Tìm theo
Neostigmine
Các tên gọi khác (7 ) :
  • (m-Hydroxyphenyl)trimethylammonium dimethylcarbamate
  • 3-Trimethylammoniumphenyl N,N-dimethylcarbamate
  • Eustigmin
  • Eustigmine
  • m-Trimethylammoniumphenyldimethylcarbamate
  • Prostigmine
  • Vagostigmine
Thuốc giãn cơ và tăng trương lực cơ
Thuốc Gốc
Small Molecule
CAS: 59-99-4
ATC: N07AA01, S01EB06
ĐG : American Regent , http://www.americanregent.com
CTHH: C12H19N2O2
PTK: 223.2915
A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H19N2O2
Phân tử khối
223.2915
Monoisotopic mass
223.144652862
InChI
InChI=1S/C12H19N2O2/c1-13(2)12(15)16-11-8-6-7-10(9-11)14(3,4)5/h6-9H,1-5H3/q+1
InChI Key
InChIKey=ALWKGYPQUAPLQC-UHFFFAOYSA-N
IUPAC Name
3-[(dimethylcarbamoyl)oxy]-N,N,N-trimethylanilinium
Traditional IUPAC Name
neostigmine
SMILES
CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C
Độ hòa tan
6.77e-02 g/l
logP
-2.2
logS
-3.6
PSA
29.54 Å2
Refractivity
75.28 m3·mol-1
Polarizability
25.08 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. By inhibiting acetylcholinesterase, more acetylcholine is available in the synapse, therefore, more of it can bind to the fewer receptors present in myasthenia gravis and can better trigger muscular contraction.
Cơ Chế Tác Dụng : A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. [PubChem] Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degredation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.. It does not cross the blood-brain barrier.
Dược Động Học :
▧ Absorption :
Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration
▧ Protein binding :
Protein binding to human serum albumin ranges from 15 to 25 percent.
▧ Metabolism :
Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver.
▧ Half Life :
The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.
Độc Tính : Overdosage of Neostigmine can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. The LD 50 of neostigmine methylsulfate in mice is 0.3 ± 0.02 mg/kg intravenously, 0.54 ± 0.03 mg/kg subcutaneously, and 0.395 ± 0.025 mg/kg intramuscularly; in rats the LD 50 is 0.315 ± 0.019 mg/kg intravenously, 0.445 ± 0.032 mg/kg subcutaneously, and 0.423 ± 0.032 mg/kg intramuscularly.
Chỉ Định : Neostigmine is used for the symptomatic treatment of myasthenia gravis by improving muscle tone.
Tương Tác Thuốc :
  • Dexamethasone The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine.
  • Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, neostigmine.
  • Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, neostigmine.
  • Prednisolone The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine.
  • Prednisone The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, neostigmine.
  • Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, neostigmine.
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Liquid - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bloxiverz
  • Công ty :
    Sản phẩm biệt dược : Prostigmin
  • Công ty :
    Sản phẩm biệt dược : Vagostigmin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01400
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4456
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509161
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07258
ChemSpider
http://www.chemspider.com/Chemical-Structure.4301.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/76014-002
PharmGKB
http://www.pharmgkb.org/drug/PA450611
Wikipedia
http://en.wikipedia.org/wiki/Neostigmine
RxList
http://www.rxlist.com/cgi/generic/neostigmine.htm
Drugs.com
http://www.drugs.com/cdi/neostigmine.html
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