Racetam
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Racetam
Racetams are a class of drugs that share a pyrrolidone nucleus. Some, such as piracetam, aniracetam, oxiracetam, pramiracetam and phenylpiracetam are considered nootropics. Others such as levetiracetam, brivaracetam, and seletracetam are anticonvulsants. Mechanism There is no universally accepted mechanism of action for racetams. Racetams generally show negligible affinity for common central nervous system receptors, but modulation of central neurotransmitters, including acetylcholine and glutamate, has been reported. Although aniracetam and nebracetam show affinity for muscarinic receptors, only nefiracetam demonstrates nanomolar interactions. Modification of membrane-located mechanisms of central signal transduction is another hypothesis. Like some ampakines, some racetams such as piracetam and aniracetam are positive allosteric modulators of the AMPA receptor. Racetams are understood to work by allosterically modulating glutamate receptors, specifically AMPA receptor ...
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Nootropic
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic dietary supplement, supplements or drugs and other substances that are claimed to improve cognitive function or to promote Relaxation (psychology), relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the Medical ethics, ethics and fairness of their use, concerns over adverse effects, and the drug diversion, diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at ...
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Levetiracetam
Levetiracetam, sold under the brand name Keppra among others, is a medication used to treat epilepsy. It is used for partial-onset, myoclonic, or tonic–clonic seizures and is taken either by mouth as an immediate or extended release formulation or by injection into a vein. Common side effects of levetiracetam include sleepiness, dizziness, feeling tired, and aggression. Severe side effects may include psychosis, suicide, and allergic reactions such as Stevens–Johnson syndrome or anaphylaxis. It is unclear if levetiracetam is safe for use during pregnancy and breastfeeding. Levetiracetam is the S- enantiomer of etiracetam. Its mechanism of action is not yet clear. Levetiracetam was approved for medical use in the United States in 1999 and is available as a generic medication. In 2020, it was the 92nd most commonly prescribed medication in the United States, with more than 7million prescriptions. Medical uses Focal epilepsy Levetiracetam is effective as single-drug ...
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Phenylpiracetam
Phenylpiracetam ( INN: fonturacetam, brand names Phenotropil Фенотропил, Carphedon), is a phenylated analog of the drug piracetam. It was developed in 1983 as a medication for Soviet Cosmonauts to treat the prolonged stresses of working in space. Phenylpiracetam was created at the Russian Academy of Sciences Institute of Biomedical Problems in an effort led by psychopharmacologist Valentina Ivanovna Akhapkina (Валентина Ивановна Ахапкина). In Russia it is now available as a prescription drug. Research on animals has indicated that phenylpiracetam may have anti-amnesic, antidepressant, anticonvulsant, anxiolytic, and memory enhancement effects. Uses A few small clinical studies have shown possible links between prescription of phenylpiracetam and improvement in a number of encephalopathic conditions, including lesions of cerebral blood pathways, traumatic brain injury and certain types of glioma. Phenylpiracetam reverses the depressant ...
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Nefiracetam
Nefiracetam is a nootropic drug of the racetam family. Preliminary research suggests that it may possess certain antidementia properties in rats. Effects Nefiracetam's cytoprotective actions are mediated by enhancement of GABAergic, cholinergic, and monoaminergic neuronal systems. Preliminary studies suggest that it improves apathy and motivation in post-stroke patients. It may also exhibit antiamnesia effects for the Alzheimer's type and cerebrovascular type of dementia. In addition, research in animal models suggests antiamnesic effects against a number of memory impairing substances, including: ethanol, chlorodiazepoxide, scopolamine, bicuculline, picrotoxin, and cycloheximide. Pharmacology Unlike other racetams, nefiracetam shows high affinity for the GABAA receptor ( IC50) = 8.5 nM), where it is presumed to be an agonist. It was able to potently inhibit 80% of muscimol binding to the GABAA receptor, although it failed to displace the remaining 20% of specific muscimol ...
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Nebracetam
Nebracetam is an investigational drug of the racetam family that is a M1 acetylcholine receptor agonist in rats. Its effects in humans have not been studied. See also * Piracetam * Aniracetam * Racetam Racetams are a class of drugs that share a pyrrolidone nucleus. Some, such as piracetam, aniracetam, oxiracetam, pramiracetam and phenylpiracetam are considered nootropics. Others such as levetiracetam, brivaracetam, and seletracetam are ant ... References Racetams Amines Experimental drugs {{nervous-system-drug-stub ...
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Phenylpiracetam
Phenylpiracetam ( INN: fonturacetam, brand names Phenotropil Фенотропил, Carphedon), is a phenylated analog of the drug piracetam. It was developed in 1983 as a medication for Soviet Cosmonauts to treat the prolonged stresses of working in space. Phenylpiracetam was created at the Russian Academy of Sciences Institute of Biomedical Problems in an effort led by psychopharmacologist Valentina Ivanovna Akhapkina (Валентина Ивановна Ахапкина). In Russia it is now available as a prescription drug. Research on animals has indicated that phenylpiracetam may have anti-amnesic, antidepressant, anticonvulsant, anxiolytic, and memory enhancement effects. Uses A few small clinical studies have shown possible links between prescription of phenylpiracetam and improvement in a number of encephalopathic conditions, including lesions of cerebral blood pathways, traumatic brain injury and certain types of glioma. Phenylpiracetam reverses the depressant ...
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Brivaracetam
Brivaracetam, sold under the brand names Briviact and Brivajoy among others, a chemical analog of levetiracetam, is a racetam derivative with anticonvulsant (antiepileptic) properties. It is marketed by the pharmaceutical company UCB. It is available as a generic medication. Medical uses Brivaracetam is used to treat partial-onset seizures with or without secondary generalisation, in combination with other antiepileptic drugs. No data are available for its effectiveness and safety in people younger than 16 years of age. Drugs.com Adverse effects The most common adverse effects include sleepiness, dizziness, nausea and vomiting. More rarely, coordination problems and changes in behaviour (such as severe depression, aggression, hostility, impatience, rage, depression, suicide ideology, etc.) can occur. Interactions Coadministration of brivaracetam with carbamazepine may increase exposure to carbamazepine-epoxide, the active metabolite of carbamazepine, and could theoreticall ...
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Piracetam
Piracetam is a drug marketed as a treatment for myoclonus. It is also used as a cognitive enhancer to improve memory, attention, and learning. Evidence to support its use is unclear, with some studies showing modest benefits in specific populations and others showing minimal or no benefit. Piracetam is sold as a medication in many European countries. Sale of piracetam is not illegal in the United States, although it is not regulated nor approved by the FDA so it is legally sold for research use only. Piracetam is in the racetams group, with chemical name ''2-oxo-1-pyrrolidine acetamide''. It is a derivative of the neurotransmitter GABA and shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid. Piracetam is a cyclic derivative of GABA (gamma-aminobutyric acid). Related drugs include the anticonvulsants levetiracetam and brivaracetam, and the putative nootropics aniracetam and phenylpiracetam. Efficacy Dementia A 2001 Cochrane review concluded that there ...
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Methylphenylpiracetam
Methylphenylpiracetam is a derivative of piracetam and a positive allosteric modulator of the sigma-1 receptor. It differs from phenylpiracetam by having a methyl group. E1R is the (4''R'',5''S'') stereoisomer of methylphenylpiracetam. Enantiomers The two R-configuration enantiomers, i.e. (4''R'',5''S'') and (4''R'',5''R''), of methylphenylpiracetam are more active positive allosteric modulators of the sigma-1 receptor than the two S-configuration enantiomers, i.e. (4''S'',5''R'') and (4''S'',5''S''). Effects E1R enhances cognition and has efficacy against cholinergic dysfunction in mice without affecting locomotor activity. Pretreatment with E1R enhanced the σ1R agonist PRE-084's stimulating effect and facilitated passive avoidance retention. It alleviated scopolamine-induced cognitive impairment. The cognition enhancing activity of E1R is higher than that of (''R'')-phenylpiracetam. Because E1R had no effect on locomotor activity, it was found to be free of potential mo ...
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Seletracetam
Seletracetam (UCB 44212) is a pyrrolidone-derived drug of the racetam family that is structurally related to levetiracetam (trade name Keppra). It was under development by UCB Pharmaceuticals as a more potent and effective anticonvulsant drug to replace levetiracetam but its development has been halted. There are two main mechanisms of action for seletracetam. The first is its high-affinity stereospecific binding to synaptic vesicle glycoprotein 2A (SV2A). Seletracetam has shown potent seizure suppression in models of acquired and genetic epilepsy, and has been well tolerated by various animal models. The second is its binding to N-type calcium channels and preventing influx of Ca2+ during high-voltage activation that is typical of epilepsy. While similar in structure to nootropic drugs, it is not expected to have cognitive enhancing properties. Seletracetam was in Phase II clinical trials under the supervision of the U.S. Food and Drug Administration (FDA) but its production i ...
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Fonturacetam Hydrazide
Phenylpiracetam hydrazide, also known as fonturacetam hydrazide, is a racetam that is a derivative of phenylpiracetam in which the amide group is replaced with a hydrazide group. It was first reported by a Russian research group in 1980 as part of a series of chemical compounds investigated as anticonvulsants. In an electroshock test it was found to have an ED50 of 310 mg/kg. Sale on the internet All piracetam derivatives are not permitted to be sold as dietary supplements in the United States. However, because they lack scheduling, piracetam derivatives like phenylpiracetam hydrazide are sold over the clear net accompanied by indications of not being for human consumption. See also * Piracetam Piracetam is a drug marketed as a treatment for myoclonus. It is also used as a cognitive enhancer to improve memory, attention, and learning. Evidence to support its use is unclear, with some studies showing modest benefits in specific popula ... References Acetamid ...
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Pramiracetam
Pramiracetam is a central nervous system stimulant and nootropic agent belonging to the racetam family of drugs. It is marketed by Menarini under the brand name Pramistar as a treatment for memory and attention deficits in aging people with neurodegenerative and vascular dementias in Italy and some Eastern European countries. Pramiracetam was discovered by scientists at Parke-Davis, at that time a division of Warner-Lambert, in the late 1970s; patents expired in 1996. Warner-Lambert conducted clinical trials in Alzheimer's Disease and abandoned that indication after Phase II trials showed mixed results; it then began to develop it as an orphan drug as an adjunct to electroconvulsive therapy for major depressive disorder, in part to take advantage of the administrative exclusivity provided by the orphan status. It licensed European rights to Menarini which continued developing it for dementias, and in 1991 it licensed US and other non-European rights to Cambridge Neuroscience, ...
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