Oxiracetam (developmental code name ISF 2522) is a
nootropic
Nootropics ( or ) (colloquially brain supplements, smart drugs, cognitive enhancers, memory enhancers, or brain boosters) are chemical substances which purportedly improve cognitive functions, such as attention, memory, wakefulness, and self ...
drug of the
racetam family and a very mild
stimulant
Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, ...
. Several studies suggest that the substance is safe even when high doses are consumed for a long period of time. However, the
mechanism of action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention o ...
of the
racetam drug family is still a matter of research. Oxiracetam is not approved by
Food and Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...
for any medical use in the United States.
Clinical findings
Oxiracetam has been studied to determine if it has an effect on symptoms of dementia,
but no consistent results were obtained in patients with
Alzheimer's dementia or organic solvent abuse.
Patients with mild to moderate
dementia
Dementia is a syndrome associated with many neurodegenerative diseases, characterized by a general decline in cognitive abilities that affects a person's ability to perform activities of daily living, everyday activities. This typically invo ...
experienced some beneficial effects, measured by higher scores on tests for logical performance, attention, concentration, memory and spatial orientation. Improvement was also seen in patients with exogenic post-concussion syndrome, organic brain syndromes and other dementias.
It seem to be ineffective for enhancing memory and cognitive function in patients with mild to moderate
TBI.
Oxiracetam-treated
laboratory mice
The laboratory mouse or lab mouse is a small mammal of the order Rodentia which is bred and used for scientific research or feeders for certain pets. Laboratory animal sources for these mice are usually of the species ''Mus musculus''. They a ...
demonstrated a significant increase in spatial learning performance as determined by the
Morris water navigation task, compared to controls. This increase in performance was correlated to an increase in membrane-bound PKC.
Pharmacokinetics
Oxiracetam is well absorbed from the gastrointestinal tract with a bioavailability of 56-82%.
Peak serum levels are reached within one to three hours after a single 800 mg or 2000 mg oral dose, with the maximal serum concentration reaching between 19 and 31 μg/ml at these doses.
Oxiracetam is mainly cleared renally and approximately 84% is excreted unchanged in the urine.
The half-life of oxiracetam in healthy individuals is about 8 hours, whereas it is 10–68 hours in patients with renal impairment.
There is some penetration of the
blood–brain barrier
The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that regulates the transfer of solutes and chemicals between the circulatory system and the central nervous system ...
with brain concentrations reaching 5.3% of those in the blood (measured one hour after a single 2000 mg intravenous dose).
Clearance rates range from 9 to 95 ml/min and steady-state concentrations when 800 mg is given twice daily range from 60 μM to 530 μM.
The highest brain concentrations of oxiracetam are found in the
septum pellucidum
The septum pellucidum (Latin for "translucent wall") is a thin, triangular, vertical double membrane separating the anterior horns of the left and right lateral ventricles of the brain. It runs as a sheet from the corpus callosum down to the f ...
, followed by the
hippocampus
The hippocampus (: hippocampi; via Latin from Ancient Greek, Greek , 'seahorse'), also hippocampus proper, is a major component of the brain of humans and many other vertebrates. In the human brain the hippocampus, the dentate gyrus, and the ...
, the
cerebral cortex
The cerebral cortex, also known as the cerebral mantle, is the outer layer of neural tissue of the cerebrum of the brain in humans and other mammals. It is the largest site of Neuron, neural integration in the central nervous system, and plays ...
and with the lowest concentrations in the striatum after a 200 mg/kg oral dose given to rats.
Oxiracetam may be quantitated in plasma, serum or urine by liquid chromatography with one of several different detection techniques.
The major metabolites of Oxiracetam include: beta-hydroxy-
2-pyrrolidone, N-aminoacetyl-
GABOB, GABOB (beta-hydroxy-GABA) and
glycine
Glycine (symbol Gly or G; ) is an amino acid that has a single hydrogen atom as its side chain. It is the simplest stable amino acid. Glycine is one of the proteinogenic amino acids. It is encoded by all the codons starting with GG (G ...
. Thus its metabolic route is exactly parallel to that of
piracetam
Piracetam is a drug that has efficacy in cognitive disorders, vertigo, cortical myoclonus, dyslexia, and sickle cell anemia; sources differ on its usefulness for dementia. Piracetam is sold as a medication in many European countries. Piracetam ...
,
aniracetam
Aniracetam (brand names Draganon, Sarpul, Ampamet, Memodrin, Referan), also known as ''N''-anisoyl-2-pyrrolidinone, is a racetam which is sold in Europe as a prescription drug. It is not approved by the Food and Drug Administration for use in t ...
,
phenylpiracetam
Phenylpiracetam, also known as fonturacetam () and sold under the brand names Phenotropil, Actitropil, and Carphedon among others, is a psychostimulant, stimulant and nootropic medication used in Russia and certain other Eastern European countr ...
, and all other members of the -racetam family, and also
pyroglutamic acid.
References
Further reading
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External links
Oxiracetam on PsychonautWiki
{{Ionotropic glutamate receptor modulators
Acetamides
AMPA receptor positive allosteric modulators
Drugs with unknown mechanisms of action
Racetams
Secondary alcohols
Stimulants