Tìm theo
Physostigmine
Các tên gọi khác (4 ) :
  • Antilirium
  • Eserine
  • Physostigmine
  • Physostol
cholinesterase inhibitors, miotics
Thuốc Gốc
Small Molecule
CAS: 57-47-6
ATC: S01EB05, V03AB19
ĐG : Amend
CTHH: C15H21N3O2
PTK: 275.3461
A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H21N3O2
Phân tử khối
275.3461
Monoisotopic mass
275.163376931
InChI
InChI=1S/C15H21N3O2/c1-15-7-8-17(3)13(15)18(4)12-6-5-10(9-11(12)15)20-14(19)16-2/h5-6,9,13H,7-8H2,1-4H3,(H,16,19)/t13-,15+/m1/s1
InChI Key
InChIKey=PIJVFDBKTWXHHD-HIFRSBDPSA-N
IUPAC Name
(3aS,8aR)-1,3a,8-trimethyl-1H,2H,3H,3aH,8H,8aH-pyrrolo[2,3-b]indol-5-yl N-methylcarbamate
Traditional IUPAC Name
physostigmine
SMILES
[H][C@]12N(C)CC[C@@]1(C)C1=C(C=CC(OC(=O)NC)=C1)N2C
Độ tan chảy
105.5 °C
Độ hòa tan
7760 mg/L
logP
1.58
logS
-2.4
pKa (strongest acidic)
14.77
pKa (Strongest Basic)
6.59
PSA
44.81 Å2
Refractivity
78.4 m3·mol-1
Polarizability
30.62 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
6.12
Dược Lực Học : Physostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor which effectively increases the concentration of acetylcholine at the sites of cholinergic transmission. Physostigmine is used to treat glaucoma. Because it crosses the blood-brain barrier, it is also used to treat the central nervous system effects of atropine overdose and other anticholinergic drug overdoses. Physostigmine can reverse both central and peripheral anticholinergia.
Cơ Chế Tác Dụng : A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. [PubChem] Physostigmine inhibits acetylcholinesterase, the enzyme responsible for the breakdown of used acetylcholine. By interfering with the metabolism of acetylcholine, physostigmine indirectly stimulates both nicotinic and muscarinic receptors due to the consequential increase in available acetylcholine at the synapse.
Dược Động Học :

▧ Metabolism :
Quickly hydrolyzed by cholinesterases
Độc Tính : Side effects include increased sweating, loss of bladder control, muscle weakness, nausea, vomiting, diarrhea, or stomach cramps or pain, shortness of breath, tightness in chest, or wheezing, slow or irregular heartbeat, unusual tiredness or weakness, watering of mouth, blurred vision or change in near or distant vision, and eye pain.
Chỉ Định : For the treatment of glaucoma, and in the treatment of severe anticholinergic toxicity.
Liều Lượng & Cách Dùng : Injection, solution - Intramuscular
Injection, solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Antilirium
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00981
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5983
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506998
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06535
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00196
ChemSpider
http://www.chemspider.com/Chemical-Structure.5763.html
PharmGKB
http://www.pharmgkb.org/drug/PA450957
Wikipedia
http://en.wikipedia.org/wiki/Physostigmine
RxList
http://www.rxlist.com/cgi/generic/physostigmine.htm
Drugs.com
http://www.drugs.com/mtm/physostigmine-ophthalmic.html
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