Tìm theo
Memantine
Các tên gọi khác (8 ) :
  • 1-Amino-3,5-dimethyladamantane
  • 1,3-Dimethyl-5-adamantanamine
  • 3,5-Dimethyl-1-adamantanamine
  • 3,5-Dimethyl-1-aminoadamantane
  • 3,5-Dimethyltricyclo(3.3.1.1(3,7))decan-1-amine
  • Memantina
  • Memantine
  • Memantinum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 19982-08-2
ATC: N06DX01
ĐG : Bryant Ranch Prepack , http://bryantranchprepack.com
CTHH: C12H21N
PTK: 179.3018
Memantine is an amantadine derivative with low to moderate-affinity for NMDA receptors. It is a noncompetitive NMDA receptor antagonist that binds preferentially to NMDA receptor-operated cation channels. It blocks the effects of excessive levels of glutamate that may lead to neuronal dysfunction. It is under investigation for the treatment of Alzheimer's disease, but there has been no clinical support for the prevention or slowing of disease progression.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H21N
Phân tử khối
179.3018
Monoisotopic mass
179.167399677
InChI
InChI=1S/C12H21N/c1-10-3-9-4-11(2,6-10)8-12(13,5-9)7-10/h9H,3-8,13H2,1-2H3
InChI Key
InChIKey=BUGYDGFZZOZRHP-UHFFFAOYSA-N
IUPAC Name
3,5-dimethyladamantan-1-amine
Traditional IUPAC Name
memantine
SMILES
CC12CC3CC(C)(C1)CC(N)(C3)C2
Độ tan chảy
258 °C
Độ hòa tan
35 mg/mL (HCl salt), 0.9 mg/mL for free base
logP
3.28
logS
-3.6
pKa (Strongest Basic)
10.7
PSA
26.02 Å2
Refractivity
54.49 m3·mol-1
Polarizability
21.82 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Memantine, an amantadine derivative, is an NMDA receptor antagonist used in the treatment of Alzheimer's disease. It differs from traditional agents used in Alzheimer's disease by acting on glutamatergic neurotransmission, rather than cholinergic. There is some evidence that dysfunction of glutamatergic neurotransmission, manifested as neuronal excitotoxicity, is involved in the aetiology of Alzheimer's disease (Cacabelos et al., 1999). As such, targeting the glutamatergic system, specifically NMDA receptors, was a novel approach to treatment in view of the limited efficacy of existing drugs targeting the cholinergic system. A systematic review of randomised controlled trials found that memantine has a positive effect on cognition, mood, behaviour, and the ability to perform daily activities. There is no evidence that memantine prevents or slows neurodegeneration in patients with Alzheimer's disease.
Cơ Chế Tác Dụng : Memantine is an amantadine derivative with low to moderate-affinity for NMDA receptors. It is a noncompetitive NMDA receptor antagonist that binds preferentially to NMDA receptor-operated cation channels. It blocks the effects of excessive levels of glutamate that may lead to neuronal dysfunction. It is under investigation for the treatment of Alzheimer's disease, but there has been no clinical support for the prevention or slowing of disease progression. Memantine exerts its action through uncompetitive NMDA receptor antagonism, binding preferentially to the NMDA receptor-operated cation channels. Prolonged increased levels of glutamate in the brain of demented patients are sufficient to counter the voltage-dependent block of NMDA receptors by Mg2+ ions and allow continuous influx of Ca2+ ions into cells, ultimately resulting in neuronal degeneration. Studies suggest that memantine binds more effectively than Mg2+ ions at the NMDA receptor, and thereby effectively blocks this prolonged influx of Ca2+ ions through the NMDA channel whilst preserving the transient physiological activation of the channels by higher concentrations of synaptically released glutamate. Thus memantine protects against chronically elevated concentrations of glutamate. Memantine also has antagonistic activity at the type 3 serotonergic (5-HT3) receptor with a potency that is similar to that at the NMDA receptor, and lower antagonistic activity at the nicotinic acetylcholine receptor. This drug has no affinity for γ-aminobutyric acid (GABA), benzodiazepine, dopamine, adrenergic, histamine, or glycine receptors or for voltage-dependent calcium, sodium, or potassium channels.
Dược Động Học :
▧ Absorption :
Well absorbed orally with a bioavailability of approximately 100%. Peak plasma concentrations are reached in 3-7 hours. Food has no effect on absorption.
▧ Volume of Distribution :
* 9 to 11 L/kg
▧ Protein binding :
45%
▧ Metabolism :
Excreted largely unchanged. About 20% is metabolized to 1-amino-3-hydroxymethyl-5-methyl-adamantane and 3-amino-1-hydroxy-5,7-dimethyl-adamantane.
▧ Route of Elimination :
Memantine undergoes partial hepatic metabolism. About 48% of administered drug is excreted unchanged in urine; the remainder is converted primarily to three polar metabolites which possess minimal NMDA receptor antagonistic activity: the N-glucuronide conjugate, 6-hydroxy memantine, and 1-nitroso-deaminated memantine. It is excreted predominantly in the urine, unchanged.
▧ Half Life :
60-100 hours
Độc Tính : Side effects include pain, abnormal crying, leg pain, fever, increased apetite. Adverse drug reactions include: dizziness, confusion, headache, hallucinations, tiredness. Less common side effects include: vomiting, anxiety, hypertonia, cystitis, and increased libido. Doses of up to 400 mg have been tolerated.
Chỉ Định : For the treatment of moderate to severe dementia of the Alzheimer's type.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Tablet - Oral - 10mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Abixa
  • Công ty :
    Sản phẩm biệt dược : Akatinol
  • Công ty :
    Sản phẩm biệt dược : Axura
  • Công ty :
    Sản phẩm biệt dược : Ebixa
  • Công ty :
    Sản phẩm biệt dược : Memox
  • Công ty :
    Sản phẩm biệt dược : Namenda
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01043
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4054
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506702
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13736
ChemSpider
http://www.chemspider.com/Chemical-Structure.3914.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50062599
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-3205-60
PharmGKB
http://www.pharmgkb.org/drug/PA10364
Wikipedia
http://en.wikipedia.org/wiki/Memantine
RxList
http://www.rxlist.com/cgi/generic3/namenda.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1682.shtml
Drugs.com
http://www.drugs.com/cdi/memantine.html
... loading
... loading