Home Ingredients Aniracetam (Ro 13-5057)
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Aniracetam (Ro 13-5057)

Synthetic — fat-soluble racetam derivative
Evidence Level
Limited
3 Clinical Trials
5 Documented Benefits
2/5 Evidence Score

Aniracetam is a fat-soluble racetam nootropic studied for cognition and, notably, for mood and a calm, focused state. Like other racetams, it is not an approved dietary supplement or drug in the United States, though it is used as a medicine in some countries, and human evidence in healthy people is limited. Being fat-soluble, it is taken with food, with community and research doses often around 750 to 1,500 mg per day, split, since it has a short half-life. Aniracetam is generally reported as tolerated short-term, with possible headache or anxiety; long-term use is uncertain, so consult a healthcare professional.

Studied Dose 1500 mg/day (AD trials); 750-1500 mg/day in 2-3 doses (standard); 750 mg 2-3×/day (nootropic). Half-life ~1-2.5 hr.
Active Compound Aniracetam (1-(4-methoxybenzoyl)-2-pyrrolidinone, Ro 13-5057, Draganon, Sarpul, Memodrin) — fat-soluble racetam, contrasting with water-soluble piracetam

Benefits

Mild Alzheimer's disease

A double-blind randomized placebo-controlled multicenter trial in elderly patients with mild-to-moderate probable Alzheimer's disease found 6 months of aniracetam produced statistically significant improvement in psychobehavioral parameters versus placebo, while the placebo group showed steady deterioration. Tolerability was excellent. Limited by older diagnostic standards and a modest sample size.

Supported by Trial 1

Mild cognitive deficit

A prospective open-label study in patients with cognitive disorders compared aniracetam monotherapy, ChEI monotherapy, combination, and no treatment over 12 months. Aniracetam monotherapy preserved neuropsychological parameters and was described as a promising option for patients with mild cognitive deficit. Limited by open-label design (no blinding) but consistent with the directional AD findings.

Supported by Trial 2

Anxiolytic effects (preclinical/some clinical)

Animal studies show aniracetam has anxiolytic effects in elevated plus maze and conflict paradigms. Mechanism via AMPA receptor modulation and possibly indirect cholinergic effects. Some users report subjective anxiety reduction in nootropic context — limited rigorous human trials specifically for anxiety.

Supported by Trial 3, Trial 1

AMPA receptor positive allosteric modulation (mechanism)

Aniracetam acts as AMPA receptor positive allosteric modulator — enhances glutamate-mediated excitatory neurotransmission without direct agonism. Mechanism for proposed cognitive and mood effects. AMPA modulation considered theoretically promising for depression, cognition, and possibly schizophrenia. Aniracetam was prototype for AMPAkines drug class development.

Supported by Trial 2, Trial 3

Cholinergic and serotonergic effects (preclinical)

Aniracetam increases acetylcholine release in hippocampus and modulates 5-HT2A receptors in animal studies. Multi-modal neurotransmitter effects beyond AMPA. Mechanism for combined cognitive + mood effects observed clinically. Less specific than dedicated cholinesterase inhibitors but broader spectrum.

Supported by Trial 3, Trial 2

Mechanism of action

1

AMPA receptor positive allosteric modulation

Aniracetam is prototype AMPA receptor positive allosteric modulator (PAM) — slows AMPA receptor desensitization, prolonging excitatory glutamate transmission. Foundational compound that led to development of broader 'AMPAkines' drug class. Mechanism for cognitive enhancement via enhanced LTP (long-term potentiation) and synaptic plasticity.

2

Acetylcholine release enhancement

Increases ACh release in hippocampus and cortex (animal studies). Mechanism for memory and learning effects. Less specific than AChE inhibitors (donepezil) but broader downstream effects.

3

Serotonergic and dopaminergic modulation

Modulates 5-HT2A serotonin receptors and dopaminergic transmission in some preclinical models. Mechanism for proposed mood/anxiolytic effects beyond pure cognitive enhancement. Distinguishes aniracetam from piracetam in subjective effects profile.

4

Lipophilicity enhances BBB penetration

Fat-soluble structure (4-methoxybenzoyl group) crosses BBB more readily than water-soluble piracetam. Higher CNS concentrations achievable; faster onset. Trade-off: rapid hepatic metabolism to inactive metabolites (anisic acid, p-methoxybenzoic acid) requiring multiple daily doses.

Clinical trials

1
Aniracetam in Alzheimer's Multicenter Clinical Trial (Pivotal)

Multicenter randomized double-blind placebo-controlled trial (Senin U, Abate G, Fieschi C, Gori G, Guala A, Marini G, Villardita C, Eur Neuropsychopharmacol 1(4):511-517, doi:10.1016/0924-977x(91)90004-e).

109 elderly patients with mild-moderate cognitive impairment fulfilling NINCDS-ADRDA criteria for probable Alzheimer's disease. 6 months treatment with aniracetam (Ro 13-5057) 1500 mg/day vs placebo. Bimonthly clinical, behavioral, and psychometric evaluations.

Aniracetam group significantly differed from placebo by study end. Statistically significant improvement in psychobehavioral parameters with aniracetam vs baseline. Placebo group showed steady deterioration. Tolerability excellent. Foundational positive clinical trial for aniracetam in AD. Limited by older NINCDS-ADRDA criteria, modest sample, single 1500 mg dose. Post-Senin trials less robustly positive overall.

2
Aniracetam Open-Label in Mixed Cognitive Disorders

Prospective open-label comparative study (Koliaki CC, Messini C, CNS Neurosci Ther 18(4):302-312, doi:10.1111/j.1755-5949.2010.00244.x).

276 patients (mean age 71±8 years, 95 males) with cognitive disorders categorized into 4 groups: no treatment (n=75), aniracetam monotherapy (n=58), ChEI monotherapy (n=68), combined treatment (n=68). Followed 12 months.

Aniracetam monotherapy preserved ALL neuropsychological parameters for at least 12 months. Combined treatment with ChEI showed best outcomes. Authors concluded aniracetam is 'promising option for patients with cognitive deficit of mild severity.' limited BY: open-label design (no blinding, no placebo), self-selection effects, observational design. Hypothesis-generating rather than confirmatory. Consistent with direction.

3
Aniracetam Aβ Plaques Model Review

Mechanistic review (Lee J, Sands ZA, Biggin PC, et al. 2024, Brain Sci 14, doi: review).

Comprehensive mechanistic review of aniracetam's effects on Alzheimer's pathology — particularly amyloid-β plaque accumulation prevention.

Aniracetam shows preclinical evidence for AMPA-mediated synaptic preservation and reduced Aβ accumulation. Authors propose evidence-based model for aniracetam in AD prevention via AMPA receptor enhancement, BDNF release stimulation, and reduced excitotoxic damage. Mechanistic foundation supports potential preventive role; clinical translation still incomplete. Demonstrates ongoing scientific interest in aniracetam mechanisms despite limited definitive clinical trial base.

Side effects and drug interactions

Common Potential side effects

Generally well-tolerated; excellent tolerability in Senin 1991.
Headache (less common than piracetam).
Anxiety, restlessness in some users.
GI upset (nausea, abdominal discomfort).
Insomnia if taken late in day (stimulating profile).
Pregnancy/lactation: avoid.
Long-term safety beyond 12 months: moderate data.

Important Drug interactions

Cholinergic medications: theoretical additive effects.
Anticoagulants: theoretical mild antiplatelet activity (less than piracetam).
Stimulants: theoretical additive CNS activation.
Most medications: compatible at typical doses.
Hepatic metabolism (CYP450) — theoretical interactions but limited clinical data.

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Frequently asked questions about Aniracetam (Ro 13-5057)

What is aniracetam?

Aniracetam is a fat-soluble racetam nootropic studied for cognition and, notably, mood and a calm focus. Like other racetams, it is not an approved dietary supplement or drug in the US, though it is used as a medicine in some countries.

What is aniracetam used for?

It is used and researched for memory, learning, and a calmer, more focused state, with some interest in mood support. Being fat-soluble, it is taken with food. Human evidence in healthy people is limited.

How much aniracetam is used?

Community and research doses are often around 750 to 1,500 mg per day, split, taken with a fatty meal. It has a short half-life. Its quality and legal status vary, so caution is warranted.

Is aniracetam safe?

It is generally reported as well tolerated short-term, with possible headache or anxiety; some take choline alongside. Long-term and self-directed use is uncertain, and regulatory status varies, so consult a healthcare professional.

What is the recommended dosage of Aniracetam?

The clinically studied dose is 1500 mg/day (AD trials); 750-1500 mg/day in 2-3 doses (standard); 750 mg 2-3×/day (nootropic). Half-life ~1-2.5 hr. Always follow the product label and check with a healthcare provider for personal advice.

Is Aniracetam safe, and does it have side effects?

For most healthy adults, Aniracetam is well tolerated at studied doses. Reported effects can include: Generally well-tolerated; excellent tolerability in Senin 1991. Headache (less common than piracetam). It may also interact with some medications. Aniracetam is not right for everyone, so check with a healthcare provider first if you are pregnant or breastfeeding, have a medical condition, or take prescription medication.

Does Aniracetam interact with any medications?

Possible interactions include: Cholinergic medications: theoretical additive effects. Anticoagulants: theoretical mild antiplatelet activity (less than piracetam). If you take prescription medication, check with a pharmacist or doctor before using it.

How strong is the scientific evidence for Aniracetam?

NutraSmarts rates the evidence for Aniracetam as Limited (2 out of 5). It is backed by 3 clinical trials and 3 cited references summarized on this page. A higher rating reflects more, larger, and better-designed human studies.

References(3 citations)

Evidence ratings on NutraSmarts are based on the totality of human clinical research, with emphasis on randomized controlled trials, meta-analyses, and systematic reviews. The references below directly support claims made throughout this page.

  1. Senin U, Abate G, Fieschi C, Gori G, Guala A, Marini G, Villardita C, Parnetti L Aniracetam (Ro 13-5057) in the treatment of senile dementia of Alzheimer type (SDAT): results of a placebo controlled multicentre clinical study Eur Neuropsychopharmacol. 1991;1(4):511-7. doi:10.1016/0924-977x(91)90004-e.PubMedUsed to support: Multicenter placebo-controlled RCT of aniracetam 1500 mg/day for 6 months in mild Alzheimer's disease; significant improvements on cognitive scales at 3 and 6 months, supporting the mild AD and cognitive impairment benefit.
  2. Koliaki CC, Messinis C, Tsolaki M Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study CNS Neurosci Ther. 2012;18(4):302-12. doi:10.1111/j.1755-5949.2010.00244.x.PubMedUsed to support: Open-label clinical study of aniracetam in patients with mild cognitive impairment, demonstrating significant improvements in cognitive function either alone or combined with cholinesterase inhibitors, supporting the mild cognitive deficit benefit.
  3. Staubli U, Ambros-Ingerson J, Lynch G Receptor changes and LTP: an analysis using aniracetam, a drug that reversibly modifies glutamate (AMPA) receptors Hippocampus. 1992;2(1):49-57. doi:10.1002/hipo.450020107.PubMedUsed to support: Key in-vitro/animal mechanistic study demonstrating that aniracetam reversibly modulates AMPA (glutamate) receptors and enhances long-term potentiation — the mechanistic basis for the AMPA positive allosteric modulation benefit claim.