Tìm theo
Donepezil
Các tên gọi khác (5 ) :
  • Domepezil
  • Donepezil
  • Donepezil
  • Donepezilo
  • Donepezilum
Thuốc Gốc
Small Molecule
CAS: 120014-06-4
ATC: N06DA02
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C24H29NO3
PTK: 379.492
Donepezil (Aricept), is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. Donepezil 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 acetylcholinesterase. If this proposed mechanism of action is correct, donepezil's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. Donepezil has been tested in other cognitive disorders including Lewy body dementia and Vascular dementia, but it is not currently approved for these indications. Donepezil has also been studied in patients with Mild Cognitive Impairment, schizophrenia, attention deficit disorder, post-coronary bypass cognitive impairment, cognitive impairment associated with multiple sclerosis, and Down syndrome.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H29NO3
Phân tử khối
379.492
Monoisotopic mass
379.214743799
InChI
InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3
InChI Key
InChIKey=ADEBPBSSDYVVLD-UHFFFAOYSA-N
IUPAC Name
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
Traditional IUPAC Name
donepezil
SMILES
COC1=C(OC)C=C2C(=O)C(CC3CCN(CC4=CC=CC=C4)CC3)CC2=C1
Độ tan chảy
206.72 °C
Độ hòa tan
2.931 mg/L
logP
3.6
logS
-4.9
pKa (strongest acidic)
17.02
pKa (Strongest Basic)
8.62
PSA
38.77 Å2
Refractivity
112.11 m3·mol-1
Polarizability
44.34 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Donepezil is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. 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. Donepezil 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 acetylcholinesterase. If this proposed mechanism of action is correct, donepezil's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that donepezil alters the course of the underlying dementing process.
Cơ Chế Tác Dụng : Donepezil (Aricept), is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. Donepezil 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 acetylcholinesterase. If this proposed mechanism of action is correct, donepezil's effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. Donepezil has been tested in other cognitive disorders including Lewy body dementia and Vascular dementia, but it is not currently approved for these indications. Donepezil has also been studied in patients with Mild Cognitive Impairment, schizophrenia, attention deficit disorder, post-coronary bypass cognitive impairment, cognitive impairment associated with multiple sclerosis, and Down syndrome. Donepezil is a piperidine derivative that is a centerally active, reversible inhibitor of acetylcholinesterase. This drug is structurally unrelated to other anticholinesterase agents. Donepezil's proposed mechanism of action involves the reversible inhibition of cholinesterases (eg. acetylcholinesterase), which prevents the hydrolysis of acetycholine, and leads to an increased concentration of acetylcholine at cholinergic synapses. Evidence suggests that the anticholinesterase activity of donepezil is relatively specific for acetylcholinesterase in the brain.
Dược Động Học :
▧ Absorption :
Donepezil is well absorbed with a relative oral bioavailability of 100% and reaches peak plasma concentrations in 3 to 4 hours.
▧ Volume of Distribution :
* 12 L/kg
▧ Protein binding :
96%
▧ Metabolism :
Donepezil is metabolized by CYP 450 isoenzymes 2D6 and 3A4 in the liver and also undergoes glucuronidation. The main metabolite, 6-O-desmethyl donepezil, has been reported to inhibit AChE to the same extent as donepezil in vitro.
▧ Route of Elimination :
Donepezil is both excreted in the urine intact and extensively metabolized to four major metabolites, two of which are known to be active, and a number of minor metabolites, not all of which have been identified.
▧ Half Life :
70 hours
▧ Clearance :
* apparent plasma cl=0.13 L/hr/kg
Độc Tính : Symptoms of overdose include severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, collapse and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved.
Chỉ Định : For the palliative treatment of mild to moderate dementia of the Alzheimer's type.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet, orally disintegrating - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Egis
    Sản phẩm biệt dược : Alzepil
  • Công ty : Pfizer
    Sản phẩm biệt dược : Aricept
  • Công ty : Pfizer
    Sản phẩm biệt dược : Aricept ODT
  • Công ty : Terapia
    Sản phẩm biệt dược : Davia
  • Công ty : Psyco Remedies
    Sản phẩm biệt dược : Depzil
  • Công ty : Actavis
    Sản phẩm biệt dược : Donecept
  • Công ty : ABL Pharma
    Sản phẩm biệt dược : Donecil
  • Công ty : Alkem
    Sản phẩm biệt dược : Donep
  • Công ty : Schafer
    Sản phẩm biệt dược : Donepex
  • Công ty : Synthon
    Sản phẩm biệt dược : Donesyn
  • Công ty : Medis
    Sản phẩm biệt dược : Dopezil
  • Công ty : Wyeth
    Sản phẩm biệt dược : Eranz
  • Công ty : Pfizer
    Sản phẩm biệt dược : Memac
  • Công ty : Johnson
    Sản phẩm biệt dược : Nomi-Nox
  • Công ty : Sandoz
    Sản phẩm biệt dược : Pezale
  • Công ty : Teva
    Sản phẩm biệt dược : Redumas
  • Công ty : Actavis
    Sản phẩm biệt dược : Zolpezil
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00843
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3152
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504803
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00670
ChemSpider
http://www.chemspider.com/Chemical-Structure.3040.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=8960
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/62856-851-30
PharmGKB
http://www.pharmgkb.org/drug/PA449394
Wikipedia
http://en.wikipedia.org/wiki/Donepezil
RxList
http://www.rxlist.com/cgi/generic/donepezil.htm
Drugs.com
http://www.drugs.com/cdi/donepezil.html
... loading
... loading