Clinical Pharmacokinetics of Acamprosate

  title={Clinical Pharmacokinetics of Acamprosate},
  author={Sylvie Saivin and Thierry Hulot and Sylvie Chabac and Adrian Potgieter and Philippe Durbin and Georges Houin},
  journal={Clinical Pharmacokinetics},
Acamprosate is a new psychotropic drug used in the treatment of alcohol (ethanol)-dependence. Recent studies suggest that acamprosate inhibits neuronal hyperexcitability by antagonising excitatory amino acids. It is available as a 333mg enteric-coated tablet, with a recommended dosage of 1.3 g/day for patients with a bodyweight <60kg and 2 g/day for patients with a bodyweight ≥60kg. Treatment with higher dose strength tablets 2 × 500mg twice daily is bioequivalent to treatment with the 2… 
Kinetic study of acamprosate absorption in rat small intestine.
Results suggest that acamprosate and taurine share, at least, an intestinal carrier system in rat jejunum, and there are probably two pathways involved in the intestinal absorption of acampingrosate: passive diffusion and mediated transport, with the former being predominant.
Acamprosate for treatment of alcohol dependence: mechanisms, efficacy, and clinical utility
Acamprosate has demonstrated its efficacy in more than 25 placebo-controlled, double-blind trials for individuals with alcohol dependence, and has generally been found to be more efficacious than placebo in significantly reducing the risk of returning to any drinking and increasing the cumulative duration of abstinence.
A Pharmacokinetic and Pharmacodynamic Drug Interaction Study of Acamprosate and Naltrexone
Disposition of acamprosate in the rat: Influence of probenecid
On average, 95% of the administered dose of acamprosate was excreted unchanged in the urine of the animals in the 0–6 h post‐administration period indicating that renal excretion is the main elimination route for this drug.
Alcohol effects during acamprosate treatment: a dose-response study in humans.
Although a trend appeared for acamprosate to increase subjective ratings of intoxication following the lower alcohol dose, adjustment for individual differences in blood alcohol level eliminated this effect, suggesting the trend was not due to a central effect of acamposate.
Rationale for combining acamprosate and naltrexone for treating alcohol dependence.
  • B. Mason
  • Medicine
    Journal of studies on alcohol. Supplement
  • 2005
These factors support investigating the efficacy and safety of combining acamprosate and naltrexone for the treatment of alcohol dependence in a large-scale multisite trial, with evaluation of potential predictors of response to each drug alone and in combination relative to placebo.
Pharmacology of acamprosate: an overview.
It is pointed out that further research is necessary in order to clearly understand the mode of action of acamprosate as well as the neurobiological mechanisms involved in alcohol dependence.
Safety and Efficacy of Acamprosate for the Treatment of Alcohol Dependence
Current clinical data on the safety, efficacy, and pharmacokinetic properties of acamprosate, as well as theories on its potential mechanism of action are summarized and a discussion of the place of acamrosate in addiction medicine and therapy is discussed.
Studies of acamprosate for the treatment of alcohol dependence
A potential mechanism by which acamprosate mediates its therapeutic effect may be by attenuating the urge to drink following an alcohol slip, and this effect may been dose-dependent.
Acamprosate for the Adjunctive Treatment of Alcohol Dependence
Although the precise mechanism of acamprosate in the treatment of alcohol-dependent patients is unclear, it may restore the balance between inhibitory and excitatory neurotransmission in the central nervous system.


Acamprosate. A review of its pharmacology and clinical potential in the management of alcohol dependence after detoxification.
Oral acamprosate, as an adjunct to psychosocial/behavioural therapies, represents a novel advance for the management of alcohol-dependent patients in the postdetoxification period and appears to be dose dependent and enhanced by the addition of disulfiram.
[Acamprosate. From pharmacology to therapeutics].
Different clinical controlled studies on patients suffering from signs of physical or psychical alcohol addiction as well as biological modifications due to their ethylic consumption showed beneficial effects of acamprosate (in weaned alcoholics after withdrawal) according to clinical criteria and for biological criteria.
Acamprosate in alcohol dependence: how does it work?
It is suggested that acamprosate may reduce craving that is associated with conditioned withdrawal and be a novel kind of agent that suppresses "craving" in weaned alcohol dependent patients.
Combined efficacy of acamprosate and disulfiram in the treatment of alcoholism: a controlled study.
It was concluded that acamprosate was a useful and safe pharmacotherapy in the long-term treatment of alcoholism and concomitant administration of disulfiram improved the effectiveness of acamposate.
Mechanism of action of acamprosate. Part I. Characterization of spermidine-sensitive acamprosate binding site in rat brain.
The results show that acamprosate binds to a specific spermidine-sensitive site that modulates the NMDA receptor in a complex way, so that low concentrations enhance activation when receptor activity is low, whereas higher concentrations are inhibitory to high levels of receptor activation.
Pharmacodynamics and Pharmacokinetics of Acamprosate: An Overview*
Acamprosate (calcium acetylaminopropane sulphonate) is the active substance of Campral and has the following chemical structure (CH3-CO-NH-CH2-CH2CH2-S03)2Ca. The molecular structure is related to
Calcium-Acetylhomotaurinate for Maintaining Abstinence in Weaned Alcoholic Patients: A Placebo-Controlled Double-Blind Multicenter Study
Drugs used for attenuating alcohol intake consist of two types: 1. Agents postulated to attenuate drinking by causing aversive consequences if alcohol is consumed after they are ingested,