Tìm theo
Rivastigmine
Các tên gọi khác (3) :
  • (S)-3-(1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
  • Ena 713 Free Base
  • m-((S)-1-(Dimethylamino)ethyl)phenyl ethylmethylcarbamate
neuroprotective agents, cholinesterase inhibitors, cholinergic agents
Thuốc Gốc
Small Molecule
CAS: 123441-03-2
ATC: N06DA03
ĐG : Atlantic Biologicals Corporation , http://www.atlanticbiologicals.com
CTHH: C14H22N2O2
PTK: 250.3367
Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22N2O2
Phân tử khối
250.3367
Monoisotopic mass
250.168127958
InChI
InChI=1S/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1
InChI Key
InChIKey=XSVMFMHYUFZWBK-NSHDSACASA-N
IUPAC Name
3-[(1S)-1-(dimethylamino)ethyl]phenyl N-ethyl-N-methylcarbamate
Traditional IUPAC Name
rivastigmine
SMILES
CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C
Độ hòa tan
2.04e+00 g/l
logP
2.3
logS
-2.1
pKa (Strongest Basic)
8.89
PSA
32.78 Å2
Refractivity
73.37 m3·mol-1
Polarizability
28.53 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Rivastigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. While the precise mechanism of rivastigmine's action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this proposed mechanism is correct, rivastigmine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact.
Cơ Chế Tác Dụng : Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase. Rivastigmine is a carbamate derivative that is structurally related to physostigmine, but not to donepezil and tacrine. The precise mechanism of rivastigmine has not been fully determined, but it is suggested that rivastigmine binds reversibly with and inactivates chlolinesterase (eg. acetylcholinesterase, butyrylcholinesterase), preventing the hydrolysis of acetycholine, and thus leading to an increased concentration of acetylcholine at cholinergic synapses. The anticholinesterase activity of rivastigmine is relatively specific for brain acetylcholinesterase and butyrylcholinesterase compared with those in peripheral tissues.
Dược Động Học :

▧ Volume of Distribution :
* 1.8 to 2.7 L/kg
▧ Protein binding :
40%
▧ Metabolism :
Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.
▧ Route of Elimination :
Rivastigmine is extensively metabolized primarily via cholinesterase-mediated hydrolysis to the decarbamylated metabolite NAP226-90. Renal excretion of the metabolites is the major route of elimination. Less than 1% of the administered dose is excreted in the feces.
▧ Half Life :
1.5 hours
▧ Clearance :
* renal cl=2.1-2.8 L/hr
Chỉ Định : For the treatment of mild to moderate dementia associated with Parkinson's disease or of the Alzheimer's type.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Capsule - Oral
Solution - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Exelon
  • Công ty :
    Sản phẩm biệt dược : Exelon Patch
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00989
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=77991
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507452
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C11766
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03822
ChemSpider
http://www.chemspider.com/Chemical-Structure.70377.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10620
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0501-15
PharmGKB
http://www.pharmgkb.org/drug/PA451262
Wikipedia
http://en.wikipedia.org/wiki/Rivastigmine
RxList
http://www.rxlist.com/cgi/generic2/rivastig.htm
Drugs.com
http://www.drugs.com/cdi/rivastigmine.html
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