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药品详细

Acamprosate(阿坎)

化学结构式图
中文名
阿坎
英文名
Acamprosate
分子式
C5H11NO4S
化学名
3-acetamidopropane-1-sulfonic acid
分子量
Average: 181.21
Monoisotopic: 181.040878535
CAS号
77337-76-9
ATC分类
N07B 未知
药物类型
small molecule
阶段
approved
商品名
Campral;
同义名
3-(Acetylamino)propanesulphonic acid;3-Acetamido-1-propanesulfonic acid;acamprosate;N-Acetylhomotaurine;
基本介绍

Acamprosate, also known 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 glutaminergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid type A receptors are activated. Reports indicate that acamprosate only works with a combination of attending support groups and abstinence from alcohol. 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. Acamprosate should not be taken by people with kidney problems or allergies to the drug.

生产厂家
  • Forest laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Williams SH: Medications for treating alcohol dependence. Am Fam Physician. 2005 Nov 1;72(9):1775-80. Pubmed
  2. Mason BJ: Treatment of alcohol-dependent outpatients with acamprosate: a clinical review. J Clin Psychiatry. 2001;62 Suppl 20:42-8. Pubmed
  3. Mason BJ, Goodman AM, Chabac S, Lehert P: Effect of oral acamprosate on abstinence in patients with alcohol dependence in a double-blind, placebo-controlled trial: the role of patient motivation. J Psychiatr Res. 2006 Aug;40(5):383-93. Epub 2006 Mar 20. Pubmed
  4. Feeney GF, Connor JP, Young RM, Tucker J, McPherson A: Combined acamprosate and naltrexone, with cognitive behavioural therapy is superior to either medication alone for alcohol abstinence: a single centres’ experience with pharmacotherapy. Alcohol Alcohol. 2006 May-Jun;41(3):321-7. Epub 2006 Feb 8. Pubmed
  5. Tsai G, Coyle JT: The role of glutamatergic neurotransmission in the pathophysiology of alcoholism. Annu Rev Med. 1998;49:173-84. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Sulfonic Acids and Derivatives
Substructures
  • Hydroxy Compounds
  • Amino Ketones
  • Sulfonyls
  • Carboxylic Acids and Derivatives
  • Sulfonic Acids and Derivatives
  • Carboxamides and Derivatives
适应症
药理
Indication For the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation
Pharmacodynamics Pharmacodynamic studies have shown that acamprosate calcium reduces alcohol intake in alcohol-dependent animals in a dose-dependent manner and that this effect appears to be specific to alcohol and the mechanisms of alcohol dependence. Acamprosate calcium has negligible observable central nervous system (CNS) activity in animals outside of its effects on alcohol dependence, exhibiting no anticonvulsant, antidepressant, or anxiolytic activity.
Mechanism of action The mechanism of action of acamprosate in maintenance of alcohol abstinence is not completely understood. Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition. in vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores this balance. It seems to inhibit NMDA receptors while activating GABA receptors.
Absorption The absolute bioavailability of acamprosate after oral administration is about 11%. The food effect on absorption is not clinically significant and no adjustment of dose is necessary.
Volume of distribution
  • 72 to 109 L
Protein binding Non detectable
Metabolism
Acamprosate does not undergo metabolism.
Route of elimination Following oral administration of CAMPRAL®, the major route of excretion is via the kidneys as acamprosate.
Half life 20 - 33 hours
Clearance Not Available
Toxicity In all reported cases of acute overdosage with acamprosate (total reported doses of up to 56 grams of acamprosate calcium), the only symptom that could be reasonably associated with acamprosate was diarrhea.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP -1.1 Not Available
Predicted Properties
Property Value Source
water solubility 1.88e+01 g/l ALOGPS
logP -1.8 ALOGPS
logP -2.8 ChemAxon
logS -0.98 ALOGPS
pKa (strongest acidic) -1.1 ChemAxon
pKa (strongest basic) -0.47 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 83.47 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 38.91 ChemAxon
polarizability 17.17 ChemAxon
药物相互作用
食物相互作用
  • Take without regard to meals.
  • Taking the product with food reduces its Cmax by 42% and total drug exposure by 23% (not considered significant).

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