How Does Modafinil Work?

I’m sure you already know a dozen or so celebrities who have used Modafinil including President Obama. A lot of folks would like to know how this smart drug works to achieve the extraordinary feeling that users claim to have experienced.

Modafinil is the most popular smart drug that helps users to stay awake, remain upbeat and optimistic, and improve their concentration to stay incredibly focused on tasks while avoiding the nervousness that’s associated with other stimulants. It’s therefore important for users to understand the way Modafinil works in their body and how it affects various functions during its action.

 

How does Modafinil compare to other stimulants?

Modafinil shares biochemical mechanisms with other addictive stimulant drugs. The drug works by binding itself to the dopamine transporter, which is the “feel good” point within the brain. The drug is classified as a schedule IV controlled substance which describes it as having a low potential for significant addiction.

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As mentioned, Modafinil uses the same biochemical mechanisms as other nootropics such as cocaine and Adderall. However, there is a huge difference in the after-effects of these amphetamines when compared to Modafinil. Modafinil is found to be weaker in inhibiting dopamine transport compared to Adderall but more selective in action sites and seems to last longer than other stimulants.

 

How Modafinil came to be

Modafinil is a racemic compound, which means that it is made up of two enantiomers. The R- and S-enantiomers have been found to have different pharmacokinetics.

Modafinil, a wakefulness-promoting drug that is taken orally, was initially approved for medical use across the United States in 1998. The Food and Drug Administration, FDA, which is the regulatory agency in the U.S., established that the drug is effective in reducing excessive sleepiness in the following sleep disorders:  obstructive sleep apnea (OSA), narcolepsy and shift work disorder (SWD).

Apart from its wakefulness-promoting effect, Modafinil produces variations in mood, perception, thinking, and feelings. It also has psychoactive and euphoric effects which are generally observed when using other Central Nervous System (CNS) stimulants.

Modafinil normally binds to the dopamine reuptake site and has been observed to cause an increase in extracellular dopamine in the brain. This produces the euphoric effects that are associated with the “feel good’ experience.

Absorption of Modafinil tablets is rapid. Peak blood concentrations have been established to occur at 2-4 hours. The effective half-life (the time it takes for the drug to pass through one’s system) of Modafinil is about 15 hours after dosing.

The effect of Modafinil can be defined by the way it affects different functions. These include;

1. Effect on Dopamine
2. Non-Dopamine effect
3. Recovery time
4. Effect on Sleep
5. Effect on Anxiety
6. Dependence and Abuse Potential
7. Timeline to kick in
8. Modafinil -> dopamine

 

Scientists had long determined the clinical action of Modafinil. What wasn’t clear were the actual targets that could be varied to react to its action.

The exact mode of action through which modafinil enhances wakefulness is unknown. However, cell-membrane monoamine transporters have been identified as potential targets

These transporters are responsible for clearing monoamines from the extracellular space surrounding the neurons. The transporters, in this case, include the serotonin transporter (SERT), the noradrenaline transporter (NET) and the dopamine transporter (DAT).

Now, the interesting part is that all receptors have an affinity for dopamine. This puts dopamine at the center of all activities. The unique observation is that the dopamine transporter has a very little affinity for dopamine compared to the noradrenaline transporter. At this point, the actual mode of action employed by Modafinil remains elusive.

Nevertheless, scientists have studied the action of amphetamines and other stimulants that enhance wakefulness and most of them inhibit the monoamine transporter.

Further examination indicated that the augmented levels of dopamine leading to extended periods of wakefulness were as a result of Modafinil homing in on the dopamine transporter (DAT).

It was concluded that the properties exhibited by Modafinil in inducing wakefulness are a result of the drug actively binding itself to the dopamine transporter. This activity has been closely associated in with augmented extracellular dopamine levels in some parts of the brain.

 

1. It’s not all about dopamine

As scientists continued studying the effects of Modafinil, more discoveries were made. The drug’s primary action was found to aim at other transmission systems apart from the dopamine signaling pathways. It was found that Modafinil affects the a1 adrenergic signaling pathway. This pathway has been found to be the main regulator of sleep-week cycles. The uncertainty is whether the wakefulness is brought about by increased levels of dopamine or as a direct hit from Modafinil.

As a dopamine receptor blocker, Modafinil has been found to influence glutamatergic (upwards), adrenergic and GABAergic (downwards) transmission.

 

2.  Why it’s easier to recover after taking Modafinil (compared to Adderall and other stimulants)

The dopamine signaling pathway is the trigger point for the prolonged epicenter of wakefulness. This fact is firmed by the fact that most smart drugs like Adderall and Modafinil act on dopamine to bring about this effect.

The interesting part is that despite Modafinil and Adderall sharing the same action point they differ considerably when it comes to side effects, with Modafinil yielding the minimum.

The big question is why does Modafinil use yield fewer side effects?

The biggest differences between Modafinil and Adderall

Both Modafinil and Adderall have side effects that can be grouped into categories that define what users experience in the aftermath in terms of sleep and anxiety.

 

3.  Modafinil, Adderall, and Sleep

There is a notable difference in the effects of Modafinil on sleep as compared to other wakefulness-enhancing methamphetamines. Methamphetamines like Adderall keep users awake at a price that has to be paid later with “extra sleep”.

It’s normal for the body to demand longer sleep after a period of wakefulness.

However, the supposition would be that Modafinil slows down the rate at which sleep accumulates during a period of wakefulness and Adderall, on the other hand, seems to increase the rate at which sleep accumulates during a given period of wakefulness.

Explanation #1: Modafinil decreases our need for sleep

It was observed that an individual’s need for sleep was the same in both cases of wakefulness induced by normal sleep deprivation and wakefulness induced by Modafinil. The conclusion here is that Modafinil does not reduce the rate at which sleep need accumulates during wakefulness.

Explanation #2: Adderall increases our need for sleep

Adderall is known to affect the noradrenergic (NET) and serotonergic (SERT) receptors. These signaling pathways are the main regulators of sleep patterns. It’s, therefore, possible that the actions of such amphetamines directly contribute to sleep debt accumulation.

In that case, Modafinil would not affect the quality or quantity of sleep or the effect would be minimal. Could this be the reason why Adderall causes much anxiety compared to Modafinil? Let’s dig further….

 

4.  Why Modafinil doesn’t cause anxiety

Most methamphetamines have been found to enhance wakefulness and restlessness.  This is due to their binding action on DAT which induces locomotor behavior that manifests in anxiety.

Some users have reported episodes of anxiety after using Modafinil. This could be as a result of the decrease in GABA. The general observation is that Modafinil will enhance wakefulness with minimal increase in movement.

The likelihood of experiencing anxiety while using Modafinil is much lower compared to Adderall.

 

5.  Why isn’t Modafinil addictive?

The growing acceptability of Modafinil makes it a plausible candidate for dependability among heavy users. Interestingly this is not the case.

The key lies in the drug’s interaction with DAT. Modafinil inhibits DAT in a way that gives the user an upbeat feeling but without the necessary “high” that is common when one uses cocaine or Adderall. This is significant because that high feeling is the trigger to addiction.

Modafinil is reported to bind mildly to the dopamine uptake site leading to a slow release of dopamine.  In contrast, amphetamines bind tightly to the dopamine transporter resulting in a faster release of dopamine.

 

6. Why does Modafinil take so long to kick in?

Modafinil binds to the DAT in a slow mechanism that releases dopamine from the system at measured intervals. This is unlike the dopamine rush experienced with amphetamines. That’s the reason it may take one or two hours to start feeling the effects of Modafinil.

 

Give it a try

Modalert is a mild nootropic whose action lasts longer and has fewer side effects compared with other smart drugs. The secret to its mildness is the slow binding to the dopamine receptor. This allows for the slow release of dopamine that helps to enhance wakefulness and focus for an extended period.

However, Modafinil remains a potent cognitive enhancer that has proved itself as the most recognizable in its class. It is a safe Eugeroic that will keep you awake, alert and at the same time enhance your mood while improving your memory.

Its efficacy has fascinated governments, academics and other professionals across the world.

Now that you know the mechanism behind Modafinil, grab one and power your productivity by staying awake and focused.