Nefiracetam

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Nefiracetam
Nefiracetam.svg
Nefiracetam3d.png
Systematic (IUPAC) name
N-(2,6-dimethylphenyl)-2-(2-oxopyrrolidin-1-yl)acetamide
Clinical data
Legal status
  • Unscheduled (US)
Routes Oral
Pharmacokinetic data
Half-life 3-5 hours[1]
Identifiers
CAS number 77191-36-7 N
ATC code None
PubChem CID 71157
ChemSpider 64299 YesY
UNII 1JK12GX30N YesY
ChEMBL CHEMBL260829 YesY
Chemical data
Formula C14H18N2O2 
Mol. mass 246.305 g/mol
 N (what is this?)  (verify)

Nefiracetam is a nootropic antidementia drug of the racetam family.[2]

Nefiracetam's cytoprotective actions are mediated by enhancement of GABAergic, cholinergic, and monoaminergic neuronal systems. It has been shown to effectively treat apathy and improve motivation in post-stroke patients. It has been shown to exhibit antiamnesia effects for the Alzheimer's type and cerebrovascular type of dementia.[3][4] In addition, it has also been shown to have antiamnesia effects against a wide variety of memory impairing substances, including: ethanol, chlorodiazepoxide (Librium), scopolamine, bicuculline, picrotoxin, and cycloheximide.[5]

Concerns[edit]

Studies of long term consumption of nefiracetam in humans and primates have shown it to have no toxicity.[6][7] However, animals which metabolize nefiracetam differently from humans and primates are at risk for renal and testicular[8][9] toxicity. Dogs especially are particularly sensitive, which has been shown to be caused by a specific metabolite, M-18.[10] Higher doses than those in dogs were needed to cause testicular toxicity in rats, although no toxicity was seen in monkeys. Additionally, there has been no evidence of toxicity during clinical trials.[6][7]

See also[edit]

References[edit]

  1. ^ http://www.ncbi.nlm.nih.gov/pubmed/1360528
  2. ^ Murphy, Keith J; Foley, Andrew G; O'Connell, Alan W; Regan, Ciaran M (29 June 2005). "Chronic Exposure of Rats to Cognition Enhancing Drugs Produces a Neuroplastic Response Identical to that Obtained by Complex Environment Rearing". Neuropsychopharmacology. doi:10.1038/sj.npp.1300810. PMID 15988469. 
  3. ^ Robinson RG, Jorge RE, Clarence-Smith K, Starkstein S (2009). "Double-blind treatment of apathy in patients with poststroke depression using nefiracetam". The Journal of Neuropsychiatry and Clinical Neurosciences 21 (2): 144–51. doi:10.1176/appi.neuropsych.21.2.144. PMID 19622685. 
  4. ^ Robinson RG, Jorge RE, Clarence-Smith K (2008). "Double-blind randomized treatment of poststroke depression using nefiracetam". The Journal of Neuropsychiatry and Clinical Neurosciences 20 (2): 178–84. doi:10.1176/appi.neuropsych.20.2.178. PMID 18451188. 
  5. ^ Hiramatsu M, Shiotani T, Kameyama T, Nabeshima T. (Feb 1997). "Effects of nefiracetam on amnesia animal models with neuronal dysfunctions". Behavioural Brain Research 83 (1-2): 107–115. doi:10.1016/s0166-4328(97)86053-6. 
  6. ^ a b M Murasaki, M Inami, J Ishigooka, H Watanabe, M Utsumi, T Matsumoto et al. (1994). "Phase I study on DM-9384 (nefiracetam)". Jpn. Pharmacol. Ther. 22: 3539–3587. 
  7. ^ a b E Otomo, K Kogure, S Hirai, F Goto, K Hasegawa, Y Tazaki et al. (1994). "Clinical evaluation of DM-9384 in the treatment of cerebrovascular disorders: early phase II study". Jpn. Pharmacol. Ther. (22): 3589–3624. 
  8. ^ Shimada, M; Shikanai, Y; Shimomura, K; Harada, S; Watanabe, G; Taya, K; Kato, M; Furuhama, K (2003). "Investigation of testicular toxicity of nefiracetam, a neurotransmission enhancer, in rats". Toxicology letters 143 (3): 307–15. doi:10.1016/s0378-4274(03)00197-8. PMID 12849691. 
  9. ^ Shimomura, K; Shimada, M; Hagiwara, M; Harada, S; Kato, M; Furuhama, K (2004). "Testicular toxicity induced in dogs by nefiracetam, a neutrotransmission enhancer". Reproductive toxicology (Elmsford, N.Y.) 18 (3): 423–30. doi:10.1016/j.reprotox.2004.01.008. PMID 15082078. 
  10. ^ Goto, Koichi; Ishii, Yoshikazu; Jindo, Toshimasa; Furuhama, Kazuhisa (3 March 2003). "Effect of Nefiracetam, a Neurotransmission Enhancer, on Primary Uroepithelial Cells of the Canine Urinary Bladder". Toxicological Sciences 1 (72): 164–70. doi:10.1093/toxsci/kfg010. PMID 12604846.