Tag: stimulants

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Nootropics Phenylpiracetam Racetams

Phenylpiracetam — Stimulant Nootropic: Effects, Dosage & Experiences

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 100–200 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

References   [ + ]

Categories
Cognitive Health

Why Do I Find Stimulants Calming?

ADHD drugs enhance human focus by expanding the levels of neurotransmitters from the prefrontal cortex of the brain which coordinate attention and behavior: norepinephrine and dopamine. Psychostimulants like methylphenidate (Ritalin) amphetamines (Adderall) encourage focus and attention, both in ADHD-diagnosed and non-ADHD-diagnosed people[1], regardless of one’s initial intellectual baseline.

Thus, giving stimulants to a person with a learning disability is like giving more time on a test: an advantage that might help anybody, but assists especially the ones in need (rather than fixing their brains).

In spite of the positive evidence[2], stimulant users do report different subjective realities: while ones get anxiety, others remain calm and relaxed. From a psychological point of view, it is assumed that part of the problem in ADHD is that the patient’s environment doesn’t stimulate their brains enough as it does in people without the disorder. As a result, ADHD-sufferers feel constantly bored and hence look for various ways to stimulate themselves by rapidly shifting their attention to something new. Therefore, in theory, by providing the missing excitement to the brain, these medicines allow ADHD people calm down and stay focused in a single activity.

Despite this highly plausible explanation, the neurological mechanism by which psychostimulants act as calming agents in humans with attention-deficit hyperactivity disorder or hyperkinetic disorder is currently unknown. Mice lacking the gene encoding the plasma membrane dopamine transporter (DAT) have elevated dopaminergic tone and are hyperactive[3], particularly when facing a novel environment. Furthermore, these mice are appreciably impaired in spatial cognitive function, and they display a decrease in locomotion in response to psychostimulants[4]. The behavioural resemblance between the DAT knockout mice and individuals with ADHD bring to mind that common mechanisms may underlie some of their conducts and responses to psychostimulants, and that dopamine D4 receptor gene might be abnormal on these individuals.[5]
“In contrast to the classical dopamine transporter (DAT)-dependent enhancement of the dopaminergic signal observed at concentrations of cocaine lower than 3 μM, the inhibitory effect of cocaine was found at concentrations higher than 3 μM. The paradoxical inhibitory effect of cocaine and methylphenidate was associated with a decrease in synapsin phosphorylation […] Interestingly, a cocaine-induced depression of DA release was only present in cocaine-insensitive animals (DAT-CI). Similar effects of cocaine were produced by methylphenidate in both wild-type and DAT-CI mice. On the other hand, nomifensine only enhanced the dopaminergic signal either in wild-type or in DAT-CI mice. Overall, these results indicate that cocaine and methylphenidate can increase or decrease DA neurotransmission by blocking reuptake and reducing the exocytotic release, respectively. The biphasic reshaping of DA neurotransmission could contribute to different behavioural effects of psychostimulants, including the calming ones, in attention deficit hyperactivity disorder”.[6]
Thus, SUNY’s researcher David Erlij and his group of researchers sustain to have recognized a network of nerve terminals where stimulation of dopamine D4 receptors exhaust motor activity.[7] This network seem to be localized deep in the brain, in the basal ganglia and the thalamus and its responses may explain the reduction in motor activity caused by psychostimulants. In this way, these results suggest that enhancing dopamine D4 transmission in the basal ganglia and the thalamus is likely part of the mechanism of the therapeutic effects of psychostimulants on ADHD patients.
In conclusion, because of genetic anomalies, people with ADHD might encounter stimulants antagonistically. While further research is required to clear up the mechanisms behind the cognitive enhancement itself (why does it also works for the healthy ones then?) at a neurological level, taking into account the subjective outcome of the individual -calm vs. nervous- becomes significant when choosing a treatment.

References   [ + ]

Categories
Bromantane Nootropics

Bromantane, A Unique Anxiolytic Stimulant (Review)

bromantane anxiolytic stimulant nootropic

Stimulants are one of the most infamous classes of drugs, whether recreational or for medical purposes. They can be unpredictable, leading to difficult side effects like anxiety, hypertension, and in extreme cases, even neurotoxicity. Members of the nootropics community have been reluctant to place the label “nootropic” on any kind of stimulant, due to these potential side effects and the risk that comes with taking them for long periods of time. However, there exists somewhat of an anomaly in the world of stimulants: the drug known as bromantane.

This unique drug is purported to possess both stimulant and anxiolytic properties. This seemingly paradoxical nature is due to bromantane’s status as an actoprotector, an obscure class of drugs that will be described below. As for bromantane’s origin: like many of the greatest cognition-enhancers, it is a product of the laboratories and pharmaceutical companies of Russia (formerly the Soviet Union).

Discovery of Bromantane

Adamantane
Adamantane, the simplest diamondoid

The discovery of adamantane in petroleum in 1933 launched a new field of chemistry dedicated to studying the synthesis and properties of polyhedral organic compounds.[1] Bromantane (also known by the trade name Ladasten (Ладастен) or its structural name of adamantylbromphenylamine) arose incidentally from the research of antiviral drugs meant to treat influenza. Amantadine, a derivative of the adamantane molecule, was being researched in the 1960s for its antiviral properties.[2] Due to the vigorous amount of research surrounding the amantadine molecule, it was soon discovered that amantadine and its derivatives possessed psychostimulant through a dopaminergic effect; thus, it has been sometimes used as a treatment for early-stage Parkinson’s disease.

Bromantane
Chemical structure of Bromantane

The new discovery of the dopaminergic properties of adamantine led to increased research on the development of new stimulants. In the 1980s, researchers at the Russian Academy of Medical Sciences in Moscow engineered the adamantine derivative bromantane as a new stimulant drug.[3]

Actoprotectors

While displaying stimulant properties, bromantane is also commonly categorized as an actoprotector, that is, a drug that “enhance[s] body stability against physical loads without increasing oxygen consumption or heat production. Or, in short, actoprotectors are synthetic adaptogens with a significant capacity to improve physical performance.”[4]

Actoprotectors, in theory, exhibit many advantages over traditional stimulants. For one, stimulants like Adderall typically cause a “crash” when its effects wear off. Actoprotectors like bromantane are purported to be more “smooth” and stable in their effects. However, many of these positive claims surrounding bromantane are somewhat dubious. Much of the research that has been conducted on actoprotectors like bromantane was based solely in the Soviet Union, and most of the literature have not been translated into other languages like English.

Adaptogens

Another actoprotector, known as Bemitil (Metaprot), was commonly given to Soviet cosmonauts and soldiers in the 1990s to increase their performance and resistance to fatigue in their respective fields of work. Bromantane was also used, albeit not as commonly as bemitil, to “shorten recovery times after strong physical exertion.”[5] Although bromantane soon fell out of use in the military, it still continued to be researched in areas such as sports medicine, as it was found to boost athletic performance. Bromantane was brought somewhat into the eyes of the public during the 1996 Summer Olympic Games, when 5 Russian athletes tested positively for using bromantane as a doping agent.[6] Bromantane was thereafter banned from use in sporting events, relegating its use to purely medical fields.

Mechanism of Action and Side Effects

Ladasten
Ladasten (Bromantane)
While bromantane’s mechanism of action is sadly not as well studied as other nootropic substances, it is known to exhibit characteristics of both stimulants (like amphetamine) and adaptogens (like Rhodiola Rosea).[7] Bromantane’s two foremost modes of action are thought to be dopaminergic and serotonergic stimulation of the nervous system. Although the mechanism is not that well understood, research has indicated that the administration of bromantane triggers a release of dopamine, as well as increasing the concentration of serotonin and 5-HIAA in the frontal cortex of the brain.[8] Bromantane also works as an anxiolytic by strengthening GABA-ergic mediation. Unlike most stimulant drugs, bromantane has not demonstrated addictive potential. Likewise, it does not appear to build a tolerance after prolonged periods of use.[9] One study suggests that high doses of bromantane (50 mg/kg) in rats can cause an increase in the DNA-binding activity of the beta-amyloid precursor protein (β-APP) gene promoter, which is linked to the pathogenesis of Alzheimer’s disease. However, the dose used in the study is about 68 times the normal prescription dose of bromantane.[10]

Uses of Bromantane

Bromantane is most commonly used in Russia as a treatment for neurasthenia, a somewhat vague medical condition that is marked by fatigue, irritability, anxiety, anhedonia and depressed mood.

The very favorable side-effect profile of bromantane is one contributing to factor to its increase in popularity as a potential nootropic substance.[11] Because “true” nootropic drugs do not carry any addictive potential, bromantane is one of the few stimulating drugs that can be said to fit this definition. Unfortunately, bromantane has not yet seen any official research regarding its exact effects of cognition and cognitive health. Due to its effects as an actoprotector, bromantane would theoretically reduce any fatigue that comes alongside long periods of mental exertion, making it a possible study aid. This effect would be enhanced by bromantane’s stimulating effects, which lead to increased motivation and concentration. A typical single dose of bromantane can range from 50 to 100 mg.[12]

Positive Effects of Bromantane

  • Enhances physical and mental endurance under stress[13]
  • Stimulation of the nervous system[14]
  • Reduces anxiety[15]
  • Enhances cognition and learning capability[16]
  • Low to no potential for addiction[17]
  • Low toxicity, especially when compared to other stimulants[18]

Negative Effects of Bromantane

As of now, there are no established side effects in the scientific literature surrounding bromantane

Subjective Experiences

As with any drug that has not been extremely well-documented in the scientific literature, it can be useful to include anecdotal reports from users to see the effects of the drug. Obviously, anecdotal reports are not to be considered hard evidence, so use good judgment. The following subjective reports have been gathered from Reddit users from /r/nootropics.

  • From /u/SocialT – “So the first time I tried it, it felt alright. The anxiolytic effect was good but I had taken a bunch of other noots, to the point where it was just a confusion of effects. But I took it (~50mg) yesterday and felt great. Calm, motivated, a very subtle kind of euphoric happy mood throughout the day. I was wide awake, and very sociable. I held a conversation for almost 3 hours with a coworker who I’d hardly ever talked to! Caffeine seemed to enhance the effect, though the comedown was a weird jittery-excited-slight unease mind state.”[19]
  • From /u/Nootrophic – “I’d like to report that this summer, I’ve took 100 mg for a month without issue and much improved effects: Stamina (++), Overall Confidence (+++), Social Confidence (++) and Motivation (+ or ++). I didn’t suffer side effects, and I stacked this dosage with insane amount of other nootropics without any issue whatsoever.”[20]
  • From /u/drejp – “I literally experienced total bliss these two weeks on Bromantane, starting from day 3-4 maybe. Depression allievated, mental and physical energy increased a lot, libido restored, excersise is rewarding and general outlook on life is very positive. It seriously felt like I got my old self back to a degree. I started to experience some sides yesterday though, I still experience mood-lifting effects, but I have the worst headaches today and general brain-fog, I have hard time thinking straight and am generally confused cognitive-wise.”[21]
  • From /u/somebodybettercomes – “I’ve been taking bromantane for over a month now, at least 50mg daily and most days I take around 100mg. The most I’ve had at once is around 200mg. So far I have not noticed any negative side effects from it. I’m generally in a better mood and more motivated than normal, less prone to anxiety. I believe it has improved my ability to stay focused. That said, I don’t feel like I am taking a stimulant. Even the few times I tried it close to bedtime I did not feel like it kept me from falling asleep or interfered with my ability to stay asleep.”[22]

Conclusion

Bromantane is a unique drug, given that it acts as a stimulant and anxiolytic simultaneously. It also serves to enhance performance by increasing the body’s resistance to mental and physical fatigue and exhaustion. Sadly, bromantane lacks the wide spectrum of research that has been invested in other more popular cognitive enhancers and stimulants. Because of this, nootropic users may want to consider trying bromantane to see if it acts as an effective drug for enhancing their cognition.

You can buy Bromantane powder at Ceretropic, or the original Russian brand (Ladasten) at Awake Brain
 

Bromantane
6
Focus
8
Mood
5.5
Memory
7
Stimulation
7
Relaxation
7
Safety
Reviewer 8

References   [ + ]