.
3. Treatment of stuttering and tic disorders in children: Phenomenon has been shown to be useful in pediatrics, particularly in the treatment of stuttering and tic disorders. It is used because of its ability to balance neurological stimuli and have a calming effect.
4. Meniere's disease and vestibular vertigo: Phenibut is a recognized treatment for vertigo due to vestibular disorders, including Meniere's disease. It helps to reduce symptoms such as dizziness and discomfort.
5. Motion sickness: The medication is also used prophylactically to prevent motion sickness. Patients report a significant reduction in the frequency and intensity of symptoms such as nausea and dizziness during travel.
6. Support during alcohol withdrawal: Another use of Phenibut is to support withdrawal symptoms in people undergoing alcohol withdrawal. It can alleviate symptoms such as anxiety and restlessness associated with withdrawal.

Use in sports & bodybuilding

Phenibut also has a wide range of applications in sports and bodybuilding, where it is used on the internet as a euphoric and performance-enhancing agent. Under synonyms such as "the smart pill", many are convinced of the benefits for athletes.

Possible side effects of Phenibut

Phenibut, a chemical compound commonly used for cognitive enhancement, poses health risks with long-term use. Regular use can lead to the development of tolerance and physical dependence, which calls into question its long-term safety.

Withdrawal symptoms are a possibility when discontinuing Phenibut. These can be comparable to those of benzodiazepines and include:

• Insomnia
• Hallucinations
• States of anxiety

Case reports document the potential of Phenibut to cause physical dependence. This can lead to neurological symptoms such as delirium. Other neurological effects may include changes in mental status ranging from low reactivity to aggressive symptoms. There is no evidence of e.g. allergic reactions.

List of possible symptoms of addiction:

1. Insomnia
2. Hallucinations
3. States of anxiety
4. Delirium
5. Changes in mental status

In summary, Phenibut poses a risk of side effects, even at lower doses. Close monitoring and a clear plan for handling Phenibut are crucial to minimize health risks.

Abuse potential of Phenibut

Dependence and toxicity

Phenibut is a chemical compound which, like other GABA agonists, can lead to dependence if taken chronically. Abrupt discontinuation of Phenibut can cause withdrawal symptoms that parallel those of benzodiazepine abuse. These symptoms may include insomnia, anxiety and hallucinations.

Although the acute toxicity of phenibut is classified as low, with a median lethal dose (LD50) of 900 mg/kg in mice and 700 mg/kg in rats, signs of intoxication may occur. These often manifest themselves in vigilance disorders and range from somnolence to psychomotor agitation, including panic and hallucinations.

Phenibut poisoning symptoms may include:

1. Somnolence
2. Psychomotor arousal
3. Panic
4. Hallucinations
5. Hepatotoxic potential

In combination with alcohol or opioids, the risk of respiratory depression increases, which increases the risk of overdose. Furthermore, long-term use of Phenibut can not only lead to the development of tolerance, but can also have a hepatotoxic potential. It is therefore important to check liver values regularly in order to detect any damage at an early stage.

Responsible use of Phenibut and strict adherence to dosage guidelines are crucial to minimize the potential for abuse and reduce health risks. Dosages of a maximum of 1 gram to 1.5 grams per intake should not be exceeded.

Comparison with similar substances

Phenibut is a compound that acts as an agonist at the GABA B receptor, in contrast to benzodiazepines, which act at the GABA A receptor. This leads to a different mode of action. At higher doses, however, phenibut can also influence GABA A receptors, which further differentiates its effect.

Similar to benzodiazepines, regular use of Phenibut carries the risk of developing tolerance and dependence. Withdrawal from Phenibut can lead to symptoms such as insomnia, hallucinations and anxiety - comparable to withdrawal from benzodiazepines.

In the treatment of withdrawal symptoms, Phenibut can be considered in conjunction with substances such as baclofen, benzodiazepines, gabapentin or pregabalin.

Comparison:

Phenibut is distinguished by its specific receptor binding and the associated psychotropic effects.