About Modafinil

Modafinil which is often sold under the brand names of Alertec, Modvigil, Modiodal, Provigil, Modalert, is a synthetic wakefulness agent which was originally made to treat narcolepsy, that’s when people fall asleep all of the sudden, but it has also proven itself to be effective when it comes to reducing fatigue, enhance cognition and increase alertness. For these reasons, it’s also known as a nootropic which has low to moderate levels of stimulation.

U.S. Food and Drug Administration (FDA) has approved its use for treating narcolepsy (as I’ve mentioned), sleep apnea and shift work sleep disorder. It has also been unofficially shown to help treat depression, ADHD, bipolar disorder, seasonal depressive disorder, Parkinson’s disease and quite a few more diseases that have fatigue as one of their characteristics.

Nowadays there’s a large group of people who are interested in nootropics and are actively using them, and because modafinil is known to be a very potent and effective nootropic, in fact perhaps the most popular, effective and widely used nootropic on earth, if we exclude caffeine, modafinil is very popular in amongst them. Nootropic users tend to be high achievement seeking people like entrepreneurs, in fact, many silicon valley entrepreneurs actively use it right now. It’s also widely used by athletes, because of its stimulant effects and because it’s easy to pass most drug tests. This is because its molecular structure is very different from that of traditional stimulants like amphetamines, cocaine, and others.

History

Adrafinil – modafinil’s precursor, which was developed in the 1970s by Lafon Laboratories in France, was then marketed as a medication for narcolepsy which was way better than the traditional medicine used – amphetamines, because it doesn’t produce or it produces way milder side effects of amphetamines like anxiety or repetitive behavior and it doesn’t seem to be addictive.

The problem with adrafinil is that it takes quite some time to work because it turns out that it actually isn’t itself psychoactive in humans. What is happening is that after ingestion, the body has to metabolize it and turn it into another substance and then that substance does it’s magic and helps in many ways that it can. And this process takes time and when you’re a narcoleptic you often need to feel the effects of your medication as soon as possible. And so the same French labs started just making and marketing Adrafinil’s metabolite, and they called it – Modafinil.

Modafinil, because it doesn’t have to be broken down by the body into another substance, is more easily processed by the body, acts faster, is more bioavailable and is less likely to damage your liver because it doesn’t need to process it.

Nowadays it’s a legal pharmaceutical medication that is used for both medicinal reasons and performance enhancement.

Chemistry

Modafinil is a synthetic molecule of the benzhydryl class. Benzhydryl compounds are comprised of two benzene rings attached to a single carbon molecule. Modafinil is classified as a sulphinyl benzhydryl molecule, as it also contains a sulphinyl group, a sulfur molecule double-bonded to an oxygen molecule, attached to the carbon of the benzhydryl group. From this sulfur group at R2, an acetamide group is bound at its free carbon through a carbonyl group to a terminal amine group. Modafinil is structurally analogous to fluorafinil, another benzhydryl stimulant.

While modafinil is a racemic mixture, a similar medication, armodafinil, consists of only the (−)-(R)-enantiomer of modafinil.

Pharmacology

I’ve said it before and I’ll say it again, drugs are only as good as the receptors in the brain that they attach to. So here’s what modafinil does to you on a biochemical level.

It’s not fully known how modafinil works, but it’s pretty clear that it affects the sleep/wake circuit of the brain. Modafinil seems to inhibit one neurotransmitter GABA and promote dopamine, norepinephrine, histamine, and hypocretin/orexin.

The increase in histamine and dopamine should be the main reason behind modafinil’s wakefulness and alertness.

Effects

There is quite a wide range of effects that modafinil induces. They tend to be, for the most part, similar to those induced by most traditional nootropics. Like I’ve said, it promotes wakefulness, alertness, and stimulation to name a few of its effects.

Compared to other drugs that have been traditionally used to induce these effects – stimulants like amphetamines, cocaine, and methylphenidate, modafinil is very different. It has not been shown to be nearly as addictive or harmful, but also not as strong in its stimulation, euphoria, and forcefulness. It’s basically significantly weaker and less noticeable than many other stimulants and it’s not much of a recreational drug, but it won’t harm you as much if any and chances of you becoming addicted to it are quite small.

Before I dwell into the details of modafinil’s effects, there’s something very important that people have to understand about it and, really about pretty much all drugs.

The effects of virtually any drug depend on the type of drug being used first of all, but also the dose, route of administration (how you take it), prior use of the drug or a cross-tolerant drugs and individual’s body weight, metabolism, sensitivity, and general genetic makeup. So remember, two different people can take the same way the same amount of the same drug and feel different effects because they’re different people.

That being said, let’s delve deep into the general subjective effects of modafinil:

 

Physical Effects

Positive

  • Appetite suppression. You very likely won’t be as hungry on modafinil as you normally are or would get. This makes it a great tool

    for weight loss or just general avoidance of certain food that you should avoid, particularly those high in sugar. Though your appetite shouldn’t be as suppressed as it would be on amphetamines or cocaine.

  • Stimulation. It pretty much has the same stimulatory effects that other traditional stimulants have, but significantly less intense or dangerous. It can make you want to physically exercise, walk, run or socialize. Involuntary effects like jaw clenching or teeth grinding also sometimes happen, usually only on very high doses and not nearly as strong as they are on amphetamines, MDMA or cocaine.

Neutral

  • Urine Odor Alteration. Your urine might have a slight smell of sulfur after taking modafinil. This happens because modafinil contains sulfur in its molecular structure and once it’s broken down, sulfur exists your body through urine.

Negative

  • Dehydration. Modafinil doesn’t directly make you dehydrated, but because it enhances your motivation and focus, you can become so immersed into your activities that you simply forget to drink water that can lead to you becoming less hydrated. So try not to forget to drink water on modafinil.

 

Cognitive Effects

Positive 

  • Focus enhancement. Your ability to focus on both, physical and mental tasks is increased on modafinil. How much? Depends on your genetics and dose and tolerance level. This makes it easier to study or play sports and makes you more efficient in them.
  • Increased Music Appreciation. Music tends to sound better on modafinil than sober. it usually sounds slightly sharper and louder.
  • Memory Enhancement. Your ability to memorize new memories and remember old ones is increased.
  • Motivation enhancement. You should be more motivated to get things done and take up new activities on modafinil.
  • Thought acceleration. Your ability to think should be enhanced and you should be able to think faster.
  • Wakefulness. One of the main aspects of modafinil. You should feel more fresh and awake, and you should feel the need to go to sleep. That’s why it’s best not to take modafinil before bedtime, though even if you do, it should make it easier to stay awake you shouldn’t have very much trouble falling asleep if you try to. Its wakefulness effect is definitely not as strong as it is on amphetamines or cocaine.

Neutral

  • Anxiety or Its Suppression. Modafinil can either suppress or increase your anxiety. That depends on the dose you take, low to moderate tend to suppress anxiety, whereas moderate to high doses tend to increase it, and your individual neurochemistry. So you can experience both and modafinil can have either positive or negative effects on your anxiety.
  • Emotionality Enhancement or Suppression. Depending on your individual neurochemistry, modafinil can either make your feelings more positive, for the most part, and pronounced, or your feelings can become slightly dulled. Both of these effects differ in intensity based on the dose that you take.
  • Time distortion. Time can either feel sped up or slowed down, depending on the user. How much? Depends on the dose