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Nootropics Phenylpiracetam Racetams

Phenylpiracetam — Stimulant Nootropic: Effects, Dosage & Experiences

Those who spend any amount of time looking into nootropics will be very familiar with the racetam class of nootropics, a group of drugs that are structural derivatives of piracetam. These drugs display variance in the details of their effects, but they all exhibit neuroprotectant and cognitive-enhancing properties.
One of these piracetam derivatives, phenylpiracetam, is appealing to many nootropic users due to its many purported benefits.

Background and Benefits

phenylpiracetam nootropicPhenylpiracetam is frequently cited to display the following effects:[1][2]

  • Memory enhancement
  • Anti-amnesia
  • Antidepressant
  • Anticonvulsant
  • Antipsychotic
  • Anxiolytic

If phenylpiracetam does indeed have these listed properties, its appeal extends beyond just the sphere of nootropics. Any drug with that kind of resume is certainly impressive. Here we will examine this unique substance and its purported effects.

Phenylpiracetam, also known by its Russian pharmaceutical names Phenotropil and Carphedon, was developed in Russia in the 1980s as a piracetam derivative, with the hopes that it would display and expand upon the nootropic properties that make piracetam such a popular drug. Specifically, phenylpiracetam is a phenylated analog of piracetam, meaning that it is essentially a piracetam molecule with a phenyl group attached. Interestingly, some have theorized that phenylpiracetam’s purported stimulant effects may be due to the molecule’s similarity to phenethylamine (and, by extension, amphetamine).

These potential stimulant properties, along with phenylpiracetam’s ability to improve physical stamina, has led to the drug being banned from use in Olympic competitions.[3]

phenylpiracetam-nootropic-stimulant

Dosage, Mechanism, and Effects

Phenylpiracetam is typically sold by online vendors in its pure powder form or as pharmaceutical tablets. Most of these sources sell a racemic mixture of the molecule, but some of the studies done on the effects of phenylpiracetam were conducted using only the R-isomer.

Phenylpiracetam Phenotropil Nootropic
Original Russian Phenylpiracetam (Phenotropil)

A single dose of phenylpiracetam typically ranges from 100200 mg. Most prescription guidelines state that phenylpiracetam can be taken 2-3 times per day, as the drug will exert effects on the body for about 4-6 hours before receding. It should be noted that most anecdotal reports from users indicate that phenylpiracetam builds up a tolerance rather quickly, so it might not be wise to use it for days in a row. That being said, the drug appears to be relatively safe to use regardless of tolerance buildup.

Phenylpiracetam’s mechanism of action still remains largely uncertain. While various studies have been conducted on its effects, few have dealt with the specifics of its pharmacology. However, one study performed on rats found that phenylpiracetam decreased the density of nACh and NMDA receptors in the hippocampus when they had previously been given scopolamine, an anticholinergic drug.

Phenylpiracetam was also found to increase the density of the D1, D2, and D3 dopamine receptors[4]. Dopamine receptors are important for motivation, arousal, pleasure, and memory.

It also appears that phenylpiracetam’s enantiomers have unique effects and properties. Most notably, studies indicate that the R-enantiomer is mostly responsible for its stimulating and cognition-enhancing effects while the S-enantiomer may be more responsible for stopping cognitive decline.[5]

One of the drug’s biggest potential uses is for treating cognitive decline brought on by diseases like Alzheimer’s. Various studies have been conducted in Russia studying the effect of phenylpiracetam on cognitive decline caused by organic causes. These studies found that phenylpiracetam improved the cognition of those with Alzheimer’s disease, and showed minor effectiveness in improving the cognition of patients afflicted with epilepsy. The drug did not, however, appear to improve cognition for those whose cognitive decline was brought on by traumatic brain injury.[6] In a study conducted on 400 patients with ischemic stroke, phenylpiracetam was able to improve cognition when taken at a dose of 400 mg per day for one year.[7]

There is currently no research conducted on phenylpiracetam’s effect on cognition in young, healthy subjects, although anecdotal reports throughout the internet suggest that it does improve cognition among those with no cognitive disorders. One study conducted on rats found that the R-enantiomer of phenylpiracetam was able to enhance cognition, but this result has not been replicated in any study using the racemic mixture.[8]

Zhiliuk, Mamchur & Pavlov[9] found that Phenylpiracetam improves the processes of learning and storing conditional skills when studying cognitive processes and functional state of mitochondria in the neocortex of alloxan-diabetic rats.[10]

Gustov, Smirnov, Korshunova IuA and Andrianova argue that Phenylpiracetam is beneficial to people who develop cognitive deficits and/or depression after encephalopathy and brain injuries.[11] It increased quality of life in patients with encephalopathy after acute lesions (30 people), brain traumas (33 people) and glioma surgery (36 people). The average Mini Mental State Examination (MMSE) scores (a 30-point questionnaire) from baseline improved in all groups. Anxiety improved and depression declined substantially, resulting in less discomfort and better ability to execute everyday activities.[12]

phenylpiracetam memorySome preliminary studies have found phenylpiracetam to have antidepressant properties. However, this area of effect has not seen as much research as the area of cognitive enhancement. A study performed on rats found that when phenylpiracetam was administered to rats, it significantly reduced depression symptoms caused by a forced-swim test.[13] A study conducted on human patients with cognitive decline concluded that phenylpiracetam is able to alleviate symptoms of depression.[14]

Perhaps one of the most unique and attractive benefits of phenylpiracetam is its ability to act as a psychostimulant. However, this effect is not very well researched, although one experiment conducted on rats found that phenylpiracetam increases locomotor activity for upwards of 2 hours.[15]

Anecdotal Reports

As with any nootropic drug that has not seen as much clinical research as one might hope, it is useful to look at anecdotal reports from users to give a fuller picture of the drug’s effects. Obviously, individual user reports are especially prone to the placebo effect and should be weighed and judged by the reader with caution.

Reddit user The_Antagonist said –

At the peak of it’s effects (about an hour in) I feel intense focus, not especially jittery, unless stacked with something else, just pure attention, and a complete abolishment of any lethargy I would have been feeling previously. It’s not really a euphoric compound, but I’ve noticed it seems to make me significantly happier when I’m accomplishing something on it. It might be the racetam effects rearing their head, but solving mathematical problems, or gaining a more complete understanding of a concept just feels plain good. This attribute [in particular], for me at least, makes it a hell of a study drug.[16]

Reddit user Notlambda

I’m not a social butterfly. I’m retarded when it comes to explaining a concept or defending an argument.
On phenylpiracetam (or daily doses of piracetam), I’m a social genius. What it feels like is that I’m not the one saying the words that I’m saying. It’s like I feed a “command” into a register in my brain that is then picked up by whatever part of my cortex deals with speech, and then I find myself just saying the perfect words to explain everything concisely.
It’s like I’m watching somebody else be awesome, but that somebody else is me. It’s really nice because I can free the rest of my mind to think about concepts while the “other” me is doing all the talking.
It’s also very subtle. I’m explaining this like it’s a dissociative experience or something like that. It’s not.[17]

From user le_unknown

I’ve had great results with phenylpiracetam. Without a doubt, it has been the nootropic that works best for me. Gives me alertness (but no jitteriness, I just feel awake and normal – kills all drowsiness), focus, and a tiny mood elevation. I’m surprised I don’t see more people talking about it…[18]

Conclusion

Phenylpiracetam’s seemingly wide array of effects and benefits makes it well worth looking into. Most notably, phenylpiracetam seems to provide many of the benefits of piracetam, while seemingly being more potent or effective in certain areas. Phenylpiracetam seems to noticeably provide cognitive capacity improvement, mood elevation, and stimulation. Experiences will vary widely among individual users, so we would highly recommend you try phenylpiracetam for yourself to see how it works for you.

You can buy Phenylpiracetam in powder form as well as in capsules at NootropicsDepot.

Phenylpiracetam
8
Focus
8
Mood
7
Memory
9
Stimulation
6
Relaxation
8.5
Safety
Reviewer 9

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Nootropics Tutorials

Nootropics: A Beginner’s Guide To Cognitive Enhancers

The realm of nootropic substances (aka cognitive enhancers or smart drugs), at the time around its conception, was reserved for the very select few who had access to these novel cognition-enhancing drugs. In recent years, nootropics have gained more widespread recognition, and are more accessible to average individuals than ever before, thanks to the rising number of online vendors and communities who make these substances accessible for all.

The term “nootropic” has been consistently more and more searched on google ever since 2011 (the year when the film Limitless was released) , and people’s interest in the subject will certainly continue to rise. Although nootropics still maintain a type of “fringe” status in the world of drugs, their infiltration into the mainstream is undeniable.

Nootropic Trend - Google searches of keyword "nootropics"

What is a Nootropic?

nootropic brainCorneliu E. Giurgea, the Romanian chemist who first synthesized piracetam, developed the concept of nootropic substance in 1972.[1] It is a combination of the Greek words “νους” (nous) meaning “mind”, and “τρoπoς” (tropos) meaning “bend” or “change”. This is what nootropics do. Essentially, they positively alter the way in which your mind works.

Nootropic drugs are a specific subtype of psychoactive substances. According to Giurgea, in order for a drug or supplement to be considered a nootropic, it must adhere to the following criteria:[2]

  1. Enhances learning and memory
  2. Enhances resistance of learned behaviors to conditions that will disrupt them
  3. Protects the brain against physical of chemical injuries (such as concussions or neurotoxic drugs)
  4. Increases the efficacy of cortical/subcortical control mechanisms of the brain (such as improving reaction time)
  5. Typically lacks negative side-effects (i.e. sedation), and possesses low toxicity

Though these criteria lay out the foundation for what a nootropic is, most modern definitions are much more general. As a more common definition, nootropics are chemical substances or herbal supplements that enhance cognition and mental function.

Caffeine
Caffeine

If we think in terms of this general definition, there is about a 90% chance you use a pseudo-nootropic substance regularly. Caffeine, the most popular drug in the world, is commonly classified as a nootropic, due to the fact that it is stimulatory and enhances attentiveness linked to cognition, learning, and memory. [3] [4]

Certain substances that don’t explicitly enhance cognition are still sometimes grouped in with nootropics. This would include substances that improve mood, reduce anxiety, or promote an overall feeling of wellbeing. Some examples of these substances are phenibut, sulbutiamine, and ashwagandha. Even if these supplements don’t have mechanisms that directly improve cognition, their mood-improving capabilities will tend to lead to an enhanced ability to focus and think clearly.

Who Uses Them?

Giurgea coined the term “nootropic” after he synthesized piracetam, which is, under Giurgea’s definition, the first substance to display purely nootropic properties. Piracetam has cognitive enhancing and neuroprotective capabilities while also possessing relatively few side effects. [5] Because of this, piracetam is commonly used to improve cognition in individuals who are experiencing the cognitive decline that comes with old age, dementia, or Alzheimer’s.

With the development of piracetam, other nootropic substances were investigated and researched for their applications in those who experience cognitive decline. Many drugs derived from piracetam (referred to as racetams) have been developed in hopes that they would yield even more benefits than piracetam. For instance, phenylpiracetam displays stimulant properties in addition to cognitive enhancement. [6] Likewise, aniracetam works as an anxiolytic. [7]

Modafinil is wakefulness-enhancing nootropic used by college students as a safer alternative to Ritalin and Adderall

Up until the past decade, these kinds of cognitive-enhancing drugs were only used extensively in clinical applications, such as treating cognitive illnesses. However, the past few years have seen tremendous growth in the use of nootropics among younger healthy individuals in hopes that they could improve their performance in work or academic studies. For example – modafinil (Provigil), a wakefulness-promoting nootropic substance, has seen increased usage among college students as an alternative to Adderall, due to the fact that it aids the brain in focusing on tasks for extended periods of time without fatigue. [8]

Many nootropic substances, such as the racetams and tianeptine (an antidepressant nootropic), are prescription drugs in Europe but are unscheduled in the United States. This has led to many of them being sold online by nootropic vendors, making them readily available for those who wish to purchase them.

Not surprisingly, Russia, the country that has developed a large number of nootropics (including Phenibut, Picamilon, Phenylpiracetam, Selank, Semax, Cerebrolysin, Emoxypine and so on), it’s the place where the keyword “nootropic(s)” is most popular in 2016[9], according to Google.

The increasing number and growth of online communities, such as the nootropics subreddit, has attracted the attention of younger individuals who seek to improve their cognitive performance and preserve their youthful cognitive capabilities. These online communities are extremely valuable sources of information on all things related to nootropics. They are open forums where anyone can ask questions about smart drugs and cognitive enhancement and engage in valuable discussion. Many newer nootropic substances have not been extensively tested in clinical settings, but anecdotal user reports can be found within these online communities.

Where Do I Begin?

If you are determined to make a go at nootropic supplementation, then logically the smart thing to do is implement the smartest ways to use smart drugs. You do not have to be a brain surgeon to begin effectively supplementing with nootropics, but understanding at least the bare bones of the foundations of a few related fields like neuroscience, neurology, and drug metabolism, is vital to getting the most out of them.

Ideally, you want a good working understanding of all the major mechanisms of action, including receptor systems involved in memory, mood and cognition (dopamine, GABAacetylcholineserotonin, etc).learning memory nootropics Attempting anything other could end up as catastrophically as fiddling with the kernel of your operating system without knowing how it works. The best way to go about it is to learn what happens to drugs inside the body, how the classic nootropics work (like Piracetam and Aniracetam), and what are some of the basic nootropic stacks.

Even though it can be a bit daunting at first, you will also want to learn how to access & read scientific researchwhat is acetylcholine (the learning and memory neurotransmitter), how it works, how the brain produces it and what is a choline precursor. Learning the major neurotransmitters, understanding the difference between excitatory and inhibitory neurotransmitters, all these are great places to start.

When first getting into the world of cognitive enhancement, the sheer number of substances out there can be very intimidating. Here is a short list that outlines some of the most popular and proven nootropics for beginners.

Wakefulness and Motivation

  • Caffeine and L-Theanine – Promotes wakefulness and is stimulating in general. The addition of L-theanine helps reduce the negative side effects of caffeine, such as anxiety. Additionally, L-theanine also improves cognition.
  • Modafinil, Armodafinil, and Adrafinil – These three compounds are chemically related. Armodafinil is the active isomer of modafinil and is thus generally more potent. Adrafinil is a prodrug to modafinil. In other words, it is metabolized into modafinil by the body. All three of these are used to promote wakefulness and reduce fatigue.
  • Rhodiola Rosea – A herb that acts as an adaptogen, meaning it aids the body in reacting positively to stressful stimuli. It typically reduces feelings of fatigue and is slightly stimulatory. It is also sometimes used to lessen the effects of caffeine withdrawal.

Note: Prescription drugs such as Adderall (amphetamine) and Ritalin (methylphenidate) are especially effective at increasing feelings of motivation. However, they carry additional side effects and risks of dependency, and should be used with caution.

General Cognition

piracetam nootropic adhd

  • Piracetam – The original racetam, was originally developed as a sleep-aid because of it’s GABA structure, when given to rats it improved their memory and cognition.
  • Noopept – Is chemically similar to piracetam but is active at a fraction of the dose (10 mg vs 1000 mg), and also increases the production of NGF and BDNF, two neurotrophic factors that promote the survival and differentiation of neurons. It typically provides an increase in cognitive ability along with mild stimulation.
  • Aniracetam – Provides cognitive effects that are similar to Noopept, but is also anxiolytic in nature. It is especially helpful in helping the brain associate different thoughts and piecing them together to form the “bigger picture.”
  • Phenylpiracetam – Similarly aids cognition like noopept and aniracetam, but it noticeably more stimulatory. It is also known to be more neuroprotective, and aids in preventing cognitive decline. It is a good alternative to Modafinil.

Note: Because racetams and noopept work through modulation of acetylcholine, they should be supplemented alongside a choline source, such as alpha-GPC or CDP-choline.

Mood Improvement

  • Tianeptine – Chemically a tricyclic antidepressant, tianeptine is novel in the fact that it improves mood while also serving as a neuroprotectant and cognitive enhancer.
  • Phenibut – an anxiolytic compound that may enhance cognition in stressful situations (like exams or a public presentation) through means of reduced anxiety.

Memory

  • Bacopa monnieri – Bacopa has been found to improve the formation, retention, and acquisition of memory. It is an adaptogen and is often taken for its anxiolytic properties
  • Huperzine A – an acetylcholinesterase inhibitor (a compound that prevents the breakdown of the neurotransmitter acetylcholine) extracted from the plant Huperzia Serrata.

What To Expect

Most nootropics rarely display immediate or noticeable acute effects on cognition and well-being (the only exception being stimulant nootropics like Modafinil and Phenylpiracetam) . In fact, they are typically used for long-term neuroprotection, and may not display immediate or noticeable results from use. The psychoactive effects of nootropics are more subtle than the effects of recreational drugs but are ultimately more beneficial. By definition, the daily use of nootropic substances should be far more sustainable than that of recreational drugs.

Nootropics are meant to be safe to use indefinitely though not all drugs sometimes referred to as “nootropics” will meet these criteria. For instance, phenibut, a GABAergic anxiolytic, is sometimes discussed as having nootropic capabilities related to anxiety reduction. However, phenibut has a fairly high risk of causing dependency or withdrawal, and should not be used on a daily basis.

coffe and modafinil pure nootropics
Modafinil is used by college students as a safer alternative to Ritalin and Adderall

Many people supplement multiple nootropics at once to maximize their cognitive benefits. These combinations of substances are referred to as “stacks”. For instance, one might stack caffeine and L-theanine because L-theanine is known to reduce the jitters and anxiety that come with caffeine. [10] When taking multiple nootropics, it is extremely important to research any potential negative interactions between substances. Examine.com is an invaluable resource for researching nootropics and their possible interactions.

Nootropics can certainly be of great benefit to those who wish to improve their cognitive function and protect their minds from degradation. However, nootropics will likely be far more beneficial when they are used in combination with exercise, a proper diet, and meditation.[11] Nootropics can only do so much, and are certainly not an excuse to neglect these other primary health factors.
In addition to this, nootropics should not be used to treat mental disorders unless under the direction of a trained health professional. It may seem tempting to use promising and novel nootropics to treat something like depression, but there is still some amount of risk involved with doing so, especially given the fact that many of the newest nootropics still require a great deal of research before they can be used clinically.

Even if “old” nootropics like racetams are totally safe, it is still a good idea to check out interactions if you’re taking prescription medications.

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Fasoracetam Nootropics Racetams Reviews

Fasoracetam: How This Nootropic May Help You Focus Better

Originally known as NS-105, Fasoracetam is one of the newest nootropics on the market. Besides being the latest racetam to be discovered, it has some unique properties unlike any other racetam on the market. Let’s find out what makes this substance a truly unique nootropic, and why you should (or should not) try it.

One of the primary effects of Fasoracetam is the modulation of metabotropic glutamate receptors II and III (mGluR).[1] mGlu receptors have been shown to be involved in synaptic plasticity and neuroprotection. In addition, LY354740, am mGlu2/3 agonist, has been shown to be effective in generalized anxiety disorder.[2]

Fasoracetam is also the only racetam that significantly enhances cAMP formation[3] and that has been shown to be potentially effective in individuals with glutamatergic gene variants that are suffering from ADHD[4]. A Phase III clinical trial is near completion, but the drug is not currently listed as an ADHD treatment by the FDA.

Fasoracetam has also shown to have antidepressant effects[5] and to counteract learned helplessness, an avoidance behavior typically associated with depression. Fasoracetam, however, does not act on serotonin and other monoamines, and researchers think the antidepressant effect may stem from its ability to upregulate GABA-B receptors.[6]

Generally speaking, Fasoracetam has shown to be more effective with chronic use, and, in the ADHD study, most benefits were felt at week five onward.[7]
Fasoracetam ADHD

Mechanism of Action

In rat studies, fasoracetam restores the function of key receptors, glutamate mGluR II and III[8].  It also upregulates GABA-B receptors through receptor antagonism[9], a fact which may be related to its ability to reverse phenibut tolerance (which is one of the few supplements reported to relieve anhedonic depression). The GABA-B receptor is very important and has been found to play a role in cognition[10], anxiety and mood.

Alcohol, a very disinhibiting and fog-inducing compound (with pleasurable effects similar to phenibut) is thought to achieve its activity by activating GABA-B and A receptors (as well as dopamine).  However, because it downregulates these receptors, prolonged use may cause anxiety and cognitive disruptions.  Phenibut binds in a similar fashion to GABA-B.

FasoracetamBecause of its relatively narrow range of receptor targets, fasoracetam does not feel like a classic stimulant nor does it alter one’s feeling of wakefulness.  It lacks clinical dopamine activity but remarkably still managed to address ADHD symptoms, according to the study.  It is not clear how fasoracetam has such a specific utility in treating ADHD, more research on other neurotransmitters may be turned up in coming years, but judging on present evidence, it seems that Fasoracetam could reduce ADHD symptoms by modulating glutamatergic receptors.

That being said, the FDA does not list Fasoracetam as an ADHD medication and it should not be used as such. Only a professional can prescribe medications for ADHD and you should not self medicate.

Although it is a newer supplement without much of a user-base, it does appear to be well-tolerated even in large doses or extended periods. Among college students, it may soon become a mainstay, alongside other trusted nootropics such as Bacopa, Modafinil, and Noopept.

Acetylcholine

In addition to the findings surrounding glutamate and ADHD, rat studies have also revealed fasoracetam to have profound cholinergic activity.  Many common nootropics work by controlling acetylcholine, including several drugs used in the treatment of Alzheimer’s.

It increases the uptake of choline at sites in key brain regions involved in intelligence and mood, the hippocampus and cerebral cortex.  This, in turn, results in increased production and release of acetylcholine.[11]
This, similarly to what has been commonly reported with piracetam, may explain a need for choline supplementation in the case of symptoms such as low mood, headache or brain-fog.

Although I personally have only ever tried piracetam and aniracetam (and found, despite a slight cognitive boost, that they both caused a slightly lowered mood, with piracetam being more stimulating and anxiety-prone while aniracetam was calm and relaxing), I haven’t read any complaints of fasoracetam and depression (on the contrary it appears to be a robust antidepressant nootropic, similar to tianeptine). This is remarkable because excessive acetylcholine production is typically associated with low mood and depression. Even with something as mild as bacopa, reports of moodiness are easy to pin down.

Since all three of the mentioned racetams seem to operate through a shared mechanism of acetylcholine, it’s not clear how fasoracetam achieves a similar cognitive boost without side effects on mood.  Perhaps it has been less trialed and as more users sample it, more negative reports will pour in.  This seems unlikely, however, given multiple reports of antidepressant effects, and at higher doses, near euphoria.

Fasoracetam and coluracetam are interesting racetams with multiple mechanisms of action compared to piracetam. Although they both share a cholinergic effect, the former modulates mGlu receptors (as well as GABA-B receptors) while the latter interacts with a process named high-affinity choline uptake.  This may explain their calm, clear effects when compared with the more bland effects of piracetam.

Glutamate

Of the eight known metabotropic glutamate receptors, only one and five are believed to increase NMDA receptor activity and neural excitation (these two are postsynaptic).  The other six receptors all function to lower NMDA (and are presynaptic), lessen excitation and thus reduce potential neurotoxicity.

By slightly lowering glutamate activity and at the same time boosting GABA-B levels, fasoracetam offers a collected state of mind compared to piracetam’s more scattered one.  Normal tasks would flow much easier, and performance would be improved without adverse effect.
While OCD and more recently schizophrenia have been described as hyperglutamatergic, ADHD has always been thought of as a condition of low glutamate.[12]

However, fasoracetam may very well regulate the metabotropic receptors in both directions and benefit everyone equally (restoring both high and low activity of the receptors to normal).

It is not clear how to explain the remarkable improvements reported in samples of both schizophrenia and ADHD. An explanation may be the selectiveness for the presynaptic mGluRs (mGluR1 and mGluR5) coupled with the fact that these receptors both elevate cAMP and lower NMDA activity. Levels of these receptors in the body are both altered in schizophrenia (so fasoracetam would produce two favorable alterations for the schizophrenic patient).

Despite all this fine talk about schizophrenia and glutamate, most of the reports surrounding fasoracetam are concerned with ADHD symptoms, specifically motivation and focus.  It is not widely known for its use as psychiatric medicine, and it may be considered by ADHD patients who have not responded well to conventional treatments. Again, it is not approved by the FDA as an ADHD treatment, and we are not suggesting people suffering from that disease to use it without a medical prescription.

GABA

As stated above fasoracetam appears to have GABA-B antagonistic properties[13], and it may upregulate these receptors and thus diminish the tolerance to GABA-B agonists like Phenibut, Baclofen, and Alcohol, and may even act as an “antidote” to a Phenibut overdose.

Before many of the newer designer supplements hit the market and much was known about fasoracetam, Noopept was one of the more recommended supplements for alcoholics to recover cognitive capacities. But in light of this newer evidence, fasoracetam may address the issue more directly. Because of its activity here, fasoracetam may eventually find use in treating age-related memory decline, dementia, and even depression. For now, the research and hype seem to surround the potential treatment of ADHD symptoms.

Dosage and half-life

Buy Fasoracetam CapsulesNo dependence potential was noted in the rhesus monkey over the course of four weeks.[14]  However. users cannot be completely absolved of concern, due to interspecies differences and the possibility of an only mildly addictive substance requiring an exceptionally long habituation period.

If its use is not completely discouraged in elderly patients, significant caution and close monitoring are recommended.  Its metabolism and clearance depend heavily on the kidneys and at least one studied has reported significant accumulation in the elderly (whose renal function is typically compromised).[15]

It is typically taken at 10mg twice daily, but it is probably best to start with 5 mg and taper up. Even though the dosage is very low, bitterness is still a problem and the use of capsules or parachuting is recommended.

Although some work their way up to 30 mg in one dose, this may not be the most effective strategy (due to a short half-life of the compound) and this pattern of use is more likely to be helped along by a large meal.  A potent nootropic with a half-life of around 90 minutes, taking it even once a day may be enough for active levels to build up in your system, but tolerance will be close behind.

You can buy Fasoracetam capsules and powder at Nootropics Depot. Fasoracetam is not approved by the FDA as an ADHD treatment.

Fasoracetam
8.5
Focus
7.5
Mood
7.5
Memory
7.5
Stimulation
7.5
Relaxation
8
Safety
Reviewer 8.8

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Nootropics Piracetam Racetams

The Story and Science of Piracetam

Piracetam, the original Racetam was created as a cognitive enhancer. It is similar to GABA, a neurotransmitter from which it is derived, and it has been used to treat cognitive decline. A fair amount of evidence shows that it can enhance cognition in people who have had a decline in such. However, there is not much in the way of studies of piracetam in people who haven’t experienced such a decline.[1]

Piracetam was created in 1964 by a Belgian pharmaceutical company named UCB. The lead scientist was Dr. Corneliu E. Giurgea, who came up with the term nootropic to describe piracetam and other similar compounds. In the 1970’s, UCB released Nootropil, the trade name for Piracetam. Nootropil is currently used in Europe.[2]

Mechanisms of Action

The basic mechanism of piracetam is not well established. However, it does appear to be non-sedative and non-stimulatory.[3] The following are some seeming mechanisms of action.

Oxygen and glucose consumption

Piracetam increases the brain’s oxygen and glucose consumption, which may be responsible for the cognitive enhancement seen in those who are impaired. [4]
A study that looked at patients with Alzheimer’s Disease and unclassified dementia showed that piracetam increased brain glucose consumption by 8-10% in people with Alzheimer’s. No such increase was seen in the group who had unclassified dementia. [5] [6]

Glutamate receptors

Chemical structure of Piracetam

Neurotransmitters carry information between neurons. The part of the neuron that receives neurotransmitters is called a “receptor.” The glutamate receptor, as the name implies, is the receptor for the neurotransmitter, glutamate. Glutamate is not only our main excitatory neurotransmitter, but it is also the precursor of GABA, our main inhibitory neurotransmitter. In very simple terms, an inhibitory neurotransmitter has a calming effect on the brain, while an excitatory neurotransmitter has a stimulant effect, and the body needs both in the right quantities to operate correctly.

Glutamate receptors are important for forming memories and learning. AMPA receptors are a type of glutamate receptors that are involved in memory storage. Piracetam acts upon the Glu2 and Glu3 AMPA glutamate receptors. Acting upon the Glu2 subtype of AMPA receptors seems to be a unique site for Piracetam. [7] Piracetam does not seem to interact with the Kainate and NMDA glutamate receptors.[8]

GABA receptors

As you may have guessed, GABA receptors are the neuronal receptor sites for the neurotransmitter, GABA. Despite being a GABA derivative, Piracetam does not interact with GABA receptors as best we know. [9] [10]

Increase in cellular membrane fluidity

Nootropil (Piracetam)Piracetam may restore brain mitochondrial cell membrane fluidity [11] and presumably enhance brain cell function.

Mitochondrial dysfunction may have a causative role in Alzheimer’s Disease [12] [13]. One in-vitro study looked at the hippocampus membranes of Alzheimer’s patients and noted that the fluidity of these cells improved with Piracetam. [14] Findings that Piracetam may improve the fluidity of mitochondrial membranes and thus mitochondrial function have been supported in animal models of Alzheimer disease and aging. These findings may explain some of Piracetam’s cognitive effects in aging and brain dysfunctions. [15]

It is still unclear what this means to healthy young people. Piracetam seems to improve cell membrane fluidity in the brains of aged rats, but not in young rats.[16]

Anti-platelet effect

Piracetam seems to have an antiplatelet effect [17][18][19] [20] [21] [22] [23] when administered in doses that have been used for cognitive improvement [24] [25] [26] [27]. The mechanism for such is not clear.

Conditions for which it has been used

Memory & Cognition in the Elderly

There appears to be a fair bit of evidence that Piracetam may improve memory and cognition in those who are cognitively impaired.

  • A meta-analysis of 19 double-blind, placebo-controlled trials using Piracetam in 1,488 elderly patients with cognitive impairment or dementia showed that the amount of individuals who improved was 112% higher with Piracetam vs. placebo. The studies included in this meta-analysis looked for clinically meaningful improvement. Waegemans et al concluded that this meta-analysis provided compelling evidence of piracetam’s efficacy in a diverse group of aged cognitively impaired people.[28]
  • However, Flicker et al concluded that there was not enough evidence to support the use of Piracetam for dementia or cognitive impairment and that many of the piracetam trials for dementia were flawed.[29]

Memory & Cognition in Healthy Subjects

nootropicsThere is weak evidence of cognitive benefit in young and healthy adults. Such benefit seems more apparent where cognition is not optimal, but there is not frank impairment (e.g., age-related decline). [30]

  • One small double-blinded study showed that Piracetam improved backward word recall, which implies short-term memory enhancement.[31]
  • Another study showed that healthy people improved their verbal learning by 8% vs. placebo over 21 days.[32]
  • Yet another study seemed to indicate that Piracetam improved cognition in 18 people over age 49 who had no sign of cognitive impairment. [33]

Dyslexia

Piracetam has been associated with improvements in verbal learning and comprehensive in boys with dyslexia or learning disorders.

  • A review of 11 double-blinded studies with nearly 600 boys aged 8 to 13 who had learning disorders or dyslexia showed that Piracetam improved comprehension and verbal learning.[34]
  • In one study, Piracetam improved verbal learning by 15%. [35]

Coronary Artery Bypass Surgery

Piracetam seems to prevent reduced cognition associated with coronary bypass surgery in some [36] [37] [38] but not all [39] studies.

Stroke

Human evidence is mixed on whether Piracetam can benefit recovery from stroke. [40] [41] [42] [43][44]

Safety

Piracetam appears fairly non-toxic. Adverse effects seem to be rare and of limited duration and limited to agitation, anxiety, clinical depression, drowsiness, headache, hyperkinesia, hypersexuality, insomnia, irritability, libido increase, nervousness, somnolence, tremor, and weight gain [45]. Piracetam appeared to be safe for as much as 18 months in Alzheimer’s patients. The LD50 is 5.6 grams/kg of body weight for rats and 20g/kg for mice.

Summary

A fair amount of evidence shows that Piracetam can enhance cognition in those who are impaired and that it has an excellent safety profile. However, clinical studies of Piracetam in people who haven’t experienced cognitive decline is scant.

Although how Piracetam works is not entirely clear, interaction with AMPA receptors may be one of the routes of actions. Besides, there is evidence that it increases acetylcholine production as well as enhance the brain’s consumption of glucose and oxygen and improve fluidity of mitochondrial cell membranes.

Piracetam
7
Focus
6
Mood
7.5
Memory
6
Stimulation
6
Relaxation
10
Safety
Reviewer 7.5

References   [ + ]

1, 2. S. D. Shorvon (2004). “Piracetam”. In Simon D. Shorvon, David Fish, Emilio Perucca, W E Dodson. The treatment of epilepsy. Wiley–Blackwell. pp. 489–495
3. Piracetam: physiological disposition and mechanism of action (1986)
4, 8, 30, 34, 45. Examine.com article on Piracetam
5. Effect of piracetam on cerebral glucose metabolism in Alzheimer’s disease as measured by positron emission tomography (1988)
6. Piracetam improves mitochondrial dysfunction following oxidative stress. (2006)
7. Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors. (2010)
9. Piracetam–an old drug with novel properties? (2005)
10. Piracetam and other structurally related nootropics. (1994)
11. Piracetam: a review of pharmacological properties and clinical uses. (2005)
12. Mitochondrial dysfunction: common final pathway in brain aging and Alzheimer’s disease–therapeutic aspects. (2010)
13. Mitochondrial dysfunction: the first domino in brain aging and Alzheimer’s disease (2007)
14. Piracetam reverses hippocampal membrane alterations in Alzheimer’s disease (1999)
15. Improved mitochondrial function in brain aging and Alzheimer disease – the new mechanism of action of the old metabolic enhancer piracetam (2010)
16. Effects of piracetam on membrane fluidity in the aged mouse, rat, and human brain. (1997)
17. In-vivo platelet inhibition by Piracetam (1979)
18. Inhibitory effect of piracetam on platelet-rich thrombus formation in an animal model (1998)
19, 24. Platelet anti-aggregant and rheological properties of piracetam. A pharmacodynamic study in normal subjects. (1993)
20, 25. Treatment of Acute Ischemic Stroke With Piracetam (1997)
21. Piracetam and platelets–a review of laboratory and clinical data. (1999)
22, 26. Piracetam versus acetylsalicylic acid in secondary stroke prophylaxis. A double-blind, randomized, parallel group, 2 year follow-up study. (2000)
23, 27. Effects of acetylsalicylic acid in stroke patients. Evidence of nonresponders in a subpopulation of treated patients. (1991)
28. Clinical efficacy of piracetam in cognitive impairment: a meta-analysis (2002)
29. Piracetam for dementia or cognitive impairment. (2001)
31. Increase in the power of human memory in normal man through the use of drugs. (1976)
32, 35. Piracetam as an aid to learning in dyslexia. Preliminary report. (1979)
33. Piracetam-induced improvement of mental performance. A controlled study on normally aging individuals. (1976)
36. Effect of piracetam on cognitive performance in patients undergoing bypass surgery (2003)
37. Cerebroprotective effect of piracetam in patients undergoing coronary bypass burgery. (2008)
38. Piracetam prevents cognitive decline in coronary artery bypass: a randomized trial versus placebo. (2006)
39. Cerebroprotective effect of piracetam in patients undergoing open heart surgery. (2011)
40. Piracetam in acute stroke: a systematic review. (2000)
41. A systematic review and meta-analysis of the efficacy of piracetam and piracetam-like compounds in experimental stroke. (2008)
42. Does long term use of piracetam improve speech disturbances due to ischemic cerebrovascular diseases. (2011)
43. Piracetam improves activated blood flow and facilitates rehabilitation of poststroke aphasic patients. (2000)
44. Restitution of alpha-topography by piracetam in post-stroke aphasia. (2001)
Categories
Aniracetam Nootropics

A Scientific Overview of Aniracetam

Aniracetam is a fat-soluble and supposedly more potent analog of piracetam. Anecdotally, it is claimed to facilitate associative thinking and creativity, as well as to reduce anxiety and depression. Although there are few human studies, it is currently used as a treatment for dementia and it’s being researched as a possible treatment for Alzheimer’s Disease, anxiety and depression.[1]

Mechanism of Action

AMPA receptors

Neurotransmitters carry information between neurons. The part of the neuron that receives neurotransmitters is called a “receptor”. The glutamate receptor, as the name implies, is the receptor for the neurotransmitter glutamate. Glutamate is not only our main excitatory neurotransmitter, it is also the precursor of GABA, our main inhibitory neurotransmitter. Glutamate receptors are important for forming memories and learning. AMPA receptors are a type of glutamate receptors that are involved in memory storage.[2] AMPA receptors are the targets of therapeutic drugs given that glutamate is believed to be involved in psychiatric and neurological disease.[3] Aniracetam seems to reduce the rate that AMPA receptor become desensitized [4] to positive stimuli like glutamate. Thus, Aniracetam and other AMPA modulators are being investigated for schizophrenia and Alzheimer’s disease. [5] It appears that aniracetam stimulates the AMPA receptor more than other racetams.

GABA receptors

Aniracetam seems to increase the effects of GABAergic inhibition. GABA is important for emotional wellbeing cognition, and improving GABA function could be potentially therapeutic for anxiety and cognitive disease. [6]

Cholinergic receptors

Aniracetam appears to enhance acetylcholine transmission, which plays an important role in cognitive function and the Alzheimer’s Disease. [7] It is theorized that the reduction of depression seen in animal studies may also be a result of Aniracetam interacting with these receptors. [8]

Serotonin and dopamine receptors

Animal studies indicate that Aniracetam may reduce anxiety and increase socialization by interacting with serotonin, dopamine, and acetylcholine receptors [9][10]. It also seems to increase the release of serotonin and dopamine, which may work together to improve mood and judgment. [11] This is an interesting aspect of aniracetam; it is the only racetam that seems to be able to reduce anxiety.

Neuroprotection

In animal studies, aniracetam seems to alleviate impairment to memory and learning caused by various means, including cerebral ischemia, cholinergic antagonists, and electroconvulsive shock.[12] Aniracetam can also protect against scopolamine-induced damage and seems more powerful than piracetam at doing so on a milligram by milligram basis. [13]

Conditions for which it has been used

There is some evidence that Aniracetam may improve memory and cognition in those who are cognitively impaired. Trial results involving elderly people who were cognitively impaired from either Alzheimer’s or other forms of dementia suggested that aniracetam may benefit theses conditions. Further trials are needed for confirmation of its safety and efficacy. Aniracetam was significantly more effective than placebo in tests at 4 and 6 months, and in a further 6-month trial was more effective than piracetam on certain testing parameters.[14]

Safety Data

Available information from trials seems to indicate that aniracetam is well tolerated. In particular, one published overview noted that aniracetam does not appear to raise in liver enzyme levels. Preliminary evidence points towards a good tolerability profile.[15]

Summary

Aniracetam is a fat-soluble racetam nootropic. Human studies are lacking, but it may prove to be a viable treatment for Alzheimer’s Disease or depression. Anecdotally, it is claimed to facilitate associative thinking and creativity, and animal studies have shown an anti-anxiety effect. In addition, as far as we can tell, there it does not seem to be associated with significant side effects and appears to be well tolerated.

Aniracetam
6
Focus
7.5
Mood
6
Memory
5
Stimulation
7
Relaxation
9.5
Safety
Reviewer 7.2

References   [ + ]