Neuroprotective and Abstinence-Promoting Effects of Acamprosate

  title={Neuroprotective and Abstinence-Promoting Effects of Acamprosate},
  author={Philippe de Witte and John M. Littleton and Philippe Parot and George K. Koob},
  journal={CNS Drugs},
Acamprosate is an abstinence-promoting drug widely used in the treatment of alcohol dependence but which has a mechanism of action that has remained obscure for many years. Recently, evidence has emerged that this drug may interact with excitatory glutamatergic neurotransmission in general and as an antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5) in particular. These findings provide, for the first time, a satisfactory, unifying hypothesis that can bring together and… 
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Research suggests that acamprosate may modulate NMDA receptors via regulatory polyamine sites, or that it may act directly on metabotropic glutamate receptors, both of which are novel for the treatment of alcohol dependence.
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Glutamatergic substrates of drug addiction and alcoholism.
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Acamprosate: recent findings and future research directions.
New evidence at the molecular and cellular level suggests that acamprosate attenuates hyper-glutamatergic states that occur during early abstinence and involves iono (NMDA)- and metabotrotropic (mGluR5) glutamate receptors along with augmented intracellular calcium release and electrophysiological changes.
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Recent developments in the pharmacotherapy of alcohol dependence have targeted the phenomenon of craving in order to improve abstinence rates, and the role of pharmacotherapy in relapse prevention has become increasingly evident.
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Treatment of alcohol-dependent outpatients with acamprosate: a clinical review.
  • B. Mason
  • Medicine
    The Journal of clinical psychiatry
  • 2001
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The glutamatergic basis of human alcoholism.
A host of findings support the hypothesis that the unifying mechanism of action of ethanol in interference with glutamatergic neurotransmission, especially through the NMDA receptor, may be considered another member of the expanding family of glutamate-related neuropsychiatric disorders.
Mechanism of action of acamprosate. Part II. Ethanol dependence modifies effects of acamprosate on NMDA receptor binding in membranes from rat cerebral cortex.
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