| Description | Acamprosate is an acetylated derivative of the GABA analog homotaurine (tramiprosate; ). Despite its structural similarity to GABA, acamprosate does not act at GABAA receptors but does decrease paired-pulse inhibition of GABAA inhibitory post-synaptic currents (IPSCs) at short inter-stimulus intervals when used at a concentration of 300 μM, indicating that it may inhibit GABAB autoreceptor-mediated inhibition of GABA release. It is an NMDA receptor modulator with antagonist or agonist effects depending on brain region, receptor subunit composition, and other factors. Acamprosate (0.26 and 0.52 mmol/kg per day, i.p.) reduces voluntary intake of ethanol in rats, an effect that can be blocked by the GABA antagonist bicuculline . Formulations containing acamprosate have been used for the maintenance of alcohol abstinence. |
| Chemical Properties | Acamprosate calcium is White Crystalline Solid |
| Originator | Campral,Merck |
| Uses | Of interest for the treatment of alcoholism. Store at -20°C |
| Uses | glucocortcoid, antiinflammatory |
| Uses | Acamprosate calcium is a synthetic amino acid and a neurotransmitter analogue that is used as an alcohol deterrent in management of alcohol dependence and abuse. Acamprosate calcium was approved for use in the therapy of alcohol dependence and abuse in the United States in 2004. |
| Uses | Of interest for the treatment of alcoholism and other neurochemical disorders. |
| Definition | ChEBI: Acamprosate calcium is an organic calcium salt. It contains an acamprosate(1-). |
| Manufacturing Process | In a 4 liter flask provided with stirring means, a bromine funnel and a
thermometer, 17.5% sodium hydroxide solution and aminopropanesulfonic
acid (homotaurine) are added.
After complete dissolution, at a temperature of between 25°-40°C, acetic
anhydride are added so as not to exceed a temperature of between 30°-40°C.
The mixture is then maintained at this temperature by heating for at least 1
h.
The solution is then concentrated in vacuum, the residue is redissolved in 2.5
L of distilled water and the mixture is concentrated again. The residue is then
dissolved in 1.6 L of distilled water, filtered, then concentrated almost
completely. Drying is terminated in an oven in vacuum. A colorless crystalline
powder of 3-acetylaminopropanesulfonate of sodium (sodium Nacetylhomotaurinate)
is obtained.
The 3-acetylaminopropanesulfonic acid may be produced by treatment of 3-
acetylaminopropanesulfonate of sodium with hydrochloric acid.
In practice it is usually used as calcium salt. |
| Brand name | Campral (Forest). |
| Therapeutic Function | Psychotropic |
| Biological Activity | GABA receptor agonist and modulator of glutamatergic systems. Reduces alcohol consumption in animal models of alcohol addiction. |
| Biochem/physiol Actions | Acamprosate calcium is a GABA γ-aminobutyric acid agonist. |
| Clinical Use | Maintenance of abstinence in alcohol dependence |
| Metabolism | Acamprosate is excreted in the urine and is not
metabolised significantly. |
| storage | Room temperature (desiccate) |
| references | 1. wilde m i, wagstaff a j. acamprosate. drugs, 1997, 53(6): 1038-1053. |