Acamprosate has been successfully used to control tinnitus, hyperacusis, ear pain, and inner ear pressure during alcohol use due to spasms of the tensor tympani muscle.In addition, alcohol also inhibits the activity of N-methyl-D-aspartate receptors (NMDARs). Chronic alcohol consumption leads to the overproduction (upregulation) of these receptors. Thereafter, sudden alcohol abstinence causes the excessive numbers of NMDARs to be more active than normal and to contribute to the symptoms of delirium tremens and excitotoxic neuronal death. Withdrawal from alcohol induces a surge in release of excitatory neurotransmitters like glutamate, which activates NMDARs. Acamprosate reduces this glutamate surge. The drug also protects cultured cells from excitotoxicity induced by ethanol withdrawal and from glutamate exposure combined with ethanol withdrawal.The substance also helps re-establish a standard sleep architecture by normalizing stage 3 and REM sleep phases, which is believed to be an important aspect of its pharmacological activity. Pharmacokinetics
Acamprosate is not metabolized by the human body. Acamprosates absolute bioavailability from oral administration is approximately 11%, and its bioavailability is decreased when taken with food. Following administration and absorption of acamprosate, it is excreted unchanged (i.e., as acamprosate) via the kidneys.Its absorption and elimination are very slow, with a Tmax of 6 hours and an elimination half life of over 30 hours. History
Acamprosate was developed by Lipha, a subsidiary of Merck KGaA.
and was approved for marketing in Europe in 1989.In October 2001 Forest Laboratories acquired the rights to market the drug in the US.It was approved by the FDA in July 2004.The first generic versions of acamprosate were launched in the US in 2013.As of 2015 acamprosate was in development by Confluence Pharmaceuticals as a potential treatment for fragile X syndrome. The drug was granted orphan status for this use by the FDA in 2013 and by the EMA in 2014. Society and culture
"Acamprosate" is the INN and BAN for this substance. "Acamprosate calcium" is the USAN and JAN. It is also technically known as N-acetylhomotaurine or as calcium acetylhomotaurinate. It is sold under the brand name Campral. Research
In addition to its apparent ability to help patients refrain from drinking, some evidence suggests that acamprosate is neuroprotective (that is, it protects neurons from damage and death caused by the effects of alcohol withdrawal, and possibly other causes of neurotoxicity). See also
Homotaurine (tramiprosate)
List of investigational anxiolytics
List of investigational antidepressants


== References ==