Adrafinil: a quick re-cap

It is worth admitting from the outset that available literature on Adrafinil is sparse in comparison to its alternative, Modafinil. This, however, should not swerve users from opting for Adrafinil.

Adrafinil began its development in France in the late 1970s and is now considered a eugeroic, i.e., a wakefulness-promoting agent. Its cognitive benefits are enhanced by noted improvements in day-time alertness, motivation, mood and energy levels.

So…does it do what it intends? Plenty of user reviewers think so.

“This product has worked remarkably for me thus far. I can definitely tell the difference between this and any other stimulants I’ve tried. The difference being Adrafinil creates a much smoother feeling of being awake and alert” (Danny on Powder City)

 “I had an increased awareness of what was going on around me, I felt very optimistic about everything, and I had almost God-like powers to think and concentrate. I felt very much awake” (Alza_36 on Drugs-forum)

“This product has worked very well just as described. I am put in a better mood, become more motivated, feel less stressed, and able to focus and problem solve much easier” (Corey on Powder City)

“Adrafanil kicked in after an hour of orally ingesting the substance, one 300 milligram capsule, and immediately I was in the zone, and knew it was the strongest nootropic I had ever taken” (Stephen on nootriment.com)

“It lacks the over-stimulation of amphetamines, and instead has a mellow openness” (LifeSucceedsDeath on Drugs-forum)

In Britain, Adrafinil is not a controlled drug and does not require a prescription. This means that it is not measured under the Misuse of Drugs Act 1971, a legislation that governs the regulation of drugs. However, Adrafinil’s legal status remains in grey area. It is lawful for purchase by British residents, but only for personal use. The drug is, however, currently legal in the U.S. and UK so can be bought, prescription free, as an alternative to Modafinil.

What was Olmifon?

However, in October 2011, Olmifon, the marketed brand name of Adrafinil, was discontinued. There are plenty of reports theorising the reasons for the discontinuation. In short, the benefits/risks of Adrafinil were reassessed by the French Government and the results were inconclusive. These findings led to Cephalon, a biopharmaceutical company and original manufacturer of Olmifon, to stop marketing the drug in France.

Despite this, the popularity of Adrafinil has risen. Why? It can still be obtained cheaply online without its manufactured moniker. There are, of course, risks to consider when buying from the internet. The drug itself may not be the real deal, so it is therefore imperative that your online manufacturer can provide a COA, or Certificate of Analysis, on demand. This means that the substance batch has undergone a third-party laboratory analysis to ensure that your purchased drug matches its label, and that it is not riddled with contaminants.

So, once acquired, how does Adrafinil actually work for you? Well, initially, let us consider Modafinil. This particular drug was developed to counteract sleep disorders such as Narcolepsy. Then, Adrafinil came along; a prodrug to its relative Modafinil. The supplementation of Adrafinil increases concentrations of Modafinil in the body.

How does Modafinil work?

When ingested, Adrifinil affects the Dopamine and Serotonin systems. Dopamine improves mood, while Serotonin plays a pivotal role in controlling our sleep cycles and pleasure feelings. Both are very powerful neurotransmitters. A neurotransmitter is:

“a chemical substance which is released at the end of a nerve fibre by the arrival of a nerve impulse and affects the transfer of the impulse to another nerve fibre, a muscle fibre, or some other structure”.

Histamines act as a neurotransmitter. The histamine receptors are found, for example, in the central nervous system. Modafinil has been found to enhance histamine activity by stimulating the central nervous system. This increased activity therefore impacts other nerve fibres/muscle fibres in the body; a process improving overall levels of stimulation, and impacting positively on focus, attention and motivation. Adrafinil generates the same results, but is not paired with the feelings of irritability, anxiousness and nervousness which are routinely experienced through the use of other stimulants.  Many reviews sing the praises of Adrafinil. One such Reddit reviewer, cccg, explained their experience:

“The first day I took them, I could focus on tasks I would have otherwise thought to be really boring, and that for hours. After a 10-12 hour day at the office and only 5 hours of sleep the night before, I had plenty of energy to go for a 10km jog, and I was running faster than ever. It felt like a bunch of warning receptors inside my body had been muted. I could now choose to either consider or dismiss signals of hunger, fatigue, desire to procrastinate, pain in my legs, or a high heart rate. This ability to DECIDE what I was going to spend my time on made me feel very powerful and in total control. I thought I was the protagonist in “Limitless”.”

Meanwhile, a Longe City user (Rhcan09) agreed that Adrafinil’s side effects excluded those typical of other stimulants:

“There were absolutely none of the side effects of caffeine or other stimulants. No jitters, no crash, no fogginess.”

Adrafinil actually gets converted into Modafinil when it reaches your liver. This is where alarm bells ring most loudly with relation to potential problems that may occur. So, now the basics have been traversed, let us consider Adrafinil side effects in full.

Firstly: Modafinil Side Effects

I will begin by considering the effects of Modafinil. This is vital in understanding Adrafinil side effects afterwards. Modafinil is the active metabolite from Adrafinil consumption. N.W Milgram’s explanation below is very helpful in understanding the relationship between the two stimulants:

Adrafinil has two metabolites, modafinil and CRL 40476. Little is known about CRL 40476. Modafinil, on the other hand, has been much more extensively studied, and the production of modafinil is likely to account for at least part of the effects of adrafinil. Thus, adrafinil has very similar pharmacological effects to modafinil. Moreover, the behavioral effects of adrafinil are more closely tied to the pharmacokinetics of its metabolite modafinil.

So, there we have it. Concentrated amounts of Modafinil are generated in the liver when Adrafinil reaches that region after ingestion. This is why considering the side effects of Modafinil are equally important to consider: not only does Modafinil have much more literature readily available for study, but it is also a component within Adrafinil itself.

So, with it being Adrafinil’s closest relative, it is worth us firstly considering Modafinil side effects. How do they compare?

Modafinil’s most commonly recorded side effect is a headache, noted in more than 1 in 10 persons. Less common, found in 1 in 100, are the following (nhs.uk):

• abnormal laboratory test results
• anxiety or worsening of anxiety
• blurred vision
• chest pain
• confusion
• constipation
• depression
• diarrhoea
• difficulty sleeping
• dry mouth
• faster heart rate
• feeling dizzy
• feeling nervous
• indigestion
• loss of appetite
• nausea
• palpitations
• paraesthesiae
• sleepiness
• stomach pain
• unusual thoughts
• vasodilatation
• weakness

That is a lot! Unsurprisingly, Modafinil side effects are discussed in abundance around the internet. Reddit users seem to be in agreement on the negative Modafinil side effects. One reviewer called adhd_patient stated:

“This is the best discussion forum I’ve found about Moda side effects. I started taking 200mg for ADHD few days ago and I’m experiencing most of the side effects mentioned here:

mild headache, drowsiness, chest pain, higher heart beat and spike in blood pressure (I’m on 3 BP meds already), lack of creativity and generally slower in thinking, also lower manual precision (like chopping stuff or kitchen work), less emotional in social interactions and less affectionate toward loved ones.”

Other users, like WizardryAwaits, take equally hard stances against Modafinil side effects:

“For me the following negative side effects are very noticeable for me after taking modafinil:

• Extreme insomnia. Even if I take half a pill (100mg) at 7:30am, by 3am the next night I will still unable to sleep, even if I feel tired, and even if I have not slept for 48 hours. It’s like a switch has been flicked in my brain which disabled my ability to fall asleep. The sleep disruption even lasts for days for me. After taking it once, only three days later do I get a good night’s sleep.
• Drastically increased effects from caffeine. My caffeine tolerance disappears completely, and the negative effects from caffeine become much more pronounced. After a single cup of coffee I was:
• Euphoric
• Very anxious/nervous
• Experiencing shaking/tremors of the hands and difficulty of fine motor control
• Having heart palpitations and heart pain
• Dry mouth
• Having to pee very frequently
• Had a panic attack”

On Longe City, user 2/1_kiwi, was equally disappointed with Modafinil side effects:

“My results with modafinil were poor, I just got headaches, felt mentally foggy and then developed insomnia. Wasn’t the wonder drug I was hoping at all.”

Adrafinil side effects

Does the same apply to Adrafinil? Well, nootriment.com notes that the most common Adrafinil side effects are:

• Stomach pains
• Nausea
• Dizziness
• Headaches

If you require a coffee, without fail, every morning, then you’d be forgiven for thinking immediately of caffeine in relation to Adrafinil side effects. If you’re unfamiliar (maybe you’re prefer a tea), then the following are what you may experience if you have withdrawals from caffeine:

• Drowsiness
• Headaches
• Irritability
• Nausea
• Vomitting

A little perspective on Adrafinil side effects

This is some indication of how Adrafinil should not be feared. Its potential side effects are very similar to those of caffeine: a drug used without trepidation by millions, and on a daily basis. Though the thought of unwanted side effects might seem scary; let us add a little perspective. When you stand at your kitchen work-top in the morning, do you stop and think: wait, wait, wait. What if I take one sip of this coffee and have crippling pains and the fear of dying for the rest of the day? When you stand in a supermarket, do you look at the array of coffee brands, thinking to yourself: “these will all do something very bad to my body. I’m stepping away immediately”? I am of course exaggerating my point here, and it is obviously very important to be wary of the drugs you ingest and to what extent they might affect you. After all, everyone has different bodily sensitivity levels. But, as with anything, things are created, tested and approved for the majority. This ultimately and always leaves a small minority displeased.  But, at the same time, this means that the possible side effects are only seen within that very minority. Others able to use Adrafinil safely, happily and daily to achieve the results they desire for their own bodies – without fear of what could happen in very rare scenarios.

Like caffeine, Adrafinil has energising effects, but with less harmful bodily repercussions than is typical for any other stimulant. Overall, the supplement is not known for causing side effects like increased blood pressure or heart problems. As with the misuse of any substance, though, these things can occur – especially for those with pre-existing conditions. Precautions must therefore be taken to avoid such occurrences. The first simple step to ensure safety is following the usage guidelines. A savvy approach wields the desired results.

Adrafinil and the liver

It is in the liver that Adrafinil is converted to Modafinil. This is where the most pertinent Adrafinil side effects might crop up.

The conversion process between Adrafinil and Modafinil essentially pertains to the former breaking down into the latter as a compound. The process puts strain on the liver and raises the levels of key enzymes in that region. A continual build-up of these enzymes may leaves lasting damage upon the liver. It is typically after six months of daily use that symptoms make themselves apparent. Different people will, however, have different sensitivity levels.

One Longe City user, ModaMinds, consolidates the necessity of taking logical approaches to the use of both Adrafinil and Modafinil to minimise the side effects. This certainly indicates the potential health risks of both drugs, showing that Modafinil should be taken no less cautiously than Adrafinil:

“…if you’re taking adrafinil five days a week, then yes there is concern for liver damage down the road. You are on a lower dosage than usual for adrafinil, but as with any med that is taken daily (or most days in a week), it is conceivable that your liver will be affected, especially when mixed with alcohol. If you switched to modafinil/armodafinil, the effects would be slowed, but if still dosing five days per week, I would still be concerned about long-term consequences.”

As with most drugs, if the recommended dosage is adhered to, Adrafinil is considered safe for healthy users. Of course, it should not be taken over a long-term period. Cycling your use will definitely help the liver clear itself and regenerate its correct levels of enzymes.

Cycling Adrafinil means that, for example, if taken daily for two weeks, then two weeks should be taken off (nootriment.com). Approaching your use in this kind of way also works at keeping tolerance of the drug down… what a positive if you want to continue reaping the benefits! After all, moderation and awareness is the key to good health.

Adrafinil liver problems

The most notable Adrafinil side effects occur after sustained use of the drug. Such problems are located primarily in the liver and pertain to the development of harmful enzymes. These, as briefly discussed above, can build up within the liver, raising the amount to levels deemed unhealthy. The saying goes that too much of anything is not good thing – this is certainly applicable both to the supplement of Adrafinil on a permanent basis and to the amount of enzymes in the liver.

Adrafinil liver enzymes

So, what exactly are enzymes? They exist in living organisms and are, essentially, catalysts for specific biochemical reactions within the body.  At the beginning of a reaction process, there exist molecules called ‘substrates’. The enzyme converts these into ‘products’. All metabolic processes in cells require enzymes to, put simply, react within the body at rates fast enough to sustain life. I know, this does all sound quite school-textbook Science, but it is nevertheless important info to know when considering Adrafinil. Why? Because, remember, the sustained use of Adrafinil affects the level of liver enzymes.

Now, various reports around the web suggest that the enzyme involved in metabolising Modafinil once Adrafinil reaches the liver is Cytochrome p-450 (refer to Andrew Parkin’s study if you fancy a complete scientific follow-up). Cytochrome p-450 (often abbreviated “CYP”) is a class of enzymes that is involved in the metabolism of many medications and is located primarily in the liver (Straight Healthcare).

In fact, Straight Healthcare provides much succinct information in relation to enzymes in the liver:

• When CYP inducers or inhibitors are taken with other medications that are metabolized by the same enzyme, they can alter the metabolism of that medication
• Certain chemicals and foods (ex. tobacco smoke and grapefruit juice) may also act as CYP inducers and inhibitors
• Drugs may be metabolized by a CYP enzyme and also inhibit or induce the enzyme at the same time
• Inducers and inhibitors can be subdivided into strong, moderate, or weak based on how much of an effect they have on the enzyme

There is further discussion on the drug interaction with relation to liver enzymes and their metabolism of said drugs. This just screams relevancy to our topic of Adrafinil side effects in the liver…

“DRUG INTERACTIONS ARE CHALLENGING”

• Information on drug interactions can be difficult to assimilate
• Certain drug interactions and metabolic pathways are well-documented, while many are not

Factors that can make drug interactions challenging include the following:

New drugs

• When a new drug is being developed, the FDA requires that it be tested for drug interactions with a small number of medications that are known to have significant interactions
• Obviously, there is no way to test a medication in every possible drug combination that may occur. This means most drugs come to market with incomplete drug interaction profiles
• After a medication is prescribed to a large number of people, other drug interactions are inevitably discovered”

What this reiterates is the necessity of realising that Adrafinil has been tested to its full potential, and on the majority. Any side effects that are possibly experienced after ingestion are therefore voiced by the minorities, and should not be cause for unwarranted fear within a new user who, it is highly probable, will fit in the ‘majority’ category.

Adrafinil liver failure

In the worst case scenario, a build-up of liver enzymes can lead to failure of the organ. Liver failure occurs when large parts of the liver are damaged beyond repair, meaning the liver itself can no longer function. It is a life-threatening condition necessitating immediate medical attention, but, most often, liver failure occurs over many years and at a gradual pace. But, do not fear; the typical causes of liver failure are long-standing or inherited conditions such as (info sourced fromwebmd.com):

·      Hepatitis B

·      Hepatitis C

·      Long term alcohol consumption

·      Cirrhosis

·      Hemochromatosis (an inherited disorder that causes the body to absorb and store too much iron)

·      Malnutrition

Adrafinil certainly does not appear in nasty lists like the above! To avoid concerns, Adrafinil users should follow our Adrafinil dosage guide: stating 600mg -1200mg of Adrafinil three times a week for a maximum of five months.  While infrequent use is certainly not said to cause liver failure, further ways of mitigating potential Adrafinil side effects would be to not taken it in conjunction with drugs shown to have similar effects on liver enzymes.

Adrafinil Liver Test

If concerns do occupy you, there are various methods of addressing worries. Liver function tests (LFTs or LFs) involve blood tests that provide useful information for a patient about their liver. Biochemical tests are indeed helpful in the evaluation and management of liver problems. They can detect the presence of disease, distinguish between different types of disorders and can even predict the extent of existing damage. These tests are routinely undertaken to ensure that any medication being used is not damaging the liver. Perfect, then, if you’re beginning to worry about potential Adrafinil side effects in this region of the body. However, there are certainly other precautions that can be taken to prevent the necessity of an LFT. This is especially reassuring if blood tests don’t appeal to you!

To prevent or mitigate Adrafinil side effects in the liver, you may begin by seeking advice from your doctor.  As with starting any new health procedure, it is important to know all the facts beforehand – especially if you suffer from other medical conditions. You could be taking other supplements or drugs, you might be pregnant (definitely don’t take Adrfinil if you’re expecting a baby!). Clearly these kinds of issues are worth prioritising when researching or contemplating using Adrafinil.

If Adrafinil is your chosen drug, then its recommended dosage should become your go-to piece of information. It is recommended on nootriment.com that between 150mg to 300mg should be taken daily and in the morning. Adrafinil is not recommended for long term use, though, and taking a break from it every now and again is advisable. Although sites like nootriment.com are helpful, it is strongly recommended that you adhere to the Adrafinil manufactureres insert for guidance.

Adrafinil Liver & Milk Thistle?

During these breaks, taking milk thistle works as a great defence against the appearance of any unwanted Adrafinil side effects. Milk thistle is a flowering herb related to the daisy family and is sometimes used as a natural remedy for problems such as jaundice, cirrhosis, gallbladder disorders and hepatitis. Some claim that it also benefits the heart by lowering cholesterol levels… another win!  Milk thistle can be taken orally in supplements or in tea and can be combined with other herbs. It restores liver health by detoxifying the organ and, if properly cycled with Adrafinil use, should evidence benefits whilst minimising the appearance of undesired side effects. Reddit user ace_trees certainly agrees that overall precautions are logical when taking Adrafinil:

“… some livers can handle years of alcoholism, meth, coke, and heroin, others develop liver damage after the occasional binge drinking in college. It really depends. If you are worried, get liver enzyme tests done. Further, not drinking soda and staying hydrated will not mitigate possible liver damage. That being said, adrafinil only on weekdays will most likely not give you liver damage, especially if you keep the doses low (300-400mg). If you are worried, supplement with milk thistle or something helps with liver health and take occasional days off.”

Adrafinil effect on liver – Summary

Whilst it may be true that the conversion of Adrafinil to Modafinil occurs in the liver specifically, it is mostly anecdotal evidence that suggests problems in this organ arise thereafter.

Having read – and, of course, I invite you to do this as well! –  a variety of user posts on the  relationship between Modafinil/Adrafinil/liver, there is, simply, a mixed bag of results. Some threads contain, as with this post from Disi on Longe City, tentative suggestions that their liver has been affected after using one of the stimulants:

“I have been reading a lot of good comments on modafinil. I used to take it for few days(maybe more than week) but as I recall I had pains in my stomach(back of…liver?)”

Meanwhile, other posts simply agree that the only way to reassure yourself about potential liver damage is to have regular check-ups. Blood tests, liver enzyme tests… they are all readily available, but should not be absolutely necessary if the recommended directs of use are adhered to! Reddit user mlhill definitely provides food for thought:

“The thing is, there are a lot of things that raise liver enzymes when they are metabolized. For example Codeine gets metabolized into morphine, codeine itself is not an effective pain killer. Even Paracetamol/APAP will raise your liver enzymes in safe therapeutic dose level.”

It is important, then, to take in all of the advice provided above. As with anything, side effects can be lessened if the label on the bottle is read and if prior-product-knowledge is as strong as it can be. There are many, many further articles on the internet that provide equal amounts of good, helpful information on Adrafinil as a supplement in its entirety.

Adrafinil side effects reddit

So, what of all of this? Well, it is certain that Adrafinil side effects should be thoroughly explored prior to the purchase of the drug. As with any new product, research is vital. That goes for legitimacy of the product (remember the COA!), the comparisons to Modafinil side effects, the recommended dosage information and, of course, precautions to be taken once the drug is used (Milk thistle!)

It is very helpful to stand back and apply a bit of perspective when considering Adrafinil side effects. It is a drug used by thousands and the potential risks are generally not seen with low, short doses – which is how the drug is advised to be taken. The excellent results that can be gained from using Adrafinil definitely outweigh thoughts of what might happen if misused.

Remember, as with any drug that can be taken by thousands, there will always be negative reviews. 95% of Adrafinil users reap the great benefits of the supplement in comparison to the small percentages that are opt-out.

As with any drug used daily and by many – from paracetamol to caffeine – the rise of any concerns in relation can easily be addressed. This Reddit user (Alza_36) quite succinctly sums up the key issues to be considered before Adrafinil is ingested:

“Consider

• Do research. Examine other posts addressing Modafinil and Adrafinil before using, and be sure it is right for you before you being dosing.

• You should take no more than 50mg on your first dose. You may be allergic, or you may be affected by this drug unusually. If you worry about the effectiveness of a dose that small, take into consideration that I had a great experience with it at only 50mg.

• Do not combine this drug with any other psychoactive drug until you know its full potential and how it affects you.

• If you plan on prolonged use of Adrafinil, I would advise you to seek your doctor for Liver Enzyme Blood Tests once a month after 3 months of use. This drug is hard on your liver, so you should also avoid Aspirin, Acetaminophen, Ibuprofen, Alcohol, or any other drug which may damage your liver.”

Adrafinil Odour

Here is a helpful tip from one of our readers

I am a regular user of Adrafinil since March 2015. I find that like many others, Adrafinil causes a lingering sulphuric odor in my pee, sweat and (sometimes) breath. Recently I have found that adding a couple of drops of clove oil to my body and hair cream will neutralize the odor from my sweat, and a couple of drops in my morning tea will neutralize the odor in my pee and on my breath. The clove oil I use is the dental type you can get at any pharmacy for about £2 or £3 a vial. I will also drink lots of water throughout the day. I am still working on a solution for my wind but I will figure that one out with my diet.