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Oxiracetam
4-Hydroxy-2-oxopyrrolidine-N-acetamide
ISF 2522, ISF-2522, Neuractiv, Neuromet, HydroxypiracetamOpen in Piru
Oxiracetam is a nootropic drug in the racetam family1 that also acts as a mild central nervous system stimulant. It is the hydroxylated analogue of piracetam.1 Oxiracetam is less potent than noopept, requiring larger doses, although its effectiveness as a nootropic in humans remains uncertain.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold250 mg
Light500-1200 mg
Moderate1200-1800 mg
Strong1800-2400 mg
Heavy2400+ mg
Duration
Onset15-30 minutes
After Effects1-6 hours
Total4-6 hours
Subjective Effects
Subjective Effects not written up yet
Pharmacology
Pharmacodynamics
Oxiracetam increases acetylcholine release in hippocampal cells, which may contribute to its effects on memory consolidation. Its protection against scopolamine-induced amnesia in rats and humans suggests that maintaining acetylcholine availability may contribute to its action. In laboratory mice, improved spatial learning was associated with increased membrane-bound protein kinase C (PKC),2 although this association does not establish a direct mechanism.
Pharmacokinetics
Oxiracetam is well absorbed from the gastrointestinal tract, with oral bioavailability of 56-82%. After single oral doses of 800 or 2000 mg, peak serum concentrations of 19-31 μg/ml occur within 1-3 hours. Elimination is mainly renal,3 with approximately 84% excreted unchanged in urine. The elimination half-life is about 8 hours in healthy individuals4 and 10-68 hours in patients with renal impairment; reported clearance rates range from 9 to 95 ml/min. Steady-state concentrations of 60-530 μM have been reported with 800 mg administered twice daily. Oxiracetam crosses the blood-brain barrier to some extent:5 brain concentrations measured one hour after a single 2000 mg intravenous dose were 5.3% of blood concentrations. In rats given 200 mg/kg orally, brain concentrations were highest in the septum pellucidum, followed by the hippocampus and cerebral cortex, and lowest in the striatum. Several major metabolites have been identified.
Interactions
Interactions not written up yet
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Prolonged, repeated use of oxiracetam produces tolerance to many of its effects, so larger doses are needed to obtain the same effects.
Without further consumption, tolerance takes approximately 1–2 weeks to return to baseline.
Without further consumption, tolerance takes approximately 3–7 days to decrease by half.
Possible cross-tolerance with all racetam nootropics (including aniracetam and piracetam)
Harm Potential
Addiction & Dependence
Psychological
LowChronic oxiracetam use is described as non-addictive with low abuse potential and no apparent psychological dependence, though this has not been clinically corroborated.
Toxicity
Half-life is reported as about 8 hours in healthy individuals and 10 to 68 hours in patients with renal impairment.
History & Culture
Oxiracetam was among the earliest synthesized derivatives of piracetam. It has also been sold by online vendors as a dietary supplement in the United States.
Legality
International
Legally available to buy and sell in most countries
By Country
Controlled / restricted2
United StatesRestrictedFederal Food, Drug, and Cosmetic Act §§ 201(g), 201(p), 301(d), and 505(a) (21 U.S.C. §§ 321(g), 321(p), 331(d), and 355(a))6789101112131415161718192021
FDA determined that an oxiracetam product marketed with cognitive-function claims was a drug under 21 U.S.C. § 321(g)(1), was not a dietary supplement or conventional food for the statutory exception, and was an unapproved new drug because it was not generally recognized as safe and effective for its claimed uses. Under 21 U.S.C. §§ 331(d) and 355(a), introducing or delivering such a new drug into interstate commerce is prohibited unless an approval under § 355(b) or (j) is effective. This classification depends on the product and its intended use; it does not make possession of oxiracetam itself a federal offense.
United KingdomRestrictedWhether an oxiracetam product is a medicinal product under regulation 2 of the Human Medicines Regulations 2012 depends on its presentation or intended pharmacological use. Regulation 46 prohibits the sale, supply, offer for sale or supply, and possession for the purpose of sale or supply of an unauthorised medicinal product, subject to the exceptions in Part 10. Regulation 167 permits supply for an individual patient's special clinical needs only when its specified conditions are met, while commercial importation of an unlicensed medicine requires an appropriate licence and prior notification to the Medicines and Healthcare products Regulatory Agency. The agency has stated that simple possession of the cognitive-enhancement medicines it identified, including oxiracetam, was not illegal.
References
Source Pages
Citations
Further Reading
Article Status
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