What Do We Know About Picamilon? Purported Uses, Side-Effects + More

PICAMILON: Uses, Side Effects, Interactions and Warnings

What Do We Know About Picamilon? Purported Uses, Side-Effects + More
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Picamilon is a chemical made in a lab. Once it has entered the body, it's broken down into gamma-aminobutyric acid and niacin, which are both dietary supplements. However, picamilon isn't a dietary supplement.

It's used as a prescription drug in Russia. In the United States, picamilon hasn't been approved as a prescription drug, and supplements containing picamilon are banned.

Picamilon is used for anxiety, stress, mental alertness, athletic performance, and many other conditions, but there is no good scientific evidence to support these uses.

How does it work?

Picamilon is broken down into gamma-aminobutyric acid (GABA) and niacin. GABA can decrease anxiety and seizures. Niacin can improve blood flow in the brain by causing blood vessels in the brain to become more open. But there is no good scientific evidence showing that picamilon has these same effects.

Insufficient Evidence for:

  • A group of eye disorders that can lead to vision loss (glaucoma). Early research shows that picamilon might improve vision in people with open-angle glaucoma.
  • Loss of bladder control in people with brain, spinal cord, or nerve injuries (neurogenic bladder). Early research shows that picamilon might improve bladder control in children with neurogenic bladder.
  • Anxiety.
  • Athletic performance.
  • Memory and thinking skills (cognitive function).
  • Mental alertness.
  • Seizure disorder (epilepsy).
  • Stress.
  • Other conditions.

More evidence is needed to rate the effectiveness of picamilon for these uses.

When taken by mouth: There isn't enough reliable information to know if picamilon is safe or what the side effects might be.

Special Precautions & Warnings:

Pregnancy and breast-feeding: There isn't enough reliable information to know if picamilon is safe to use when pregnant or breast-feeding. Stay on the safe side and avoid use.

We currently have no information for PICAMILON Interactions

The appropriate dose of picamilon depends on several factors such as the user's age, health, and several other conditions. At this time there is not enough scientific information to determine an appropriate range of doses for picamilon.

Keep in mind that natural products are not always necessarily safe and dosages can be important. Be sure to follow relevant directions on product labels and consult your pharmacist or physician or other healthcare professional before using.

View clinical references for this vitamin or supplement

References:

Avula B, Chittiboyina AG, Sagi S, et al. Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States. Drug Test Anal. 2016;8(3-4):334-43. View abstract.

Borisenko SA. Effects of drugs on blood-brain barrier permeability in rats chronically intoxicated by ethanol. Ann Ist Super Sanita 1990;26(1):39-42. View abstract.

Dorofeev BF, Kholodov LE. Pikamilon pharmacokinetics in animals [abstract only]. Farmakol Toksikol 1991;54(2):66-9. View abstract.

Kolomoitseva EM, Ermakova VN, Abdulkadyrova MZh. Results of pikamilon use in the treatment of patients with open-angle glaucoma [abstract only]. Vestn Oftalmol 1994;110(4):4-7. View abstract.

Mirzoian RS, Gan'shina TS, Kosoi MIu, Aleksandrin VV, Aleksandrin PN. Effect of pikamilon on the cortical blood supply and microcirculation in the pial arteriole system [abstract only]. Biull Eksp Biol Med 1989;107(5):581-2. View abstract.

Sapegin ID, Beketov AI. The effect of pikamilon and fenibut on the blood supply of the brain at rest and under gravitational exposures [abstract only]. Eksp Klin Farmakol 1993;56(1):28-31. View abstract.

U.S. Food & Drug Administration. Picamilon in dietary supplements. Available at https://www.fda.gov/food/dietary-supplement-products-ingredients/picamilon-dietary-supplements. Updated November 29, 2017. Accessed September 21, 2019.

Vishnevskii EL, Guseva NB. Validation of the treatment of the neurogenic bladder in children with myelodysplasia using pikamilon [abstract only]. Urol Nefrol (Mosk) 1998;(2):27-30. View abstract.

Source: https://www.webmd.com/vitamins-supplements/ingredientmono-1582-picamilon.aspx?activeIngredientId=1582&activeIngredientName=picamilon

GNC Supplements May Contain Dangerous Fillers

What Do We Know About Picamilon? Purported Uses, Side-Effects + More

GNC supplements are under investigation for allegations regarding false and misleading advertising.

In 2015, the Attorney General of New York sent letters to GNC and other supplement marketers telling them that DNA testing was unable to prove the supplements contained the labeled substances. As a result of the inability to verify the claimed herbal ingredients, the AG called for sales of many popular supplements to cease.

The New York Attorney General’s office had found only 21 percent of the test results from store brand herbal products contained verifiable DNA from the plants listed on the labels. The other 79 percent consisted of fillers or other plant material.

Some GNC supplements were even found to contain fillers made of powdered legumes, the category of plant life that includes peanuts and soybeans. People who are allergic to these substances would never know the supplements were a potential health hazard to them.

The AG’s office sent the supplements to a lab that uses DNA bar coding, which is the same testing used to determine fraud in the seafood industry. Plants, animals, have specific DNA that can be compared to categorized DNA in a computerized database.

Consumers might be surprised to learn that the U.S. Food and Drug Administration (FDA) does not have the power to regulate supplements.

False advertising of what the pills and powders can do are also an issue, dietary supplement marketing.

A 1994 federal law made the supplement industry exempt from FDA oversight, which means the supplement manufacturing and labeling system is completely dependent upon the ethical behavior of the marketers.

What Do GNC Supplements Contain?

One GNC lawsuit alleged products Turbo Shred and Meltdown Peach Mango were marketed as herbal supplements, but actually contained amphetamine-type stimulants. The purportedly herbal products contained BMPEA and picamilon, a synthetic chemical that was developed in Russia, where it is sold as a prescription drug to treat depression and anxiety.

In December 2016, GNC agreed to a $2.25 million settlement with the Department of Justice. In a statement, the DOJ noted that “[a] lengthy investigation conducted by the U.S. Food and Drug Administration (FDA), the U.S.

Attorney’s Office for the Northern District of Texas and the Consumer Protection Branch of the Department of Justice’s Civil Division revealed that GNC’s practices related to ensuring the legality of products on its shelves were lacking.

At that time, the Department of Justice noted that GNC’s OxyElite Pro Advanced Formula sold in 2013 contained 1,3-dimethylamylamine (DMAA), which is sometimes referred to as geranium extract on labeling.

The DOJ said two soldiers died after taking DMAA, which has been linked to cardiovascular events such as heart attacks.

The supplement also was blamed for causing several liver problems, some of which required the patients to seek liver transplants.

GNC allegedly didn’t know the supplements were tainted, but the DOJ also said GNC didn’t test its own products for purity. The company that made OxyElite was USPLabs, which was indicted in 2015 for making the claim that only natural ingredients were used in its products.

In another heart-breaking case, a hospital gave an infant a probiotic supplement, and the baby died in December 2014. Tests later proved the probiotic was tainted with yeast.

After the baby’s death, the FDA issued a new warning to the public that the supplement industry is not under its regulatory control. This includes supplements for pets as well.

Source: https://topclassactions.com/lawsuit-settlements/consumer-products/supplements/885595-gnc-supplements-may-contain-dangerous-fillers/

Picamilon

What Do We Know About Picamilon? Purported Uses, Side-Effects + More

Developed in a 1969 Soviet research facility, picamilon is the brainchild of the same scientists who have produced many of the world’s most famous chemical compounds [1]. The drug was studied as an anxiety reducing agent (anxiolytic) because it could cross the blood brain barrier and produce GABA and niacin for cognitive enhancing effects [2][3].

In recent years, American smart drug manufacturers have gotten into trouble for using picamilon in their products not because it is dangerous, but more because it is patented to a Russian pharmaceutical company [4].

It is still used and beloved by many within the nootropics communities. It is common to compare picamilon to other anxiety relieving drugs, such as phenibut [5].

Also Known As

Pikamilon, pikatropin, nicotinyl-gamma-aminobutyric acid, nicotinoyl-GABA

Picamilon Benefits

There are millions of people struggling with anxiety daily and usually, this is the main factor in poor mental performance. Numerous studies suggest reducing anxiety is helpful for both improving quality of life and happiness, but also mental performance. The majority of picamilon benefits revolve around reducing anxiety (anxiolytic).

While these picamilon benefits are not well studied, Russian and Japanese scientists found this synthetic compound to be a great prodrug for GABA [6].

Much of the current research is in Russian, however picamilon crosses the blood brain barrier where regular GABA does not [7].

The purpose is to entice picamilon benefits activating GABA receptors to reduce anxiety as an alternative to benzodiazepines [8].

The second component of picamilon is a niacin molecule (vitamin B1), which is a vasodilator (opens up the blood vessels) [9]. There are a host of picamilon benefits for people deficient in vitamin B1 as well.

A final benefit of picamilon comes directly from the community suggesting that the drug not only helps with sleep, but also improves sleep continuity. The user suggested that picamilon helped maintain deeper sleep over the night.

Compared to other anxiolytics, the picamilon benefits seem understudied. While there are still plenty of vendors and anecdotal evidence to suggest it can successfully reduce anxiety, it is harder to find scientific literature on the subject.

Picamilon vs Phenibut

One common comparison amongst community members is picamilon vs phenibut. According to one comprehensive thread, a picamilon supplement can be used daily whereas phenibut cannot [10]. It seems picamilon has less strong of an anxiolytic and GABAminergic response than phenibut.

For many people, this is a helpful difference. Phenibut is a potent sedative and mood lifter, which has garnered attention for withdrawal and tolerance effects. In fact, many people seek a phenibut high to get the greatest effects.

In contrast, picamilon is considered far safer for consumption on a regular basis. One member, by the name of “bose25” mentions using picamilon daily in the morning and evening to reduce symptoms of anxiety. While the effect is strong for one hour, the subtle reduced anxiety is still helpful for him in many situations.

Keep in mind, the picamilon vs phenibut debate includes much speculation and anecdotal evidence. We don’t recommend basing your decisions on these reports alone.

Picamilon Side Effects

The major picamilon side effects will have more to do with your product and dosage than the drug itself. A 2015 study by Harvard and University of Mississippi found a wide range of picamilon dosage recommendations (30 products) and one product with no picamilon at all [11].

There seem to be anecdotal picamilon side effects when combining the drug with others (such as piracetam). The experience was described as a “manic state”, which suggests some caution should be used when stacking picamilon with other nootropics.

Finally, some people complain of picamilon increasing sleepiness or drowsiness, though this does not seem a common complaint.

Picamilon Dosage

The picamilon dosage most recommended online seems to be in the 100 – 200 mg per day range. Most of the scientific literature has no information for human picamilon supplement doses, but this seems to be the starting point for many users.

Because picamilon is lacking in research and particularly the data for human doses, it may be useful to follow a “Shulgin method” approach to the compound. This starts with a microdose (10 – 15 mg) of picamilon so as to determine allergies or adverse reactions.

After this, consume 50 – 100 mg dose and gauge the adverse reactions again before going to a full 200 mg picamilon dosage. Most of the data suggests you will be fine within this dose range.

How and Where to Buy Picamilon

After the 2015 FDA crackdown on various vendors selling picamilon, most have stopped. Many of the most well-known vendors and supplement producers do not touch the substance now that the FDA has gone after a few companies.

This may be because the rights are owned by a Russian pharmaceutical company and is considered a prescription drug in many former Soviet bloc countries. It’s possible to buy picamilon online, but not recommended. We do not have faith or understanding of any of the vendors currently.

If you are seeking a product to reduce anxiety, we may suggest something ashwagandha. This is a natural, anxiety relieving Ayurvedic option, but may not be the most potent for some people. For purely potency, it may be useful to utilize something phenibut for anxiety relief, but not on a daily basis.

Selected Community Experiences

“Picamilon is fine for every day use from my experience, though I tend to have weekends (and any days where I don't leave the house) off. I use ~100mg per dose, once in the morning and another just before I go out either shopping or with friends after work.

It appears to reduce the severity of any anxiety I get and significantly reduces paranoia and social anxiety. I would say it has a noticable effect for up to an hour and then it's subtle, but still helps reduce anxiety.

Phenibut seems to make me feel a little bit intoxicated” [12] – bose25

“Picamilon was worthless for me, and phenibut nearly destroyed my life, even though the high was amazing.” [13] – masterblaster2119

“I've tried Picamilon for sleep, and yeah – it both helps onset of sleep and gets in the way of sleep continuity. In me, Phenibut will remedy this, but due to cost reasons I just use Picamilon during awake hours intermittently.” [14] – Guacamolium

Picamilon Reviews

We must rely heavily on picamilon reviews to make our decisions as there is little scientific evidence and even less in the English language. The above-mentioned picamilon reviews are positive and most online have a similar stance. However, this is not the only information to use in making buying decisions for nootropics picamilon.

Despite the positive and modest picamilon reviews online, it is important to take every substance carefully and protect your long-term interests.

References (Click to Expand)

Source: https://www.nootropedia.com/picamilon/

Why Picamilon Was Banned in the US

What Do We Know About Picamilon? Purported Uses, Side-Effects + More

Letizia Le Fur / Getty Images 

Picamilon, also known as nicotinoyl-gamma-aminobutyric acid, is a synthetic drug that combines niacin (vitamin B3) with gamma-aminobutyric acid (a neurotransmitter with anti-anxiety effects). Picamilon was discovered in Russia in the 1960s and continues to be sold in the country as a prescription drug, where it is believed to treat mood disorders, improve memory, and prevent dementia.

Picamilon is not approved as a prescription drug in the United States. Moreover, in 2015, the U.S. Food and Drug Administration (FDA) ruled that picamilon cannot be sold as a dietary supplement because it does not fit the definition ascribed by the federal regulator. Subsequently, the FDA ordered five companies to remove it from their products.

Despite the functional ban, there are manufacturers in the United States who claim to use picamilon in many of their multi-ingredient supplements.

  • Pikatropin
  • Pikamilon
  • Nicotinyl-GABA

Picamilon is considered a nootropic drug, an ill-defined group of drugs and supplements used in alternative medicine to enhance brain function.

On the surface, the rationale behind picamilon's use seems sound enough. Among its many functions, niacin is involved in vasodilation (the widening of blood vessels).

For its part, gamma-aminobutyric acid (GABA) is able to stimulate brain receptors but is largely unable to cross the blood-brain barrier that divides the brain from the rest of the body.

By combining the two, picamilon is believed to transport GABA more effectively to the brain and, in doing so, treat such conditions as:

In addition, picamilon is thought to sharpen memory, enhance athletic performance, and protect against Alzheimer's disease.

Despite the list of purported benefits, the evidence supporting the claims is fundamentally weak.

A 2010 review of study from Duke University concluded that, while picamilon is able to activate brain receptors in the test tube, it is unable to be broken down in the body by an enzyme known as amidase.

The process, known as amidase hydrolysis, is needed to break the niacin and GABA molecules apart.

Without it, niacin and GABA will remain attached and unable to bind to—much less activate—GABA receptors in the brain.

At present, there is little evidence that picamilon can treat any medical condition.

Given that niacin and GABA are both well-tolerated and essential to human function, it would seem reasonable to assume that picamilon is safe. However, little is known about the long-term safety of picamilon use, particularly at higher doses.

Side effects are relatively mild and may include headache, dizziness, nausea, and flushing due to an associated drop in blood pressure. People being treated for hypertension (high blood pressure) should avoid picamilon as it may trigger acute hypotension (low blood pressure).

Other drug interactions include:

  • Alcohol
  • Barbiturates phenobarbitol
  • Benzodiazepines Xanax (alprazolam) and Valium (diazepam)
  • High-dose aspirin
  • Sedatives Ambien (zolpidem) and Halcion (triazolam)
  • Uric-acid-reducing drugs Zyloprim (allopurinol)

Due to the lack of research, picamilon should not be used during pregnancy or breastfeeding. Its safety in children has also not been established.

There are no guidelines for the appropriate use of picamilon. Moreover, picamilon is not approved for use as either a prescription drug, an over-the-counter drug, or a dietary supplement in the United States.

If you do a casual search of Google using the keyword “picamilon,” you will find dozens of nootropic remedies promising to treat everything from sleep difficulties to stress.

Many of these do not contain picamilon but include other forms of GABA derived from lactic acid bacteria.

(It can only be assumed that “picamilon” was used for the purpose of search engine optimization to attract customers.)

However, there are a handful of formulations that claim to contain picamilon. Clearly, there is no way to check the authenticity of the claims. Furthermore, manufacturers who use picamilon in their products are subject to legal action by the FDA.

Why was picamilon banned by the FDA?

Roughly translated, the Federal Food, Drug, and Cosmetic Act (FFDCA) defines “dietary supplement” as a vitamin, mineral, herb, amino acid, or extract that is used to increase the dietary intake of a naturally occurring substance in the body. This includes metabolites (compounds that are broken down into their bioactive elements as part of normal metabolism).

Because picamilon is a chemical synthesized in the lab with a unique mechanism of action, the FDA decided that it did not meet the FFDCA definition. Until such time as the manufacturer submits the product to human clinical trials, picamilon is unly to ever be approved.

Interestingly, picamilon and a drug called vinpocetine were both under investigation by the FDA at more or less the same time. At the time, both were sold as prescription drugs in Russia but available as dietary supplements in the United States.

Because vinpocetine was derived from lesser periwinkle (Vinca minor) plant, the FDA eventually allowed it to be classified as a dietary supplement. As a drug synthesized in the lab, picamilon was not.

Detractors argued that the FDA ruling was arbitrary given that vinpocetine is not found in the Vinca minor plant (or anywhere else in nature) but is entirely man-made. Supporters of the ruling believe that the FDA should have gone one step further and banned vinpocetine as well.

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Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.

  1. Kopelevich VM, Gunar VI. Some approaches to the directed search for new drugs nicotinic acid. Pharma Chem J. 1999 Apri;33(4):177-87. doi:10.1007/BF02509934

  2. U.S. Food and Drug Administration. Picamilon in Dietary Supplements. Silver Spring, Marylands; November 30, 2015.

  3. Mirzoian RS, Gan'shina TS. The new cerebrovascular preparation pikamilon. Farmakol Toksikol. 1989 Jan-Feb;52(1):23-6.

Additional Reading

  • Avula B, Chittiboyina AG, Sagi S, et al. Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States. Drug Test Anal. 2016;8(3-4):334-43. doi:10.1002/dta.1853
  • Goldberg JS. Selected Gamma-Aminobutyric Acid (GABA) Esters may Provide Analgesia for Some Central Pain Conditions. Perspect Medicin Chem. 2010;4:23-31. doi:10.4137/PMC.S5490

Source: https://www.verywellhealth.com/the-benefits-of-picamilon-89498

Using the Dietary Supplement Label Database to Identify Potentially Harmful Dietary Supplement Ingredients

What Do We Know About Picamilon? Purported Uses, Side-Effects + More

1. Knapik JJ, Steelman RA, Hoedebecke SS, Farina EK, Austin KG, Lieberman HR. A systematic review and meta-analysis on the prevalence of dietary supplement use by military personnel. BMC Complement Altern. Med.2014;14:143. [PMC free article] [PubMed] [Google Scholar]

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3. Lieberman HR, Marriott BP, Williams C, et al.Patterns of dietary supplement use among college students. Clin Nutr. 2015;34(5):976–985. [PubMed] [Google Scholar]

4. Austin KG, Price LL, McGraw SM, McLellan TM, Lieberman HR. Longitudinal trends in use of dietary supplements by U.S. Army personnel differ from those of civilians. Appl Physiol Nutr Metab. 2016;41(12):1217–1224. [PubMed] [Google Scholar]

5. Tainted Products Marketed as Dietary Supplements. fda.govhttps://www.accessdata.fda.gov/scripts/sda/sdNavigation.cfm?sd=tainted_supplements_cder&displayAll=false&page=6.Updated April 16, 2018. Accessed April 19, 2018.

6. Saldanha LG, Dwyer JT, Holden JM, et al.A structured vocabulary for indexing dietary supplements in databases in the United States. J Food Comp Anal. 2012;25(2):226–233. [PMC free article] [PubMed] [Google Scholar]

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8. Vinpocetine in Dietary Supplements. fda.gov. https://www.fda.gov/food/dietarysupplements/productsingredients/ucm518478.htm.Updated November 29, 2017. Accessed March 14, 2018.

9. Request for Comment on the Status of Vinpocetine. regulations.gov. https://www.regulations.gov/docket?D=FDA-2016-N-2523.Published September 7, 2016. Accessed May 31, 2018.

10. Cohen PA. Vinpocetine: An Unapproved Drug Sold as a Dietary Supplement. Mayo Clin Proc. 2015;90(10):1455. [PubMed] [Google Scholar]

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12. Eliason MJ, Eichner A, Cancio A, Bestervelt L, Adams BD, Deuster PA. Case reports: Death of active duty soldiers following ingestion of dietary supplements containing 1,3-dimethylamylamine (DMAA). Mil Med. 2012;177(12):1455–1459. [PubMed] [Google Scholar]

13. Gee P, Tallon C, Long N, Moore G, Boet R, Jackson S. Use of recreational drug 1,3 Dimethylamylamine (DMAA) associated with cerebral hemorrhage. Ann Emerg Med. 2012;60(4):431–434. [PubMed] [Google Scholar]

14. Archer JR, Dargan PI, Lostia AM, et al.Running an unknown risk: a marathon death associated with the use of 1,3-dimethylamylamine (DMAA). Drug Test Anal. 2015;7(5):433–438. [PubMed] [Google Scholar]

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16. FDA issues warning about body-building products labeled to contain steroid and steroid- substances. fda.gov. https://www.fda.gov/Drugs/DrugSafety/ucm509979.htm.Updated June 20, 2017. Accessed April 19, 2018.

17. Attipoe S, Cohen PA, Eichner A, Deuster PA. Variability of Stimulant Levels in Nine Sports Supplements Over a 9-Month Period. Int J Sport Nutr Exerc Metab. 2016;26(5):413–420. [PubMed] [Google Scholar]

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Source: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6372126/

5 Worst Nootropics For Business Professionals (& Which To Use Instead!)

What Do We Know About Picamilon? Purported Uses, Side-Effects + More

Let’s face it, being at your best mentally and physically is quite the task for business professionals, especially considering the ever-increasing work demands in modern society. Many people find themselves slaving away in a cubicle for 10 hours a day, staring at a computer screen until their eyes bleed.

Needless to say, this is not healthy for anyone (in fact, it can kill you). With the job market being so competitive these days, any advantage you can use to perform better than John or Jane Doe in the neighboring cubicle should be considered.

After all, losing your job because of poor performance won’t look good on your resume considering that you ultimately can control how you perform.

Naturally, this makes many business professionals wonder what they can do from a dietary standpoint to optimize their motivation and cognitive function on a daily basis.

The simple answer, for most people, is to reach for that fresh pot of coffee in the break room. Unfortunately, caffeine has a relatively short half-life and only goes so far; once it wears off you’re back to feeling subpar and unmotivated.

Given this, we are going to break down the worst and best nootropics for business professionals to consider using to maximize mental performance and productivity throughout the day.

L-DOPA is an amino acid that humans (and some animals) synthesize naturally from L-tyrosine. L-DOPA is a direct precursor to catecholamines (dopamine, adrenaline, and noradrenaline).

As such, supplementing with L-DOPA is purported to increase feelings of pleasure and motivation, since dopamine and adrenaline play a large role in reward-driven behavior.

However, L-DOPA stimulates both the central and peripheral nervous systems (actually more so just the latter). [1]

For many users, this results in a multitude of unwanted side effects, such as jitters, inability to sit still, nausea, muscle spasms, and feeling restless. Obviously, those are not going to make you more productive while sitting behind a computer or trying to think critically.

Your best bet is to avoid L-DOPA and opt for a different dopamine precursor instead, L-tyrosine or DL-phenylalanine.

Picamilon

Picamilon is a synthetic compound originally created in the Soviet Union. It’s technically a prodrug of GABA – the primary inhibitory neurotransmitter in humans. GABA is thought to play a key role in reducing anxiety and stress, and anti-anxiety medications, benzodiazepines, generally target GABA receptors.

Picamilon is a particularly intriguing nootropic because it permeates the blood-brain barrier and is broken down to niacin (vitamin B3) and GABA.[5] In turn, GABA receptors are activated and the niacin works to expand and relax blood vessels in the brain.

Sounds pretty great, right?

While picamilon is generally a beneficial nootropic, it’s not a reliable one to find over-the-counter or online since it’s patented to a Russian pharmaceutical company (picamilon is a common prescription drug in Russia). In the U.S., however, picamilon is not approved as a drug and does not meet the statutory definition of a dietary ingredient.

Thus, any supplement sold in the U.S. that contains picamilon is misbranded and can’t be trusted. You might be able to find it overseas, but again, there’s no way to really know if it’s picamilon or another chemical.

GABA (Gamma-Aminobutyric Acid)

Since picamilon isn’t a reliable option, many people assume that the prudent thing to do is simply consume GABA supplements.

Problem solved, right? Nope. That’s not how it works, unfortunately.

Taking pure GABA (orally) is an inefficient means of increasing GABA levels in the brain since it doesn’t readily cross through the blood-brain barrier.[8] In fact, picamilon was created to circumvent that issue.

GABA supplements may have some benefits regardless of their poor absorption in the brain, but they are generally not ideal for a productive day at the office.

1,3-DMAA (1,3-Dimethylamylamine)

Despite being banned by the FDA circa 2012, 1,3-Dimethylamylamine (1,3-DMAA) is still found in various sports supplements, particularly “black market” pre-workout formulas.

Some companies simply hide 1,3-DMAA under the guise of “geranium extract,” which is quite misleading. 1,3-DMAA started as a party drug used throughout much of Europe and slowly made it’s way into dietary supplements throughout the U.S. after more people became aware of potent stimulating properties (and euphoria in high enough doses).

Interestingly, 1,3-DMAA has a similar chemical structure (and effect) as ephedrine – a popular fat-loss ingredient that was banned by the FDA over a decade ago.

A case study from 2012 reported that two active-duty soldiers died from cardiac arrest after consuming pre-workout products with 1,3-DMAA.[12] Shortly thereafter, many supplement companies began to remove the harmful ingredient from their products.

Modafinil

Modafinil has become an increasingly popular nootropic of choice, thanks mostly to the ability to promote wakefulness and feelings of arousal. It is typically used as a prescription for treating conditions narcolepsy and erratic circadian rhythms.

The mechanisms behind modafinil are still relatively unclear, but research suggests that this nootropic works by indirectly stimulating secretion of a neuropeptide called orexin and possibly by inhibiting dopamine reuptake.[6]

Orexin-containing neurons potently excite nuclei in the brain that play important roles in wakefulness, such as the dopamine, norepinephrine, and acetylcholine systems.[7]

While modafinil is a prescription medication in the U.S under the brand name Provigil; many overseas vendors claim to have “pharmaceutical grade” modafinil tablets that you can buy online without a prescription.

Similar to picamilon, there is no reliable way to assess the quality of these modafinil pills other than word of mouth and anecdotes.

Moreover, modafinil can have serious side effects and may be just as addicting as Adderall according to some new evidence, thereby increasing the lihood of abuse and health complications.[9]

Higenamine

Higenamine is a plant-derived compound that acts as an agonist for adrenoreceptors in the body. By activating the adenylate cyclase enzyme, higenamine effectively increases cellular levels of cAMP which induces a variety of stimulatory effects and enables a stronger response to adrenaline.[8]

While higenamine may seem beneficial, a recent peer-reviewed study from Harvard University warns that supplements containing this compound should be avoided due to the unpredictable nature of it and inaccurate labeling.[10]

In fact, many of the sports supplements containing higenamine that were analyzed had more than twice as much higenamine as the labels claimed.

With a stimulant of this nature, the difference between taking 50 mg and 100 mg could result in drastic ramifications, especially cardiovascular issues.

L-Theanine

If you’re the type of person to start the workday off with a strong cup of joe, then L-theanine is precisely the nootropic you need to consider for maximizing your productivity. L-theanine is an amino acid found naturally in green tea leaves that works synergistically with caffeine by prolonging its effects.[2]

Even better, L-theanine helps take the “edge” off of caffeine so you don’t feel jittery. L-theanine also modulates your brainwaves (electrical impulses) in such a fashion as to make you feel calm yet attentive.[3]

Some people to refer to the effects of L-theanine as “alert relaxation.” It’s tough to think of a much better feeling to have while working (especially if your job is stressful).

L-theanine typically only needs to be dosed at 100 mg per day (taken with or without caffeine), but some people may use up to 200 mg per day for increased benefit.

Acetyl-L-Carnitine (ALCAR)

ALCAR is a highly bioavailable form of L-carnitine (a quaternary ammonium compound found naturally in red meat, hence the prefix “carni-”). L-carnitine is crucial for transporting long-chain fatty acids into the mitochondria of cells so that they can be burned for energy.

Unfortunately, oral L-carnitine supplements are not well absorbed, nor do they readily cross the blood-brain barrier.

ALCAR, on the other hand, is able to pass through the blood-brain barrier and enhance mitochondrial activity in neurons. Research suggests that this effect can benefit cognitive function, energy levels, and slow the aging process.[4]

The most benefit from ALCAR supplementation seems to be at a dose of 2,000 mg per day (split into two doses). Start by taking 1,000 mg prior to breakfast; if you don’t notice much benefit, take another 1,000 mg in the afternoon on an empty stomach.

Theobromine

Theobromine is the primary alkaloid found in cacao and is essentially a methylated version of caffeine. Its primary role in the body is being a phosphodiesterase (PDE) inhibitor, thereby increasing cellular levels of cyclic adenosine monophosphate (cAMP) – an intracellular molecule that helps transmit signals from substances outside of cells.

While structurally and mechanistically similar to caffeine, studies suggest that theobromine has differential contributions to mood and cognition enhancement, which is precisely why it rounds out the CAFFEINE L-THEANINE formula.[11]

Nootropics for Business Professionals: Start Conservatively

Avoid the worst nootropics that were discussed in this article, especially if you’re a business professional; the last thing you want to do is show up to work looking you’re coked your mind (or high on Adderall).

The good news is that the right nootropics (aka “smart drugs”) can be a healthy and effective alternative to dangerous and addictive pharmaceuticals and illicit drugs.

Whether you’re a desk jockey, a data analyzer, a CEO, a writer, or whatever mentally demanding job you might have, the recommended nootropics for business professionals in this guide are sure to boost your cognitive function and promote a calm disposition while you navigate your stressful workday.

If you’re new to the world of smart drugs, try starting with a simple formula that contains two or three nootropics, such as CAFFEINE L-THEANINE. As you gain more experience using nootropics you’ll get a clearer sense of which ones work optimally for you.

Furthermore, don’t overlook what you’re eating on daily basis, as nutrition plays a major role in your mental performance. For even greater productivity and less stress during the day, you can give intermittent fasting (IF) a try. Click here to read more about IF.

References

[1] Goodwin, F. K., Murphy, D. L., Brodie, H. K., & Bunney, W. E. (1970). L-DOPA, catecholamines, and behavior: a clinical and biochemical study in depressed patients. Biological Psychiatry.

[2] Juneja, L. R., Chu, D. C., Okubo, T., Nagato, Y., & Yokogoshi, H. (1999). L-theanine—a unique amino acid of green tea and its relaxation effect in humans. Trends in Food Science & Technology, 10(6), 199-204.

[3] Kobayashi, K., Nagato, Y., Aoi, N., Juneja, L. R., Kim, M., Yamamoto, T., & Sugimoto, S. (1998). Effects of L-theanine on the release of alpha-brain waves in human volunteers. Nippon Nogeikagaku Kaishi, 72(2), 153-157.

[4] Hagen, T. M., Wehr, C. M., & Ames, B. N. (1998). Mitochondrial Decay in Aging: Reversal through Supplementation of Acetyl‐l‐Carnitine and N‐tert‐Butyl‐α‐phenyl‐nitrone. Annals of the New York Academy of Sciences, 854(1), 214-223.

[5] Akopian, V. P., Balian, L. S., & Avetisian, N. A. (2006). The effect of hypokinesia on depression and on the central GABA-A receptor complexes in the rat brain. Eksperimental'naia i klinicheskaia farmakologiia, 69(2), 10-13.

[6] Willie, J. T., Renthal, W., Chemelli, R. M., Miller, M. S., Scammell, T. E., Yanagisawa, M., & Sinton, C. M. (2005). Modafinil more effectively induces wakefulness in orexin-null mice than in wild-type littermates. Neuroscience, 130(4), 983-995.

[7] Peyron, C., Tighe, D. K., Van Den Pol, A. N., De Lecea, L., Heller, H. C., Sutcliffe, J. G., & Kilduff, T. S. (1998). Neurons containing hypocretin (orexin) project to multiple neuronal systems. Journal of Neuroscience, 18(23), 9996-10015.

[8] Zhang, N., Lian, Z., Peng, X., Li, Z., & Zhu, H. (2017). Applications of Higenamine in pharmacology and medicine. Journal of ethnopharmacology, 196, 242-252.

[9] Krishnan, R., & Chary, K. V. (2015). A rare case modafinil dependence. Journal of pharmacology & pharmacotherapeutics, 6(1), 49-50.

[10] Pieter A. Cohen, John C. Travis, Peter H. J. Keizers, Frederick E. Boyer & Bastiaan J. Venhuis. (2018). The stimulant higenamine in weight loss and sports supplements. Clinical Toxicology

[11] Mitchell, E. S., Slettenaar, M., Vd Meer, N., Transler, C., Jans, L., Quadt, F., & Berry, M. (2011). Differential contributions of theobromine and caffeine on mood, psychomotor performance and blood pressure. Physiology & behavior, 104(5), 816-822.

[12]Eliason, M. J., Eichner, A., Cancio, A., Bestervelt, L., Adams, B. D., & Deuster, P. A. (2012). Death of active duty soldiers following ingestion of dietary supplements containing 1, 3-dimethylamylamine (DMAA). Military medicine, 177(12).

Source: https://primalone.co/blogs/all/5-worst-nootropics-for-business-professionals-and-which-to-use-instead

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