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acamprosate is an approved drug (FDA (2004))
Compound class: Synthetic organic
Comment: Acamprosate is a NMDA glutamate receptor antagonist and a positive allosteric modulator of GABAA receptors.
Marketed formulations contain acamprosate calcium (PubChem CID 155434).
View more information in the IUPHAR Pharmacology Education Project: acamprosate
|No information available.|
|Summary of Clinical Use|
|Used alongside behavioural therapy to maintain alcohol abstinence in alcohol-dependent patients.
In 2014, the European Medicines Agency granted this drug orphan designation for the treatment of fragile X syndrome [2-3]. A Phase 2/III clinical trial for this indication is underway (NCT01911455). Another Phase 2/III clinical trial is recruiting patients to evaluate any benefit from acamprosate in autism disorder (NCT01813318).
|Mechanism Of Action and Pharmacodynamic Effects|
|This drug acts as an antagonist of NMDA glutamate receptors and as a positive allosteric modulator of GABAA receptors. The glutaminergic hypothesis links this neurotransmitter system to alcohol dependence and withdrawal . In addition, cortical and limbic arousal (sympathetic activation) levels are believed to be upregulated during alcohol withdrawal, as a 'bounce-back' response to alcohol-induced down-regulation of GABAA receptors. Acamprosate-potentiated GABAA activity helps to inhibit this elevated arousal. These two mechanisms appear to act together to provide the clinical benefits observed with use of this drug.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT01813318||Study of Acamprosate in Autism||Phase 2/Phase 3 Interventional||Children's Hospital Medical Center, Cincinnati|
|NCT01911455||Study of Acamprosate in Fragile x Syndrome||Phase 2/Phase 3 Interventional||Children's Hospital Medical Center, Cincinnati|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)