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Oxiracetam is a synthetic molecule derived from piracetam and differs from its parent molecule by the addition of a hydroxyl group on the 4-carbon of the pyrrolidinone ring.
It has been observed to improve some age-related cognitive deficits and mitigate scopolamine-induced deterioration in cognitive processes, but has not had any positive results in the treatment of Alzheimer’s disease.
Oxiracetam is commonly used as a nootropic compound for cognitive enhancement, particularly the improvement of memory, but has not illustrated any effect on otherwise healthy young adults.
However, the drug has been observed to improve learning and memory in normal animals as well as those with cerebral impairment. [2] It has also been implicated in the formation of long-term memory. [13]
Product Name: Oxiracetam
Chemical Name: 4-hydroxy-2-oxo-pyrrolidinoacetamide
Formula: C6H10N2O3
Molecular Weight: 158.1552 g/mol
CAS Number: 62613-82-5
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Cognitive Function- Heightens focus, alertness & perception
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Oxiracetam Chemical Structure
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Oxiracetam is a synthetic molecule of the racetam family. It is structurally similar to piracetam and differs only by an additional hydroxyl group attached to the pyrrolidinone ring.
Oxiracetam is a chiral drug that exists as both (S)- and (R)- oxiracetam. Clinically, oxiracetam is used in its racemic form.
It is possible for enantiomers, such as (R)- and (S)- oxiracetam, to exhibit different pharmacokinetic, toxicological and pharmacodynamic properties. [3]
For instance, (S)-oxiracetam is responsible for most of the observed pharmacological activity of the racemic mixture and is more effective than (R)-oxiracetam.
It has more activity “inducing long-term potentiation in rat hippocampal slices, potentiating glutamate stimulated Ca2+ uptake in cultures cerebellar granule cells and reverting the scopolamine including amnesia in rats.” [3]
Oxiracetam Pharmacokinetics
Oxiracetam has a bioavailability of approximately 73% and is well absorbed from the gastrointestinal tract. It is distributed throughout the body and has a relatively quick elimination time.
In a pharmacokinetic study of oxiracetam involving 4 health males between the ages of 20 – 26, 90% of the administered drug was excreted via urine within 24 hours.
Serum levels after both oral and intravenous administration (2000 mg) dropped rapidly after the first few hours: within 10 hours of oral administration the blood serum levels of oxiracetam were one-tenth of the peak value. [2]
- Heightens focus, alertness and perception
- Promotes better analytical thinking and memory
- Boosts energy and reduces mental fatigue
Oxiracetam Mechanisms of Action
Oxiracetam’s exact mechanism of action remains ill-defined; however, a number of studies have indicated biochemical and neurological consequences of oxiracetam administration.
In particular, oxiracetam seems to affect the cholinergic system and increases neurotransmission in the hippocampal region of the brain.
Researchers observed that oxiracteam at doses of 100 and 300 mg/kg i.p., increased acetylcholine (ACh) utilization, but not steady state ACh levels.
Further, repeated daily administration of 100 mg/kg of oxiracetam increased high-affinity choline uptake (HACU) in the rat hippocampus by 31%.
A similar increase in HACU was observed after a one-time dose of 300 mg/kg i.p.; even three hours after the administered dose, HACU rate remained 40% higher.
The researchers used these observations to hypothesize that “oxiracetam enhances the activity of the septohippocampal cholinergic pathways, and to a lesser extent the, of the cortical cholinergic network.” [4]
Oxiracetam was observed to increase neurotransmission in the CA1 rat hippocampal region.
As the authors note, the enduring increase in neurotransmission shared characteristics with long-term potentiation (LTP), which happens primarily in the hippocampus and may be a physiological site for learning and memory. [5]
LTP in the hippocampus also involves glutamatergic neurotransmission.
In rat hippocampal slices, researchers observed oxiracetam increased the release of glutamate evoked by depolarization; however, whether oxiracetam directly acted on glutamatergic neurons or via another neurotransmitter channel remains unknown. [6]
Oxiracetam Therapeutic Effects
Oxiracetam has been observed to improve some cognitive performance of individuals experiencing cognitive decline (see below); however, it has not been shown to improve cognitive decline in individuals diagnosed with Alzheimer’s disease (based on a one month trial). [7]
Oxiracetam was observed to significantly improve quality of life in patients with dementia and statistically improve their performance on neuropsychological tests.
In the double-blind, placebo-controlled study, researchers observed that patients who received 800 mg oral doses of oxiracetam twice daily over the course of 12 weeks significantly improved in their ability to perform some cognitive tasks.
This includes controlled association tests, the recall of a short story and Raven’s Progressive Matrices, compared to the placebo group. [8]
In a year-long study involving 96 patients who suffered from cognitive disorders secondary to primary degenerative dementia, individuals who received 1600 mg/day oxiracetam showed an improvement in simple reaction time and cognitive function (based on Attention Matrix test).
Comparatively, the cognitive and global functions of the placebo group showed a marked decline from baseline scores. [9]
Improvement of global evaluation in patients with multi-infarct dementia (MID) also led researchers to conclude that oxiracetam may be of some benefit to those who suffer from MID. [13]
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Anti-Amnesic Effects
Oxiracetam has been observed to reduce the severity of electroshock-induced amnesia in animal models. [10]
In a test involving 12 healthy volunteers, oxiracetam was observed to mitigate scopolamine-induced cognitive impairment.
Individuals who received either 800, 1600 2400 mg oxiracetam displayed improved cognitive test scores compared to the placebo group. [11]
Memory
No research studies have examined the impact of oxiracetam on memory and cognitive function in otherwise healthy human individuals. Instead, human studies have focused on the impact of oxiracetam on individuals already experiencing cognitive decline.
However, oxiracetam has been observed to improve memory in animals that are normal, young and aged (based on their performance of applied memory tests). [12]
Oxiracetam Safety and Side Effects
Oxiracetam is well tolerated by humans. Most clinical studies report few, if any, negative side effects.
However, in one clinical trial a small percentage of participants did report unwanted effects, including dry mouth, nycturia, dizziness, gastralgia and skin dischromia. [8]
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- Malykh AG, Sadaie MR. Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders. Drugs. 2010 Feb 12;70(3):287-312.
- Perucca E, Albrici A, Gatti G, Spalluto R, Visconti M, Crema A. Pharmacokinetics of oxiracetam following intravenous and oral administration in healthy volunteers. Eur J Drug Metab Pharmacokinet. 1984 Jul-Sep;9(3):267-74.
- Zhang Q, et al. Comparative pharmacokinetic studies of racemic oxiracetam and its pure enantiomers after oral administration in rats by a stereoselective HPLC method. J Pharm Biomed Anal. 2015 Jul 10;111:153-8. doi: 10.1016/j.jpba.2015.03.039. Epub 2015 Apr 4.
- Spignoli G, Pedata F, Giovannelli L, Banfi S, Moroni F, Pepeu G. Effect of oxiracetam and piracetam on central cholinergic mechanisms and active-avoidance acquisition. Clin Neuropharmacol. 1986;9 Suppl 3:S39-47.
- Pugliese, A. M. et al. Effect of the nootropic drug oxiracetam on field potentials of rat hippocampal slices. Br J Pharmacol. 1990 Jan; 99(1): 189–193.
- Marchi, M., Besana, E., Raiteri, M. Oxiracetam increases the release of endogenous glutamate from depolarized rat hippocampal slices. Euro J Pharmacology. 1990 Aug;185(2-3): 247-249.
- Green RC, Goldstein FC, Auchus AP, Presley R, Clark WS, Van Tuyl L, Green J, Hersch SM, Karp HR. Treatment trial of oxiracetam in Alzheimer's disease. Arch Neurol. 1992 Nov;49(11):1135-6.
- Bottini G, Vallar G, Cappa S, Monza GC, Scarpini E, Baron P, Cheldi A, Scarlato G. Oxiracetam in dementia: a double-blind, placebo-controlled study. Acta Neurol Scand. 1992 Sep;86(3):237-41.
- Rozzini R, Zanetti O, Bianchetti A.Treatment of cognitive impairment secondary to degenerative dementia. Effectiveness of oxiracetam therapy. Acta Neurol (Napoli). 1993 Feb;15(1):44-52.
- Mondadori C, Classen W, Borkowski J, Ducret T, Buerki H, Schadé A. Effects of oxiracetam on learning and memory in animals: comparison with piracetam. Clin Neuropharmacol. 1986;9 Suppl 3:S27-38.
- Preda L, Alberoni M, Bressi S, Cattaneo C, Parini J, Canal N, Franceschi M. Effects of acute doses of oxiracetam in the scopolamine model of human amnesia. Psychopharmacology (Berl). 1993;110(4):421-6.
- Cavoy A, Van Golf-Racht B, Delacour J. Relationships between arousal and cognition-enhancing effects of oxiracetam. Pharmacol Biochem Behav. 1994 Feb;47(2):283-7.
- Mondadori C, Möbius HJ, Borkowski J. The GABAB receptor antagonist CGP 36,742 and the nootropic oxiracetam facilitate the formation of long-term memory. Behav Brain Res. 1996 May;77(1-2):223-5.
- Baumel B, Eisner L, Karukin M, MacNamara R, Katz RJ, Deveaugh-Geiss J. Oxiracetam in the treatment of multi-infarct dementia. Prog Neuropsychopharmacol Biol Psychiatry. 1989;13(5):673-82.
Article last updated on: July 24th, 2018 by Nootriment