Oxiracetam - NutraPedia
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Oxiracetam Overview
1) Studied Conditions
Oxiracetam has been studied for a variety of conditions, primarily within the scope of cognitive enhancement and neurological disorders. This includes:
- Alzheimer's disease
- Dementia
- Cognitive impairment in the elderly
- Memory disorders
- Attention deficit disorder
2) Efficacy in Treating Conditions
The effectiveness of oxiracetam in treating the above conditions has shown mixed results. Some studies suggest modest improvements in memory and cognitive function, particularly in individuals with cognitive impairment or neurological disorders. However, more extensive clinical trials are needed to fully determine its efficacy, as results have been inconsistent and not universally conclusive.
3) Health Benefits
As a nootropic, oxiracetam may offer several health benefits, including:
- Enhanced memory and learning
- Increased attention span and concentration
- Improved cognitive function
Note that these benefits are mostly based on anecdotal evidence and limited clinical studies.
4) Potential Downsides
While oxiracetam is generally well-tolerated, there are potential downsides, such as:
- Mild side effects, including headaches, nausea, and insomnia
- Potential for overstimulation or anxiety
- Lack of long-term safety data
- Regulatory status is not clear in all countries, which may affect availability and quality assurance
5) Genetic Variations Impact
Current research on oxiracetam does not provide a comprehensive understanding of its interaction with specific genetic variations. While individual responses to nootropics can vary widely, there is no clear consensus or solid evidence connecting oxiracetam's effects to particular genetic profiles. As pharmacogenomics advances, more information may become available on how genetic variations influence the efficacy and safety of oxiracetam.
Oxiracetam Research Summary
Introduction
Oxiracetam, a nootropic drug, is known for its cognitive-enhancing properties. This summary presents research findings on the creation of oxiracetam derivatives, their biological activities, and the effects of oxiracetam on various neurophysiological processes.
Oxiracetam Derivatives and Synthesis
New N-substituted derivatives of 4-hydroxy-2-pyrrolidinones, similar to oxiracetam, were synthesized using an effective N-alkylation method. Oxiracetam was observed to stimulate phospholipid and protein synthesis in rat brain tissues more effectively than piracetam.
AMPA Receptors and Cognitive Enhancement
Oxiracetam enhances calcium influx through AMPA receptors in neurons without affecting other glutamate receptors. It increases the number of AMPA binding sites in synaptic membranes, suggesting a mechanism for its cognitive-enhancing effects.
Glutamate Release and Cognitive Function
The drug improves cognitive function by enhancing the release of endogenous glutamate in the rat hippocampus during neuronal activation. Oxiracetam was found to be the most potent cognitive enhancer among various N-substituted 2-pyrrolidinone derivatives tested.
Measurement Techniques for Oxiracetam
Advanced chromatography techniques have been developed to accurately measure oxiracetam concentrations in human plasma, assisting pharmacokinetic studies and ensuring precise dosing for therapeutic effectiveness.
Neurotransmitter Release
Oxiracetam increases the release of neurotransmitters like glutamate and acetylcholine in the rat hippocampus, which is not observed in synaptosomes, suggesting a non-terminal mechanism of action.
Memory Enhancement and Cholinergic Activation
Oxiracetam and aniracetam counteract memory impairment and brain acetylcholine reduction caused by scopolamine, indicating activation of cholinergic pathways in the brain.
Protein Kinase C (PKC) Activity
Oxiracetam increases PKC activity in the cortex and may affect NMDA receptor activity, pointing to a common mechanism for various cognition-enhancing drugs.
Clinical Applications and Drug Interactions
Clinical trials have shown oxiracetam to be effective and safe for treating dementia, with positive outcomes on cognitive functions and no significant side effects. Additionally, oxiracetam has been found to prevent memory impairment caused by scopolamine and other amnesic conditions in animal studies.
Conclusion
The body of research on oxiracetam demonstrates its potential as a cognitive enhancer, with effects mediated through AMPA receptor modulation, increased neurotransmitter release, and PKC activity. It has shown promise in clinical settings for improving memory and cognitive deficits associated with dementia.
References:
- Cyclic GABA-GABOB analogues. III - Synthesis and biochemical activity of new alkyl and acyl derivatives of 4-hydroxy-2-pyrrolidinone
- Nootropic drugs positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-sensitive glutamate receptors in neuronal cultures
- Oxiracetam increases the release of endogenous glutamate from depolarized rat hippocampal slices
- Cyclic GABA-GABOB analogues. IV. Activity on learning and memory
- Rapid quantitative analysis of oxiracetam in human plasma by liquid chromatography/electrospray tandem mass spectrometry
- Determination of oxiracetam in human plasma by reversed-phase high-performance liquid chromatography with fluorimetric detection
- Aniracetam augments, and midazolam inhibits, the long-term potentiation in guinea-pig hippocampal slices
- Effects of oxiracetam on neurotransmitter release from rat hippocampus slices and synaptosomes
- Restoration of age-related receptor deficits in the central nervous system, a common mechanism of nootropic action?
- Temporally distinct pre- and post-synaptic mechanisms maintain long-term potentiation
- Interactions between oxiracetam, aniracetam and scopolamine on behavior and brain acetylcholine
- Cognition stimulating drugs modulate protein kinase C activity in cerebral cortex and hippocampus of adult rats
- A new type of glutamate receptor linked to inositol phospholipid metabolism
- Cellular mechanism of action of cognitive enhancers: effects of nefiracetam on neuronal Ca2+ channels
- Enhancement of hippocampally-mediated learning and protein kinase C activity by oxiracetam in learning-impaired DBA/2 mice
- Oxiracetam antagonizes the disruptive effects of scopolamine on memory in the radial maze
- Effects of oxiracetam on learning and memory in animals: comparison with piracetam
- Oxiracetam prevented the scopolamine but not the diazepam induced memory deficits in mice
- Oxiracetam prevents the MK-801 induced amnesia for the elevated plus-maze in mice
- Relationships between arousal and cognition-enhancing effects of oxiracetam
- Oxiracetam prevents haloperidol-induced passive avoidance impairment in mice
- The GABAB receptor antagonist CGP 36,742 and the nootropic oxiracetam facilitate the formation of long-term memory
- Delayed emergence of effects of memory-enhancing drugs: implications for the dynamics of long-term memory
- Improvement of avoidance acquisition by the nootropic drug oxiracetam in mice
- Avoidance facilitation by nootropics
- The memory-enhancing effects of the piracetam-like nootropics are dependent on experimental parameters
- The effects of ascorbic acid and oxiracetam on scopolamine-induced amnesia in a habituation test in aged mice
- Effect of oxiracetam on scopolamine-induced amnesia in the rat in a spatial learning task
- Oxiracetam prevents the hippocampal cholinergic hypofunction induced by the NMDA receptor blocker AP7
- Oxiracetam and D-pyroglutamic acid antagonize a disruption of passive avoidance behaviour induced by the N-methyl-D-aspartate receptor antagonist 2-amino-5-phosphonovalerate
- Putative cognition enhancers reverse kynurenic acid antagonism at hippocampal NMDA receptors
- Effects of acute doses of oxiracetam in the scopolamine model of human amnesia
- Oxiracetam in the treatment of multi-infarct dementia
- Oxiracetam in the treatment of multi-infarct dementia and primary degenerative dementia
- Oxiracetam in the treatment of primary degenerative and multi-infarct dementia: a double-blind, placebo-controlled study
- Oxiracetam in dementia: a double-blind, placebo-controlled study
- Treatment trial of oxiracetam in Alzheimer's disease
- Excitatory amino acids and neuronal plasticity: modulation of AMPA receptors as a novel substrate for the action of nootropic drugs
- [3H]aniracetam binds to specific recognition sites in brain membranes
- Activity of putative cognition enhancers in kynurenate test performed with human neocortex slices
- Oxiracetam prevents electroshock-induced decrease in brain acetylcholine and amnesia
- Atropine, scopolamine, and ditran: comparative pharmacology and antagonists in man
- A decrease in brain catecholamines prevents oxiracetam antagonism of the effects of scopolamine on memory and brain acetylcholine
- Effect of oxiracetam and piracetam on central cholinergic mechanisms and active-avoidance acquisition
- Effects of nootropic drugs on brain cholinergic and dopaminergic transmission
- Cortical cholinergic inputs mediating arousal, attentional processing and dreaming: differential afferent regulation of the basal forebrain by telencephalic and brainstem afferents
- The "kynurenate test", a biochemical assay for putative cognition enhancers
- Possible peripheral adrenergic and central dopaminergic influences in memory consolidation
- Catecholamines and aversive learning: a review
- The role of dopamine in locomotor activity and learning
- The effect of levetiracetam on status epilepticus-induced neuronal death in the rat hippocampus
- Utility of an elevated plus-maze for dissociation of amnesic and behavioral effects of drugs in mice
- Specificity of piracetam's anti-amnesic activity in three models of amnesia in the mouse
- Delay-dependent impairment of reversal learning in rats treated with trimethyltin
- Effects of delay, intertrial interval, delay behavior and trimethyltin on spatial delayed response in rats
- Trimethyltin encephalopathy
- Quantitating silver-stained neurodegeneration: the neurotoxicity of trimethlytin (TMT) in aged rats
- Behavioural, biochemical and histological effects of trimethyltin (TMT) induced brain damage in the rat
- Oxiracetam pre- but not post-treatment prevented social recognition deficits produced with trimethyltin in rats
- Influence of piracetam and oxiracetam on the content of high-energy phosphates and morphometry of astrocytes in vitro
- Interaction between nootropic drugs and methamphetamine on avoidance acquisition but not on locomotor activity in mice
- Effects of oxiracetam-nicotine combinations on active and passive avoidance learning in mice
- Effects of oxiracetam, physostigmine, and their combination on active and passive avoidance learning in mice
- Enhancement of radial maze performances in CD1 mice after prenatal exposure to oxiracetam: possible role of sustained investigative responses developed during ontogeny
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