| Systematic (IUPAC) name | |
|---|---|
| 3-Acetamidopropane-1-sulfonic acid | |
| Clinical data | |
| Pregnancy cat. | C[1] (US) B2 (AU) |
| Legal status | POM (UK) ℞-only (US) |
| Routes | Oral (333mg tablets of acamprosate calcium)[1] |
| Pharmacokinetic data | |
| Bioavailability | 11%[1] |
| Protein binding | Negligible[1] |
| Metabolism | Nil[1] |
| Half-life | 20 to 33 hours[1] |
| Excretion | Renal[1] |
| Identifiers | |
| CAS number | 77337-76-9 |
| ATC code | N07BB03 |
| PubChem | CID 155434 |
| DrugBank | APRD00661 |
| ChemSpider | 136929 |
| UNII | N4K14YGM3J |
| KEGG | D07058 |
| ChEBI | CHEBI:51042 |
| ChEMBL | CHEMBL1201293 |
| Chemical data | |
| Formula | C5H11NO4S |
| Mol. mass | 181.211 g/mol |
| SMILES | eMolecules & PubChem |
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Acamprosate, also known as N-acetyl homotaurine[2] and by the brand name Campral, is a drug used for treating alcohol dependence.
Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism, possibly by blocking glutamatergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid (GABA) type A receptors are activated.[3] Reports indicate that acamprosate only works with a combination of attending support groups and abstinence from alcohol.[4][5] Certain serious side effects include diarrhea, allergic reactions, irregular heartbeats, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence.[6] Acamprosate should not be taken by people with kidney problems or allergies to the drug.[7]
Campral is manufactured and marketed in the United States by Forest Laboratories, while Merck KGaA markets it outside the US. It is sold as 333 mg white and odorless tablets of acamprosate calcium, which is the equivalent of 300 mg of acamprosate.[1]
Contents |
Alcohol inhibits activity of biochemical receptors called N-methyl-D-aspartate receptors, or NMDARs, so that 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 produce the symptoms of delirium tremens and excitotoxic neuronal death.[8] Withdrawal from alcohol induces a surge in release of excitatory neurotransmitters like glutamate, which activates NMDARs.[9] Acamprosate reduces this glutamate surge.[10] The drug also protects cultured cells from excitotoxicity induced by ethanol withdrawal[11] and from glutamate exposure combined with ethanol withdrawal.[12]
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, or possibly other insults).[2][10] For example, acamprosate has been found to protect cultured cells from damage induced by ischemia (inadequate blood flow).[13] The drug also protected infant hamsters from brain damage induced by injections of the toxin ibotenic acid (which exacerbates excitotoxicity, the harmful over-activation of glutamate receptors).[14]
One Brazilian study has shown that Acamprosate may be an effective treatment for tinnitus (persistent ringing in the ears due to hearing loss).[15]
While the Food and Drug Administration (FDA) in the United States approved this drug in July 2004, it has been legal in Europe since 1989. After it approved the drug, the FDA released this statement:
While its mechanism of action is not fully understood, Campral is thought to act on the brain pathways related to alcohol abuse. Campral was demonstrated to be safe and effective by multiple placebo-controlled clinical studies involving alcohol-dependent patients who had already been withdrawn from alcohol, (i.e., detoxified). Campral proved superior to placebo in maintaining abstinence (keeping patients off alcohol consumption), as indicated by a greater percentage of acamprosate-treated subjects being assessed as continuously abstinent throughout treatment. Campral is not addicting and was generally well-tolerated in clinical trials. The most common adverse events reported for patients taking Campral included headache, diarrhea, flatulence, and nausea.[16]
The Scripps Research Institute conducted a double blind study comparing acamprosate and placebos, in combination with psychotherapy, in the effectiveness of treating alcohol dependence. The researchers concluded that acamprosate is "safe and effective" as acamprosate increased the percentage of alcohol-free days.[17]
Another study was conducted by Princess Alexandra Hospital in Brisbane comparing the use of acamprosate, naltrexone, or both drugs at once (with each pharmacological treatment also paired with cognitive behavioral therapy) in a twelve-week study.[18] This study concluded that a combination of medications was generally more popular and yielded better results than using either drug alone, as outlined below.
| Percentage attending program | Abstinence rates | Average number of days abstinence1 | Days until first breach of abstinence1 | |
|---|---|---|---|---|
| Acamprosate group | 66.1% | 50.8% | 45.07 days | 26.79 days |
| Naltrexone group | 79.7% | 66.1% | 49.95 days | 26.7 days |
| Drug combination group | 83.1% | 67.8% | 53.58 days | 37.32 days |