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Aniracetam is a nootropic drug that has a relatively short half-life compared to related cognitive enhancers.
It is considered to have the shortest half-life of the commonly used racetam nootropic agents and is describe as having a shorter duration of effects.
It also has the quickest kick-in time or onset of effects. Users report feeling the effects within 30 minutes of taking their first dose.
What is Aniracetam’s half-life and how should this affect how you take your dosages to maximize its effects?
Aniracetam does have a short detection period in your blood stream, but it can actually continue to remain pharmacologically effective for a longer period of time than it is elimiated from the body.
This is because its mechanism of action is significantly attributed to its three primary metabolites. After it has been broken down in the body, these metabolites appear to be effective for a greater duration. Buy Aniracetam online at this link.
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Aniracetam Research Summary
Related Topics
- What is Aniracetam?
- User Reviews
- Effects and Benefits
- Aniracetam for Anxiety
- Dosage Suggestions
- Using Aniracetam Powder
- Best Way to Take
- Side Effects
- Aniracetam for Sale
- Buyer's Guide
- Is Aniracetam Legal?
- Stacking with Piracetam
- Stacking with Choline
- Comparison to Piracetam
- Comparison to Oxiracetam
- Comparison to Pramiracetam
- Comparison to Noopept
Aniracetam is a nootropic agent that was developed shortly after the introduction of Piracetam to clinical practice in the 1960’s.
Piracetam was the first every nootropic drug identified by Dr. Corneliu Giurgea. He discovered that this compound could enhance brain function in experimental animals, but that it lacked the physiological effects and side effects of a sedative or stimulant.
At this time, there was a surge of research activity to develop analogues to Piracetam that exhibited positive effects on cognition with a low risk of side effects.
Aniracetam was the first candidate developed that showed therapeutic benefits. It was found to be 3-5 times stronger than Piracetam and was lipophilic (fat soluble), which resulted in better absoprtion from the gut.
Aniracetam falls into the Racetam family which is the most widely used group of nootropic agents today.
All racetams have a 2-oxo-pyrrolidine base in their chemical structure and seem to work by increase acetylcholine actiivty in the brain. Other examples of this family include Oxiracetam, Pramiracetam, Phenylpiracetam, Coluracetam, Fasoracetam and Nefiracetam.
It was also the first ever Ampakine compound, so-named because it increased stimulation of the AMPA receptors for the excitatory neurotransmitter glutamate.
One interesting point of note you will often see in Aniracetam research reviews is a discussion of its short half-life. Compared to other racetam, it appears to have a very rapid onset of effects and a short-lived duration.
In addition to demonstrating positive effects for memory, attention, vigilance, and complex reasoning, this nootropic has also been shown to improve anxiety, depression and certain sleep disorders.
Aniracetam has been extensively studied both in humans and in animal models. It is used clinically in certain countries in Europe for the treatment of Senile Dementia, Alzheimer’s Disease and cognitive decline of a cerebrovascular origin.
It is available with a prescription in these countries under the brand names Referan, Memodrin, and Draganon. Aniracetam is currently unregulated and does not require a prescription within the United States, Canada or Australia.
Aniracetam Half Life
Depending on which source you read, you may see the half-life of Aniracetam reported as 0.5 hours or 1 – 2.5 hours. What explains this discrepancy?
A half-life describes the time it takes for an initial quantity to reduce its value by half. In biology, the half-life can refer to one of two different measurements.
The elimination half-life is the time it takes for the concentration of a drug in the body to be reduced to one half. This is sometimes referred to as the plasma half-life where plasma refers to the liquid fraction of blood.
The biological half-life is the time it takes for a drug to lose half of its pharmacological efficacy or for the effects to be decreased by half. This is sometimes referred to as the terminal half-life.
In other words, the elimination half-life is a measure of how long half the dosage of Aniracetam can be detected in your blood while the biological half-life is a measure of how long the effects will last.
These two time values may be the same, but in the case of Aniracetam they are not. The plasma elimination half-life in humans is 0.5 hours and the biological half-life of the effects is 1 – 2.5 hours.
Other studies have reported a half-life of up to 4.5 hours, but these involve non-human species.
This half-life is short in comparison to other nootropics like Piracetam and Pramiracetam which can last between 6-8 hours.
Some individuals view this as a reason to favor these longer-lasting nootropic agents over Aniracetam, but this is not a good indicator of therapeutic efficacy.
Furthermore, these values can vary from person to person and depending on the circumstances under which it is used. A number of different factors can affect the rate at which this substance is metabolized and excreted from the body.
Some individuals may be slow metabolizers of the drug or may eliminate it at a different rate depending on liver or kidney function. There may also be external factors relating to other drugs being administered concomitantly, whether it was taken with food or the form this drug was taken in.
Higher dosages can also result in longer clearance and metabolization times for this drug. At high doses, this results in a non-linear increase in the half-life.
In a human clinical trial conducted by researchers at Hoffmann-La Roche, there were significant differences in the plasma concentrations of this nootropic across six individuals after a single oral 1g dosage.
Peak plasma concentrations differed among the group by a factor of 8x and the time it took to reach baseline plasma levels varied by 3x. This reflects differences in its rate of absorption, hepatic metabolism and in its elimination from the body.
You should think of the half-life as an approximation. We all respond to drugs differently and how you metabolize this compound may be different from what is observed in other individuals.
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Duration of Effects
The fact that this compound has a plasma half-life of 0.5 hours does not mean that the effects will start to decline immediately after 30 minutes. Based on user reviews, Aniracetam’s benefits are noticeable for up to 3-5 hours after taking it.
How is it that this nootropic gets eliminated from the body at a faster rate than it loses its efficacy?
Once this smart drug is ingested orally, it gets circulated throughout the body and transported to the liver. The liver breaks it down or metabolizes it into compounds known as metabolites.
While some of the effects of this smart drug may be attributed to its direct actions, many appear to be the result of its metabolites. The primary metabolites in humans are N-Anisoyl-GABA, P-Anisic Acid and 2-pyrrolidinone.
These chemical have been extensively studied in rats and mice, but not as much in humans. Research shows that many of the effects of Aniracetam can be mimicked by directly administering these compounds that it gets broken down into.
Because the elimination half-life of the metabolites is quite a bit longer than aniracetam itself, the result is that the duration of effects lasts beyond the time that Aniracetam is detectable in plasma.
In research studies, the metabolites have been detectable in the body for up to 6 hours after administration.
One study found that after administering Aniracetam dosages for 12 weeks, the metabolites N-anisoyl-GABA and 2-pyrrolidinone were detectable in the cerebrospinal fluid suggesting potential for bio-accumulation.
Dosage Schedule:
Aniracetam is a fat soluble nootropic which means that it is faster acting than its counterparts of Oxiracetam or Piracetam.
Under normal settings, Aniracetam is thought to reach its peak plasma concentration levels within about 20 to 30 minutes of oral administration. After this time, plasma levels decline steadily for a couple hours.
However, most users report that it takes about 1 hour before the observable benefits of Aniracetam reach their maximum potential. This points to the fact that the blood plasma levels do not directly correlate with the optimal period of effectiveness that this supplement exhibits.
To the degree that Aniracetam’s effects are slightly shorter lasting than other nootropics, this can be counteracted by splitting your dosage up throughout the day.
A typical Aniracetam dose consists of between 750 mg and 1500 mg per day (sometimes more). You may determine that the best way to use this nootropic is by taking 250 mg – 500 mg three times per day or every 3 hours. This will supply a consistent stream of the active ingredient to your brain, resulting in sustained benefits.
According to one study, the dose-efficacy curve suggests that a 1000 mg dosage is the most effective (compared to 250mg and 500mg doses). [3]
Aniracetam is fat soluble and should be consumed with some type of lipid source like milk, fish oil, olive oil or food. However, even when taken on an empty stomach it appears to be well-absorbed from the gut.
If you experience nausea, esophageal irritation or stomach pain after use, you may want to take your dosage with a meal in the future.
This product is sold in the form of a capsule or tablet or as a bulk powder, sometimes with flavoring agents added. It has also been sold as a liquid suspension for injection, but this use is limited to treatment of patients with cerebral ischemia.
The powder is generally cheaper to buy, but is widely recognized as having an unpleasant, bitter taste. Oral capsules can be used to mask the taste, though this product may have a slower onset of effects compared to preparing the powder into a liquid solution.
Aniracetam powder and capsules should also be stacked with a choline supplement such as Alpha GPC, CDP Choline or Centrophenoxine. 750 mg of Aniracetam has been used in a stack with 200 mg of Alpha GPC, 300 mg of CDP Choline or 250 mg of Centrophenoxine powder.
Pharmacodynamics
This nootropic is fat-soluble and is presumed to be better absorbed from the intestines when taken with a meal or a fat source. Even in a fasted state, Aniracetam is rapidly absorbed from the gut following oral administration.
One study found that 90% of the oral dose was absorbed and metabolize in the body. Most of this metabolization occurs in the liver.
Only a very small amount of orally ingested Aniracetam will cross the blood-brain barrier and reach the neurons in tact. The reported absolute systemic bioavailability of this drug is 0.2%.
This means that only 0.02% of the Aniracetam dosage that you consume will make it to your neurons (the point of therapeutic action) in its original form.
One study of the pharmacokinetics of Aniracetam in the rat brain found that this compound crossed the blood-brain barrier at a low rate after oral ingestion.
The metabolite 2-pyrrolidinone seemed to have better transportation across the blood-brain barrier and had the highest concentrations in brain regions. It appears that many of the nootropic effects are mediated by the metabolites. [2]
When examining research studies on Aniracetam, this is an important point to remember. Based on this pharmacokinetic profile, there is doubt about how relevant in vitro studies on this drug are.
In vitro experiements are done on cultures of cells that have been removed from living tissue and grown in a petri dish, flask or other type of vesicle in a laboratory environment.
In these studies, Aniracetam is directly added to the medium that the cells are grown in and the effects on cells are observed. These studies are used to make informed guesses about how a drug will affect cells in vivo or in a living animal.
However, since only a very small amount of aniracetam does cross the blood-brain barrier and interact directly with cells in the brain, it is unlikely that in vitro studies can tell us much about the mechanisms of an oral Aniracetam dosage.
Two of the major metabolites – anisic acid and p-methoxyhippuric acid – reached peak levels two hours after oral administration and returned to baseline at six hours. This observation was made in patients with a mean age of 84.5 years.
In elderly individuals, the half-life and the AUC (Area Under the Curve) for this drug and its metabolites are both significantly higher. The AUC is a measure of the total concentration or exposure to the drug over time.
This study found that the half-life of Aniracetam’s metabolites was 4 to 7 times greater in elderly patients with cerebrovascular disease compared to young volunteers. [1]
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Aniracetam Benefits:
This nootropic supplement is considered to be the most effective Racetam for anti-anxiety purposes. It is thought to work by affecting a number of neurotransmitters within the brain including Dopamine and Serotonin.
Dopamine is a chemical which plays a role in feelings of pleasure, a positive mood, the reward circuitry in the brain and ambition. It is also involved in movement control and the ability to direct attention to a specific task.
Increasing levels of Dopamine and Serotonin together may have a positive effect on mood, resulting in a relaxed sense of focus as well as less stress and anxiety.
This cognitive enhancer may also interact with the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), but findings on this have been conflicting so far. All racetam nootropics are indirect derivatives of GABA, but their effects do not appear to be significantly mediated by direct actions on this neurotransmitter system.
Some users find themselves experiencing enhanced sensory perceptions, especially in the areas of sight and sound. Colors seem brighter and more beautiful, sounds more rich and clear. Aniracetam also contributes to increased alertness as well as boosting motivation levels for some people.
Additional benefits associated with Aniracetam are related to cognitive function. It has been shown to promote memory and learning capacity, reasoning and information processing in patients with different forms of cognitive impairment.
Some user reviews of Aniracetam describe improvements in memory ability and increased ease of recalling information. While there is limited research into the effects of this nootropic on memory performance in healthy adults, it has been shown to enhance long-term memory retention in individuals with Alzheimer’s disease.
It works by amplifying cholinergic neurotransmission in the brain. This refers to chemical messages sent between neurons using the neurotransmitter acetylcholine. Aniracetam appears to have effects on the pre-synaptic (message sending) and post-synaptic (message receiving) neural receptors.
It is believed to modulate these receptors, so they are more responsive to the presence of acetylcholine and to increase the amount of this neurotransmitter released by neurons.
Acetylcholine levels are particularly low in Alzheimer’s patients. Medications that increase cholinergic activity (such as cholinesterase inhibitors) are commonly used in the treatment of Alzheimer’s and Dementia.
Aniracetam also has a positive effect on glutamate receptors belonging to the AMPA class. These neuroreceptors are involved in long-term memory formation and the process of long-term potentiation.
This refers to the mechanism by which neurons form long-term connections between each other at synapses. LTP is described as the strengthening of a signal between two neurons, causing them to be activated at the same time.
Through this effect on AMPA glutamate receptors, Aniracetam is purported to promote synaptic plasticity and increased ability for the brain to adapt and learn new information.
Aniracetam Side Effects:
Aniracetam is reported to be safe and is generally well tolerated based on data from clinical trials. Side effects are generally mild and do not usually require individuals to stop taking it.
There are some potential side effects reported by individuals who have taken it. These include insomnia, headaches, anxiety, vertigo, nausea, diarrhea, and muscle pain or jaw tension.
The most common adverse effect is a headache, which may be caused by depletion of available acetylcholine stores in the neurons. Use of a choline supplement is reported to ameliorate this side effect for many individuals.
The specific choline source taken and the dosage it is used in can affect the presence of negative effects. Some individuals feel that this cognitive enhancer is more effective when combined with choline in a stack while others say it increases the frequency of unwanted effects.
Some individuals report that side effects are worse when they start using this nootropic and begin to decline as use is continued. Adverse effects typically disappear within a few hours after a dosage is taken.
While the negative effects are mild in the majority of users, some individuals report experiencing severe anxiety, gastrointestinal discomfort, skin rash, changes in mood or brain fog after taking a dosage. Different people will react to this product in different ways.
It is recommended to start with a low dose to determine how this nootropic supplement affects you before taking the standard therapeutic dosage. Consult with a doctor before deciding to use it to determine whether Aniracetam is safe for you or whether it may interact with other drugs or supplements you are using.
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- Endo H, Tajima T, Yamada H, Igata A, Yamamoto Y, Tsuchida H, Nakashima Y, Suzuki Y, Ikari H, Iguchi A. Pharmacokinetic study of aniracetam in elderly patients with cerebrovascular disease. Behav Brain Res. 1997 Feb;83(1-2):243-4.
- Ogiso T1, Uchiyama K, Suzuki H, Yoshimoro M, Tanino T, Iwakai M, Uno S. Pharmacokinetics of aniracetam and its metabolites in rat brain. Biol Pharm Bull. 2000 Apr;23(4):482-6.
- Saletu B, Grünberger J, Linzmayer L. Quantitative EEG and psychometric analyses in assessing CNS-activity of Ro 13-5057--a cerebral insufficiency improver. Methods Find Exp Clin Pharmacol. 1980 Oct;2(5):269-85.
- Fushiki S, Matsumoto K, Nagata A. Neurite outgrowth of murine cerebellar granule cells can be enhanced by aniracetam with or without alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA). Neurosci Lett. 1995
- Sourander LB, Portin R, Mölsä P, Lahdes A, Rinne UK. Senile dementia of the Alzheimer type treated with aniracetam: a new nootropic agent. Psychopharmacology (Berl). 1987
- Pontecorvo MJ, Evans HL. Effects of aniracetam upon the delayed matching-to-sample performance of monkeys and pigeons. Ann N Y Acad Sci. 1985
- Canonico V, Forgione L, Paoletti C, Casini A, Colonna CV, Bertini M, Acito R, Rengo F. [Efficacy and tolerance of aniracetam in elderly patients with primary or secondary mental deterioration]. Riv Neurol. 1991
- Ogiso T, Uchiyama K, Suzuki H, Yoshimoro M, Tanino T, Iwakai M, Uno S. Pharmacokinetics of aniracetam and its metabolites in rat brain. Biol Pharm Bull. 2000
- Togashi H, Nakamura K, Matsumoto M, Ueno K, Ohashi S, Saito H, Yoshioka M. Aniracetam enhances glutamatergic transmission in the prefrontal cortex of stroke-prone spontaneously hypertensive rats. Neurosci Lett. 2002
- Cai S, Wang L. Determination of aniracetam's main metabolite, N-anisoyl-GABA, in human plasma by LC-MS/MS and its application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2012
Article last updated on: March 13th, 2018 by Nootriment