Oxiracetam (developmental code nameISF 2522) is anootropic drug of theracetam family and a very mildstimulant.[2][3] Several studies suggest that the substance is safe even when high doses are consumed for a long period of time.[4][5][6] However, themechanism of action of theracetam drug family is still a matter of research. Oxiracetam is not approved byFood and Drug Administration for any medical use in the United States.
Oxiracetam has been studied to determine if it has an effect on symptoms of dementia,[7] but no consistent results were obtained in patients withAlzheimer's dementia or organic solvent abuse.[7]
Patients with mild to moderatedementia 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.[7] It seem to be ineffective for enhancing memory and cognitive function in patients with mild to moderateTBI.[8]
Oxiracetam-treatedlaboratory mice demonstrated a significant increase in spatial learning performance as determined by theMorris water navigation task, compared to controls. This increase in performance was correlated to an increase in membrane-bound PKC.[9]
Oxiracetam is well absorbed from the gastrointestinal tract with a bioavailability of 56-82%.[7]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 theblood–brain barrier with brain concentrations reaching 5.3% of those in the blood (measured one hour after a single 2000 mg intravenous dose).[7]
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 theseptum pellucidum, followed by thehippocampus, thecerebral cortex and with the lowest concentrations in the striatum after a 200 mg/kg oral dose given to rats.[7] Oxiracetam may be quantitated in plasma, serum or urine by liquid chromatography with one of several different detection techniques.[10]
^Valzelli L, Baiguerra G, Giraud O (June 1986). "Difference in learning and retention by Albino Swiss mice. Part III. Effect of some brain stimulants".Methods and Findings in Experimental and Clinical Pharmacology.8 (6):337–41.PMID3736279.
^Parnetti L, Mecocci P, Petrini A, Longo A, Buccolieri A, Senin U (1989). "Neuropsychological results of long-term therapy with oxiracetam in patients with dementia of Alzheimer type and multi-infarct dementia in comparison with a control group".Neuropsychobiology.22 (2):97–100.doi:10.1159/000118599.PMID2518332.
^Itil TM, Menon GN, Songar A, Itil KZ (1986). "CNS pharmacology and clinical therapeutic effects of oxiracetam".Clinical Neuropharmacology.9 (Suppl 3): S70-2.doi:10.1097/00002826-198609003-00011.PMID3594458.
^Perucca E, Parini J, Albrici A, Visconti M, Ferrero E (1987). "Oxiracetam pharmacokinetics following single and multiple dose administration in the elderly".European Journal of Drug Metabolism and Pharmacokinetics.12 (2):145–8.doi:10.1007/bf03189889.PMID3691580.S2CID11415210.
^Fordyce DE, Clark VJ, Paylor R, Wehner JM (February 1995). "Enhancement of hippocampally-mediated learning and protein kinase C activity by oxiracetam in learning-impaired DBA/2 mice".Brain Research.672 (1–2):170–6.doi:10.1016/0006-8993(94)01389-y.PMID7749739.S2CID13191058.
^Baselt R (2014).Disposition of Toxic Drugs and Chemicals in Man (10th ed.). Seal Beach, CA: Biomedical Publications. pp. 1524–1525.
Villardita C, Grioli S, Lomeo C, Cattaneo C, Parini J (1992). "Clinical studies with oxiracetam in patients with dementia of Alzheimer type and multi-infarct dementia of mild to moderate degree".Neuropsychobiology.25 (1):24–28.doi:10.1159/000118805.PMID1603291.
Mondadori C, Classen W, Borkowski J, Ducret T, Buerki H, Schadé A (1986). "Effects of oxiracetam on learning and memory in animals: comparison with piracetam".Clinical Neuropharmacology. 9 Suppl 3 (Supp.3):S27 –S38.doi:10.1097/00002826-198609003-00006.PMID3594453.
Krylova IN, Antonova LV, Kamenskiĭ AA, Iasnetsov VV (1991). "[A comparative study of the nootropic properties of piracetam and oxiracetam]".Farmakologiia i Toksikologiia.54 (1):14–16.PMID1860490.
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