Acamprosate
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| Non-proprietary name | Acamprosate | |||||||||||||||||||||
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| Drug class |
Adjuvant therapeutic agent for alcohol cessation |
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| Physical state |
firmly |
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| Melting point |
270 ° C (acamprosate calcium) |
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| solubility |
poor in water (5 g l −1 at 20 ° C, calcium salt) |
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| Toxicological data |
> 10000 mg kg −1 ( LD 50 , mouse , oral , acamprosate calcium) |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Acamprosate, N- acetylhomotaurin , is a drug that is used in the supportive treatment of alcoholic illness , more specifically to support abstinence in alcohol-dependent patients.
The substance, also known as N- acetylhomotaurine, is related to the neurotransmitters active in the brain - amino acids γ-aminobutyric acid (GABA), glutamate and taurine .
Working principle
Acamprosate, an analogue of the amino acid homotaurin, dampens the hyperexcitability of the brain triggered by the messenger substance glutamate by occupying the receptors of the nerve cells and thereby preventing the docking of glutamate molecules. Homotaurin is a GABAergic agonist.
Since alcoholics have a particularly high amount of glutamate in the brain (the reason is unclear), acamprosate is used in the (outpatient) therapy of alcoholism to reduce the desire for alcohol. However, not every alcoholic reacts to acamprosate. Acamprosate is not suitable for treating the symptoms of alcohol withdrawal.
Pharmacokinetics
Less than 10 percent of the dose is absorbed from the gastrointestinal tract . Simultaneous consumption of food reduces absorption. The resorption rate is therefore subject to large individual fluctuations. Maximum blood levels are reached after about 4 hours. Acamprosate crosses the blood-brain barrier, is not bound to plasma proteins and is not subject to any biotransformation . It is excreted unabated by the kidneys and has a plasma half-life of 13 hours.
Development history
In 1984 Acamprosat was developed by the small French company Meram for the therapy of epileptics and alcohol addicts. As early as 1987, Meram received preliminary approval for the substance in France. In 1989, the company launched the active ingredient on the local market. To prepare for EU-wide approval, the French company Lipha (a subsidiary of Merck KGaA) took over the substance and carried out twelve placebo-controlled multicenter studies with a total of around 4,000 patients. In December 1995, Campral was approved in Germany. In mid-March 1996, Lipha launched a drug containing acamprosate as Campral ® on the German market. In July 2004, Campral ® was approved in the USA "for maintaining alcohol abstinence in alcohol-dependent patients who are already alcohol-abstinent at the start of treatment"; the sales partner in the USA is Forest Laboratories . In 1999 Campral received the Galenus von Pergamon Prize .
Anti-craving
Acamprosate is used as an anti- substance craving substance in alcohol withdrawal. The patient should be abstinent for about 5 days before taking it. Concomitant use of acamprosate and alcohol does not change the pharmacokinetics of either acamprosate or alcohol.
Side effects
Common side effects include diarrhea ( diarrhea ), bloating ( flatulence ), nausea and vomiting, itching and rash. Acamprosat does not affect the ability to drive and it is not known to be addictive.
Interactions
Interactions with other drugs or alcohol are not expected.
Pharmaceutical information
Acamprosate is effective orally . The calcium salt is used medicinally.
Trade names
Acamprosat is commercially available in Germany, Austria and Switzerland under the name Campral.
Web links
- Internet presence for Campral in the USA
- Monika Wimmer: The discreet way out of addiction. In: Berliner Zeitung . January 18, 2006, p. 15 , accessed June 18, 2015 .
- Kolja Jahnke: The effect of acamprosate on the stimulus reactivity of abstinent alcohol addicts (PDF; 982 kB) Inaugural dissertation of the Medical Faculty of the Albert Ludwig University of Freiburg i.Br., presented in 2008
- for side effects and interactions see page 13 of the medication regulation in practice ~ Edition 1/2000 March (archive version) ( Memento from August 30, 2006 in the Internet Archive )
Individual evidence
- ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, p. 4, ISBN 978-0-911910-00-1 .
- ↑ a b c data sheet Acamprosate calcium from Sigma-Aldrich , accessed on March 18, 2011 ( PDF ).
- ↑ Entry on acamprosate. In: Römpp Online . Georg Thieme Verlag, accessed on May 30, 2014.
- ↑ Collins GB, McAllister MS, Adury K. Drug adjuncts for treating alcohol dependence. Cleve Clin J Med. 2006 Jul; 73 (7): 641-4, 647-8, 650-1. Review. PMID 16845975
- ↑ a b c Information for healthcare professionals (summary of the product characteristics) Campral from Merck (Schweiz) AG - as of July 2007 .
- ↑ Merck - Campral® receives US approval . Finanznachrichten.de. July 30, 2004. Retrieved July 5, 2010.
- ↑ ROTE LISTE 2017, Verlag Rote Liste Service GmbH, Frankfurt am Main, ISBN 978-3-946057-10-9 , p. 157.
- ↑ AGES-PharmMed, accessed on August 17, 2009.
- ↑ Swiss Medicines Compendium , accessed on August 17, 2009.
literature
- Bernhard van Treeck : Drugs and Addiction Lexicon . Schwarzkopf and Schwarzkopf, Berlin 2004, ISBN 3-89602-542-2 .
