Acamprosate
Systematic (IUPAC) name
3-Acetamidopropane-1-sulfonic acid
Identifiers
CAS number	77337-76-9
ATC code	N07BB03
PubChem	71158
DrugBank	APRD00661
Chemical data
Formula	C10H20N2O8S2
Mol. mass	181. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug ATC code N07 is a section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the Sulfur or sulphur (ˈsʌlfɚ see spelling below) is the Chemical element that has the Atomic number 16 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 211 g/mol
Pharmacokinetic data
Bioavailability	11%[1]
Protein binding	Negligible[1]
Metabolism	Nil[1]
Half life	20 to 33 hours[1]
Excretion	Renal[1]
Therapeutic considerations
Pregnancy cat.	C[2] (US) B2 (AU)
Legal status	POM(UK) ℞-only(US)
Routes	Oral (333mg tablets of acamprosate calcium)[1]

Acamprosate, also known by the brand name Campral, is a drug used for treating alcohol dependence. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity The hour (symbol h) is a unit of Time. It is not an SI unit but is accepted for use with the SI Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The United States of America —commonly referred to as the For a topic outline on this subject see List of basic Australia topics. The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route Alcohol dependence, as described in the DSM-IV, is a psychiatric diagnosis describing a Physical dependence on alcohol.

Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism, possibly by blocking glutaminergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid (GABA) type A receptors are activated. The brain is the center of the Nervous system in animals All Vertebrates and the majority of Invertebrates have a brain In Biochemistry, a receptor is a Protein molecule embedded in either the Plasma membrane or Cytoplasm of a cell to which a mobile signaling Gamma-aminobutyric acid (GABA is the chief inhibitory Neurotransmitter in the Mammalian Central nervous system. ^[3] Reports indicate that acamprosate only works with a combination of attending support groups and abstinence from alcohol. In a support group, members provide each other with various types of help usually nonprofessional and nonmaterial for a particular shared usually burdensome characteristic Abstinence is a voluntary restraint from indulging a desire or appetite for certain bodily activities that are widely experienced as giving pleasure In Chemistry, an alcohol is any Organic compound in which a Hydroxyl group ( - O[[hydrogen H]]) is bound to a Carbon ^[4] Certain serious side effects include allergic reactions, irregular heartbeats, and low or high blood pressure, while less serious side effects include headaches, insomnia, and impotence. Allergy is a disorder of the Immune system often also referred to as Atopy. Dysrhythmia redirects here For the American band see Dysrhythmia (band. Blood pressure is also the title of a short story by Damon Runyan in Guys and Dolls and Other Stories A headache ( cephalalgia in medical terminology is a condition of pain in the Head; sometimes Neck or upper back pain may also be interpreted Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity ^[5] Acamprosate should not be taken by people with kidney problems or allergies to the drug. The kidneys are complicated organs that have numerous biological roles ^[6]

Campral is manufactured and marketed in the United States by Forest Laboratories, while Merck KGaA markets it outside the US. Merck KGaA (EMD Chemicals in the United States and Canada is a German -based chemical and Pharmaceutical company. It is sold as 333 mg white and odorless tablets of acamprosate calcium, which is the equivalent of 300mg of acamprosate. For other uses of the words gram or gramme see Gram (disambiguation. White is a Color, the perception which is evoked by Light that stimulates all three types of color sensitive Cone cells in the Human eye A tablet is a mixture of active substances and Excipients usually in powder form pressed or compacted into a solid ^[1]

Contents 1 Approval 2 Study results 3 Physiological action 3.1 Possible neuroprotection 4 References

Approval

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. The United States of America —commonly referred to as the 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. The brain is the center of the Nervous system in animals All Vertebrates and the majority of Invertebrates have a brain 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. Placebo is a substance or procedure a patient accepts as medicine or therapy but which has no specific therapeutic activity In health care clinical trials are conducted to allow safety and Efficacy data to be collected for new drugs or devices e. , detoxified). Drug rehabilitation (often drug rehab or just rehab) is an umbrella term for the processes of medical and/or psychotherapeutic treatment for dependency 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. Abstinence is a voluntary restraint from indulging a desire or appetite for certain bodily activities that are widely experienced as giving pleasure Campral is not addicting and was generally well-tolerated in clinical trials. The term " addiction " is used in many contexts to describe an obsession compulsion or excessive Physical dependence or psychological dependence such as The most common adverse events reported for patients taking Campral included headache, diarrhea, flatulence, and nausea. An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences A headache ( cephalalgia in medical terminology is a condition of pain in the Head; sometimes Neck or upper back pain may also be interpreted In Medicine, diarrhea, also spelled diarrhoea (see spelling differences) is frequent loose or liquid Bowel movements Acute diarrhea Flatulence is the production of a mixture of gases in the digestive tract of Mammals that are byproducts of the digestion process Nausea ( Latin: Nausea, Greek:, " Sea-sickness " also called wamble) is the sensation of unease and discomfort "^[7]

Study results

The Scripps Research Institute conducted a double blind study comparing the effectiveness between using acamprosate and placebos in combination with psychotherapy. The Scripps Research Institute ( TSRI) is a Medical research facility that focuses on research in the basic Biomedical sciences Primarily located The blind method is a part of the Scientific method, used to prevent research outcomes from being influenced by either the Placebo effect or the Observer Placebo is a substance or procedure a patient accepts as medicine or therapy but which has no specific therapeutic activity Psychotherapy is an Interpersonal, relational intervention used by trained psychotherapists to aid clients in problems of living The primary end-point evaluated was percentage of alcohol-free days. The researchers concluded that acamprosate is "safe and effective". ^[8]

Another study was conducted by Princess Alexandra Hospital in Brisbane comparing the use of acamprosate, naltrexone, and both drugs at once in a twelve-week study. This article is about the hospital in Woolloongabba, Australia. Brisbane ( is the state capital of Queensland. Brisbane is the third most populous city in Australia and the most populous city of Queensland Naltrexone is an Opioid receptor antagonist used primarily in the management of Alcohol dependence and Opioid dependence. ^[9] Three groups of 59 patients were tested with cognitive behavioral therapy; each group with each form of treatment outlined for this study. See also Cognitive Therapy Cognitive Behavioral Therapy ( CBT) is an umbrella-term for psychotherapeutic systems that deal with cognitions interpretations The results are 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

¹ This statistic applies to patients who could not remain abstinent throughout the entire 84-day period.

This study concluded that a combination of medications was generally more popular and yielded better results than using either drug alone.

Physiological action

Alcohol inhibits activity of biochemical receptors called N-methyl-D-aspartate receptors, or NMDARs, so that chronic alcohol consumption leads to the overproduction of these receptors. In Biochemistry, a receptor is a Protein molecule embedded in either the Plasma membrane or Cytoplasm of a cell to which a mobile signaling The NMDA receptor ( NMDAR) is an Ionotropic receptor for Glutamate ( NMDA ( N -methyl D -aspartate is a name of its selective Thus, sudden alcohol abstinence causes these excessive numbers of NMDARs to be more active than normal and to produce the symptoms of delirium tremens and excitotoxic neuronal death. Delirium tremens (colloquially the DTs, " the horrors " " the fear "" the shakes "" jazz hands "" Excitotoxicity is the pathological process by which nerve cells are damaged and killed by glutamate and similar substances ^[10] Withdrawal from alcohol induces a surge in release of excitatory neurotransmitters like glutamate, which activates NMDARs. Withdrawal, also known as withdrawal/abstinence syndrome, refers to the characteristic signs and symptoms that appear when a drug that causes Physical dependence is See Chemical synapse for an introduction to concepts and terminology used in this article Glutamic acid (abbreviated as Glu or E) is one of the 20 Alpha Amino acids It is not among the human Essential amino acids Its ^[11] Acamprosate reduces this glutamate surge. ^[12] The drug also protects cultured cells in excitotoxicity induced by ethanol withdrawal. ^[13] and by glutamate exposure combined with ethanol withdrawal. ^[14]

Possible neuroprotection

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 effects of alcohol withdrawal and possibly other insults). The term neuroprotection refers to mechanisms within the Nervous system which protect Neurons from Apoptosis or Degeneration, for example following Neurons (ˈnjuːɹɒn also known as neurones and nerve cells) are responsive cells in the Nervous system that process and transmit information ^[12] For example, acamprosate has been found to protect cultured cells from damage induced by ischemia (inadequate blood flow). Cell culture is the process by which prokaryotic, or eukaryotic cells are grown under controlled conditions In Medicine, ischemia ( Greek ισχαιμία, isch- is restriction hema or haema is Blood) is a restriction ^[15] Also, the drug protected infant hamsters from brain damage induced by injections of the toxin ibotenic acid, which exacerbates excitotoxicity (the harmful overactivation of glutamate receptors. Brain damage, or Acquired brain injury, is the destruction or degeneration of Brain cells. Ibotenic acid is a Chemical compound that is naturally occurring in the Mushrooms Amanita muscaria and Amanita pantherina Excitotoxicity is the pathological process by which nerve cells are damaged and killed by glutamate and similar substances Glutamic acid (abbreviated as Glu or E) is one of the 20 Alpha Amino acids It is not among the human Essential amino acids Its In Biochemistry, a receptor is a Protein molecule embedded in either the Plasma membrane or Cytoplasm of a cell to which a mobile signaling ^[16]

References

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