A New Chapter in Anti-anxiety

To phenibut, or not to phenibut.

We live in a world that thrives on productivity. The rise of biohacking, the widespread use of Adderall, and the ever-present "grindset" mentality all highlight how deeply society values efficiency and self-improvement. But as people push themselves harder, the pressure to perform has led to a sharp rise in anxiety and stress.

With this cultural shift, combined with ongoing global conflicts and the lasting effects of the pandemic, prescriptions for anti-anxiety medications have skyrocketed. Even more concerning is the increasing number of overdose deaths linked to benzodiazepines, which have more than quadrupled between 1999 and 2010 (1). In this environment, people are searching for safer, more accessible alternatives—ones that bypass barriers like high costs, insurance limitations, and the risk of overdose.

The Rise of Phenibut

Recently, driven by the demand for anxiolytics, beta-phenyl-gamma-aminobutyric acid HCl (also known as Phenibut) has become a fast favorite. Available as a pill or a powder that can be mixed with any liquid, Phenibut is a GABA derivative that promotes relaxation, reduces anxiety, and enhances mood.

In the 1960s, the V.V. Zakusov Research Institute of Pharmacology in the Soviet Union developed Phenibut to enhance the performance of cosmonauts and military personnel. Its effectiveness and broad therapeutic window (the dosage range where a drug is effective without causing harmful side effects) have contributed to its growing popularity. While not approved by the FDA, Phenibut remains widely used across Europe and Russia.

While much safer than benzodiazepines, it may not be the best solution for daytime anxiety. While a very effective nootropic, it has a few side effects that can limit its use. The two most prominent that come to mind are its ability to sedate and the risk of dependence.  

Enter Tofisopam

is an atypical benzodiazepine. It is very chemically similar to drugs like Valium and Xanax. While the rearrangement of a few molecules may not seem like it would make a huge difference, it allows it to act as an anxiolytic without causing sedation, muscle relaxation, or significant cognitive impairment. This makes it perfect for treating generalized anxiety and daytime use.

Another factor that could make Tofisopam a preferred choice over Phenibut is its lower risk of dependence. While it's not recommended to take this nootropic daily and stop suddenly, the risk of addiction is significantly lower than with Phenibut. 

It's important to note that at higher doses Phenibut can cause euphoria. In people predisposed to addiction, this side effect can serve as positive reinforcement, motivating them to use it repeatedly despite the adverse effects that tend to arise. While Phenibut can be helpful in the treatment of anxiety, insomnia, and alcohol withdrawals, there is mounting evidence that long-term Phenibut abuse is highly dangerous. This information is crucial to keep in mind and be aware of the potential risks.

With its unique properties, Tofisopam may offer a safer and more effective alternative to managing anxiety. Hopefully offering a safer option for people struggling with anxiety.

A Quick Overview of Tofisopam

Unlike phenibut, which acts as a GABA-B agonist (similar to baclofen and gabapentin), tofisopam primarily increases the availability of GABA without activating the benzodiazepine receptor. This difference in mechanism of action allows tofisopam to reduce anxiety without causing sedation.

without causing sedation, Tofisopam has been proven comparable to diazepam in treating Generalized Anxiety Disorder. As an added benefit, there are few reports of cognitive impairment, unlike Phenibut, which is known to impair cognition, motor function, and memory at high doses. 

Dosage

The standard dosage range is 50 – 100 mg (1-2 tablets) taken 1-3 times daily with a maximum recommended daily dose of 300 mg. For elderly patients, the daily dose should be reduced, and monitoring by a healthcare provider is strongly recommended.

Side effects

Like all medications and nootropics, there are a few side effects to be aware of:

List of Side Effects

• Agitation

• Confusion

• Constipation

• Convulsions (in patients with epilepsy)

• Decreased appetite

• Dry Mouth

• Headache

• Increased flatus

• Increased irritability

• Insomnia

• Muscle pain

• Muscle tension

• Nausea

Take Away

Both Phenibut and Tofisopam are effective anxiolytics but differ significantly in their mechanisms, side effects, and risks. While Phenibut is a potent GABA-B agonist that enhances relaxation and mood, it carries a risk of sedation, dependence, and cognitive impairment, especially at higher doses. 

While Tofisopam may be a better choice for managing anxiety, it's crucial to consult with a licensed clinician or healthcare professional before starting any new nootropics. This guidance can provide reassurance and ensure the best possible treatment plan.

Ultimately, while both have their uses, Tofisopam may be the better choice for managing anxiety without significant drawbacks.

The FDA has not approved these products in the article. All statements on this page are for informational purposes only and have not been evaluated by the FDA.

1. Marcus A. Bachhuber, Sean Hennessy, Chinazo O. Cunningham, and Joanna L. Starrels.  Increasing Benzodiazepine Prescriptions and Overdose Mortality in the United States, 1996–2013. American Journal of Public Health: April 2016, Vol. 106, No. 4, pp. 686-688. doi: 10.2105/AJPH.2016.303061