Modafinil

Modafinil


Summary: Modafinil is a powerful stimulant that promotes ‘wakefulness’ and treats sleep disorders. It prevents daytime sleepiness and fatigue, as well as offering nootropical benefits such as enhancing mood, increasing mental alertness, increasing motivation, improving reaction time, reducing fatigue, and even enhancing memory.



Introduction


What is Modafinil?

In use by the French army, the American Air Force, the Indian Air Force, and Canadian astronauts….. (astronauts!) (R). Modafinil is a powerful stimulant that promotes wakefulness and treating daytime sleep disorders such as narcolepsy – excessive, uncontrollable daytime sleepiness. Besides tats, it offers nootropic benefits such as enhancing mood, increasing mental alertness, increasing motivation, improving reaction time, reducing fatigue, and even enhancing memory.

As a prescription medicine, Modafinil is available in the US, Canada, the UK, and almost every developed country today. It is also available in the UAE where I had it prescribed for a month. Aside from the original name, it also sells under brand names Provigil, Modvigil, and Alertec. It’s a eugeroic (a class of medical drugs that promotes wakefulness and alertness) used to treat conditions such as narcolepsy, a disorder that decreases the ability to regulate sleep-wake cycles, as well as the effects of shift work and similar sleep disorders. It’s used off-label by students, businesswomen, men, and shift-workers due to its nootropic effects.

Modafinil, sold under the brand name Provigil among others, is a medication to treat sleepiness due to narcolepsy, shift work sleep disorder, or obstructive sleep apnea. In OSA continuous positive airway pressure is the preferred treatment.

Wikipedia

Benefits & Effects


Modafinil Improves Alertness

Although its effects are comparable to amphetamines like Adderall, which produce a temporary increase in cognition, Modafinil reports providing smoother and jitter-free energy. It also has fewer side effects and better toleration. Furthermore, it has low abuse and addiction potential. I don’t think I ever heard of any “Modafinil addict.” Definitely not Dave Asprey.

Reduces Fatigue

Modafinil increases resistance to fatigue more than amphetamines, along with improving mood, motivation, and reaction time. It is also effective at reducing “impulse response,” i.e., bad decisions. A study on forty-one military subjects receiving Modafinil shows better scores in not only fatigue but also reaction time. Additionally, measurable scores are showing in performance, mood, logical thinking, and even memory. (R)

Improves Cognition

It improves cognitive function by increasing wakefulness and enhancing mental performance during a sleep-deprivation state.
A by-product of the ground-breaking stimulant Adrafinil, Modafinil acted faster and was promoted as a different drug in the 1970’s. After extensive clinical trials, Modafinil got the FDA’s approval to use as hypersomnia treatment. (R)

Reduces Daytime Sleepiness

Modafinil is useful for shift workers. It is used to help pilots staying alert throughout operations by the American military.
According to the World Health Organization, off-label users take Modafinil as a Nootropic. Moreover, with that, reports showing they get the most cognitive boost as well as most of the compelling benefits when they are not sleep-deprived. It is useful for both, still. (R)

Enhances Learning Capacity

Modafinil is powerful strengthening the ability to learn and expanding the capacity to process information. Research confirms that it reinforces mental endurance and performance, especially in cases of drug dependence and ADHD individuals. According to the clinical trials, Modafinil enhances mood, performance, response time and even memory in healthy individuals as well as those who are sleep-deprived.

Effective Neuroprotectant

Experiments further suggest Modafinil promotes brain health. In brain tissue, its inhibitors properties decrease the manifestation of damaging free radicals, thereby making it an effective neuroprotectant (R), (R), (R).

Reduces Anxiety and Anger Response

Although less of a featured trait, Modafinil seems to have the ability to reduce anxiety as well as decreasing anger. A result of the reduction it allows in the reactivity stimuli within the brain (R). There is a paradoxical study (R) for the curious cats like myself. The research shows that on the contrary, Modafinil increases aggression and anxiety in a subject taking a 100mg dose. When the treatment is doubling to 200mg, the items display a reduction in anxiety. It’s a case where less is not more and more is more.

Reduces ADHD and Multiple Sclerosis Symptoms

Modafinil is one of the standard stimulants for the treatment of attention hyperactivity deficit disorder (ADHD). Furthermore, research suggests that it is an effective treatment for memory impairment in cases of multiple cases of sclerosis. Current clinical trials measure modafinil as a treatment for conditions such as depression, psychosis, seasonal depression, and even drug addiction. It confirms that it strengthens mental performance, thereby becoming beneficial in ADHD and drug dependence. (R) (R)

Mechanism of Action


The unique mechanisms of action differentiates Modafinil effect from the traditional stimulants though they are similar. Modafinil activates neurons by focusing on the hypothalamus and amygdala, unlike amphetamine, methylphenidate, and other central nervous stimulants that only induce wakefulness by general widespread neuronal activation. The precise mechanisms of Modafinil action have not been identified regarding locating a single site of action, though it modulates the brain’s histamine, serotonin, norepinephrine, orexin, and dopamine systems. However, it is evident that Modafinil’s effect on numerous essential neurotransmitters is at the heart of its potency, both as a eugeroic and nootropic.

Orexin Neuropeptide

Orexin neurons exist in the hypothalamus but project to many different parts of the brain including several areas that regulate wakefulness. Leading cause of Narcolepsy is lack of orexin, which Modafinil addresses by acting on orexin neurons. Activation of these neurons also increases production of histamines and other important neurotransmitters that are related to wakefulness and alertness.

On Histamine

Histamine is known to allergies and local immune responses, it also plays an essential part in regulating the sleep/wake cycle. Modafinil actions elevate hypothalamic histamine, a known wakefulness mechanism.

On Dopamine

Dopamine is an essential neurotransmitter associating with stimuli/reward response, and therefore can enhance mood as well as increase motivation and focus. Modafinil works by blocking the receptors that remove dopamine from synapses, which raises levels of dopamine available for instant use in the brain. Unlike amphetamines, which stimulate the release and increase of dopamine levels in a high but rapid amplified manner. This indirect gradual action on the dopamine system is a primary feature of how Modafinil works in the brain. It decreases the “rush” type of euphoria that associates with addiction.

On Norepinephrine

Modafinil increases the availability of norepinephrine, a stimulant neurotransmitter that promotes wakefulness and increases alertness in the hypothalamus. How Modafinil increases norepinephrine levels isn’t clear.

On Glutamate

Modafinil elevates levels of glutamate, the primary neurotransmitter in the brain which is responsible for excitement, by activating the extracellular release of glutamate in the hypothalamus. Glutamate plays a crucial role in human’s psychological functions, playing a significant role in Modafinil’s enhancing effects. Such effects include increased memory, focus, and even brain modification. Not all that Modafinil has to offers is clear, but more than 40 years of extensive research reveals its powerful effects.

Effects in Comparison to Amphetamines

Despite causing the lesser motor activity increase when comparing to methamphetamine, a 1997 study still reported that Modafinil is a better inhibitor of sleep drive and a producer of more periods of wakefulness. Although it is possible to get to addiction to Modafinil is also being proposed as a treatment for methamphetamine and cocaine addictions, restoring normal levels of learning ability and generally yielding more positive results than amphetamines. (R)

Effects on Exercise and Sports Performance

Modafinil enhances sports and exercise performance by the duration of time before exhaustion and reduces the feelings of fatigue. In 2004, it got banned by Anti-Doping Agencies. (R)

Effects on Cognitive Abilities

Several years of research explain that Modafinil improves a big range of psychological feature talents. From memory and fluid intelligence to each abstract and personal memory, government performance, pattern recognition, and performance on tasks that requires a high level of thinking. Further research also states that Modafinil’s effects may be most marked among low-performing subjects. Though Modafinil might end up in anxiety, clinical trials have examined that it improves mood in healthy subjects. (R) (R)

Dosage


Modafinil is safe for continuous use at moderate doses (100-200 mg). Large-scale clinical trials show no significant indications of tolerance over periods of up to several months.

Side Effects


Commonly reported side effect of modafinil (although minor) can include anxiety, insomnia, headache, nausea, digestion issues, dizziness, diarrhea, dry mouth, and inflammation. Many of these side effects are temporary. If they persist, its advisable to seek professional advice.

Conclusion


Everyone responds differently to nootropics, but decades of research have shown modafinil is safe, effective, and well-tolerated. If you’re into maximizing cognitive abilities and minimizing fatigue, modafinil is a nootropic worth trying. My personal experience with it has been very interesting and positive. I mostly noticed the massive interest in learning as well as the capacity to process information. Nevertheless, I still prefer Adrafinil over Modafinil, even though they are almost identical products.

L-Theanine

L-Theanine


Summary: L-theanine is a natural amino acid, often called the “natural xanax”. It almost only exists in green tea leaves. It works brilliantly in unwinding and relaxing the body and brain without causing drowsiness, while reducing stress and increasing cognitive function. Due to not causing drowsiness, it is the perfect choice to combine with stimulants of any sort to take the edge off.




Introduction


What is L-Theanine?

L-theanine is a relaxing, non-sedating amino acid that is synergistic with stimulants to ‘take the edge off.’ Especially with coffee, it synergizes so well resulting in clean energy, furthermore preventing the nasty caffeine crash that many people experience after caffeine intake. It is also useful on its own, promoting relaxation and minimizing stress without causing drowsiness. A combination of L-theanine with caffeine at a 2:1 ratio is increasing in popularity as a remarkably synergetic combination that boosts cognition and attention.

It is an amino acid that naturally exists in green tea leaves as its main active ingredient, and that is the only source that provides it. It is famous for its fantastic nootropic features such as improving memory, expanding learning capacity, as well as providing a calming, zen-like effect.

L-Theanine, for the most part, is a relaxing but not sedating amino acid that is synergistic with stimulants such as caffeine as it can ‘take the edge off’. It is effective by itself in the standard supplemental dosages as well, and although it can be attained via a diet high in green tea ingestion that is the only dietary source of L-Theanine

Examine.com

Benefits & Effects


L-Theanine Reduces Anxiety & Stress

A review by researchers of a small set of trials concluded that there are benefits of L-theanine in reducing acute stress and anxiety in people with stressful conditions. [R]

Oral intake of L-theanine in rats at feasible dosages reduces circulating biomarkers of stress with or without an actual stressor being present. Therefore, it reduces the adverse effects of stress such as memory impairment. Reductions of perceived stress reported in human subjects given oral theanine at the standard dosages. [R] [R] [R]

L-Theanine Improves Memory, Attention, and Cognition

In a 16-week long study on individuals with mild cognitive impairment, supplementing with l-theanine shows an improved delayed recognition as well as immediate recall comparing to those receiving a placebo during a mental exercise. Furthermore, attention span and alertness levels increased during the memory test. [R]

Theanine Enhances Sleep Quality

Theanine enhances sleep quality. In a study measuring sleep time with individuals supplementing with L-theanine, sleep time increases by 11 and up to 21%, therefore making it a valuable compound for achieving better nighttime sleep. (R)

Promotes Longevity and Increases Lifespan

In a study using the model organism C. elegans, L-theanine shows to promote longevity and promote healthy and increased lifespan. Due to those findings, the study suggests that the compound might have similar effects on mammals and humans (R)

Reduces Symptoms of Depression

L-Theanine intake for a period of eight weeks during an open-label study helped easing depressive symptoms, anxiety, sleep disturbance, as well as cognitive impairments in subject suffering major depressive disorder. (R)

Promotes Relaxation without causing Drowsiness

Theanine is proving to be a great agent in promoting relaxation without the accompanying effect of drowsiness. The company developing ‘suntheanine’, l-theanine supplement, won the 1998’s Food Ingredient Research Award for the outstanding research and findings. (R)

Significantly Reduces Symptoms of Schizophrenia

In persons diagnosed schizophrenia receiving 400mg L-theanine in addition to antipsychotic medication for eight weeks were able to reduce anxiety as well as psychopathology symptoms significantly. (R)

Enhances Blood Flow and Stimulates Nitric Oxide Production

Theanine appears to promote nitric oxide formation at relatively low concentrations and is likely practically relevant following oral ingestion. (R)

Reduces Negative Effects of Caffeine & Improves Cognitive Boosting Effects

Theanine and caffeine are typically found together in tea. A combination of caffeine and theanine together significantly improves alertness, reduce fatigue, and improves task-switching accuracy.

High dose caffeine (250 mg, equivalent to 2.5 cups of coffee) has some negative effects, such as jitters and increased blood pressure. Theanine was able to mitigate the increase in blood pressure.

L-Theanine decreases the negative and jittery effects of caffeine in rats.

However, human studies found that L-Theanine helps reduce caffeine jitters, although the changes were not significant.

L-Theanine changes the pharmacological profile of caffeine in humans, as the combination of caffeine and L-Theanine have somewhat different cognitive enhancement effects.

Selfhacked

Additional Benefits

Large studies in humans have not been undertaken; however, several smaller-scale studies (fewer than 100 participants) have shown increased alpha wave generation and lowered anxiety, along with benefits to sleep quality in people with ADHD. [R]


Mechanism of Action


L-theanine has a comparable chemical composition to glutamate, an amino acid that assists in the transmission of nerve impulses in the brain. Thereby, providing a host of benefits for the mind. It has a remarkable ability of crossing the blood-brain barrier, which means that it reaches the brain directly. Furthermore, it has positive effects on stress levels proving to increase both dopamine and serotonin levels in brain; which are two of the brain’s feel-good chemicals. Green tea is known to be effective at helping people relax due to the positive impact on those neurotransmitters.

Theanine is an antagonist of the NMDA receptors (albeit with fairly weak efficacy) and can inhibit synaptic release of glutamate via blocking the transporter competitively. Theanine may also reduce glutamate levels, but this is also a fairly weak mechanism requiring a high concentration of theanine

Examine

Dosage


How to Take L-Theanine?

The effective l-theanine dose is 200mg.

For optimal nootropic results, take l-theanine with caffeine (coffee or supplement, whatever suits you) at a 2:1 ratio. As a stack, it would be:

  • L-Theanine 200mg
  • Caffeine 100mg

For those interested, you can actually purchase a supplement pre-made that has 200 mg Theanine & 100 mg Caffeine pressed into one capsule. I’ve personally used and still use Nootropic Depot’s.

Note: if you have anxiety or hypertension, you may want to skip caffeine entirely as it aggravates the symptoms.

Experimenting is the best way to find out how you react to it.


Side Effects


L-theanine is very safe as very high doses have failed to cause toxicity. However, that doesn’t mean you should go for such high dosage. (R)

L-theanine is exceptionally reliable. Furthermore, it is classified Generally Recognized as Safe by the Fraud and Deception FDA in the US.


Conclusion


L-Theanine is a natural safe amino acid offering many benefits. It’s a popular choice for individuals wanting a simple and effective way to boost their mental performance. Alone, with caffeine, or even with an advanced nootropic stack; L-theanine is worth trying.


Further Reading



Adrafinil

Adrafinil

SummaryAdrafinil is a stimulating nootropic that fights fatigue, increases the brain’s capacity of processing information, boosts energy, as well as enhances subjective well-being. It metabolizes in the body into the widely popular Modafinil (Adrafinil vs Modafinil comparison below). It’s a useful supplement for pulling through long, mentally demanding tasks, learning new topics, or working in shifts as opposed to fixed schedule.




Introduction


What is Adrafinil?

Adrafinil is a synthetic nootropic supplement that acts as a central nervous system stimulant. Previously known as Olmifon, and often mistaken with Modafinil, it is a stimulant that does not produce amphetamine-like effects.

It is a precursor to Modafinil. That means it leads to increased concentrations of modafinil in the body.  Adrafinil combats fatigue, boosts energy, improves attention, concentration and focus. It’s also known to enhance mood, motivation, and reaction time. Its potential cognitive benefits extends further to improving memory and increasing the brains capacity of learning, digesting, and processing information.

An invention from the 1970’s by French pharmaceutical company Lafon Laboratories, which manufactured, branded and marketed the invention in Europe under the name Olmifon. It spread throughout Europe and became widely prescribed by practitioners as a treatment for narcolepsy and related sleep disorders that has symptoms of heavy and excessive daytime drowsiness. As well as widely used off-label for its nootropic and stimulating effects.

In 2011, production of Olmifon ended when the french regulating authorities reversed its legality.

Its unregulated in the US, Canada, and most other countries around the world. It can be found in drugstores and online on many, many vendors and it is very widely used by people for combating fatigue, enhancing energy, stimulation, and boosting overall cognitive function

Adrafinil is a eugeroic that was formerly used in France to promote alertness, attention, wakefulness, mood, and other parameters, particularly in the elderly.

Wikipedia

Adrafinil vs Modafinil Comparison

Many people often compare adrafinil vs modafinil upon hearing of it. Usually because they try to get modafinil and find out its prescription medication, so they go for the non-[rescription, online-available alternative.

What popularizes it the most as a nootropic is the fact that its the closest legal, prescription-free to the “limitless” modafinil. But for those who knew and were familiar with it before this movie association know its profound effect and can differentiate between it and that of modafinil. In fact, many users actually report preferring adrafinil vs modafinil for certain, slightly different nootropic effects that each produces.

Although Adrafinil metabolizes into Modafinil after ingestion, it still requires a higher dosage to reach the level of effectiveness that one would feel from modafinil. For example, modafinil is mostly prescribed in dosages of 100 to 200 mg. Adrafinil often sells in the lowest dosage being 300mg. So in order to achieve the same concentration level of modafinil using adrafinil, one would have to be aware of this and measure the dosage following that pattern, as required.

Modafinil is often prescribed therapeutically in doses of 50mg being the lowest effective. For comparison, taking 300mg Adrafinil, which is the smallest manufacturing dose, would actually be more effective than the lowest effective dose of modafinil.

Although it cannot be an exact figure due to the fact that breakdown and metabolizing varies from each individual to another, a general and easy way of understanding and remembering the math of adrafinil vs modafinil in terms of dosages, or at least how I personally measure it when taking either one, is that that 100mg of Modafinil is more or less equals to 300mg Adrafinil.

Personal Thought

From my personal, own experience: the effect of Adrafinil 300mg  is much more felt in comparison to Modafinil 100mg. During the period I was prescribed Modafinil, I would have to take 200mg in order to achieve what I would achieve from 300mg of Adrafinil. 

Benefits & Effects


Increases Mental Clarity & Heightens Focus

Although it is initially developed for its wakefulness-promoting qualities, Adrafinil continues showing significant cognitive benefits as well. For individuals suffering daytime exhaustion due to night work or sleep difficulties, adrafinil increases the physical and mental energy required for an active life. It also improves mental clarity and heightens focus.

Promotes Wakefulness & Boosts Energy

Adrafinil is an overall beneficial stimulant, preventing daytime drowsiness and dramatically increasing energy and attentiveness without the hyperactivity and jitteriness associated with stimulants. Users report a profound sense of well-being, stress reduction, and overall enrichment experiences. Those outcomes are primarily due to Adrafinil’s impact on dopamine.

Improves Learning Capacity & Memory Formation

In addition to promoting wakefulness and increasing energy, adrafinil holds many nootropic benefits such as improved learning capacity, better memory creation, as well as recollection. Reports indicate that it sharpens focus and increases the ability to maintain it, along with providing mental clarity, and easing mentally demanding work, especially that which extends over a prolonged period.


Mechanism of Action


How Does Adrafinil Work?

Adrafinil acts on the adrenergic system, the part of the nervous system that releases adrenaline. Typically considered in charge of the “fight or flight” response, a rapid release of adrenaline boosts energy and increases alertness. While not all of adrafinil’s actions are entirely understood, it is assumed to replicate the positive effect of adrenaline release by supporting adrenergic neurotransmitters.

The Breakdown

Adrafinil is a synthetic prodrug, which means that its an inactive compound that metabolizes into an active form inside the body. The process of metabolizing it produces the drug, modafinil, which is an FDA-approved treatment for necropsy and similar sleep disorders. The pharmacological effects of adrafinil are practically identical to those of Modafinil.

Though the exact chemical mechanisms of it are unclear, researchers hypothesize that in its metabolized form it functions as an adrenergic receptor agonist. One of its first actions is the enhanced production and release of the neurotransmitter hypocretin, which in turn triggers the increased production of dopamine, histamine, and norepinephrine; all of which are directly related to alertness and energy, which considerably explains adrafinil’s stimulant qualities.

The remarkable mood and cognitive effects it produces result from different actions, such as the positive modulation of glutamate receptors, and inhibiting the breakdown of glutamate. Those actions lead to better neuronal communication, which improves memory and focus and creates better cognitive functions.

Serotonin Neurotransmitter

It also stimulates the release of serotonin, which enhances mood by reducing anxiety levels. It also inhibits the breakdown of dopamine, a neurotransmitter that is mainly responsible when it comes to the brain’s pleasure and reward responses.


Dosage


How to Take Adrafinil?

Recommendations vary greatly among different users.

The lowest dose Adrafinil is produced in is 300 mg. However, most nootropist would say, and prefer, a dose of 600mg taken once in the morning. And the highest yet credible dosage is 1,200mg taken as 2 doses. A morning dose of 600mg and an afternoon “boost” dose of another 600mg.

At the doses of 300 to 600mg, it is a safe and very effective nootropic. It is a potent nootropic, therefore it’s advised to give your body a chance to adapt to it at lower doses and only gradually increase as you feel required after evaluating the effect of 300mg.

Due to its potency and wakefulness-promoting properties, it is advisable to take it in the morning or early afternoon only to avoid interfering with the sleep cycle, otherwise you wouldn’t be able to fall asleep easily at night. (although that doesn’t apply to those who know that time is actually an illusion).

It is also advisable to take it on an empty stomach to allow for optimal absorption. It kicks in and effects start to be felt around 45 minutes to an hour after ingestion.

For continuous and prolonged use, it is very advisable to use on a sequence (or cycle) of two weeks on, and one week off to detox and maintain tolerance as well as prevent potential dependency for certain people.


Side Effects


What Are Adrafinil Side Effects?

The most typical side effects of adrafinil are headaches, dizziness, nausea, and stomach discomfort. The most severe relates to liver function. Additionally, there is potential for increased risk of high blood pressure and heart problems when taking high doses.

Should you experience any side effects, stop using and seek professional medical advice.


Conclusion


Adrafinil’s mixture of mental and physical benefits make it valuable for individuals looking for more energy, stamina, and psychological acuity. Its a powerful nootropic with potent stimulant qualities. Used responsibly, it offers a unique and profound nootropic boost that one grows to appreciate.


User Experience


Here is three random experiences from adrafinil reddit nootropic community on their thought of adrafinil:

I love adrafinil for a once-every-couple-of-weeks ‘I need to work 11 hours today’ usage. I can take 300mg at 6:30 or 7 in the morning, and still be alert and clear headed at the office when 7 or 8pm rolls by. But I try not to use it any more than once a week, because of the possible liver implications.

WhatAboutLightly

Adrafinil is very strange for me. I noticed somewhat sporadic efficacy. Additionally, for me, I was getting bad headaches. I called them “core headaches” as they seemed to originate from the very “core” of my brain. and not in the front like other areas. now I am still uncertain if this was because of adrafinil or phenylpiracetam. but once I started experiencing core headaches frequently even without taking any nootropic whatsoever, I quit adrafinil. It did go away after a while, but again I am not sure if this was just a rebalance or due to…other things I have been up to. Good write up though. I am not certain I can answer any of the questions since I haven’t gone back to adrafinil yet…thinking of trying modafinil if I can manage to procure it, and see if that has a cleaner, more mildly-stimulating/focusing effect like I was looking for.

multipl3x

My simple protocol for Adrafinil is to only take it if I sleep poorly. and know that I still need to perform the next day. For me that means that I take it infrequently, but it’s a lifesaver every time.

stevetheguy

Further Readings


The Ultimate Nootropics Frequently Asked Questions List