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Aniracetam

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Other names[1]

1-(4-Methoxybenzoyl)-2-pyrrolidinone, 1-(4-Methoxybenzoyl)pyrrolidin-2-one, 1-p-Anisoyl-2-pyrrolidinone, Ampamet, Aniracetamun, Aniran, Conectol, Draganon, Memodrin, Referan, Pergamid, Sarpol, Sarpul.

Important Information

Aniracetam Dosage Information

The current treatment dosage for senile dementia is 1.5 g/day[3][6]. While absorbed very rapidly per oral (p.o.) due to its high lipophilicity, aniracetam has very low bioavailability (the amount of unchanged aniracetam that reaches systemic circulation) because it undergoes extensive first-pass metabolism; the bulk of the dose is broken down into metabolites after its first pass through the liver during the digestive process[5].

For treating memory and attention issues originating from degenerative or cerebrovascular disease in elderly patients, the recommended dosing is 1.5 g as a single daily oral dose or two 0.75 g oral doses taken daily. For treating anxiety and/or depression, patients in Japan are prescribed 3 x 0.2 g oral doses per day[7].

Relevant Articles

 

Aniracetam Background

Aniracetam was developed in 1970s by Hoffmann-La Roche, a company owned by Roche Holding AG[2][19]. It falls into a class of similarly-structured nootropics called racetams. Members of this class are structurally similar, but small differences yield a range of different chemical properties. While all racetams can pass through the blood-brain barrier, aniracetam is one of the more lipophilic (less hydrophilic) in the hydrophilicity spectrum, as can be seen below in the excerpted table; more positive log P values reflect higher lipophilicity, whereas more negative log P values reflect higher hydrophilicity. This trait affects how the body metabolizes aniracetam (rapid absorption, but low bioavailability, as discussed in dosing)[5].


(Table 2 from [5])

Aniracetam is currently used to treat elderly senile dementia – Alzheimer’s type (SDAT) patient[6].

Aniracetam Mode of action

As with all racetams (e.g. piracetam), aniracetam’s specific mode of action is murky. Aniracetam indirectly contributes to neurotransmission via activating nicotinic (post-synaptic) acetylcholine receptors, thus contributing to the cholinergic (acetylcholine-producing) system; this system is typically damaged in Alzheimer’s patients, resulting in memory deficits[6].

Aniracetam’s Benefits

Generally, researchers have observed aniracetam to[6]:

  1. promote formation of new synapses,
  2. exhibit neuroprotection towards artificially-induced amnesia, and
  3. enhance synaptic plasticity.

These could be the driving factors behind its cognition enhancement and antidepressant effects.

Recently, researchers have begun exploring aniracetam’s efficacy in treating CNS disorders causing impulsiveness, fear and anxiety, depression, post-traumatic stress disorder, sleep disorders, and cardiovagal abnormalities[9].

Toxicity Information
The median lethal dosage (LD50) for Aniracetam is rather high–for mice, two different studies have reported doses of 3.6-4.5 g/kg, per oral[4]. Aniracetam is generally well tolerated. Researchers did not observe an increase in liver enzyme levels in patients taking aniracetam (typically, enzymes reside in liver, but if liver is injured, these enzymes spill into blood stream[8]). Typical adverse effects, if they arise, are: unrest, anxiety, uneasiness, insomnia; other less common adverse effects include: headaches, somnolence, vertigo, mild epigastric pain, nausea, diarrhoea, rash. These effects were typically temporary and didn’t require termination of treatment[6].

The absence of negative interactions with other drugs allows clinicians to either prescribe aniracetam as a monotherapy or part of a combined treatment[6].

Administration Methods
Unfortunately, in the various papers we reviewed for human subjects, the “methods” section was fairly vague in administration specifics (e.g. “a single oral dose of aniracetam”, “oral doses of aniracetam”, “orally administered aniracetam”, etc.[3][5][6][7]). The most explicit answer for human studies were “aniracetam [capsules] 1500 mg per os”[11] or aniracetam 2mg; 100mg; and 200 mg intravenously (i.v.)[11].

As an interesting side note, in this specific study exploring aniracetam’s protective effects against artificially-induced cognitive impairment (scopolamine) in 26 healthy, male subjects, aged 19-34 years old, the researchers found that 1500 mg per oral aniracetam capsules produced significant benefits, whereas the 2 mg and 200mg intravenous aniracetam produced benefits in a number of tests that could have been attributed to chance (not statistically significant). As the researcher underlines in his discussion section, it is possible that the cognitive battery and subjective scale tests in this specific study are only able to highlight benefits granted from oral dosages; in other words, the experimental design could have been favorable to oral administration. Thus, the only conclusion was that 1500 mg aniracetam per oral dose is effective, and NOT that intravenous administration of 2 mg and 200 mg aniracetam is ineffective.[11]

It appears that oral administration via suspension is the more popular administration route in the comparably larger pool of aniracetam animal studies that we reviewed. Close to the administration time (e.g. 60-90 minutes before administration), researchers dissolved aniracetam in either a few milliliters of distilled or salinated water, and added certain emulsifiers, such as sodium carboxymethylcellulose or carboxymethylcellulose (CMC) at varying concentrations, and/or 1-2 drops of Tween-80[12][13][14][15][16][17]. Emulsifiers were added to keep the lipophilic aniracetam powder in solution[18], as lipophilic powders generally do not dissolve in water or water-based liquids (e.g. fruit juice).

References

  1. ^  aGenericDrugs.com
  2. ^ Wikipedia.org. Note: I couldn’t find a copy of the original patents referenced in the Wiki article sources, “Patent EP 5 143 Hoffmann-La Roche 1978” and “Patent EP 44 088 Hoffmann-La Roche 1978”.
  3. ^ PubMed.
  4. ^ ChemIDplus Lite.
  5. ^ ScienceDirect.
  6. ^ Wiley.
  7. ^ Pubmed
  8. ^ MedicineNet.
  9. ^ Wiley.
  10. ^ Aniracetam Structure Details
  11. ^ SAGE journals.
  12. ^ ScienceDirect.
  13. ^ ScienceDirect.
  14. ^ ScienceDirect.
  15. ^ ScienceDirect.
  16. ^ ScienceDirect.
  17. ^  ScienceDirect.
  18. ^  DTIC Online.
  19. ^  Amazon.

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 2 reviews
by Draco on
crazy lucid dreams!

I've been pretty much chasing lucid dreams for months, i'm not sure why but aniracetam seems to help. I take 800mg before bed mix in milk as a fat source. I stack this with 5-HTP and also use galantamine.

by Mike on
Aniracetam

I've had very good experiences with Aniracetam. I took pretty low doses (750mg) with Alpha-GPC. It worked well for me. I felt a definite (although slight) increase in energy and focus. I had a more profound effect than Piracetam or Pramiracetam. Other than Coluracetam and Noopept it's the best of the racetams that I've tried personally.