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When it comes to treating patients who suffer from sleep related disorders such as narcolepsy, doctors have a number of medication options. One of these drugs is Modafinil, the generic form of Provigil.
Modafinil is part of a class of drugs known as wakefulness promoting agents. While Modafinil can help manage sleep related disorders, it will not cure the condition.
This drug is also used off-label to treat ADHD and ADD, and has demonstrated a significant efficacy towards helping patients with these conditions. Modafinil is also used extensively as a nootropic cognitive enhancer.
But there are some doctors who have expressed warnings about the potential for addiction to this drug. How serious is this risk? Before taking Modafinil, it is important to consider the risks associated with potential addiction.
Alertness
Mental Acuity
Focus- Stimulates wakefulness in the brain
- Promotes mental acuity & processing
- Enhances focus, motivation & energy
Modafinil and Adrafinil
Related Topics
- What is Modafinil? (Provigil)
- How Does Provigil Work?
- Effects and Benefits
- User Reviews
- Typical Experiences
- Recommended Dosages
- How to Take
- Provigil Uses
- Use for ADHD
- Effects on Weight Loss
- Negative Side Effects
- Abuse Warnings & Dangers
- Comparison to Adrafinil
- Comparison to Armodafinil
- Comparison to Adderall
- Where to Buy
- Generic Modafinil Brands
- Is Modafinil Legal?
- How to Get Modafinil
- Review of Online Sources
Modafinil was first discovered in 1976 by Michel Jouvet, a scientist working for Lafon Laboratories in France. The discovery of this compound came about due to testing to determine the mechanism of action of another related compound, Adrafinil.
Adrafinil is one of a group of benzhydryl sulfinyl compounds that were developed by Lafon in 1974. It was found that in the body, Adrafinil is broken down in the liver into its component parts, the inactive modafinilic acid, and the active Modafinil.
Adrafinil and Modafinil are considered eugeroic compounds, meaning that they promoting wakefulness or alertness. While they have stimulant-like effects, they are not in fact related chemically to traditional amphetamine or methylphenidate based stimulants.
Effects of Modafinil/Provigil
The exact mechanism through which Modafinil works in the body remains unknown. It has been seen to affect multiple different neurotransmitters in the body including Histamine, Dopamine, Norepinephrine, and Orexin (also known as Hypocretin).
Some current research suggests that Modafinil boosts levels of Dopamine – a chemical in the brain that promotes wakefulness and increases alertness. It is thought that it does this by blocking the transport of Dopamine.
Additionally, Modafinil increases levels of Orexin, a neuropeptide that regulates wakefulness, arousal, and appetite. Orexin in turn stimulates Histamine, a neurotransmitter with similar effects. Studies with rats showed increases in Histamine and locomotor activity as primary results after administering the drug.
Modafinil is a nootropic drug, sometimes also called a “smart” drug. The impact of these drugs enhances an individual’s memory, attention, motivation, and cognitive abilities.
Studies have shown that Modafinil can improve mental performance and accuracy in cognitive tests for sleep-deprived individuals.
Many are concerned that smart drugs can be addictive or cause withdrawal symptoms when stopping their use. While individuals may be at risk of addiction and withdrawal from Modafinil, these symptoms are considerably less relative to comparable drugs such as Ritalin and Adderall.
When Doctors Prescribe Modafinil
Modafinil has several uses for adults. It is most often associated as a treatment for sleepiness resulting from narcolepsy, a disorder that results in excessive daytime sleepiness.
It is the drug of choice for many individuals with mild to moderate sleep issues. As a result, it has largely replaced Ritalin and other stimulants once used to treat narcolepsy. These drugs are associated with significant risks due to side effects, tolerance and their addiction potential.
Modafinil is also used to treat patients with shift work sleep disorder. These people experience excessive sleepiness while working late night or overnight shifts. Modafinil has been seen to improve performance and attention at work when it is taken before a shift.
Doctors sometimes prescribe Modafinil as an adjunct treatment for obstructive sleep apnea/hypopnea syndrome. While sleeping, breathing is labored or temporarily stops multiple times per night, leading to poor sleep quality and excessive daytime sleepiness.
Sometimes treatment with a breathing device worn during the night is not enough to eliminate all sleepiness, and Modafinil is sometimes prescribed in these cases.
Narcolepsy and obstructive sleep apnea patients usually take their Modafinil dosage in the morning. Those with shift work disorder typically take the medication an hour before reporting to work.
Studies have shown that patients taking Modafinil experience as much as a 50 percent improvement in their ability to remain awake. The same patients also experienced a reduction of up to 25 percent in involuntary sleep incidents. Increased alertness appears to persist for around eight hours.
Modafinil is commonly used “off-label” for uses outside of its approved uses. One of the most common off-label uses of Modafinil is for the treatment of attention-deficit hyperactivity disorder (ADHD). Multiple double-blind placebo-controlled studies have shown that compared to a placebo, Modafinil is significantly better at improving scores on a variety of tests of ADHD symptoms, including the ADHD Rating Scale-IV School and Home Versions and the DSM-IV ADHD Behavior Checklist.
As mentioned above, Modafinil is also very commonly used as a nootropic drug. Users say that it improves memory, concentration, focus, productivity, and alertness.
- Increases energy, wakefulness and motivation
- Boosts mental performance and focus
- Supports memory and cognition
Modafinil Tolerance, Dependence, and Withdrawal
At this stage, evidence of Modafinil’s addictive potential is largely anecdotal. Some scientific studies that have been conducted in the fairly long-term (10 years) have shown that no significant number of pediatric patients using Modafinil for narcolepsy developed tolerance.
However, some prescribing physicians have expressed concern that the long-term use of this medication could cause the patient to require higher and higher daily doses in order to achieve the same level of relief from sleepiness issues or the same cognitive enhancement benefits.
One way to steer clear of the potential risk of developing Modafinil tolerance problems is to avoid taking the drug on seven consecutive days of a week. Some patients are advised to skip a dose one or even two days each week.
Modafinil withdrawal symptoms after discontinuation of the drug depend on a case to case basis and length of time the individual has been on the medication.
In addition to feeling increased fatigue, patients have reported decreased attention span, shortness of breath, depression, anxiety, and sleepiness. Individuals who have been on the drug for years should taper their doses rather than suddenly stop taking Modafinil .
Physicians and patients should weigh the risks of taking the drug on a long-term basis. Potential tolerance towards the drug should be closely monitored by the physician.
Individuals at highest risk are those with current or past addictions to substances like cocaine, alcohol, or nicotine. Patients with a family history of addiction might also face elevated risk.
Methods to Avoid Modafinil Tolerance
There are various methods out there for avoiding a Modafinil tolerance issues. User reviews and suggestions on forums online provide many different tips and tricks for hopefully avoiding this occurrence with long-term Modafinil use. The following are some of the most recommended ways to avoid developing a Modafinil tolerance:
1. Limit Dosage Level
There are no officially recommended dosages for Modafinil off-label uses. In most cases, people who are using Modafinil as a smart drug will follow the guidelines set for approved sleep disorders when determining their dosages.
Modafinil is often prescribed at a dosage of 200 mg per day for narcolepsy, shift work sleep disorder, and obstructive sleep apnea/hypopnea syndrome. Typically nootropic uses take similar dosages. Sometimes a lower dosage of 100 mg per day is enough for some people to get the benefits they want.
For most uses, Modafinil is typically taken once in the morning. Sometimes the dose is split into one dose in the morning and another near noon to extend the effective hours.
Taking a higher dosage for an extended amount of time could possibly lead to developing a Modafinil tolerance. Some people have been known to take dosages of 400 mg per day, often split in to a few doses during the day for prolonged effects and increased wakeful hours.
While this may work for the short term, continually taking high dosages is not recommended due to the greater potential for side effects, and possible Modafinil tolerance as your body adjusts to the high amount.
2. Limit Weekly Usage
While Modafinil is often prescribed for use for sleep disorders on an every day basis, it possibly should not be taken this way for off-label uses such as cognitive enhancement. Similarly to limiting your dosage amounts, limiting how often you use Modafinil may help to avoid a tolerance issue.
The amount of Modafinil in your system may begin to build up if you are taking the drug every day. This could lead to a feeling of diminished effects as your body adjusts, and the eventual increasing of dosage to regain those benefits.
It is recommended by many users to not take Modafinil back-to-back on consecutive days. Instead, skipping at least a day in between doses is a common way that users try to avoid developing a tolerance. Some users have reported using Modafinil as few as one time a week to help keep the effects strong each time they take the drug.
3. Cycle Usage
Hand in hand with limiting your weekly usage of Modafinil is limiting your overall on and off times with the drug. Especially in people who are taking Modafinil a few times a week, having a break could help prevent a tolerance issue.
Some people have reported using Modafinil straight for two weeks to really focus on exam prep or preparation for a large presentation, and then taking a two week break. While taking Modafinil every day in a week is not typically recommended to help avoid tolerance, the use of a comparatively long off period may help reduce that risk and keep effects at a regular level when doses resumes.
Other cycles that have been reported include using Modafinil for 1-4 days per week for a few months straight, and then taking between two weeks to a month off. Because of the long period on Modafinil even at lower dosage, a longer period off may be required.
Some users report the effects feel stronger again when they start Modafinil after a break, which may indicate that a tolerance had started before they stopped dosages.
4. Use Magnesium Supplements
Some users have reported having success avoiding or reducing Modafinil tolerance by taking magnesium supplements. Magnesium is an essential dietary mineral that is known to have effects on brain health.
In research, magnesium has been seen to affect the NMDA receptors in the brain and help prevent over-excitability. These receptors are known to play a crucial role in the development of tolerance, addiction, and withdrawal.
While a study done in rats showed that a combination of calcium and magnesium was able to help prevent the development of addiction and tolerance to morphine, research is lacking in humans. How effective this method may be is still unknown, but anecdotally it has been said to work.
Many Modafinil users have reported that taking magnesium supplements is able to “reset” their tolerances and allow them to feel the effects of the drug again at normal levels.
5. Substitute Alternatives
While cycling off can be important to help avoid developing a Modafinil tolerance, many people do not want to go for an extended period of time without their normal cognitive boost. One way to keep getting nootropic effects when not on Modafinil is to look in to some alternatives.
It is smart to not become reliant on any one smart drug, as that can be when issues arise. Instead having a few different compounds that you cycle between may help keep effects of each optimal.
Because Modafinil is a prescription drug, it is already hard for people to get for off-label uses. Because of this, many nootropic users have instead turned to the use of non-prescription Modafinil alternatives such as Adrafinil or the Racetams.
Adrafinil, as discussed previously, is the prodrug of Modafinil. This means that that the body breaks down Adrafinil into the active Modafinil when it is ingested. Because it is not a perfect conversion, a higher dosage of Adrafinil must be taken to get the same effects as a lower Modafinil dosage.
The effects from Adrafinil are said to be very similar to those of straight Modafinil. There is a longer lead time before effects are felt as the drug is metabolized in the body, but then the effects should be comparable to taking Modafinil.
There is the potential for a buildup of hepatotoxic enzymes that accumulate from the breakdown of Adrafinil in the liver, so it is not recommended to use it every day. Instead it is often saved for special occasions and times when an extra cognitive boost is needed.
Because it affects the same neurotransmitter systems as Modafinil, Adrafinil should ideally be used as an alternative for Modafinil, instead of an addition to a nootropic cycle. Switching from one to the other will not help to avoid tolerance, and they should ideally be used separately.
One class of nootropics that have been used when cycling off Modafinil are the Racetams. Originating with the parent compound Piracetam, this group of substances have been seen to have effects on the cholinergic neurotransmission systems in the brain and central nervous system. Increased levels of Acetylcholine are tied to improved general cognition, as well as enhanced memory formation and recall.
Since the development of Piracetam in the 1960s, more potent derivatives have been developed, including Aniracetam, Oxiracetam, Pramiracetam, and Phenylpiracetam. The Racetams can be used as a substitute for people who cannot get Modafinil legally, as well as for people who are looking for an alternative while they are off of Modafinil.
Some other Modafinil alternatives that have been suggested by users to be used in a cycle when off Modafinil include the nootropic supplements Alpha Brain by Onnit Labs and Sulbutiamine.
Modafinil Addiction Concerns
Some studies have suggested that Modafinil can be habit forming and that there is a potential of addiction. This is a significant concern among those who seek the medication as a cognitive enhancer.
Brain scans of 10 healthy male subjects who took either the brand (Provigil) or a placebo showed that the former blocked Dopamine transporters.
These transporters take dopamine away from receptors on neurons. By blocking the removal of Dopamine, Modafinil increases activation of Dopamine brain receptors, creating a neurological reward response.
Increased interest in the potential of Modafinil addiction has generated additional studies. Because the drug has been shown to break down neurotransmitters that cocaine and methamphetamine require, researchers are looking at whether Modafinil could help patients who are addicted to these narcotics.
Since medications tend to affect individuals in different ways, researchers believe Provigil could prove highly addictive to certain patients who are vulnerable to the way it works. The potential for large-scale abuse seems limited, however.
Side Effects of Modafinil
The primary side effects associated with Modafinil include headache and nausea. Headaches are the number one most reported side effect in research studies and user reviews. It has been estimated that over 35% and as much as 50% of people who take Modafinil may experience headaches at some point.
Other mild side effects that have been reported include:
- Diarrhea
- Nose and throat congestion
- Dry mouth
- Back pain
- Anxiety
- Nervousness
- Dizziness
- Psychiatric side effects
- Insomnia
In some cases, side effects may occur when you first start taking Modafinil. Like any drug, your body must adjust to the compound in your system, and it is possible to develop some side effects. In cases where an adjustment period is necessary, side effects often diminish after a few weeks.
Sometimes the occurrence of side effects is simply due to dosage level. Just as taking too high of a dosage for too long may lead to tolerance, too high of a dosage for your personal physiology may lead to side effects. For some people, reducing the dosage can help to eliminate or reduce side effects to a manageable level. If possible, you can try gradually increasing your dosage back to normal levels, but only do so if you are not seeing the benefits you want at a lower dosage.
There is the possibility of developing a rare, but serious skin and mucous membrane disorder when using Modafinil, including Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), or drug reaction with eosinophilia and systemic symptoms (DRESS).
While the evidence is not fully conclusive at this time, it is thought that some people have a genetic predisposition to developing these reactions when they take certain drugs, including Modafinil. The incidence of this condition in clinical research is very low, with no cases having been reported in studies in adults, and one case (the diagnosis was later recanted) having been reported in in a pediatric study.
It is important to be aware of the possibility however. If you develop a fever, flu-like symptoms, and a spreading, blistering rash, than stop doses of Modafinil and seek medical attention immediately.
Drug Interactions and Contraindications
Modafinil is contraindicated with a large number of other drugs. Modafinil has been seen to have negative interactions with the following drugs:
- hormonal/steroidal contraceptives
- Midazolam
- Triazolam
- Cyclosporine
- Diazepam
- Propranolol
- Phenytoin
- Clomipramine
- Omeprazole
- Warfarin
- MAOIs
- Cold and flu medications containing chlorpheniramine, hydrocodone, phenylephrine, and/or guaifenesin
This is not an exhaustive list of all the drugs that Modafinil is contraindicated with. It is important to speak with your doctor to determine any and all interactions that Modafinil may have with medications or supplements you are currently taking.
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Article last updated on: May 12th, 2018 by Nootriment