Acamprosate
Acamprosate Uses, Dosage, Side Effects, Food Interaction and all others data.
Alcohol use disorder is responsible for a large worldwide burden of morbidity, premature mortality, and economic consequences resulting from accidents, violence, incarceration, decreased productivity, and increased healthcare spending.
Acamprosate, also known by the brand name Campral, is a drug used for the maintenance of alcohol abstinence. It is a structural analogue of the neurotransmitter γ-aminobutyric acid (GABA). Acamprosate is the first medication specifically formulated for the maintenance of alcohol abstinence in ethanol-dependent patients after alcohol detoxification, unlike naltrexone and disulfiram. It was first approved by the FDA in 2004 and initially marketed by Forest Laboratories.
Acamprosate acts on the CNS, aiding in the restoration of normal glutaminergic neuron activity. Pharmacodynamic studies have shown that acamprosate calcium reduces alcohol intake in alcohol-dependent individuals, likely through effects on NMDA receptors and calcium channels. It is a safe and well-tolerated drug for patients with alcohol dependency and improves the likelihood of alcohol abstinence.
| Trade Name | Acamprosate |
| Availability | Prescription only |
| Generic | Acamprosate |
| Acamprosate Other Names | Acamprosate, Acamprosato, Acamprosatum, N-acetyl homotaurine, N-Acetylhomotaurine |
| Related Drugs | Vivitrol, naltrexone, disulfiram, Antabuse, Campral, Revia |
| Weight | 333mg |
| Type | Tablet, Oral Delayed Release Tablet |
| Formula | C5H11NO4S |
| Weight | Average: 181.21 Monoisotopic: 181.040878535 |
| Protein binding | Acamprosate is not protein bound. Prescribing information mentions that acamprosate protein binding is negligible. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Mylan |
| Available Country | United Kingdom, United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Acamprosate is a medication used to maintain alcohol abstinence in patients with alcohol dependence.
Acamprosate is indicated for the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation. It is also indicated for the maintenance of alcohol abstinence in patients who have undergone alcohol detoxification. This drug should be used with a psychosocial support program providing adequate support.
Acamprosate is also used to associated treatment for these conditions: Alcohol Abstinence, Alcohol Dependency
How Acamprosate works
The mechanism of action of acamprosate for the maintenance of alcohol abstinence has not been established. Chronic alcohol exposure is believed to modify the balance between neuronal excitation and inhibition. Results of studies in animals suggest acamprosate may interact with glutamate and GABA neurotransmitter systems in the CNS, supporting the hypothesis that acamprosate restores the balance between neuronal excitation and inhibition. Evidence shows that acamprosate directly binds and inhibits GABA B receptors and indirectly affects GABA A receptors.
Toxicity
The intraperitoneal LD50 in male mice is 1.87 g/kg. In reported cases of acute overdosage with acamprosate (doses of up to 56 grams of acamprosate calcium) diarrhea was the only reported symptom attributable to acamprosate. In the case of an overdose, supportive and symptomatic treatment is recommended.
Food Interaction
- Take with or without food. Food decreases drug absorption, but not to a clinically significant extent.
[Minor] Administration with food may decrease the bioavailability of acamprosate.
The clinical significance is unknown.
Acamprosate Disease Interaction
Volume of Distribution
At steady state concentrations, the distribution of acamprosate is about 20L. Following intravenous administration, the volume of distribution is about 72-109 L (an estimated 1 L/kg).
Elimination Route
Acamprosate is absorbed in the gastrointestinal tract. The absolute bioavailability of acamprosate after oral administration is about 11%. The effect of food absorption is clinically insignificant and no adjustment of the dose is necessary with regard to meals. After repeated oral doses of 666 mg 3 times a day, steady-state concentrations are achieved within 5 to 7 days, with plasma concentration ranging between 370 to 650 micrograms/L.
Half Life
In pharmacokinetic studies, enteric-coated acamprosate tablets demonstrate a terminal elimination half-life 10-fold higher than reported 3 hour half-life after intravenous infusion of acamprosate. After two oral doses of acamprosate 333mg, the terminal half-life ranges between 20 - 33 hours.
Clearance
Severe renal insufficiency decreases the elimination of acamprosate, and is a contraindication. An acamprosate dose of 333mg, three times daily, is recommended for moderate renal impairment (creatinine clearance of 30-50 mL/min).
Elimination Route
Half of acamprosate excretion occurs as unchanged acetyl-homotaurine in urine, and the other half possibly by biliary excretion. The kidneys are primarily responsible for the elimination of acamprosate.
Innovators Monograph
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