Yohimbine Safety – What does the science say?

Yohimbine is an energizing and metabolism-boosting supplement derived from the Yohimbe tree. It increases levels of adrenaline in the body and inhibits an enzyme in cells that normally suppresses fat burning. It is often used as an aphrodisiac because of its effects on vitality. It is also sometimes used as a wakefulness-promoting supplement.[1]

Clinical studies have found that Yohimbine is effective as an aphrodisiac and energizing supplement that is generally well-tolerated. [2] [3] The serving size used in studies is generally around 5 mg, taken once to four times daily. At this amount, the benefits of Yohimbine generally outweigh the mild side effects experienced by some participants.[4]

However, when taken at larger servings, Yohimbine presents a number of concerning side effects. Not only this, but it has been found to interact with numerous medications and to aggravate a number of medical conditions. As a result, it is important that anybody using Yohimbine be aware of the potential adverse effects associated with it.

What are Yohimbine side effects?

When used at the recommended serving size, it is unusual to experience adverse effects. However, some people may experience one or more of the following, even when taken at the recommended serving size. Increasing the serving size increases the chances of experiencing these side effects:

• Upset stomach
• Excitation, tremor
• Sleep problems
• Anxiety or agitation
• High blood pressure
• Racing heartbeat
• Dizziness
• Drooling
• Sinus pain
• Irritability
• Headaches
• Frequent urination
• Bloating
• Rash
• Nausea, and vomiting.[5]

Using excessively large amounts of Yohimbine (HCL) can put you at risk for more severe side effects such as:

• Irregular or rapid heartbeat
• Kidney failure
• Seizure
• Difficulty breathing
• Paralysis
• Hypertensive crisis
• Very low blood pressure
• Heart problems [1]

As with all supplements, there is also a rare chance of experiencing an allergic reaction. According to WebMD, one person reported an allergic reaction involving:

• Fever
• Chills
• Listlessness
• Itchy, scaly skin
• Progressive kidney failure
• Auto-immune effects.

In 2010, a retrospective review examined all cases of serious side effects that were reported to the California Poison Control System (CPCS) between 2000 and 2006. A total of 238 cases were identified. Of these, around half required only medical monitoring. Around 10% of cases required de-contamination therapy with charcoal and benzodiazepines. Less than 4% of cases required antihypertensive medication, and 2% required supportive care in a hospital.[6]

According to this review, the most common side effects reported to the CPCS included:

• Gastrointestinal distress
• Increased heart rate
• Anxiety
• Hypertension (high blood pressure).

If there are so many side effects, why do people use Yohimbine?

It’s important to remember that many people are able to use Yohimbine without experiencing any negative effects. The most important factor is to not exceed the recommended serving size and to always use the lowest possible serving that allows you to feel the desired effects.

It is also important to consider Yohimbine’s interactions with other substances, which we’ll get to below.

In 2001, researchers published a study on the efficacy and toxicology of Yohimbine. In the article, the researchers reviewed the results of 26 clinical studies on human participants with either normal blood pressure or high blood pressure. Overall, servings ranging from 5 mg – 20 mg tended to have little to no effects on heart rate or blood pressure, with few mild adverse effects being reported, if any at all. In some studies, participants’ blood pressure was increased mildly with no effect on heart rate.[7]

The same review also considered a further 11 studies on male participants. Adverse effects included increased blood pressure, gastrointestinal disturbances, headache, difficulty sleeping, frequent urination, and increased anxiety, in some participants. However, Yohimbine was generally well-tolerated and effective in its measured outcomes. [2]

Overall, the consensus is that Yohimbine, when used at the correct serving size, confers more benefits than side effects. It is good for promoting sexual vitality and wakefulness, and many people around the world are able to use it to their overall benefit. Again, the most important factor determining the risk of negative effects is the serving size. Using the correct serving size reduces the chances of side effects.

Quality concerns about Yohimbine safety

There are two complicating factors when reviewing Yohimbine for safety.

First, the quantity of Yohimbine in any given supplement is not always as listed on the supplement facts panel.

In 2016, researchers working with Examine.com and the US Food and Drug Administration conducted a study on 49 different brands of dietary supplements listing Yohimbine as an ingredient. They also tested the supplements for Corynanthine and Rauwolscine – two derivatives of Yohimbine that sometimes occur alongside the compound, especially in natural extracts.

The results were concerning. They found that the actual amount of Yohimbine in the supplements varied dramatically. Furthermore, 78% of the brands did not list the amount of Yohimbine in their supplement blend. Those that were labelled often showed inaccurate amounts (actual content ranged from 23% to 147% of the labelled content).[8]

Second, supplement brands often sell Yohimbine as a ‘stack’ – often in combination with other energizing or stimulating supplements. As we discuss below, Yohimbine has numerous interactions with other substances, and ‘stacking’ this supplement can be dangerous to your health if it is not done properly.

As an example, medical professionals from Derby, Connecticut, reported two cases of acute liver toxicity in patients who were using a popular weight-loss supplement stack that contained Yohimbine. The supplement stack contained a number of other energizing substances that can affect liver health. So, it is not possible to say whether these effects were from Yohimbine or any of the other ingredients, or a combination of all of them.[9]

Check Out Our Range of Yohimbine HCl

Can you overdose on Yohimbine?

Absolutely. Even though Yohimbine is of natural origins and is classified as a dietary supplement, it is nevertheless extremely powerful and needs to be used responsibly.

Two cases of fatal overdose from Yohimbine products were reported in the Journal of Analytical Toxicology, in 2013. According to the article, neurotoxic effects have been reported from as little as 200 mg (the recommended serving size is around 8 – 16 mg).

At 1.8 grams, a person experienced unconsciousness. At servings of 3 and 5 grams, two people experienced seizures and hypertension, with the larger serving inducing unconsciousness. The 5-gram serving previously reported resulted in blood concentrations of 5,240 ng Yohimbine / mL. A 37-year-old man was found dead with similar blood concentrations, indicating that 5 grams Yohimbine (and possibly much less) has the potential to cause a fatal overdose in humans.[10]

What are the concerns about Yohimbine interactions?

Yohimbine interacts with many different substances and medications. Of special importance are the following interactions, which may increase the effects of Yohimbine and potentially lower the amount needed to experience negative effects.

Antidepressants: Especially monoamine oxidase inhibitors (MAOIs), which increase the number of catecholamines in the brain. Taking Yohimbine with this type of medication may increase the risk of hypertensive crisis.

Blood pressure medication: Medication like Clonidine is used to lower blood pressure for people with hypertension. Taking Yohimbine may reduce the effectiveness of this medication.

Stimulants (including caffeine): Stimulants increase signalling through the nervous system. These effects make you feel energized and more awake. Yohimbine is a powerful energizing supplement and combining it with these types of substances can over-stimulate the nervous system, leaving you jittery, anxious, and at a greater risk of hypertension.

IMPORTANT: Yohimbine’s interactions are not limited to those discussed above. DO NOT USE YOHIMBINE IF YOU ARE TAKING ANY MEDICATION. [11]

Warning for people with existing medical problems

If you have any existing medical issues, it is very important that you speak to your doctor before using Yohimbine or supplements that contain Yohimbine. Depending on your medical condition, Yohimbine may be dangerous to your health.

Yohimbine may aggravate the following conditions:

• Bleeding disorders
• Liver disease
• Anxiety disorders
• Schizophrenia
• Post-traumatic stress disorder (PTSD)
• Heart disease
• Depression
• Diabetes
• Prostate problems

Pregnant and breastfeeding women: There is not enough data to evaluate the safety of Yohimbine for your unborn child or baby.

Surgery: Yohimbine may affect the way that your blood clots, and may interact with the drugs used to keep you under anaesthetic. Do not use Yohimbine for at least 2 weeks prior to surgery. [5]

Anxiety: People with anxiety are advised to avoid Yohimbine as it may trigger extreme anxiety and panic attacks.[12]

Overview of Yohimbine Safety – Is Yohimbine safe?

Although this article may seem to shed a negative light on Yohimbine’s safety, the general consensus is that the benefits outweigh the potential negative effects, when used correctly. Around the world, many people are able to use this supplement within the correct serving range, to their benefit – see the discussion boards on Reddit.com.[13]

However, Yohimbine is unlike other dietary supplements in terms of how potent it is. This supplement really stresses the need to be responsible and to do some background research prior to using it. Overusing Yohimbine can be seriously harmful to your health and, in extreme cases, may result in loss of consciousness, seizures, and death.

Always stick to the recommended serving suggestion, and always use the lowest amount necessary to feel the desired effects. (The recommended serving size is one to two servings of 4 mg, taken once to twice daily). However, many people are able to experience benefits at much lower serving sizes. We recommend starting with 2 mg to assess how your body responds.

While information on Yohimbine’s potential side effects is readily available on the internet, it is possible that many people may not think to go out and research the supplement before using it – which is why we’ve published this article!

If you know anybody who is thinking about taking Yohimbine, please share this article with them! The more people are informed, the less likely it is that they will experience negative effects.

DO NOT USE YOHIMBINE IF YOU ARE TAKING ANY MEDICATION.

DO NOT TAKE YOHIMBINE IF YOU HAVE ANY UNDERLYING MEDICAL CONDITIONS.

References:

[1] Patel, K. (2018). Yohimbine. Examine.com [online] Available at https://examine.com/supplements/yohimbine/

[2] Ostojic, S. (2006). Yohimbine: the effects on body composition and exercise performance in soccer players. Res Sports Med, 14(4):289-99.

[3] Ernst, E., Pittler, M.H. (1998). Yohimbine for erectile dysfunction: a systematic review and meta-analysis of randomized clinical trials. J Urol, 159(2):433-6.

[4] Vogt, H.J., Brandl, P., Kockott, G., Schmitz, J.R., Wiegand, M.H., Schadrack, J., Gierend, M. (1997). Double-blind, placebo-controlled safety and efficacy trial with yohimbine hydrochloride in the treatment of nonorganic erectile dysfunction. Int J Impot Res, 9(3):155-61.

[5] Yohimbe. (2018). WebMD.com [online] Available at:  https://www.webmd.com/vitamins/ai/ingredientmono-759/yohimbe

[6] Kearney, T., Tu, N., Haller, C. (2010). Adverse Drug Events Associated with Yohimbine-Containing Products: A Retrospective Review of the California Poison Control System Reported Cases. Annals of Pharmacotherapy 44(6), 1022–1029.

[7] Tam, S. W., Worcel, M., Wyllie, M. (2001). Yohimbine: a clinical review. Pharmacology & Therapeutics, 91(3), 215–243.

[8] Cohen, P. A., Wang, Y.-H., Maller, G., DeSouza, R., Khan, I. A. (2015). Pharmaceutical quantities of yohimbine found in dietary supplements in the USA. Drug Testing and Analysis, 8(3-4), 357–369.

[9] Dara, L., Hewett, J., Lim, J. K. (2008). Hydroxycut hepatotoxicity: a case series and review of liver toxicity from herbal weight loss supplements. World journal of gastroenterology, 14(45), 6999-7004.

[10] Anderson, C., Anderson, D., Harre, N., & Wade, N. (2013). Case Study: Two Fatal Case Reports of Acute Yohimbine Intoxication. Journal of Analytical Toxicology, 37(8), 611–614.

[11] Horn, J.R., Hansten, P.D. (2012). Yohimbine: Old Drug with New Interactions. Pharmacytimes.com [online] Available at: https://www.pharmacytimes.com/publications/issue/2012/july2012/yohimbine-old-drug-with-new-interactions

[12] Charney, D.S., Heninger, G.R., Breier, A. (1984). Noradrenergic function in panic anxiety. Effects of yohimbine in healthy subjects and patients with agoraphobia and panic disorder. Arch Gen Psychiatry, 41(8):751-63.

[13] Yohimbine - Very underrated nootropic or am I missing something? (2018). Reddit.com [online] Available at: https://www.reddit.com/r/Nootropics/comments/8m1f27/yohimbine_very_underrated_nootropic_or_am_i/

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Taking Agmatine with Kratom - The Top Agmatine Stacks

Around the world, people are searching online for Agmatine stacks and how to use this powerful neurotransmitter supplement together with Kratom. In this article, we look into how to use Agmatine to help with Kratom tolerance, as well as some of the other top Agmatine stacks.

Agmatine itself is often used in pre-workout stacks to boost energy levels and physical performance. It is also effective at reducing stress, supporting a healthy mood, and has neuroprotective and cardioprotective benefits too. It’s one of our favourite health-promoting supplements and may also help to support healthy cognition and memory.

What is Kratom?

Kratom (Mitragyna speciosa) is a tropical plant that is indigenous to Thailand, Indonesia, Malaysia, Myanmar, and Papua New Guinea. It has been used in traditional medicine in Southeast Asia for centuries.[1]

At low serving sizes, Kratom is said to have energizing and alertness-enhancing effects, while larger servings are used for calming, relaxation, and pain relief.

Although Kratom is beneficial to most people who use it, it can cause problems if it is misused. When taken in excess, Kratom stimulates receptors in the brain called opioid receptors. These receptors are also the targets for certain pain-relief medications as well as a number of illicit substances.[2]

As with all compounds that stimulate opioid receptors, too much Kratom can cause respiratory depression (slow, shallow breathing). When combined with alcohol or other sedatives, this can be very dangerous to your health. A number of deaths have been linked to Kratom, but almost always when combined with alcohol or opioid medication.[3]

Daily use of Kratom can cause tolerance to build fairly quickly. This means that a larger serving is required to experience the same effects as before. Naturally, this comes with a greater risk of adverse effects. Furthermore, once tolerance has developed, if you stop using Kratom right away, you may be in for a nasty, and dangerous surprise – known as Kratom withdrawal.[4]

Why Take Agmatine with Kratom?

Although there is not yet any research published on the combination of Agmatine and Kratom, animal studies and anecdotal reports from the internet indicate a positive relationship.

In one study, researchers examined the effects of Kratom on dependence and tolerance to morphine, in mice. The results showed that Agmatine not only blocked the development of tolerance but also increased the pain-relief effects by a factor of 3.[5]

Clearly, this is a very interesting relationship that might even extend to other pain-relief substances (including Kratom). However, more research is needed to properly understand these effects and how they might work in humans.

In one online forum, a Kratom user posted his experience combining with Agmatine:

“…1.5g now achieves the same effect as 3g for me and is perhaps still too much. All I did was add agmatine. It’s got a long half-life of what I think might be 10 hours where it exerts its actual effect on NMDA receptors…”[6]

On another forum, a user posted a similar experience:

“Twice today I tried 500 mg of agmatine sulfate 30 min before burning kratom… With the NGSMD it made it more uplifting with slightly more enjoyment. This evening with the RHB I am feeling quite content and have a feeling of well-being…  Agmatine is supposed to reduce tolerance and I think it just may.”[7]

There appears to be at least a moderate positive relationship between the two, with Agmatine improving the effects of Kratom, reducing the required amount to feel desirable effects, and thereby decreasing the risk of developing tolerance.

Check Out Our Range of Agmatine Sulfate

Other Agmatine Supplement Stacks:

Apart from Agmatine with Kratom, people also search for other supplement stacks to synergize this great substance. We’ve listed a few of our favourites below:

1.     Agmatine with Creatine

Creatine is one of the best-researched supplements in the world. It is known to help with energy levels and to boost physical performance during exercise.[8]

Creatine is a high-energy compound produced in the human body as phosphocreatine. This compound releases energy in cells to protect against stress. Creatine has additional protective effects on the brain, heart, liver, and bones. It may help to improve muscle gain for bodybuilders, and helps muscles to retain water.[9]

The combination of Agmatine and creatine is great for anyone looking for a high-performance pre-workout supplement stack. Both these supplements are known for their energy-boosting effects and their ability to support healthy exercise performance and cognition.

However, there is one thing to remember – creatine and Agmatine have opposite effects on NMDA receptors in the brain (see: How Agmatine Works). According to the supplement’s information page, Examine.com, these two supplements shouldn’t be taken at the same time if it’s the cognitive effects that you’re after.

However, taking them together is still effective for muscle building and athletic performance. You could also split the servings – i.e. Agmatine in the morning, creatine in the evening.

Agmatine Sulfate	Creatine Phosphate
+ Supports physical energy levels	+ Improves physical energy levels and exercise performance
+ Helps to reduce sensations of pain	+ Supports muscle gain
+ Promotes a healthy mood	+ Reduces fatigue

2.     Agmatine with Caffeine

Caffeine is arguably the most important energizing substance known to man, simply because of its prevalence around the world. An estimated 80% of Americans start their day with a cup of coffee.

By the way – have you heard about combining Caffeine with L-Theanine? Check out our blog post on this great supplement stack here: Caffeine with Theanine.

In one animal study, researchers examined the effects of combining Agmatine with caffeine. They found that Agmatine blocked some of the locomotor-stimulant like effects of caffeine, in male mice (but not in female mice).[10]

This combination hasn’t been studied in humans, but there is some anecdotal evidence that Agmatine may increase the energizing effects of Caffeine.[11] It’s a supplement stack that’s definitely worth trying. In terms of biochemical effects, both Agmatine[12] and caffeine[13] work as antagonists of NMDA receptors, which strengthens the argument for a synergistic relationship.

Agmatine Sulfate	Caffeine
+ Supports healthy cognition	+ Improves energy levels and wakefulness
+ Helps to support healthy blood pressure	+ Boosts mood
+ Reduces feelings of stress	- Can cause mild anxiety

 

3.     Agmatine with L-Citrulline / L-Arginine

In the human body, Agmatine is synthesized from L-Arginine, an amino acid which, itself, is synthesized from L-Citrulline. These amino acids are typically included in protein shakes, often used by athletes or bodybuilders.

L-Arginine is a conditionally essential amino acid. It is important for maintaining healthy blood flow by directly stimulating nitric oxide production in the body. It is sometimes used as a dietary supplement to support exercise performance but unfortunately does not have very good absorption into the bloodstream.[14]

L-Citrulline is an amino acid sometimes used as a sports performance and cardiovascular health supplement. Studies have shown that Citrulline reduces fatigue and improves exercise performance, and may boost physical power output. It has better absorption and efficacy than L-Arginine supplements.[15]

According to Examine.com, Agmatine does not go well with either L-Citrulline or with L-Arginine. The reason is that L-Citrulline and L-Arginine compete with Agmatine at some brain receptor sites, and can diminish its beneficial effects.[16]

As a result, it is actually better to not take Agmatine supplements with protein-rich foods (and especially not a protein shake) because these often contain L-Arginine or Citrulline.

However, if you were to take Agmatine as a pre-workout, and waited at least 1 hour before using an amino acid supplement, it would be unlikely for these interactions to occur.

Agmatine Sulfate	L-Arginine	L-Citrulline
Synthesized from L-Arginine	Synthesized from L-Citrulline	Essential amino acid
+ Reduces sensations of pain	+ Supports a healthy circulatory system	+ Reduces fatigue
+ Reduces feelings of stress	+ Mildly improves blood flow	+ Reduces muscle soreness
+ Energizing effects	- Ineffective uptake into blood stream	+ Boosts nitric oxide production

 

How to Take Agmatine Sulfate

Agmatine is a white to off-white powder with a bitter taste and a sulfur-like smell. It is soluble in water and is best taken orally in a liquid beverage of your choice. Use a micro-scoop to measure the correct serving size. Alternatively, you can use the ‘toss and wash’ method.

Agmatine’s recommended serving size is between 600 – 1200 mg, taken once or twice daily. It is not recommended to exceed a daily serving size of 2400 mg (2.4 grams).

It is best taken in the morning, or around 15 – 30 minutes before exercising. It can be used as pre-workout or added to a pre-workout mix. It has good absorption and the effects are usually felt within 15 – 30 minutes.

If you’re taking Agmatine with other supplements, it is recommended to use a smaller serving size, as it may potentiate (increase) the effects of a number of other substances. This is especially true for Kratom and other relaxing or stress-relief supplements.

DO NOT TAKE AGMATINE ALONGSIDE ANY MEDICATION. It has not been studied fully in humans and may cause dangerous interactions.

Check Out Our Range of Agmatine Sulfate

Medical Disclaimer

Not intended to treat, diagnose, or cure any disease or ailment. Use with CAUTION.

References:

[1] Fluyau, D., & Revadigar, N. (2017). Biochemical Benefits, Diagnosis, and Clinical Risks Evaluation of Kratom. Frontiers in psychiatry, 8, 62.

[2] White, C.M. (2017). Pharmacologic and clinical assessment of kratom. Am J Health Syst Pharm. 2018 Mar 1;75(5):261-267. Review.

[3] US Food and Drug Administration. (2018). Statement from FDA Commissioner Scott Gottlieb, M.D., on the agency’s scientific evidence on the presence of opioid compounds in kratom, underscoring its potential for abuse. Fga.gov [online] Available at: https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm595622.htm

[4] Singh, D., Müller, C.P., Vicknasingam, B.K. (2014). Kratom (Mitragyna speciosa) dependence, withdrawal symptoms and craving in regular users. Drug Alcohol Depend, 1;139:132-7.

[5] Li, J., Li, X., Pei, G., Qin, B.Y. (1999). Effects of agmatine on tolerance to and substance dependence on morphine in mice. Zhongguo Yao Li Xue Bao.

[6] Agmatine sulfate is amazing for tolerance. (2017). Reddit.com [online]. Available at: https://www.reddit.com/r/kratom/comments/7lck4q/agmatine_sulfate_is_amazing_for_tolerance/

[7] Agmatine Sulfate. (2015). Ilovekratom.org [online]. Available at: http://www.ilovekratom.com/kratom-forum/kratom-discussion/2748-agmatine-sulfate

[8] Kamel, P. (2018). Creatine. Examine.com [online] Available at: https://examine.com/supplements/creatine/

[9] Bemben, M.G., Lamont, H.S. (2005). Creatine supplementation and exercise performance: recent findings. Sports Med, 35(2):107-25.

[10] Uzbay, T., Kose, A., Kayir, H., Ulusoy, G., Celik, T. (2010). Sex-related effects of agmatine on caffeine-induced locomotor activity in Swiss Webster mice. Eur J Pharmacol, 25;630(1-3):69-73.

[11] Is agmatine good with caffeine? (2016). Reddit.com [online] Available at: https://www.reddit.com/r/Nootropics/comments/595u8z/is_agmatine_good_with_caffeine/

[12] Yang, X.C., Reis, D.J. (1999). Agmatine selectively blocks the N-methyl-D-aspartate subclass of glutamate receptor channels in rat hippocampal neurons. J Pharmacol Exp Ther. 288(2):544-9.

[13] Diler, A.S., Ziylan, Z.Y., Üzüm, G. (2013). N-methyl-D-aspartate Receptors Are Involved in Caffeine-Induced Facilitation on Memory Retention of Passive Avoidance Learning in Rats. Journal of Caffeine Research, 3:4, 169-174

[14] Kamel, P. (2018). Arginine. Examine.com [online] Available at: https://examine.com/supplements/arginine/

[15] Kamel, P. (2018). Citrulline. Examine.com [online] Available at:  https://examine.com/supplements/citrulline/

[16] Kamel, P. (2018). Agmatine. Examine.com [online] Available at: https://examine.com/supplements/agmatine/

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What is Agmatine Sulfate and What Does it Do?

Agmatine is amazing! But what is it, really!?

This fascinating neurotransmitter has been used in research for pain-relief, cognitive enhancement, and anti-inflammation studies and is prized by many bodybuilders for its pre-workout abilities.[1] It was first discovered by a German scientist called Albrecht Kossel, in 1910 – but it took over 100 years for researchers to figure out what it actually does! [2]

In the human body, Agmatine is made from the amino acid, L-arginine. It is also a product of bacterial metabolism so it can be found in a number of fermented foods, including wine, beer, sake, tofu, and soy sauce.[3] Although it is found in the brain, the comound is actually produced mostly by gut bacteria.[4]

Agmatine is a neurotransmitter, which means that it helps signals to pass between nerve cells in the central nervous system.[5] Other well-known neurotransmitters include acetylcholine, serotonin, and GABA. As a neuromodulator, Agmatine interacts with many different neurotransmitter systems in the brain.[6]

In the United States, this compound is not regulated by the FDA and is available as a dietary supplement. The neurotransmitter itself is a little unstable, which is why Agamatine is sold in the sulfate form. This helps to allow for easier storage and a longer shelf-life and may help to improve its efficiency.

How Agmatine Works

Agmatine works in a number of ways to produce its effects and benefits (see our article on Top Agmatine Benefits). It acts as a neuromodulator, neuroprotector, and cytoprotector to defend the body against stress and toxins.¹

You might already know that Agmatine regulates nitric oxide (NO) synthesis. The neuromodulator regulates the set of nitric oxide synthase enzymes (iNOS, eNOS, and nNOS) to reduce their production of NO in various parts of the body.[7] Although nitric oxide has many benefits in the body, too much of it can be a bad thing (as with everything!). According to a recent literature review:

“The increased formation of NO was found to have neurotoxic effects and can contribute to the pathogenesis of stroke and other neurodegenerative disorders.”[8]

Too much nitric oxide is bad for both acute and chronic inflammation in the body, and Agmatine may help to reduce these effects by regulating its production.

Other important ways that this supplement works:

☞ Binds to NMDA receptors and prevents glutamate from binding at these receptors. This protects cells and prevents cell death from glutamate toxicity.[9]

☞ Binds strongly to α-2-adrenergic receptors and improves their activity.[10] These receptors are targeted by many different neurotransmitters and man-made compounds. Activating them helps to reduce blood pressure, and also stimulates nitric oxide synthesis.[11]

☞ Blocks the actions of nicotinic acetylcholine receptors.[12] Other compounds with similar effects are used as muscle relaxants and to reduce and control blood pressure.[13]

☞ Binds to, and activates imidazoline receptors with good efficacy.[14] Activating these receptors causes the body to release β-endorphins (natural ‘feel-good’ compounds that help to reduce pain and stress).[15]

☞ Activates AMPA receptors in mTOR (rapamycin) biochemical pathway. The mTOR protein regulates cell growth and is used in protein synthesis, and activating this pathway is known to improve mood.[16]

☞ Activates the Nrf2 pathway.[17] This biochemical system is a powerful producer of antioxidant proteins in the body and helps to protect cells against the negative effects of stress, toxins, and inflammation.[18]

Check Out Our Range of Agmatine Sulfate

Agmatine as a Pre-Workout and Cognitive Enhancer

Athletes and bodybuilders often wonder about using this supplement as a pre-workout to improve energy and performance. It is an ingredient in many pre-workouts, so it seems pretty logical to ask about using Agmatine alone.

Agmatine has regulatory effects on nitric oxide – it can both decrease its production (at low serving sizes), and stimulate its synthesis (at larger servings).[19] While many pre-workouts are used because of their pro-NO effects, Agmatine sulfate is not necessarily the best option to boost nitric oxide levels. That doesn’t mean that it can’t be used as a pre-workout!

Recent studies show that blood glucose levels tend to decrease after taking Agmatine. Its interactions with imidazoline receptors mean that the supplement allows for extra glucose to be deposited into skeletal muscle cells – boosting energy levels.¹⁴ This accounts for the reduction in blood glucose – what was circulating in the blood has been deposited into muscle cells.

Furthermore, its effects at α-2-adrenergic receptors and on NMDA receptors means that it is able to produce a noticeable improvement in energy levels. These benefits are also great for anyone looking to improve mental focus and alertness. Recent studies have found that it accumulates in areas of the brain that are associated with learning and memory – indicating that it has a role to play in these functions.[20]

Overall – a moderate pre-workout and effective cognitive booster!

Agmatine Sulfate for Mood and Stress

Recently, studies have shown that this supplement may be effective at reducing stress and improving mood, through its numerous effects on neurotransmitter systems and other biochemical systems in the body.

These benefits are especially related to its effects on releasing endorphins – natural ‘feel-good’ hormones that help to reduce stress and improve mood. A number of studies have pointed to the efficacy of these effects.

In one study, the long-term effects (4 - 5 years) of daily large servings was researched. The authors note that it can sometimes be used for pain relief, especially relating to the nervous system. They also note that it is effective for mood, stress, and cognition. The researchers found that no adverse effects were reported in over 1015 people who partook in the study.[21]

Overall – Good increase in mood and supports stress-reduction!

How to Take Agmatine?

Agmatine has been studied at large servings, for long periods of time and there were no adverse effects reported. However, it is still not recommended to exceed the serving size suggestion for this supplement.

The recommended serving size for Agmatine is 600 – 1200 mg, taken once to twice per day. Agmatine Sulfate is usually sold in a powder form. Use a micro-scoop to measure the correct serving size.

This supplement has a high solubility in water so it can easily be dissolved. It can be taken with a glass water, juice, or simply washed down the throat. You could also add the supplement to a healthy smoothie to kick-start your day!

Side Effects and Warnings

Apart from the study we mentioned above, where over 1050 participants took part, over the course of 4-5 years, not much other research has been done on this supplement’s side effects. This is a pretty large study, though, and the fact that no adverse effects were reported is significant.

In another study, over 51 days, researchers tested the effects of different serving sizes – 1.4 grams, 2.7 grams, and 3.6 grams, taken daily in three divided servings. At the largest serving size, some participants reported stomach cramps, which faded after a few days.[22]

Summary: Most studies show no side effects when used at the correct serving size.

Summary – What is Agmatine Sulfate?

★ A naturally-occurring neurotransmitter produced in the human body from L-arginine. It is also synthesized by bacteria and is found in a few fermented food types.

★ The sulfate form allows better absorption and storage stability.

★ This neurotransmitter interacts with many different biochemical systems in the brain and body.

★ It produces mood improvements, helps support healthy cognitive performance, and can be used to increase energy levels. 

★ It is also effective at protecting the body against stress and toxins, through its anti-inflammatory and antioxidant effects.

★ Researchers have studied this supplement for use in pain relief. 

★ The recommended serving size is 600 – 1200 mg, taken once to twice per day.

★ Most studies show that no side effects are reported when used at the correct serving size.

Check Out Our Range of Agmatine Sulfate

References:

[1] Kamel, P. (2018). “Agmatine”. Examine.com [online] Available at: https://examine.com/supplements/agmatine/

[2] Kossel, A. (1910). "Über das Agmatin“. Zeitschrift für Physiologische Chemie (in German). 66: 257–261.

[3] Galgano, F., Caruso, M., Condelli, N., & Favati, F. (2012). Focused review: agmatine in fermented foods. Frontiers in microbiology, 3, 199. doi:10.3389/fmicb.2012.00199

[4] 1: Raasch W, Regunathan S, Li G, Reis DJ. (1995). Agmatine, the bacterial amine, is widely distributed in mammalian tissues. Life Sci, 56(26):2319-30.

[5] Reis, D.J., Regunathan, S. (2000). Is agmatine a novel neurotransmitter in brain? Trends Pharmacol Sci, 21(5):187-93. Review.

[6] Reis D.J., Regunathan, S. (1998). Agmatine: a novel neurotransmitter? Adv Pharmacol, 42:645-9.

[7] Auguet, M., Viossat, I., Marin, J.G., Chabrier, P.E. (1995). Selective inhibition of inducible nitric oxide synthase by agmatine. Jpn J Pharmacol, 69(3):285-7.

[8] Víteček, J., Lojek, A., Valacchi, G., Kubala, L. (2012). Arginine-Based Inhibitors of Nitric Oxide Synthase: Therapeutic Potential and Challenges. Mediators of Inflammation, 2012:318087.

[9] Kim, H.S., Park, I.S., Lim, H.K., Choi, H.S. (1999). NMDA receptor antagonists enhance 5-HT2 receptor-mediated behaviour, head-twitch response, in PCPA-treated mice. Arch Pharm Res, 22(2):113-8.

[10] Molderings, G.J., Menzel, S., Kathmann, M., Schlicker, E., Göthert, M. (2000). Dual interaction of agmatine with the rat alpha(2D)-adrenoceptor: competitive antagonism and allosteric activation. Br J Pharmacol, (7):1706-12.

[11] Giovannitti, J. A., Thoms, S. M., & Crawford, J. J. (2015). Alpha-2 adrenergic receptor agonists: a review of current clinical applications. Anaesthesia progress, 62(1), 31-9.

[12] Loring, R.H. (1990). Agmatine acts as an antagonist of neuronal nicotinic receptors. Br J Pharmacol, 99(1):207-11.

[13] Nicotinic Antagonists. (2018). Drugbank.ca. [online] Available at: https://www.drugbank.ca/categories/DBCAT000919

[14] Chang, C.H., Wu, H.T., Cheng, K.C., Lin, H.J., Cheng, J.T. (2010). “Increase of beta-endorphin secretion by agmatine is induced by activation of imidazoline I(2A) receptors in adrenal gland of rats.” Neurosci Lett,  14;468(3):297-9

[15] Dalayeun, J.F., Norès, J.M., Bergal, S. (1993). Physiology of beta-endorphins. A close-up view and a review of the literature. Biomed Pharmacother, 7(8):311-20.

[16] Neis, V.B., Moretti, M., Bettio, L.E., Ribeiro, C.M., Rosa, P.B., Gonçalves, F.M., Lopes, M.W., Leal, R.B., Rodrigues, A.L. (2016). Agmatine produces antidepressant-like effects by activating AMPA receptors and mTOR signaling. Eur Neuropsychopharmacol, 26(6):959-71.

[17] Freitas, A.E., Egea, J., Buendía, I., Navarro, E., Rada, P., Cuadrado, A., Rodrigues, A.L., López, M.G.. (2015). Agmatine induces Nrf2 and protects against corticosterone effects in hippocampal neuronal cell line. Mol Neurobiol, 51(3):1504-19.

[18] Freitas, A.E., Egea, J., Buendia, I., et al. (2016). Agmatine,  by Improving Neuroplasticity Markers and Inducing Nrf2, Prevents Corticosterone-Induced Depressive-Like Behavior in Mice. Mol Neurobiol, 53(5):3030-3045.

[19] Satriano, J. (2003). Agmatine: at the crossroads of the arginine pathways. Ann N Y Acad Sci, 1009:34-43. Review.

[20] Liu P, Jing Y, Collie ND, Chary S, Zhang H. Memory-related changes in L-citrulline and agmatine in the rat brain. Hippocampus. 2009 Jul;19(7):597-602.
[21] Gilad, G.M., Gilad, V.H. (2014). Long-term (5 years), high daily dosage of dietary agmatine–evidence of safety: a case report. J Med Food, 17(11):1256-9.

[22] Keynan, O., Mirovsky, Y., Dekel, S., Gilad, V.H., Gilad, G.M. (2010). Safety and Efficacy of Dietary Agmatine Sulfate in Lumbar Disc-associated Radiculopathy. An Open-label, Dose-escalating Study Followed by a Randomized, Double-blind, Placebo-controlled Trial. Pain Med, 11(3):356-68.

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This Is Why We're Starting Our Day With Caffeine and Theanine

Do you know the story about Kaldi the Ethiopian goatherd? Legend has it, over a thousand years ago, Kaldi, an observant Abyssinian goatherd, took note of the berries that his goats were eating with such enthusiasm.

Being an adventurous young man, Kaldi decided to try the berries himself. To his delight, the berries made him feel elated and energized. He filled his pockets with them and took them to his tribe’s chief monk.

He and the monk tried cooking the berries in a pot. But, the resulting drink was the most bitter brew they had ever tasted. Disgusted, the monk threw the berries into the fire – roasting the world’s first coffee beans! The two smelled the delicious aroma coming off the fire, and coffee was born.[1]

Today, coffee is the second most consumed drink in the world (second only to tea), and the world’s most prevalent stimulant.[2] But, as we all know, it has its drawbacks. Aside from the mental focus, mood enhancement and energizing effects, coffee can make you jittery, give you sweaty palms, a racing heart, a headache, and – worst of all – it can make you feel anxious.[3]

Enter L-Theanine…

What’s so Great About L-Theanine?

Theanine is one of the main active ingredients found in green tea and also in several species of mushrooms.

It helps to promote relaxation without causing drowsiness and is especially useful when taken alongside caffeine. It is best known for its ability to reduce mental fatigue and feelings of stress.[4] Theanine is also able to improve cognitive performance – perhaps not to the same extent as caffeine, but definitely, enough to be noticeable.[5]

Researchers have found that Theanine can help to promote healthy sleep. It is not a sedative, though, so the sleep-promoting benefits are thought to be related to its stress-reducing effects.[6]

One of the best things about Theanine is that it has almost zero toxicity levels – it is very safe and may even confer some health benefits. Researchers have shown that it helps with inflammation and may improve blood flow.[7]

At small to medium servings, it is a mild cognitive enhancer and a mellower alternative to caffeine. At larger servings, it can be used to help promote healthy sleep.

In your brain, Theanine helps to increase the production of GABA and dopamine and may help to reduce cortisol – also known as the ‘stress hormone’.[8] [9] [10] Theanine’s relaxing and stress-reducing properties help to reduce the common side effects felt from caffeine.

How do we know this is true? Well, apart from all the research that’s been done on these two compounds, you can actually test this yourself without even using any supplements.

Tea contains both Caffeine and Theanine. A typical cup of green tea contains around 35 mg of Caffeine and no more than 10 mg of Theanine.[11] [12]

A better test would be to use black tea (which is made from the same plant as green tea, just processed differently). A cup of black tea usually contains around 20-30 mg caffeine and 20 – 25 mg Theanine. [12]  [13]

Even if you drank 2-3 cups of tea in a row, it’s unlikely that you’d notice any of the side effects associated with coffee. That’s because the Theanine content is blocking those effects.

The obvious problem with tea – which contains both caffeine and L-Theanine, is that the levels of these compounds are way too low. To get a similar kick to what you feel from a strong cup of coffee, you’d need to drink several cups of tea. You’d be using the bathroom far too regularly to be functional.

Check Out Our Range of L-Theanine Products

Why combine Caffeine and Theanine?

The combination of Caffeine and Theanine is sometimes considered to be the ‘original nootropic’. Nootropics are substances that improve cognitive function, memory, creativity, or motivation.

In 2017, researchers conducted a study on 20 healthy young individuals, who were given either placebo, caffeine, l-theanine, or a cup of black tea. The researchers measured a number of outcomes like cognitive reaction time and neurophysiological measures of attention.

They found that caffeine and theanine both improved cognitive performance significantly more than placebo or black tea, BUT the combination of theanine and caffeine improved cognitive performance by a long shot! [14]

This is why so many people are using Theanine combined with caffeine – either by taking Theanine capsules alongside a cup of coffee, or bypassing the coffee altogether and using Caffeine + Theanine capsules. This is sometimes called a ‘supplement stack’ – where you take two different supplements together for their synergistic relationship.

Why take Caffeine + Theanine capsules?

L-Theanine capsules are formulated with 200 mg Theanine per capsule – which, when combined with a cup of coffee (around 50 – 100 mg), will produce noticeable benefits in terms of focus, alertness, and cognitive function.

Caffeine + L-Theanine capsules are packed with 100 mg caffeine and 150 mg Theanine, for people who’d prefer to skip out on coffee. That’s the equivalent caffeine content of a strong, large cup of coffee, combined with the Theanine content of several strong cups of tea.

If you compare capsules to powder supplements, they’re just much easier to take! No need for micro-scoops or measuring scales, simply pop the capsule in your mouth and swallow!

In terms of monetary savings, let’s assume you’re drinking a large cup of strong coffee every morning – with a full 100 mg caffeine. The average large-sized coffee sets you back around $3. This is without any Theanine, mind you.

Now, if you were to purchase a 300 count tub of caffeine + Theanine capsules, this is the equivalent of 300 cups of coffee WITH added L-Theanine! If you were buying a cup of coffee every morning, that’d cost you over $900. So you can imagine how much you’re saving by using these capsules.

Even if you’re a coffee addict and you definitely won’t cut out the morning brew – well, the noticeable benefits that you feel from adding a Theanine capsule to your morning coffee, in terms of cognitive performance and mood: these benefits are well worth the price!

How do you take Theanine and Caffeine capsules?

Caffeine and L-Theanine capsules contain 100 mg Caffeine and 150 mg L-Theanine. The synergistic relationship between the two is what’s important! For these capsules, the recommended serving size is 1-2 capsules, once or twice daily.

In terms of Theanine, 200 mg is the ideal serving size for most people – and that’s how much is in a single capsule. To use Theanine as a mild cognitive enhancer, a lower serving size is recommended. For sleep, you’ll need a larger serving size of around 400 mg (or two capsules).

The one thing to remember is that large servings of well over 400 mg may make you feel a bit drowsy. So you just need to watch for that. But, taking 1-2 capsules, once or twice daily definitely shouldn’t produce any negative effects, so it’s actually a great mellow alternative to caffeine.

Check Out Our Range of L-Theanine Products

What are the Side Effects of Theanine and Caffeine?

As we mentioned before, Theanine is relatively free from side effects and may actually help to reduce some of the adverse effects that people feel from caffeine.

At larger servings, it may cause slight drowsiness and headaches but these are not generally present at the recommended serving size.

Unfortunately, caffeine isn’t as benign as Theanine and needs to be used responsibly.
Even at small servings, caffeine can increase your blood pressure and your heart rate. It is a vasoconstrictor, which means that it causes the blood vessels to get smaller (although it is thought that Theanine may counter this effect to a certain level).

There are several important points to remember about caffeine use:

• It has a long half-life of over 6 hours, so don’t use it any time close to sleep!
• It is possible to overdose on caffeine. Anything above 400 mg8 per day is said to be unhealthy, so it’s important to stick to the recommended serving size.
• Caffeine is addictive and can cause withdrawal symptoms after prolonged use.

Please use these capsules responsibly- as with all supplements!

* Medical Disclaimer

Not intended to treat, diagnose, or cure any disease or ailment. Use with CAUTION.

References:

[1] Nzegwu, N. (1996). The History of Coffee. Africaresource.com. [Online]. Available at:   https://www.africaresource.com/house/news/our-announcements/21-the-history-of-coffee

[2] Daly, J.W., Holmén, J., Fredholm, B.B. (1998). [Is caffeine addictive? The most widely used psychoactive substance in the world affects same parts of the brain as cocaine]. (Article in Swedish). Lakartidningen, 16;95(51-52):5878-83.

[3] Spritzler, N. (2017). 9 Side Effects of Too Much Caffeine. Healthline.com [Online]. Available at:  https://www.healthline.com/nutrition/caffeine-side-effects

[4] Patel, K. (2018). Theanine. Examine.com. [Online]. Available at: https://examine.com/supplements/theanine/

[5] Dodd, F. L., Kennedy, D. O., Riby, L. M., Haskell-Ramsay, C. F. (2015). A double-blind, placebo-controlled study evaluating the effects of caffeine and L-theanine both alone and in combination on cerebral blood flow, cognition and mood. Psychopharmacology, 232(14), 2563–2576.

[6] Rao, T.P., Ozeki, M., Juneja, L.R. (2015). In Search of a Safe Natural Sleep Aid. J Am Coll Nutr, 34(5):436-47.

[7] Hwang, Y.P., Jin, S.W., Choi, J.H., Choi, C.Y., Kim, H.G., Kim, S.J., Kim, Y., Lee, K.J., Chung, Y.C., Jeong, H.G. (2017). Inhibitory effects of l-theanine on airway inflammation in ovalbumin-induced allergic asthma. Food Chem Toxicol, 99:162-169.

[8] Yokogoshi, H., Kobayashi, M., Mochizuki, M., Terashima, T. (1998). Effect of theanine, r-glutamylethylamide, on brain monoamines and striatal dopamine release in conscious rats. Neurochem Res, 23(5):667-73.

[9] Nathan, P.J., Lu, K., Gray, M., Oliver, C. (2006). The neuropharmacology of L-theanine(N-ethyl-L-glutamine): a possible neuroprotective and cognitive enhancing agent. J Herb Pharmacother, 6(2):21-30.

[10] White, D.J., de Klerk, S., Woods, W., Gondalia, S., Noonan, C., & Scholey, A. B. (2016). Anti-Stress, Behavioural and Magnetoencephalography Effects of an l-Theanine-Based Nutrient Drink: A Randomised, Double-Blind, Placebo-Controlled, Crossover Trial. Nutrients, 8(1), 53.

[11] West, H. (2017). How much caffeine is in green tea? Healthline.com. [online] Available at https://www.healthline.com/nutrition/caffeine-in-green-tea

[12] Lee, J. (2013). L-Theanine for Anxiety – Self Medicating Anxiety with Tea? Choosehelp.com. [online]. Available at: https://www.choosehelp.com/topics/complementary-alternative-therapies/l-theanine-for-anxiety-2013-self-medicating-anxiety-with-tea

[13] Mayoclinic Staff. (2017). Caffeine content for coffee, tea, soda and more. Mayoclinic.org. [online]. Available at: https://www.mayoclinic.org/healthy-lifestyle/nutrition-and-healthy-eating/in-depth/caffeine/art-20049372

[14] Kahathuduwa, C.N., Dassanayake, T.L., Amarakoon, A.M.T., Weerasinghe, V.S. (2017). Acute effects of theanine, caffeine and theanine-caffeine combination on attention. Nutr Neurosci. Jul;20(6):369-377.

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The Top 10 Best Phenibut Alternatives for Stress Reduction and Healthy Sleep

In this article, we explore the Top 10 Phenibut alternatives available today. These naturally-derived dietary supplements are able to provide similar benefits to those of Phenibut, but with a lower risk of overuse/abuse or side effects. While natural supplements are often thought to be milder in their effects, many of these supplements are very powerful and can definitely be considered on par with Phenibut’s effects.

This article is especially useful for anyone who has used Phenibut in the past but experienced difficulties in terms of side effects or overuse; or for somebody looking for the benefits offered by Phenibut but who would prefer using a supplement with less risk of adverse effects or simply prefers taking supplements of natural origins.

Why Phenibut?

Many people around the world take Phenibut as a powerful mood-boosting and stress-reducing dietary supplement. When taken at the recommended serving size, Phenibut helps to promote a healthy mood, as well as supporting feelings of relaxation and sociability.[1] It is often preferred by people who tend to be very busy or have a lot of stress in their lives, as a way to calm the mind and help support healthy sleep.

This Russian-developed compound targets areas in the brain called GABA-receptors.[2] GABA is a neurotransmitter that is responsible for ‘dulling’ the signals sent from the Central Nervous System (CNS) to the brain. This is especially important to help with promoting sleep at night and is also essential for maintaining a balanced mood and nervous system. In fact, GABA is so effective at calming the body that many tranquillizers and sedatives target similar receptors in the brain. Alcohol, for example, is a GABA agonist, meaning that it activates GABA receptors.

In general, GABA-agonists are known for their efficacy in reducing stress, promoting relaxation, and supporting a healthy mood, as well as being useful at helping with sleep. However, most compounds that activate GABA receptors have a drawback of making people feel tired or groggy, and negatively affecting motor coordination. Phenibut is unique because it was specially engineered to deliver the benefits of GABA activation without the sedative-like side-effects that categorize this group of compounds, and this is the reason why so many people around the world love using it.

Check Out Our Range of Phenibut

Why Do People Search for Phenibut Alternatives?

Despite the pleasant benefits of Phenibut, it needs to be used responsibly and with care. Unlikely most dietary supplements, Phenibut is not of natural origins. It is typically synthesized in a laboratory and was originally designed to help improve the efficiency of Russian cosmonauts in space.[3] This means that it needs to be taken at the correct serving size and cycled correct, to avoid the risk of experiencing unpleasant adverse effects.

The recommended serving size is between 500 – 2000 mg per day, taken in 2-3 smaller split servings. Never take more than 1000 mg of Phenibut in a single serving, and do not use more than twice per week. A smaller serving size is better to promote a mild improvement in mood and reducing stress. Smaller servings are ideal for promoting better sociability. At larger servings, the sleep-promoting benefits of this supplement become more apparent.

There are some important reasons why people search online for Phenibut alternatives. Mostly, these relate to the potential adverse effects from overusing this supplement. The three most important reasons why some people prefer Phenibut alternatives are that they encounter:

1.     Phenibut Side Effects

The most common reason that people choose to seek out different, but similar, supplements to Phenibut is because they experience some form of side effect. Side effects are generally uncommon at the recommended serving size, but some people can have a great sensitivity and be more prone to encountering these adverse effects.

Phenibut side effects can include one or more of the following: nausea, sedation, irritability and agitation, anxiety, headache, dizziness, allergic reactions. At larger servings, some people encounter adverse effects like motor impairment, loss of balance, and hangovers.[4] That being said, the overwhelming majority of people who use this supplement are able to do so without experiencing any of the above mentioned negative effects.

2.     Phenibut Withdrawal

This is the reason why it is so important to use Phenibut responsibly – within the recommended serving size and not more than twice per week. The reason for this is that it is possible to build a tolerance to Phenibut’s effects over time and when used at large servings, which can lead to dependence.

If you regularly take large Phenibut servings or use it for days or weeks consistently, you may experience withdrawal symptoms when stopping. Symptoms of Phenibut withdrawal can include negative thoughts, depression, lethargy, prolonged insomnia, persistent restlessness, stress and panic attacks. At least one person experienced mild and temporary psychosis as a result of withdrawal symptoms from prolonged heavy Phenibut intake. [5]

3.     Interactions and Overdose

Phenibut, being a GABA agonist supplement, has the potential to interact with a number of other supplements and compounds. It is very important to consult with your doctor before taking this supplement if you are using any medication or have any underlying medical conditions. The most important interactions to be aware of are between Phenibut and alcohol, and between Phenibut and benzodiazepines.[6]

Unlike most naturally-derived supplements, which are generally safe at all serving sizes, Phenibut can be dangerous to your health if taken above the recommended serving suggestion. Taking this supplement at servings above those recommended on the bottle can lead to adverse effects, and can potentially land you in hospital.

It is important to remember that, although Phenibut is sold online as a dietary supplement and has helped many people around the world to deal with stress and to improve their mood and sleep patterns, it is not like other ‘natural’ supplements, and has the potential to cause harm to your body if taken irresponsibly. If you feel that you may not be able to use Phenibut responsibly, we highly recommend checking out these Top 10 Phenibut alternatives below:

Top 10 Phenibut Alternatives

1.     LiftMode’s Sleep Capsules

• Combination of Four Top Supplements in a Single Capsule
• Promotes Strong Feelings of Calm & Relaxation
• Assists with Healthy Sleep and Stress-Reduction

Similarity to Phenibut: ★★★★★

This great new addition to LiftMode’s catalogue provides the user with no less than four top calming supplements in a single capsule. The supplement stack is specially formulated to provide the best combination of naturally-derived supplements for stress-reduction, mood-boost and to promote healthy sleep.

In terms of its similarity to Phenibut, this is, most likely, as close as you’ll get with an alternative. The Sleep Aid capsules contain a combination of Melatonin, Oleamide, Ascorbic acid (Vitamin C), and L-Tetrahydropalmatine (L-THP) – all of natural origins, and without any of the potential hazards of using Phenibut. Our favourite Phenibut alternative on this list!

Check Out Our Range of Sleep Stack Capsules!

2.     GABA

• Great for Supporting Healthy Sleep
• Provides a Natural Serving of GABA: The Calming Neurotransmitter
• Helps to Promote a Healthy Immune System

Similarity to Phenibut: ★★★☆☆

GABA (Gamma-aminobutyric acid) is a well-known calming neurotransmitter. As a natural hormone, it helps the body to ‘dull’ signals from the immune system, promoting rest, relaxation, and stress-reduction.[7] Many calming supplements and compounds target GABA receptors in the brain, and by using this supplement, you simply make more GABA available in the body.

The best-known effects of GABA supplements are for reducing stress and promoting healthy sleep. Studies have pointed to its efficacy at reducing the time taken to fall asleep.[8] However, it is not known to produce the same mood-boosting effects as Phenibut. We’d recommend this Phenibut alternative to someone who is more interested in a stress-reducing and sleep-promoting supplement.

3.     5-HTP

• Significant Improvements in Mood
• Helps to Maintain a Healthy Metabolism
• Supports Healthy Sleep

 

Similarity to Phenibut: ★★★☆☆

5-HTP (5-Hydroxytryptophan) is a powerful amino-acid and the biochemical precursor to serotonin. When you take 5-HTP supplements, a large amount of this becomes available in the brain to synthesize serotonin, a vital neurotransmitter for supporting a healthy mood.[9]

Serotonin is also important for maintaining physiological and psychological functions in the body. These include supporting a healthy emotional state, promoting healthy sleep, and support for a healthy appetite, memory, learning, sex drive, immune systems, and muscle tone.[10] 5-HTP supplements are typically extracted from a plant called Griffonia Simplicifolia, which contains concentrations as high as 20%! Recommended especially to people who enjoy the mood-lifting effects of Phenibut.

4.     L-Theanine + Caffeine

• Powerful Cognitive Enhancer
• Strong Mood Booster
• Energizing and Stimulating

Similarity to Phenibut: ★★☆☆☆

The combination of L-Theanine and Caffeine is especially great for people who use Phenibut as a tool to combat stress and improve focus. Although this supplement combination works in a very different way to Phenibut – providing a mental and physical energy boost, in contrast to the more calming and relaxing effects of Phenibut – some of its benefits are seen as similar to those of Phenibut.

For many people, the stress-reducing effects of Phenibut help them to focus better at work or studies. The combination of L-Theanine and Caffeine has been shown to be highly effective at promoting healthy cognitive performance and supporting learning and mental focus.[11] L-Theanine is also well-known for its ability to support relaxation.[12]

5.     Magnolia Bark Extract

• Promotes a Calm, Relaxed State of Mind
• Effectively Reduces Stress
• Helps to Support a Healthy Circulatory System

 

Similarity to Phenibut: ★★★★☆

Magnolia Bark Extract is rich in plant alkaloid compounds called Magnolol and Honokiol. Both of these alkaloids have been studied in depth for their ability to promote relaxation, reduce stress, and to support a positive mood.[13] Studies have also indicated the potential to use this great plant-extract as a natural sleep aid since it is effective in reducing the time taken to fall asleep.[14]

Magnolia Bark Extract has been used in Traditional Chinese Medicine (TCM) for centuries, as a health-promoting remedy. Its traditional name is Houpu. Some people use this supplement for its potential cognitive benefits, although these are still being studied in more detail. This is one of our top Phenibut alternatives because of its similarity in terms of benefits on mood, stress, and sleep promotion.

Check Out Our Range of Magnolia Bark Extract

6.     Oleamide

• Relaxation and Mood-lift
• Supports Healthy Sleep
• Neuroprotector and Anti-inflammatory

 

Similarity to Phenibut: ★★★☆☆

Oleamide (cis-9,10-octadecenoamide) is a naturally-occurring fatty acid that is produced by the human brain to help promote sleep. It is a derivative of oleic acid, which is found in olive oil. When used as a dietary supplement, Oleamide is great for promoting relaxation, reducing stress, and improving mood.[15] Additionally, studies have shown that Oleamide is effective at reducing the time taken to fall asleep and also at protecting the brain from stress.[16]

Some people think of Oleamide as a ‘lighter’ version of Phenibut. It must be said, however, that it’s sleep-promoting effects are generally considered better than those of Phenibut. It is a little lighter on the mood-boosting and sociability-enhancing effects but is also without the potential for adverse effects.

7.     Baicalin

• Powerful Antioxidant & Anti-Inflammatory
• Promotes a Healthy Circulatory System
• Used for Vitality, Relaxation, and Well-Being

Similarity to Phenibut: ★★★★☆

Baicalin is one of our all-time favourite health-promoting supplements and a powerful bioflavonoid. It is the active compound found in the Chinese Skullcap and is an integral part of Traditional Chinese Medicine. It has been used for centuries for promoting health, vitality and relaxation. Studies have indicated that Baicalin has strong anti-stress benefits and can help to support a healthy brain.[17]

Like Phenibut, Baicalin acts on GABA receptors, albeit at a slightly lower potency.[18] One of the top things about this supplement is that it is very soluble in water, so it can easily be dissolved in a healthy juice for breakfast, to kick-start your day! All-in-all, this natural alternative comes really close to Phenibut’s effects and is easily one of our top recommendations. We love that it packs in a health-boosting punch in addition to it’s Phenibut-like effects.

Check Out Our Range of Baicalin

8.     Melatonin

• One of the World’s Best Natural Sleep Aids
• Potent Antioxidant Benefits for Good Health
• Helps to Improve Mood

 

Similarity to Phenibut: ★★★☆☆

Melatonin is one of the best-known natural sleep aids available today. It is the brain’s ‘sleep hormone’ and is responsible for regulating the circadian rhythm. Melatonin is produced by the pineal gland from serotonin, in response to changes in the dark-light cycle.[19] Melatonin supplements are also great antioxidants and help to support a healthy body by destroying dangerous ‘free-radicals’.[20]

Melatonin is recommended as a natural alternative for people who use Phenibut for its sleep-promoting effects. Study-after-study has indicated that Melatonin supplements are effective, not only at reducing the time taken to fall asleep but also at improving overall sleep quality. Some people who take Melatonin claim that it also helps to promote an improved mood and to support feelings of well-being.

9.     L-Tetrahydropalmatine (L-THP)

• Blocks voltage-activated L-type calcium channels
• Promotes a healthy circulatory system
• Works as an anti-stress and calming supplement

 

Similarity to Phenibut: ★★★★☆

Levo-Tetrahydropalmatine (L-THP) is a plant compound found in Corydalis yanhusuo – which is an essential component to many Traditional Chinese remedies. This plant extract has been used for centuries as a herbal health tonic. Pure L-THP has been available in China for over half a century, where it is used as a pain-relief and anti-inflammatory compound. As a dietary supplement, it is best known for its beneficial effects on dopamine receptors, and for helping to reduce sensations of pain.[21]

Just like Phenibut, and unlike any of the other alternatives on this list, L-THP is a powerful blocker of calcium-gated channels (Ca2+ channel blocker).[22] This means that it prevents calcium from entering into the cells of the heart and blood vessel walls, which helps to support a healthy circulatory system.

BONUS TIP: We recommend trying a combination of L-THP, taken along with either of our 4-star Phenibut alternatives: Baicalin or Magnolia Bark Extract.

This natural combination mimics both of Phenibut’s key mechanisms: Ca2+ channel blocking, along with stress-reducing GABA-binding effects. In fact, it may just be the best bet for producing a really powerful natural alternative!

Check Out Our Range of L-Tetrahydropalmatine

10.  Agmatine Sulphate

• Supports cognitive health
• Helps to reduce stress and promote a healthy mood
• May help with fitness performance and to support a healthy circulatory system

Similarity to Phenibut: ★★★☆☆

Agmatine sulphate is a neurotransmitter that has only recently been understood. It is used for receptor signalling in pathways of the central nervous system (CNS) and is stored in the synaptic vessels.[23] Recent studies of Agmatine suggest that it has some great benefits, that may be very similar to those of Phenibut. The results of these studies are echoed by Agmatine reviews on internet forums. Its benefits include reducing feelings of stress, promoting an improved mood, and also good support for cognition, learning, and memory.

Like Phenibut, Agmatine may also provide neuroprotective benefits and support a healthy circulatory system.[24] It is found in many food sources and is produced naturally in the human body. As a result, Agmatine is generally considered safe for use and relatively free of side effects. As a result, it is a great alternative for people who enjoy the cognitive effects of Phenibut but are concerned about potential adverse effects.

Other Alternatives

There are a number of different Phenibut alternatives that could also be beneficial but are not currently offered on LiftMode.com. Although these products are not currently listed on our catalogue, we are working to include more of them in the future. Stay tuned for more information!  Other Phenibut alternatives include:

Ashwagandha: Also called ‘Indian Ginseng’, it is a part of Ayurvedic medicine, where it is used to maintain youth. It has effective benefits for pain-relief and stress reduction.

Lemon Balm: Traditionally used to improve mood and cognitive function. Recent research points to its additional benefits in reducing stress.

Passion Flower: Also known as Passiflora, this plant extract was long used by Native Americans for a variety of conditions. Some studies point towards its benefits on stress reduction and mood, through GABA receptors.

Kava: A plant endemic to the South Pacific islands and long used as a ceremonial drink to promote relaxation. Recent studies point to its stress-reducing and sleep-promoting effects.

Mulungu: Used for centuries by indigenous people in the Central and South Americas, the bark of the Mulungu tree is effective at supporting a healthy mood and reducing stress.

Magnesium: Magnesium, especially when taken in an easily-absorbable form, appears to be effective at reducing stress - which, scientists say, may be the result of a nutrient deficiency.

Lavender Oil: Lavender has been used in aromatherapy since ancient times for many different conditions. Today, research suggests it may be an effective means of reducing stress without the potential for abuse.

Conclusion

In summary, Phenibut is a fantastic dietary supplement for supporting a healthy mood, reducing stress, and promoting restful sleep. Thousands of people around the world successfully use this supplement without experiencing any negative side effects. However, it needs to be used responsibly. Overuse can be detrimental to your health. As a result, many people online are searching for natural/safer Phenibut alternatives.

Our favourite Phenibut alternatives include LiftMode Sleep Capsules and a combination of Levo-Tetrahydropalmatine (L-THP) with either Baicalin or Magnolia Bark Extract. This combination mimics the biological mechanisms underlying Phenibut’s effects, using naturally-derived supplements without the risk of adverse effects. There are many other dietary supplements that mimic one or more of Phenibut’s benefits, although often with slightly milder effects.

References:

[1] Shul'gina GI, Ziablitseva EA. [Effect of the GABA derivative phenibut on learning]. (Article in Russian). Vestn Ross Akad Med Nauk. 2005;(2):35-40.

[2] Lapin I. Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug. CNS Drug Rev. 2001 Winter;7(4):471-81.

[3] Högberg L, Szabó I, Ruusa J. [Phenibut yielded withdrawal symptoms and psychosis. Drugs for cosmonauts–now marketed as dietary supplements online]. (Article in Swedish). Lakartidningen. 2013 Apr 17-23;110(16):825-7.

[4] Phenibut. (2018). WebMD.com, available online from https://www.webmd.com/vitamins/ai/ingredientmono-1184/phenibut [Accessed August 3, 2018]

[5] Högberg L, Szabó I, Ruusa J. Psychotic symptoms during Phenibut (beta-phenyl-gamma-aminobutyric acid) withdrawal., Journal of Substance Use. 2013, 18(4): 335-338

[6] Samokhvalov AV, Paton-Gay CL, Balchand K, Rehm J. Phenibut dependence. BMJ Case Reports. 2013;2013:bcr2012008381.

[7] Wu C, Sun D. GABA receptors in brain development, function, and injury. Metabolic brain disease. 2015;30(2):367-379.

[8] Boonstra E, de Kleijn R, Colzato LS, Alkemade A, Forstmann BU, Nieuwenhuis S. Neurotransmitters as food supplements: the effects of GABA on brain and behavior. Frontiers in Psychology. 2015;6:1520.

[9] Hinz M, Stein A, Uncini T. 5-HTP efficacy and contraindications. Neuropsychiatric Disease and Treatment. 2012;8:323-328.

[10] Mohammad-Zadeh LF, Moses L, Gwaltney-Brant SM. Serotonin: a review. J Vet Pharmacol Ther. 2008 Jun;31(3):187-99.

[11] Kahathuduwa CN, Dassanayake TL, Amarakoon AMT, Weerasinghe VS. Acute effects of theanine, caffeine and theanine-caffeine combination on attention. Nutr Neurosci. 2017 Jul;20(6):369-377.

[12] Kimura K, Ozeki M, Juneja LR, Ohira H. L-Theanine reduces psychological and physiological stress responses. Biol Psychol. 2007 Jan;74(1):39-45.

[13] Rempel V, Fuchs A, Hinz S, et al. Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55. ACS Medicinal Chemistry Letters. 2013;4(1):41-45.

[14] Woodbury A, Yu SP, Wei L, García P. Neuro-Modulating Effects of Honokiol: A Review. Frontiers in Neurology. 2013;4:130.

[15] Boger DL, Henriksen SJ, Cravatt BF. Oleamide: an endogenous sleep-inducing lipid and prototypical member of a new class of biological signaling molecules. Curr Pharm Des. 1998 Aug;4(4):303-14.

[16] Coyne L, Lees G, Nicholson RA, Zheng J, Neufield KD. The sleep hormone oleamide modulates inhibitory ionotropic receptors in mammalian CNS in vitro. British Journal of Pharmacology. 2002;135(8):1977-1987.

[17] Srinivas NR. Baicalin, an emerging multi-therapeutic agent: pharmacodynamics, pharmacokinetics, and considerations from drug development perspectives. Xenobiotica. 2010 May;40(5):357-67.

[18] Wang F, Xu Z, Ren L, Tsang SY, Xue H. GABA A receptor subtype selectivity underlying selective anxiolytic effect of baicalin. Neuropharmacology. 2008 Dec;55(7):1231-7.

[19] Costello RB, Lentino CV, Boyd CC, et al. The effectiveness of melatonin for promoting healthy sleep: a rapid evidence assessment of the literature. Nutrition Journal. 2014;13:106.

[20] Reiter RJ, Tan DX, Mayo JC, Sainz RM, Leon J, Czarnocki Z. Melatonin as an antioxidant: biochemical mechanisms and pathophysiological implications in humans. Acta Biochim Pol. 2003;50(4):1129-46.

[21] Gong X, Yue K, Ma B, Xing J, Gan Y, Wang D, Jin G, Li C. Levo-tetrahydropalmatine, a natural, mixed dopamine receptor antagonist, inhibits methamphetamine self-administration and methamphetamine-induced reinstatement. Pharmacol Biochem Behav. 2016 May;144:67-72

[22] Liu TT, Qu ZW, Qiu CY, Qiu F, Ren C, Gan X, Peng F, Hu WP. Inhibition of acid-sensing ion channels by levo-tetrahydropalmatine in rat dorsal root ganglion neurons. J Neurosci Res. 2015 Feb;93(2):333-9.

 [23] Halaris A, Plietz J. Agmatine: metabolic pathway and spectrum of activity in brain. CNS Drugs. 2007;21(11):885-900.

[24] Xu W, Gao L, Li T, Shao A, Zhang J. Neuroprotective role of Agmatine in Neurological Diseases. Curr Neuropharmacol. 2017 Aug 8

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