Tìm theo
Acamprosate
Các tên gọi khác (5 ) :
  • 3-Acetamido-1-propanesulfonic acid
  • Acamprosato
  • Acamprosatum
  • N-acetyl homotaurine
  • N-Acetylhomotaurine
alcohol deterrents
Thuốc Gốc
Small Molecule
CAS: 77337-76-9
ATC: N07BB03
ĐG : Forest Pharmaceuticals , http://www.forestpharm.com
CTHH: C5H11NO4S
PTK: 181.21
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C5H11NO4S
Phân tử khối
181.21
Monoisotopic mass
181.040878535
InChI
InChI=1S/C5H11NO4S/c1-5(7)6-3-2-4-11(8,9)10/h2-4H2,1H3,(H,6,7)(H,8,9,10)
InChI Key
InChIKey=AFCGFAGUEYAMAO-UHFFFAOYSA-N
IUPAC Name
3-acetamidopropane-1-sulfonic acid
Traditional IUPAC Name
acamprosate
SMILES
CC(=O)NCCCS(O)(=O)=O
Độ hòa tan
1.88e+01 g/l
logP
-1.1
logS
-0.98
pKa (strongest acidic)
-1.1
pKa (Strongest Basic)
-0.47
PSA
83.47 Å2
Refractivity
38.91 m3·mol-1
Polarizability
17.17 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ 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
Độc Tính : 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.
Chỉ Định : For the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation
Liều Lượng & Cách Dùng : Tablet, delayed release - Oral - 333 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00659
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=71158
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506657
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02780
ChemSpider
http://www.chemspider.com/Chemical-Structure.64300.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-3330-01
PharmGKB
http://www.pharmgkb.org/drug/PA10344
Wikipedia
http://en.wikipedia.org/wiki/Acamprosate
RxList
http://www.rxlist.com/cgi/generic3/campral.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cam1691.shtml
Drugs.com
http://www.drugs.com/cdi/acamprosate.html
... loading
... loading