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Adrafinil is commonly used as an alternative to the nootropic drug Modafinil which requires a prescription and can be very expensive.
Adrafinil has the same effects as this more popular drug, giving you increased levels of alertness and mental energy.
However, one of the potential side effects of Adrafinil (also known as Olmifon) is the build-up of harmful enzymes in your liver.
This Adrafinil liver toxicity (or hepatocixity) has been well documented and is something you need to keep in mind when considering whether or not this is a supplement to add to your routine.
But it is important to put the effects of Adrafinil on your liver into perspective and understand just how serious this problem is or how likely you are to develop issues.
Most people may not be aware that even well-known and reliable or ‘safe’ products also have a level of liver side effects associated with them.
As a comparison, Tylenol which contains Acetaminophen has a similar degree of liver toxicity with Adrafinil. In fact, the chief metabolite found in this commonly used over the counter medication is considered to be very poisonous.
Of course, there are a number of excellent benefits as well as ways in which the potential liver issues can be reduced. It will be up to you to determine whether those promised benefits outweighs the small chance of risk.
In order to do that, you should first understanding what exactly Adrafinil is, how it works, possible side effects, and exactly how it can affect the liver. It is also very important to know about liver toxicity in general.
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History of Adrafinil
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Adrafinil was first developed by researchers at the French pharmaceutical company Lafon Laboratories in 1974. Experimental medicine professor Michel Jouvet and another scientist were researching new analgesics when they developed a group of benzhydryl sulfinyl compounds, including Adrafinil.
It was found that Adrafinil does not have analgesic effects, but instead is a eugeroic, or wakefulness promoting compound.
During testing to determine what Adrafinil’s mechanism of action is in the body, Modafinil was discovered. When ingested, Adrafinil is transported to the liver, where it is broken down into modafinilic acid and Modafinil. Modafinil was determined to be the primary active compound in Adrafinil. and what causes Adrafinil’s effects in the body.
In animal studies Adrafinil and Modafinil were seen to cause increased locomotor activity, and even hyperactivity at higher dosages.
Because of its wakefulness producing effects, Adrafinil was first tested in human trials in 1977-78 as a treatment for the sleep disorder narcolepsy. In multiple double-blind placebo-controlled studies, Adrafinil was seen to improve wakefulness and reduce excessive daytime sleepiness associated with narcolepsy.
In 1986, Adrafinil was approved as a treatment for narcolepsy in France. In 2001, the American pharmaceutical company Cephalon Inc bought Lafon.
Marketed under the brand name Olmifon by Lafon and then Cephalon, Adrafinil had been approved for widespread use in Europe but is currently not regulated by the US FDA or by Health Canada.
In 2011, Cephalon was acquired by Teva Pharmaceutical Industries. Working as a subsidiary of Teva, Cephalon still produces the brand name version of Modafinil, Provigil. However, they began scaling back their production of Adrafinil as it is a less potent non-prescription medication. In 2011 Cephalon stopped producing Olmifon.
Adrafinil is now produced as a generic product from a number of manufacturers worldwide today though, so it is still available even though Cephalon no long produces it.
How Does Adrafinil Work?
As mentioned before, Adrafinil is technically in a class of substances known as eugeroics. Eugeroic simply means ‘good arousers,’ which is fitting since this class of compounds are primarily used as wakefulness agents.
It has stimulant-like effects, but with less harmful side effects than the typical stimulants because it uses a different pathway of action.
In addition to being able to promote alertness and wakefulness, there are some noted Nootropic effects. This includes boosting one’s mood and mental energy. In many cases it also helps to enhance attention span, concentration, and even focus. Some of the results may tend to improve productivity, mental performance and even reduce signs of depression.
Adrafinil’s primary mechanism of action is through its breakdown into Modafinil, and the effects this metabolite produces. The exact mechanism of action of Modafinil is still unknown at this time, however it has been seen 
to effect the Dopamine, Serotonin, and Histamine neurotransmitter systems.
Dopamine and Serotonin are both very powerful neurotransmitters that contribute significantly to the way we think and feel at any given moment.
Dopamine helps to promote an enhanced mood and feelings of general well-being. Serotonin plays a pivotal role in controlling our sleep cycles and feelings of pleasure.
Modafinil acts as a Dopamine reuptake inhibitor and a transport inhibitor, allowing for higher circulating levels. Modafinil has been seen to increase levels of Serotonin in the brain.
Adrafinil also has a positive effect on Histamine and the catecholamine Norepinephrine. These hormones control your level of stimulation and help to direct your focus, attention and motivation to important stimuli.
Modafinil has been seen to activate Orexin neurons and Orexin-stimulating neurons. Orexin is a neuropeptide that, like Histamine, plays a role in the regulation of wakefulness, arousal, and appetite. The Orexin in turn stimulates the release of Histamine in the hypothalamus.
- Increases energy, wakefulness and motivation
- Boosts mental performance and focus
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Adrafinil Liver Effects
As mentioned earlier, Adrafinil is broken down in the liver into modafinilic acid and Modafinil. The process of breaking down and conversion can put some strain on the liver and raise levels of key enzymes.
The enzymes that break down Adrafinil are SGOT, GGPT, and hepatic alkaline phosphatase. These enzymes are common and critical ones produced by the liver to metabolize various compounds. They are a necessary and needed part of bodily functioning.
However, over time, if the levels of these enzymes continue to build it could cause long-term liver damage. These symptoms can become apparent after six months of daily use but different people will have different sensitivity levels.
Despite this, taking Adrafinil at recommended dosage levels is still considered to be safe for healthy individuals. Ideally, you should not be taking an Adrafinil dosage every day but rather cycling it to give your liver a chance to clear out those low levels of harmful enzymes and not let them accumulate.
Some people only take Adrafinil one or two days a week to ensure they do not run into any problems. If your liver does not have enough chance to rest, these chemicals can begin to accumulate and cause issues.
Of course, anyone who already has a history of liver issues should probably not take this without talking to a qualified medical professional.
Additionally, it should not be mixed with any other drugs or alcohol, as alcohol and many other drug compounds are metabolized through the liver as well, and could cause undue strain.
Adrafinil Liver Toxicity In Perspective
The problem with the liver in general is that it acts as a big processing center for the body. Anything that is not excreted unchanged by the body ends up going through the liver.
We put a lot of strain on our livers every time we drink alcohol, eat certain foods, or take supplements or drugs that are metabolized in the liver. Unfortunately, some chemicals are harder on the liver than others and require higher levels of enzymes to be broken down and then utilized or excreted.
These enzymes are necessary for proper functioning, but as mentioned before, can accumulate and become toxic at higher levels.
Even common over-the-counter medications like ibuprofen and acetaminophen have been noted to be harmful on the liver when used on a long-term basis.
So, it would not be technically correct to think of Adrafinil (or even Modafinil) as being poisonous or toxic to liver when used responsibly. Instead, it is recommended that to prevent potential liver damage, Adrafinil only be used on an occasional basis instead of daily.
The key thing to remember when using any medications or supplements is proper safe dosages and usage schedules. Many people safely use Adrafinil as a nootropic compound, but they try to maintain moderate dosages and reasonable schedules.
If you are taking or considering taking Adrafinil on a regular basis, then it is recommended that you have your liver enzyme levels monitored by your doctor regularly. While taking Adrafinil on an infrequent basis is recommended, keeping track of your personal levels if you take frequent may help you prevent liver damage and take breaks if your levels become elevated.
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Adrafinil Side Effects
Adrafinil is generally well tolerated in most users who take it as appropriate dosages. However, unlike many other Nootropics, Adrafinil does carry a slightly higher risk for some negative side effects. This is especially true when taken at high doses.
Some more serious side effects can include increased blood pressure and heart related issues. Potential users who have existing heart and high blood pressure issues should avoid supplementation and consult with a qualified health professional. It should also not be combined with other stimulants like coffee and caffeine.
The recommended dosage for Adrafinil powder is between 150 and 300 mg per day. Of course, you should always start out with the lowest effective dosage in order to give your body time to adjust. You may even want to start lower than this range until you have become familiar with exactly how it works.
Some very rare, but serious side effects that can occur with Adrafinil usage are any of a series of skin and mucous membrane reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS).
There is strong evidence that some people who have certain human leukocyte antigens have a genetic predisposition and susceptibility to developing these severe cutaneous conditions when they take select medications, including antibiotics, anesthetics, and Adrafinil or Modafinil.
Stop taking Adrafinil immediately and speak with your doctor right away if you develop flu-like symptoms and a rash that spreads and blisters.
As mentioned previously, to avoid the risk of Adrafinil Liver Toxicity, you should take this compound sparingly and not on a continuous basis. Read user reviews online if you want to learn more about how this supplement will affect you.
Other Nootropic Options
In most countries, such as the United States, the UK, and Canada, Adrafinil is an unscheduled, unregulated compound that is available without a prescription. You can buy Adrafinil online from a variety of reliable, safe nootropic vendors.
However, in some countries, such as Australia, Adrafinil like Modafinil, is considered a prescription medication only. People in these places, as well as any people who may be concerned with Adrafinil liver toxicity issues (either hypothetically, or because they have had issues before) often turn to other nootropics such as the Racetams to use as cognitive enhancing smart drugs.
The Racetams are a family of compounds that have positive effects on the neurotransmitter Acetylcholine. Acetylcholine is linked to general cognition, executive function, memory, and learning ability.
All the Racetams are based off of their parent compound, Piracetam. Piracetam is the first nootropic ever developed. It was first developed in the 1960s by a Romanian scientist working for UCB Pharma in Belgium. He created the word nootropic to describe his new compound – it comes from Greek origins and translates roughly to “to turn the mind.”
The derivatives of Piracetam were all developed after this first compound, and are all more potent nootropics that have additional cognitive effects. Some of the most common Racetams include Oxiracetam, Aniracetam, Phenylpiracetam, and Pramiracetam.
Phenylpiracetam is considered one of the strongest Racetams. It is considered to be 50-60 times as potent as Piracetam. Users says that it has strong mental energy effects, which can make it a decent substitute for the alertness promoting effects of Adrafinil.
Like Adrafinil, the Racetams are unregulated, unscheduled compounds in many countries of the world. In some places, laws surrounding the sale of these items can make them difficult to find, but they are legal to buy and own. They are available from many different specialized nootropic stores online.
If the potential of Adrafinil liver toxicity prevents you from using this nootropic smart drug, them consider using an alternative such as one of the Racetams.
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- Vaille C, Chariot J, de La Tour J, Souchard M. [Effect of clonidine and adrafinil on biliary secretion in the rat]. Ann Pharm Fr. 1983
- Siwak CT, Gruet P, Woehrlé F, Muggenburg BA, Murphey HL, Milgram NW. Comparison of the effects of adrafinil, propentofylline, and nicergoline on behavior in aged dogs. Am J Vet Res. 2000
Article last updated on: April 13th, 2018 by Nootriment