Introduction to Phenibut
Phenibut, a GABA analogue developed in St. Petersburg, Russia during the 1960s, holds structural similarity to the neurotransmitter gamma-aminobutyric acid (GABA) yet boasts unique effects. Unlike GABA, Phenibut crosses the blood-brain barrier, binding to GABA receptors and potentially elevating dopamine levels, which may underpin its mood-enhancing properties. Besides its known anxiolytic and cognitive-enhancing effects, Phenibut shows promise in alleviating social anxiety disorder, a condition often unresponsive to typical GABA agonists.
Historical Background: Development in Russia in the 1960s
Originating in Russia during the 1960s, Phenibut was designed as an aid for cosmonauts to combat stress and anxiety 1 without hampering cognitive function. Over time, its use expanded, finding a place in the treatment of various neurological disorders including PTSD, anxiety, depression, and insomnia.
Mechanism of Action: GABA analogue that crosses the blood-brain barrier
Phenibut’s mechanism of action is primarily through its structural similarity to GABA, allowing it to bind to GABA receptors in the brain. Unlike GABA, Phenibut can cross the blood-brain barrier due to the addition of a phenyl ring in its structure 2, enhancing its effects. Moreover, it has the potential to increase dopamine levels, which could contribute to its mood-enhancing and anxiolytic effects.
Is Phenibut Legal in AUS?
Legal Status: Unapproved for medical use in the US, status in Australia
In the United States, Phenibut is not approved for medical use, although it is available as a supplement. The legal status of Phenibut in Australia is different, as it is a controlled substance, making its purchase, possession, or use without a prescription illegal.
TGA (Therapeutic Goods Administration) Stance on Phenibut
The Therapeutic Goods Administration (TGA) in Australia has categorized Phenibut as a Schedule 9 substance, indicating it has a high potential for abuse and no recognized medical use.
Where to Buy Phenibut
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Online Retailers: Availability in powder or capsule form
Phenibut can be purchased online in various forms including capsules and powder. It’s often marketed as a nootropic or sleep aid, available from retailers specializing in supplements. However, legality and availability may vary by region, requiring buyers to verify local regulations.
Phenibut Forms
Capsules
- Dosage: Capsules offer a convenient way to measure and administer Phenibut, with common dosages ranging from 250 to 500 mg.
- Convenience: Pre-measured doses in capsule form provide ease of use and portability.
Powder
- Dosage: Powder form allows for adjustable dosages, though precision scales are recommended to ensure accurate measurement.
- Preparation: Powdered Phenibut requires careful measurement and may be mixed with water or another beverage for consumption.
Phenibut and Alcohol
Interaction between Phenibut and alcohol
Combining Phenibut with alcohol can lead to enhanced sedation, impaired cognition, and potentially dangerous respiratory depression 3, especially for individuals new to Phenibut or with low alcohol tolerance.
Risks and considerations
The effects of Phenibut can be delayed; it’s advised to avoid alcohol for at least 12 hours post-ingestion 4. Prior consultation with a healthcare provider is crucial, especially for those pregnant, breastfeeding, or with underlying health conditions.
Phenibut vs GABA
Comparison of effects
While both Phenibut and GABA work to reduce anxiety and promote relaxation, Phenibut crosses the blood-brain barrier due to its structural modifications, potentially offering enhanced effects.
Differences in mechanism of action
Both substances interact with GABA receptors, yet Phenibut’s ability to also affect dopamine levels presents a unique mechanism of action, possibly contributing to its mood-enhancing effects.
Phenibut Benefits
For Sleep
Phenibut can be effective in improving sleep quality 5 for some people, although it’s not a regulated sleep aid and has not been approved by the FDA for this purpose.
Antidepressant
Phenibut may help to alleviate symptoms of depression and anxiety in some people, but it’s not a regulated antidepressant and has not been approved by the FDA for this purpose.
Cognitive Enhancement
There is some evidence that Phenibut can improve cognitive function in some people 6, but more research is needed to confirm these findings.
Exercise Recovery
There is limited evidence on the effects of Phenibut on exercise recovery. More research is needed to determine whether Phenibut is effective for this purpose.
Human Growth Hormone Boost
Phenibut has been shown to increase human growth hormone levels 7 in some studies, but more research is needed to determine the long-term effects of this.
Phenibut Side Effects
Causing Depression
- Risks and Studies: Phenibut may initially alleviate anxiety and mood issues, but prolonged use could exacerbate or cause depressive symptoms 8.
Liver: Increased risk of fatty liver disease with misuse
- Prolonged misuse of Phenibut can lead to liver issues 9 including fatty liver disease.
Additional Side Effects
- General side effects include nausea, anxiety, headaches, dizziness, and overall sedation.
- Misuse or high dosage can lead to loss of balance, impaired coordination, hangover-like symptoms, physical dependence, and addiction.
- Overdose signs include nausea, vomiting, low blood pressure, low body temperature, lethargy, extreme drowsiness, delirium, and loss of consciousness.
Phenibut Dangers
Addiction and Withdrawal: Physical dependence, addiction, and withdrawal symptoms
- Phenibut carries a risk of physical dependence and addiction, especially with prolonged use. Withdrawal symptoms can be severe, necessitating medical supervision for safe discontinuation.
Overdose Risks: Signs and symptoms of overdose, risks when combined with other depressants like alcohol, opioids, or sedatives
- Overdose risks are heightened when Phenibut is combined with other depressants, leading to potentially life-threatening scenarios.
Phenibut Dose
Recommended Dosages: Starting low at 200 – 300 mg per day, avoiding alcohol or benzodiazepines 10
- A low initial dose is advised to assess individual tolerance, avoiding combinations with alcohol or benzodiazepines due to interaction risks.
Factors affecting dosage
- Body Weight: Higher body weight may necessitate a higher dose.
- Tolerance: Past use or concurrent depressant use may increase tolerance, requiring a higher dose.
- Individual Response: Sensitivity varies, some may require a lower dose for desired effects.
Safety Tips
- Limit intake to once daily, not exceeding 3-5 consecutive days.
- Avoid use if pregnant, breastfeeding, or having underlying health conditions.
- Refrain from Phenibut if on other medications, including over-the-counter ones.
- Seek medical attention if adverse effects occur.
How Long Does Phenibut Last?
Duration of effects
Phenibut’s effects can last several hours, peaking at 2-4 hours post-ingestion 11.
Half-life
The half-life, the time taken for half of the drug to be eliminated from the body, ranges from 5.3 to 6.6 hours for Phenibut. For instance, if Phenibut has a half-life of 5 hours, half is eliminated after 5 hours, the remaining half over the subsequent 5 hours, and so on, taking several days for complete elimination.
Factors affecting Phenibut’s effects
- Dosage
- Frequency of use
- Individual tolerance
- Metabolism rate
- Weight
- Age
- Underlying health conditions
- Other medications being taken
Conclusion
Phenibut, with its potential for anxiety relief, sleep improvement, and cognitive enhancement, presents a captivating scope of benefits. However, the risks associated with its misuse, such as addiction, liver damage, and severe withdrawal symptoms, underscore the necessity for caution. The legal constraints and unregulated status of Phenibut further complicate its use. As such, a thorough comprehension of Phenibut’s effects, dosages, and interactions is crucial for anyone considering its usage. Moreover, consulting with healthcare professionals is highly advised to navigate the risks and benefits effectively, ensuring a safe and informed approach towards Phenibut use.
References
- Morales, M. (2021, November 9). Russian Drug Phenibut is More Than Just Stress, Anxiety Treatment in Space for Cosmonauts; 1950s Medicine Helps Ease Other Symptoms Too. Science Times. Retrieved from https://www.sciencetimes.com/articles/34410/20211109/russian-drug-phenibut-more-stress-anxiety-treatment-space-cosmonauts-1950s.htm[↩]
- Lapin, I. (2001). Phenibut (beta-phenyl-GABA): A tranquilizer and nootropic drug. CNS Drug Reviews, 7(4), 471-481. PubMed[↩]
- Geoffrion, L., M.D., Generes, W. M. (Ed.), & Kelley, R., NREMT (Rev.). (2023, June 2). Phenibut Addiction, Side Effects, Withdrawal, and Treatment. American Addiction Centers. https://americanaddictioncenters.org/phenibut[↩]
- Zinnia Health. (n.d.). Mixing Phenibut and Alcohol: Side Effects and Dangers. Retrieved from https://zinniahealth.com/substance-use/phenibut/with-alcohol[↩]
- evidencelive.org. (n.d.). Phenibut. Retrieved from https://evidencelive.org/phenibut/[↩]
- Napoletano, F., Schifano, F., Corkery, J. M., Guirguis, A., Arillotta, D., Zangani, C., & Vento, A. (2020). The Psychonauts’ World of Cognitive Enhancers. Frontiers in Psychiatry, 11. https://doi.org/10.3389/fpsyt.2020.546796[↩]
- Iocco, A. (2021, March 22). Phenibut Risk of Addiction. Resurgence Behavioral Health. Retrieved from https://resurgencebehavioralhealth.com/blog/phenibut-risk-of-addiction/[↩]
- Zheng, K. H., Khan, A., & Espiridion, E. D. (2019). Phenibut Addiction in a Patient with Substance Use Disorder. Cureus, 11(7), e5230. https://doi.org/10.7759/cureus.5230[↩]
- Zinnia Health Editorial Staff. (2023, August 23). What are the side effects of phenibut abuse? Zinnia Health. https://zinniahealth.com/substance-use/phenibut/side-effects[↩]
- Tomen, D. (2023, June 14). Phenibut. Nootropics Expert. https://nootropicsexpert.com/phenibut/[↩]
- Fraighten, C. (2023, May 17). How Long Does Phenibut Last?: Duration, Prolonging Effects, and Nootropic Combinations. Epimodels. Retrieved from https://www.epimodels.org/nootropics/how-long-does-phenibut-last/[↩]
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