Sleep

Nootropics and smart drugs that support, and promotes, sleep quality. A collection listing all nootropics and smart drugs tagged under sleep.

sleep nootropics tag

OverviewBenefits and EffectsMechanism of ActionDosageSide EffectsLegal StatusUser Experience


Summary: Phenibut is a a GABAergic agent that works on the GABA neurotransmitter distinctly reducing anxiety. It also lessens depression, and PTSD symptoms, improving sleep, and providing an overall feeling of ease and well-being. Due to the euphoric-like effects it offers, users prefer to stick to occasional use rather than frequent in respect of its abuse and addiction risk potential.

Phenibut Video TTS

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Overview

What is Phenibut?

Phenibut might not have as widespread use as other nootropics on the market. However, it has demonstrated numerous benefits over tens of decades through both formal studies and anecdotal documentation. It's a nootropic designed to simulate the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts on the central nervous system. It marketed as a psychotropic with a positive effect on mental capability and improved neurological functioning. The anxiety diminishing effects of phenibut are the most praised of all its attributes. Once anxiety is resolved, natural sleep patterns and enhanced cognitive processes shortly start following.

Phenibut was invented in the Soviet Union almost half a century ago. A fascinating, documented anecdote reveals that Russian cosmonauts were supplementing with phenibut especially during the 1975 mission Apollo-Soyuz at the joint of the USSR and US. It remains in use to date in Russia as a treatment and remedy to many conditions including anxiety, depression, prevention of motion sickness, even alcohol withdrawal syndrome, to name a few. Not to mention, of course, its nootropic attributes.

Phenibut dosage
Phenibut Skeletal Structure

Phenibut, sold under the brand names Anvifen, Fenibut, and Noofen among others, is a central nervous system depressant with anxiolytic and stimulant effects which is used in the treatment of anxiety, insomnia, and for a variety of other indications.

Wikipedia


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Benefits and Effects

What Are Phenibut Benefits?

  1. Reduces Anxiety and Stress Levels
  2. Increases Sociability
  3. Promotes Healthy Sleep Patterns and Quality
  4. Improves Symptoms of ADHD
  5. Promotes better sleep quality
  6. Neuroprotective: it prevents damage to neuronal cells under stress
  7. Increases Sociability and Enhances Mood

Supporting Research:

Reduces Anxiety and Stress Levels

Anyone who suffers from anxiety knows that it can be extremely hard to control, it’s not just something that can simply be ‘switched’ off. When taking Phenibut, you will be able to gain more control. Once administered, you can expect to feel more relaxed and composed.

This attribute is the most appreciated benefit of phenibut which is documented by Izyaslav Lapin (R). Anxiety is often the result of overactivity in brain's concentration and overthinking and analyzation of unnecessary, or irrelevant matters; often with the inability to realize the direction to which the train of thought is heading. Turning down and resting the continuous and distracting neuron processing frees the negative thought preoccupation which in turn opens a fresher, vibrant, and often productive range of possibilities.

Increases Sociability

The anxiolytic effect leads to openness towards social interaction which by itself is an issue almost always associating with anxiety disorders. Studies suggest phenibut to be a promoter of enhanced cognitive processing, but the fundamental reason practically still due to the anxiety relief. Those seeking to improve interaction in social settings report better results with the supplement in comparison with alcohol or prescription medication such as benzodiazepines. While attempted anxiety-reduction using traditional tranquilizers often lead to drowsiness and reduction in motor skill and cognitive ability, phenibut seems to mitigate the feelings, except without the associating and undesired side effects that associate with traditional prescription medication. [R]

Promotes Healthy Sleep Patterns and Quality

People living through the depression, anxiety, stressful life events, while going through hormonal changes such as menopause, often report degenerating sleep quality, sleep disturbance, and insomnia. While melatonin is a remarkable and beneficial supplement to consider, some require pharmaceutical sleep aid for more sedating and sleep-inducing effects. Lack of continuous quality sleep can cause an impairment in cognitive processing, opening the way to more anxiety and more sleep disturbance. Used consciously, Phenibut an excellent supplement that can restore significant, natural sleep patterns, duration, and quality. The ability to fall asleep, remain asleep, maintaining an extended period of healthy, rejuvenating deep sleep is attainable with phenibut. [R] [R]

May Improve ADHD

Since phenibut improves attention, it may also help with ADHD symptoms. In one clinical trial of 50 children with ADHD, it improved cognition, self-control, sustained, attention, and memory after 1 month (500-700 mg/day). One month is a short time for evaluating ADHD effects; long-term studies need to determine if the beneficial effect can be sustained. – Selfhacked

My Thought on That

Well I am ADHD and have taken Phenibut and similar “GABA-acting” drugs, such as gabapentin for about a year. Its interesting that, at the time, I had not been diagnosed with ADHD yet and was not aware nor had a clue what ADHD is. I self-medicated with gabapentin and phenibut along the way, and now years later, looking back at how routinely I was taking it, I realize the reason I was hooked and amazed by it was its effect on me as an ADHD, prior to any anxiety triggers that might associate. It was a transformative medication – but overtime, mister W (withdrawals) had been sitting and just waiting for me to get off it in order to introduce himself – and that horrible experience was almost equally as transformative.


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Mechanism of Action

How Does Phenibut Work?

Gamma-aminobutyric acid (also known as GABA) is the chief inhibitory neurotransmitter in our central nervous system.The blood-brain barrier makes supplementing with GABA close to being ineffective due to its inability to bypass the blood-brain barrier. However, phenibut crosses the barrier due to the addition of the phenyl group molecule. Once in the brain, it slows the neuronal excitability, resulting in the effects as mentioned earlier.

GABA frees up channels in the neurons, reduces the function of other neurotransmitters, and diminish collective fears and anxieties in the neuron. It remains vague whether or not phenibut binds to the GABA receptor, although some studies suggest that it only does so in high concentrations.

Lapin’s research found that phenibut increases the levels of dopamine as well. Dopamine is another vital neurotransmitter in the central nervous system. It regulates emotions and creates the reaction of what we call motivation.

More from the Web

In order to affect one’s cognitive functioning, mood, and overall relaxation levels, this supplement needs to cross the blood-brain barrier. GABA cannot effectively do this, while Phenibut can. This is due to a phenyl group that is attached to GABA’s structure.

Naturally, GABA balances out the effects of chemicals that stimulate neurons. When neurons are overstimulated, this can lead to feelings of anxiety and restlessness. Since Phenibut works like GABA, it helps to restore this balance.

The result is neurons firing only when they’re supposed to. Once Phenibut reaches the brain, it targets GABA receptor sites.

It is believed that Phenibut is non-selective, as it stimulates both GABA-A and GABA-B receptors. This allows you to feel a sense of relaxation, lessening anxiety. This is fairly different than other nootropic supplements, which is why it’s beneficial in a stack.

Phenibut also stimulates dopamine receptors, which is key in terms of your mood. Once dopamine is increased, you will experience a more positive mood. Users also tend to experience high levels of motivation, allowing them to achieve more.


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Dosage

How to Take Phenibut?

Phenibut is a potent compound. Start at the lowest effective dose and monitor your response to it, then adjust according to your needs. A dose of 250 mg is a good starting point for first-timers with no tolerance. 500 mg would be ideal in my opinion.

Phenibut effects build up gradually, so avoid taking a second dose without a reasonable timeframe in between. Initial kick-in is around 45 minutes after consumption, and optimal peak effect is usually 2 hours later.

Phenibut is GABA (the major calming neurotransmitter in your brain) with a phenyl ring attached, which allows the molecule to pass your blood-brain barrier and reach receptors in your brain. Phenibut was originally developed for Russian astronauts, to ease the stress of flight and help them sleep in space. It relieves anxiety and drives you into deeper sleep. Phenibut is also a nootropic: it boosts cognition, giving you relaxed clarity of thought.

For people trying to figure out which capsules to buy, here's how much phenibut I can pack into each capsule size (using liftmode fine crystals phenibut HCL powder):

Terms:

“Packed body” is when you press as much powder as you can into the long inner portion of the capsule.

“Entirely packed capsule” is when you pack the cap (top) of the capsule and the body of the capsule as tightly as you can while still being able to close it to the point of “popping” together.

Size 000

Packed body: ~1100-1150
Entirely packed: ~1200-1250

Size 00

Packed body: ~800 mg
Entirely packed: ~850 mg

Size 1

Packed body: ~410mg
Entirely packed: ~430mg

Dave Aspey on Phenibut

Phenibut can be addictive, so it’s very important to take it correctly. The two common mistakes people make are taking phenibut daily and increasing the dose over time. Phenibut’s effects last for 48-72 hours, so you only want to take it once every three days (twice a week max).

You also want to cycle it to avoid tolerance. Go two weeks on phenibut, two weeks off. Don’t go past 250 mg doses; if you stop feeling the effects at 250mg, cycle off for a couple weeks. Don’t mix phenibut with alcohol, either. It amplifies the effects, which can be dangerous.

Dose: 250 mg (never higher)

Time: Anytime, but only twice a week max (Monday and Thursday, for example).

Do two weeks on phenibut, two weeks off.

Dave Asprey


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Side Effects

What Are Phenibut Side Effects?

Like anything we put inside our body, the best source of measurement and criticism is the human body itself. To avoid adverse effects, start at a low dose and see your body's reaction and adaptation to it.

Often individuals report dizziness and drunk-life sensation as a side effect. On the other hand, many people use to supplement with phenibut for the very same impact.

The experience is entirely subjective. Rarely users report fatigue, nausea, and stomach discomfort. People on epilepsy medication or MAO inhibitors are advised to consult a professional doctor before taking phenibut. Alcohol should be consumption should cautiously within reasonable limits ion due to the synergistic effects of alcohol and phenibut.

Avoid taking on a daily basis.

Phenibut has high abuse potential. If taken regularly, be mindful of possible withdrawal effects upon discontinuation. It's wise to limit intake to once or twice a week. Thereby maintain a low tolerance, enjoy its benefits, and avoid building a destructive habit of use. Do not underestimate the power of phenibut and do your research if you decide to include it in your stack.


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Phenibut Withdrawals

Important and useful resource on phenibut usage, abuse, withdrawals, and much more can be found on reddit's phenibut sub. Please use with caution.

It is very important to be aware of the possible withdrawal effect upon discontinuation of phenibut which can be mild to wild, depending on whether or not it has been abused or not, the dosage, period of use, amongst other things. An example from the wilder end is the following opinion, from a long-time, high-dose phenibut (ab)user:

In my experience it is the worst feeling ever. If you had problems in your life anyway, and were using Phenibut to mask them, then they will come back twenty times as bad. Withdrawal strips away any optimistic delusions the Phenibut might have given you, and puts you into a state of intense ‘depressive realism'. You see things seemingly for how they are, and find it physically impossible to believe in potential hope of a miracle happening. You are forced to confront the crushing hopelessness of your situation. Any optimism you remember from your Phenibut days seems like meaningless self-delusion. Regrets and doubts multiply. You start planning for the worst, expecting the worst.

Waking up at 3am every morning after ultra-depressing dreams, your energy reserves are depleted. Your range of vision widens so you can see out of the corners of your eyes, like a prey animal. It feels like there are cold, damp, grey clouds above your eyes. Vision becomes blurry and you feel old. Smiling becomes physically impossible and fake. Breathing is difficult, you can hold your breath for a long time before having to force yourself to take a big, stressful gulp of air. You may get audible hallucinations, such as hearing a chorus of a particular song repeated over and over again, almost mockingly loudly, when you lie in bed. Things like tooth pain that were masked with GABA are felt again. If you were worried about balding, your scalp will feel cold. Your worst fears will be played upon, as if by a demon, and exaggerated. You find it easy to believe in Hell, but impossible to believe in Heaven.

It gets worse for the first three days, then stays bad, becomes manageable by the end of the first week of cold turkey, though you stay melancholy for about two more weeks. This is based on having taken a relatively high dose daily for several months. With more sensible dosage, the withdrawal will be far milder.


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Phenibut Warnings

The following reddit page is valuable for anyone using or planning to use or stop phenibut:

  1. Phenibut Warnings
  2. Phenibut Dependence
  3. Phenibut Overdose

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Legal Status

Is Phenibut Legal?

Australia and Hungary

As of 2018, Phenibut is not a controlled substance in any country apart from Australia and Hungary.

In 2015, it was suggested that the legal status of phenibut in Europe should be reconsidered due to its recreational potential.

In February 2018, the Australian Therapeutic Goods Administration declared it a prohibited (schedule 9) substance, citing health concerns due to withdrawal and overdose. [R]

As of 14 November 2018, Hungary added phenibut and 10 other items to its New Psychoactive Substances ban list. [R]

Dubai, Abu Dhabi, UAE

While the subject on nootropics is quite a grey area, Phenibut as per the law is unregulated. This means that it is not illegal to posses for personal use, however, it is not permitted for retail sale. If you order Phenibut from oversees, if has a chance of being siezed by customs, but that won't be an issue of serious importance where customs will be on the lookout for the person who ordered Phenibut to Dubai/Abu Dhabi/UAE. That wouldn't be something to worry about as far as you are placing an order (aside from the risk of losing your money due to siezing), however, it is an issue for companies importing the product from manufacturers for reproduction and sale. We have had a handful of manufacturer shipments siezed by customs in Dubai which caused us to remove Phenibut from our inventory. However, every now and then, we do manage to restock it, so if you are looking to order phenibut within the UAE, shipped locally which guarantees the delivery of product as well as cash on delivery to eliminate risk, you can check our store for Phenibut 250mg capsules availibility.

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User Experience

This is one of the most interesting user experiences I've read on Phenibut. It was posted by on Phenibut sub-reddit:

Reddit Review

We all love phenibut. It removes our social anxiety (which everybody has nowadays), removes inhibitions we have as humans, removes a mental condition we didn't know we had before the use of this substance, makes us more motivated so we can focus on tasks.

Phenibut is a substance which is very handy to treat all of this. You can use it for the rest of your life. You will have continuous anxiolysis, but the motivational aspects will disappear. This is because of a down-regulation of GABA-B on the lesser hand and especially down-regulation of your dopamine receptors. It's called tolerance.

I was 3 years addicted and I have a long road of nootropic use behind me. Herbal extracts, synthetic nootropics, soft- and hard drugs… Some to get high, others to make me smarter and others to remove phenibut tolerance. But 99% of these maybe 100+ compounds I used really helped.

However I discovered 2 very useful substances on my long road.

First of all, memantine. It's an Alzheimer's medication. It works as an NMDA-antagonist. NMDA receptors are receptors in your brain part of the glutamate system, used for learning and memory. These are said to reverse tolerance for stimulants such as caffeine and amphetamine. Phenibut can be classified as a relaxant and stimulant, and while it has like all the other stimulants tolerance problems, NMDA antagonists come in handy to reduce this. Various reports of people you can find on the internet indeed back this claim up. Other compounds who work in this system are ketamine, DXM (cough surpressant), MXE and N20. We also call these compounds dissociatives. Memantine is dissociative in higher doses as a recreational drug but for Phenibut it's more suited in 1-10mg doses for tolerance reduction. It's also a dopamine agonist. You read that good: an NMDA-antagonist (reduces tolerance for dopaminergic stimulants) and dopamine antagonist. So memantine is a stimulant while reducing tolerance for stimulants. In my use of this substance I learned this: start low – with 1 mg to begin with. Because memantine is also a nicotinic acetylcholine receptor, it can have anti-nootropic effects the first week while starting. This may contribute to initial worsening of cognitive function during early memantine treatment and is the reason why many people don't take memantine for longer than I week and why you can't find many succesful reports on the internet. I was very succesful in doing this but had to way for minimum 2 weeks. Memantine is also the best in the 2 chemicals I describe in the post when comparing price/efficacy. You can find 10 grams for €75 on the internet (contact me when interested).

The other succesful substance I used is fasoracetam. It's a nootropic in the racetam family. Some other nootropics in this family are piracetam and aniracetam. 2 famous nootropics known for there ability to increase blood flow in your brain and make you more sharper. But only fasoracetam has the ability to increase GABA-B receptors in the brain. It's no GABA-B agonist and no GABA-B antagonist. This is good to know because GABA-B antagonists have a negative on your ability to relax in the beginning and are dangerous in general (because they can damage your nervous system). GABA-B antagonists don't know as far as I know, so this is purely hypothetical. Just wanted to say fasoracetam is an ideal substance. Fasoracetam is more expensive compared to memantine, I can find 10 grams on the internet for €60. Since you need to use higher doses (10-50mg) it will cost you more.

Because of my discovery of these substances and success with it, I decided to be a social butterfly and highly motivational person for the rest of my life. I decided it long before I discovered this, but I couldn't make it true because of the disappearment of phenibut's effects. I hope I stay them for the rest of my life.

My current method? I make 000 capsules which hold approximately 800mg powder. With a weighing scale I weigh 100g phenibut, 2.5g fasoracetam and 0.5g memantine. Then I mix it. By doing this I get a nice mixture of these powders. Be aware, people will say this is not 100% mixed because you do it manually. But this is not a huge problem, it's not really a bad thing if you get sometimes 1 mg memantine and other times 3 mg memantine. If you want to do it more precisely, you can buy a super accurate weighing scale and put 1mg memantine every morning under your tongue. But you lose the comfort of easy dosing.

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Conclusion

Phenibut is a useful anxiety-relieving supplement that does not cause the infamous drowsiness often accompanying anxiety medication. It is well-studied and standing amongst the top in line when it comes to anxiety relief, sleep regulation, and cognitive improvement.

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Frequently Asked Questions

What is Phenibut?

Phenibut, sold under the brand names Anvifen, Fenibut, and Noofen among others, is a central nervous system depressant with anxiolytic and stimulant effects which is used in the treatment of anxiety, insomnia, and for a variety of other indications.

Where can I buy Phenibut?

Based off my experience, I'd only only tried and therefore recommend Nootropic Depot's Phenibut. But you can simply search online and make your choice from the different vendors. And make sure you research those vendors too, before actually making a purchase.

Is Phenibut Legal?

As of 2018, Phenibut is not a controlled substance in any country apart from Australia and Hungary.

In 2015, it was suggested that the legal status of phenibut in Europe should be reconsidered due to its recreational potential.

In February 2018, the Australian Therapeutic Goods Administration declared it a prohibited (schedule 9) substance, citing health concerns due to withdrawal and overdose.

As of 14 November 2018, Hungary added phenibut and 10 other items to its New Psychoactive Substances ban list.

How long does the effect of Phenibut last?

The average half-life of phenibut is around 5.3 hours. The peak effects of phenibut can take four to six hours to appear when it's taken orally, although the effects are felt on average around two hours after it's taken and usually you will feel it for more than 6 hours.

How to take Phenibut?

Start at the lowest effective dose (250mg) and monitor your response to it, then adjust according to your needs. A dose of 250 mg is a good starting point for first-timers with no tolerance. 500 mg would be the ideal in my opinion.

Phenibut effects build up gradually, so avoid taking a second dose without a reasonable timeframe in between. Initial kick-in is around 45 minutes after consumption, and optimal peak effect is usually 2 hours later.

How long does it take Phenibut to kick in?

Phenibut has a long onset time of around 1.5 – 2 hours until its peak effect, for most people. The time that it takes to kick in depends on the amount of food in your stomach, your metabolism, the dosage, and how you took it. Taking Phenibut sublingually results in a faster onset time that taking it with water or juice.

How much Phenibut should I take?

For first-time, 250mg, If you're experienced and know well enough about it, you can take 500mg. The best approach is to start low and see how you react to it, and increase accordingly if needed. But keep in mind that it takes around an hour and a half to be felt, so make sure you keep about 2 hours interval between doses.

How can I buy Phenibut in Dubai?

If you'd like to buy phenibut in dubai or abu dhabi, as well as get more information about nootropics, availibility, and more, go to the “Nootropics in Dubai” page under the resources tab on the menu. Alternativley, you can click here

Is Phenibut Legal in Dubai, UAE?

White the subject on nootropics is quite a grey area, Phenibut as per the law is unregulated. This means that it is not illegal to posses for personal use, however, it is not permitted for retail sale. If you order Phenibut from oversees, if has a chance of being siezed by customs, but that won't be an issue of serious importance where customs will be on the lookout for the person who ordered Phenibut to Dubai/Abu Dhabi/UAE. That wouldn't be something to worry about as far as you are placing an order (aside from the risk of losing your money due to siezing), however, it is an issue for companies importing the product from manufacturers for reproduction and sale. We have had a handful of manufacturer shipments siezed by customs in Dubai which caused us to remove Phenibut from our inventory. However, every now and then, we do manage to restock it, so if you are looking to order phenibut within the UAE, shipped locally which guarantees the delivery of product as well as cash on delivery to eliminate risk, you can check our store for Phenibut 250mg capsules availibility.

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Further and Related Readings

  1. If you're intrigued by Phenibut, you might like and find Fasoracetam quite interesting too due to the two nootropics interaction. You may also find Agmatine Sulfate & Sunifiram worth exploring.
  2. Reddit's Phenibut Endless Information (from first-hand experiences)
  3. PhenibutWikipedia
  4. Nootropics Information Frequently Asked Questions

FDA on Phenibut

Phenibut is a substance that does not meet the statutory definition of a dietary ingredient.

The Federal Food, Drug, and Cosmetic Act (FD&C Act) defines a dietary ingredient as a vitamin; mineral; herb or other botanical; amino acid; dietary substance for use by man to supplement the diet by increasing the total dietary intake; or a concentrate, metabolite, constituent, extract, or combination of the preceding substances. Because phenibut does not fit any of the categories of dietary ingredients under the FD&C Act, any dietary supplements that declare phenibut as a dietary ingredient are misbranded.

Phenibut is also known as:

  • fenibut
  • phenigam
  • PhGaba
  • Phenigamma
  • Phenygam
  • 4-Amino-3-phenylbutanoic acid
  • β-(aminomethyl)benzenepropanoic acid
  • beta-(Aminomethyl)hydrocinnamic acid
  • β-phenyl-γ-aminobutyric acid

Phenibut in Dietary Supplements

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What is Melatonin? Benefits & EffectsMechanism of ActionDosageSide EffectsUser Experiences

Summary: Melatonin plays several roles in the body, including helping to regulate blood pressure, boost immune function, antioxidative, and manages cortisol levels, in addition to regulating the body’s circadian rhythm. That’s why melatonin is often referred to as the body’s sleep hormone.

Melatonin Video TTS

Overview

What is Melatonin?

Melatonin is a multitasking hormone produced by the brain’s pinecone-shaped pineal gland. [R]

Melatonin plays several roles in the body, including helping to regulate blood pressure, boost immune function, and manage cortisol levels. [R] [R]

But melatonin is probably best known for its soporific powers. Chief among its responsibilities is regulating the body’s circadian rhythm so it knows when to rest and when to wake up. That’s why melatonin is often referred to as the body’s sleep hormone.

Benefits and Effects

What Are the Melatonin Benefits?

  1. Regulates Circadian Rhythm and Enhances Sleep Quality
  2. Alleviates Anxiety and Depression Symptoms
  3. A Potent Antioxidant
  4. Supports BDNF
  5. Strengthens the Blood-Brain Barrier
  6. Neuroprotective
  7. Replaces Benzos for Sleep

Supporting Research:

Regulates Circadian Rhythm and Enhances Sleep Quality

Melatonin increases the quality of sleep. The Circadian Rhythm influences the body’s sleeping habits. Think of it as a built-in clock that controls our bodies processes 24 hours a day. Scientists have observed that Melatonin normalizes the Circadian rhythm which can sometimes become distorted due to modern lifestyle. [R]

Alleviates Anxiety and Depression Symptoms

Conditions like depression and anxiety usually worsen by a disturbed, intermittent or a lack of a sleeping pattern. Having these disturbances regulated can alleviate the symptoms of these conditions, not mainly offering a cure but by far offering an improvement in the standard of life. [R]

Melatonin is a Potent Antioxidant

Antioxidant enzymes roles within our bodies are to help clean the cells in our bodies and filter our bloodstream from harmful cells. Melatonin increases the rate at which our body produces these enzymes that would be naturally. These molecules in question can also bond to what is called Reactive Oxygen Species (ROS) & Reactive Nitrogen Species (NOS) which can decrease the level of damage each of these can cause respectively.

The benefits directly from this are that Melatonin prevents any harm coming to your organ systems or tissues. These advantages combined make Melatonin a very useful protectorate within your body internally. These antioxidants can also have benefits for the most critical organ in our body, our brain. [R]

Melatonin Supports BDNF

Nerve cells are also protected by the increase of these enzymes produced by Melatonin, having a positive onward affect towards the spinal cord including white matter and optic nerves. Its regeneration is down to something called the ‘Brain-Derived Neurotrophic Factor’ (BDNF); in simple terms, this is a protein responsible for the nerves regeneration and well-being within our brains. [R]

Strengthens the Blood-Brain Barrier

Melatonin strengthens the ever significant barrier between the brain and our blood. If the strength of this barrier were to deteriorate and for example leak, this can lead to cognitive dysfunction (also known as brain fog) and could potentially result in future to conditions such as Alzheimer’s. [R]

Melatonin is Neuroprotectant

In addition to defending against conditions such as Alzheimer’s development, Melatonin can also aid as a coping mechanism for users who have Parkinson’s. Melatonin in tests was shown to prohibit cell death and brain damage, sometimes as a cause of a leaky blood-brain barrier.

Referring back to the regulation of sleep, this can also help people who, however, there is currently no proof it helps with any of the other side-effects of the condition. [R]

Melatonin Replaces Benzos for Sleep

Its widely known that benzos usually depress the natural levels of melatonin within our bodies. Our recommendation is if you are using one of these drugs for sleep, it would be wise to start using melatonin instead. Moreover, start weaning yourself off the benzos. [R]

Mechanism of Action

How Does Melatonin Work?

Melatonin works together with your body’s circadian rhythm. In simple terms, the circadian rhythm is your body’s internal clock. It lets you know when it’s time to sleep, wake and eat. Melatonin also helps regulate your body temperature, blood pressure and hormone levels. [R]

Melatonin levels start to rise in your body when it is dark outside, signaling to your body that it is time to sleep. [R]

It also binds to receptors in the body and can help you relax. For instance, melatonin binds to receptors in the brain to help reduce nerve activity. In the eyes, it can help reduce dopamine levels, a hormone that enables you to stay awake. [R] [R]

Melatonin is controlled by light and darkness. When we’re awake and the sun’s out, we don’t produce any melatonin. But at night, the onset of darkness signals to our pineal gland to release melatonin into the bloodstream. Your melatonin levels begin to increase about two hours before you go to bed, typically around 9 p.m., and peak about five hours later. As melatonin levels rise throughout our body — it’s found in a variety of our organs, including our eyes, bones, ovaries/testes and gut — our body knows it’s time to drift off to Slumber Town. [R]

“The melatonin receptors are named MT1 and MT2, and are G-protein coupled receptors (GPRCs) coupled to Gi proteins (a heterotrimer of α, β, and γ that dissociates into α and βγ when the receptor is activated). These two receptors are quite different from each other, as they structure pharmacological characteristics and chromosomal location, yet both have high affinity for melatonin. A third ‘receptor' exists, known as MT3, but it is not a GPRC like MT1/2. Due to the cytoplasmic protein quinone reductase II having the same melatonin binding properties as ‘MT3', and deletion of quinone reductase II causing ‘MT3' to disappear, MT3 may just be quinone reductase II.” – Examine.com

Dosage

How To Take Melatonin?

You’ll see melatonin recommended in a range of doses, starting at around 0.5 milligrams up to 10 milligrams for people with sleep disorders, with the most common dosage being around 3 milligrams.

But even this is probably way more than you need.

You’re better off basing your melatonin intake on increments that mirror how much melatonin our bodies produce at night. According to clinical studies, the optimal dose is 0.3 milligrams. [R]

Melatonin Overdose

Even though the overwhelming verdict is that melatonin is safe, you can have too much of a good thing. Overdosing on melatonin has not been shown to be fatal, but it can produce the aforementioned side effects, like dizziness and grogginess. In one known case, after taking 24 milligrams of melatonin, a man became lethargic and disoriented, but returned to normal and did not continue to have issues once he lowered his dosage.

In addition, large doses could potentially cause amenorrhea (skipped periods) in women, due to it suppressing gonadotropin-releasing hormones, but if you can easily remedy this side effect by simply stopping your supplements. [R]

Side Effects

Are There Side Effects to Melatonin?

Overall, the side effects of melatonin are pretty harmless. Unlike other sleep aids, like benzodiazepines and z-drugs (think: Ambien and Lunesta), it does not cause dependence or withdrawal symptoms. [R]

The most commonly reported side effect is daytime drowsiness. Other side effects include nausea, headache, and dizziness. [R]

If course, if you’re taking other medications, you should check with your physician before popping a melatonin. It has been known to interact with some antidepressants, blood pressure medications, sedatives, antibiotics, and antihistamines. [R]

Up to 240 mg and 500 mg oral and intravenous injections of melatonin taken acutely is not associated with any toxicological effects. [R]

A handful of large scale, 6-12 month studies, suggest continued administration of melatonin does not result in tolerance. – Examine.com

Conclusion

There's great amount of evidence suggesting as well as proving the benefits of supplementing with melatonin whether for sleep purposes or overall general health. Best practices when supplementing with melatonin for long-term benefits is to take a microdose of 300 mcg on daily basis before bedtime.

This microdose will serve a host of benefits most noteworthy of which is antioxidation and supporting mitochondria and antioxidation.

Many Nootropic focused companies are now aware of this and its benefits and so finally starting to see products in microdoses such as Nootropic Depot's, which I have personally been using for a long time. Prior to which, I tried a couple of different products at the doses of 3 mg and it made me very heavy and groggy for a long time.

User Experience

Reddit Review

A reddit user documented his experience after 2 years of using microdose of melatonin as recommended alongside magnesium, and his realization of how beneficial it had been working for him after he stopped.

I took Magnesium Citrate (200-400mg) and Melatonin (0.3mg) both every night for over 2 years and thought they didn't make much difference in my sleep. It turned out to be very wrong – I now remember how poor my sleep was 3 years ago, before starting to take them. I wake up from the slightest noise and can't go back to sleep for many hours afterwards – even if I wake up after only 4 hours, I would need to wait 3 hours before I fall asleep again, without Magnesium and Melatonin. This has been this way since I was a child. I find Melatonin is better for actually falling asleep initially, while Magnesium is better for maintaining quality sleep afterwards.

Second Reddit User Experience

I have learned the same lesson with melatonin in that less is more. I took 30 mg one evening and had very unsettling and vivid dreams. Not restful at all. I find 5 mg timed release works well. If you are interested in another natural sleep / relaxation aid, I have had success with Red Bali Kratom.

Further and Related Readings

From the blog: Melatonin for Sleep: How Effective Is It?

Wouldn’t it be great if you could pop a pill for better sleep? A pill that’s non-habit-forming, doesn’t require a prescription, and doesn’t make you do strange things like eat in your sleep? Well, maybe you can. While more satisfying zzz’s in pill form sounds too good to be true, there’s promising evidence that melatonin, the naturally occurring hormone in our bodies, can be harnessed as a supplement for better sleep.

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Pending review. Contribute to this article.

OverviewBenefitsMechanisms of ActionDosageStackSide Effects

Summary: Picamilon is a nootropic that enhances cognitive function and increases mental energy while reducing stress and anxiety. Its unique blend of energizing and relaxing impacts makes picamilon an outstanding supplement for learners during examination periods or anyone in stressful circumstances who could benefit from faster, clearer thinking.

Overview

What is Picamilon?

Picamilon is a distinctive nootropic that enhances cognitive function and increases mental energy while reducing stress and anxiety emotions. Its unique blend of energizing and relaxing impacts makes picamilon an outstanding supplement for learners facing examinations or for anyone in stressful circumstances who wants to think rapidly and clearly.

Picamilon's unique traits make it a truly distinctive supplement. It boosts brain function like all nootropics, enhancing memory, concentration, motivation, the span of attention, and overall productivity. However, its energizing impacts are only half the image; it also calms, relaxes, and generates a tranquilizing effect that decreases stress and anxiety emotions considerably.

This combination of energizing and calming effects, along with its low price, prepared accessibility, and absence of severe side effects, makes picamilon an increasingly common option for anyone who wishes to handle stress and anxiety while maximizing their cognitive skills.

Picamilon was first created in Russia somewhere between the years 1969 and 1971 as part of the Institute's studies into possibly performance-enhancing substances.

Today, picamilon is a prescription drug in Russia and is used to treat a range of conditions and disorders ranging from depression to migraine, neuroinfections, senile psychosis, certain kinds of glaucoma, and even acute intoxication with alcohol.

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Benefits and Effects

  1. Improves Learning and Memory
  2. Supports Concentration, Focus, and Mental Stamina
  3. Mood Stabilization
  4. Relaxes Without Causing Drowsiness
  5. Reduces Blood Pressure
  6. Improves Sleep Quality

Supporting research:

Improves Learning and Memory

The wide variety of impacts of Picamilon includes both cognitive enhancement and mood management. It has been shown to promote faster and more comfortable learning pace as well as enhancing both memory retention and recall speed.

Supports Concentration, Focus, and Mental Stamina

By stimulating better blood flow and circulation in the brain, picamilon has critical beneficial impacts on a broad range of cognitive functions, including improving the capacity to concentrate on thinking and improving general mental energy or endurance.

Mood Stabilization

It has been shown that Picamilon has substantial anti-anxiety impacts, significantly decreasing stress effect. It can also assist relieve depression.

Relaxes Without Causing Drowsiness

Users report that taking picamilon outcomes in a pleasant sensation of relaxation without mental fog or grogginess that is usually associated with sedatives or tranquilizers. Most individuals say it provides them a feeling of “calm energy.”

Reduces Blood Pressure

While not positive in all instances, the capacity of picamilon to decrease blood pressure can be a significant advantage to those with hypertension that is enhanced by stress and anxiety.

Improves Sleep Quality

While a single supplement seems contradictory to increase energy and create rest better, many picamilon consumers claim it does just that. Since it is not a tranquilizer, sedative, or muscle relaxer, this impact could be due to the stress reduction and anti-anxiety characteristics of picamilon insignificant portion.

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Mechanisms of Action

Picamilon is a mixture of niacin and GABA or gamma-aminobutyric acid, two prevalent but essential nutrients. Separately each plays a critical role in brain health but linked to produce unique advantages in a compound that they respond synergistically.

Picamilon’s real strength is the capacity of the niacin element to cross the blood-brain barrier, a semi-permeable capillary filter intended to safeguard the brain and to bring with it the connected GABA element. As a result, GABA, a powerful neurotransmitter that can not cross the blood-brain barrier alone, is transferred into the central nervous system for use across the brain and body.

The real mechanism of action picamilon operates through is both fast and direct. It is a water-soluble compound that is easily absorbed and within an hour of ingestion reaches peak bioavailability.

Picamilon is hydrolyzed or chemically divided back into distinct parts of niacin or nicotinic acid and GABA after crossing the blood-brain barrier. The role of niacin acts as a vasodilator, increasing blood flow in the brain and enhancing oxygen and other nutrients absorption. At the same moment, this vital inhibitory neurotransmitter, which operates by decreasing neuronal excitability, raises the brain concentrations of the GABA element.

The cognitive enhancement impacts of Picamilon can be primarily ascribed to the enhanced effectiveness created by the improved circulation of the brain blood and oxygen absorption. The enhanced blood flow in the brain also enhances the delivery and uptake of glucose and other nutrients, which can boost alertness, concentrate, motivation, and brain energy as a whole. It is also thought to have an essential antioxidant impact that helps break down and remove toxins in the brain.

Picamilon's relaxing and calming impacts are produced by the enhanced concentrations of GABA, a powerful neurotransmitter that operates by inhibiting neuronal firing, decreasing stress and anxiety emotions by generating a slightly sedative impact.

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Dosage

How To Take Picamilon?

Although picamilon is usually deemed well tolerated and has no severe side effects, it is a potent complement and should be used responsibly. It is wise, as with all supplements, to begin with, the smallest effective dosage possible and gradually boost as required.

Recommendations for daily dosage differ significantly, depending on the special effects you hope to experience in no small measure. Typical is a cumulative dosage of 50 to 400 mg per day, with most customers finding efficacy between 100 and 200 mg divided over two to three doses. However, it may be best for those mainly interested in cognitive enhancements of picamilon and lower dosages of overall mood stabilization, while those looking for significant rises in energy levels may want to create up to higher dosages.

Picamilon operates comparatively fast and is relatively durable. Users say that impacts are usually visible within one hour of intake and last for 4 to 6 hours. It is water-soluble and can be taken on an empty stomach in either capsule or powder form.

While some users prefer cycling picamilon with other nootropics with an anti-anxiety element, there is no negative impact of proof taking it daily.

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Stack

Picamilon can be taken alone daily, cycled with other supplements or combined with other nootropics in many ways.

The behavioral improvement characteristics of picamilon will be potentiated in a pile with racetam-class nootropics such as piracetam or pramiracetam. However, depending on which racetam supplement you are combining with picamilon, you may also experience, or both, increased energy or relaxation effects.

Combined with ampakine racetam supplements like aniracetam and oxiracetam, both of which have stimulant characteristics, the energy-boosting and mood-modulating impacts of picamilon will be increased.

Some users claim that combining picamilon with other supplements such as kava can boost their energy-producing characteristics while using it in conjunction with relaxing supplements such as valerian will strengthen their calming aspects.

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Side Effects

Picamilon is usually regarded as safe and well tolerated, but there have been reports of some side effects. The most severe prospective side effect is low blood pressure, so if you understand that you are susceptible to hypotension or have reason to worry about low blood pressure, you should consult a medical practitioner before taking picamilon.  

Allergies and rashes of the skin have been recorded as side effects, but are not prevalent. Such side effects typically include headaches, lightheadedness or dizziness, and nausea. Red skin flushing is also sometimes revealed as a standard and harmless side effect of niacin.

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Conclusion

Picamilon is a natural nootropic, and with excellent reason: it can both energize and relax, it is secure and well-tolerated, it has very few reported side effects, it combines well with other supplements, and it is inexpensive and easily accessible. Picamilon provides advantages that are difficult to beat for anyone who wishes or needs to handle their moods and retain ideal cognitive function under pressure.

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Further and Related Readings

Picamilon in Dietary Supplements (FDA Post on Picamilon):

Picamilon is a substance that does not meet the statutory definition of a dietary ingredient.

The Federal Food, Drug, and Cosmetic Act (the Act) defines a dietary ingredient as a vitamin; mineral; herb or other botanical; amino acid; dietary substance for use by man to supplement the diet by increasing the total dietary intake; or a concentrate, metabolite, constituent, extract, or combination of the preceding substances. In contrast, picamilon is a unique chemical entity synthesized from the dietary ingredients niacin and gamma-aminobutyric acid. Picamilon is absorbed into the body, crosses the blood-brain barrier and accumulates in the brain as a separate chemical entity. Because picamilon does not fit any of the categories of dietary ingredients under the Act, any products marketed as dietary supplements that declare picamilon as a dietary ingredient are misbranded.

The FDA has provided expert testimony to the Oregon Attorney General’s office stating that picamilon is not a dietary ingredient.

Picamilon is used as a prescription drug in Russia for a variety of neurological conditions. It is not approved as a drug in the U.S.

Picamilon is also known as:

  • pikatropin
  • pikamilon
  • nicotinyl-gamma-aminobutyric acid
  • nicotinyl-GAB
  • Recent FDA Action on Dietary Supplements Labeled as Containing Picamilon
  • December 2015

On November 30, 2015, the FDA issued warning letters to five companies whose products marketed as dietary supplements claim to contain picamilon. These products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient.

Under existing law, including the Dietary Supplement Health and Education Act passed by Congress in 1994, the FDA can take action to remove products from the market, but the agency must first establish that such products are adulterated (e.g., that the product is unsafe) or misbranded (e.g., that the labeling is false or misleading).

The companies have 15 business days from the date of receipt of the letter to communicate to the agency the specific steps they will take to bring their products into compliance with the law.

The agency will continue to update this page in the event additional actions are taken related to picamilon.

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melatonin for sleep

Melatonin for Sleep: How Effective Is It?

  • 4 min read
Melatonin is a hormone produced by the brain’s pineal gland. It plays several roles in the body, including helping to regulate blood pressure, boost immune function, and manage cortisol levels.